Pharmacology is the science dealing with drugs.
Two branches:
1. PharmacoKinetics → Effect of Body on Drug
2.PharmacoDynamics → Effect of Drug on Body
PHARMACOKINETICS
••Aka ADME Study
––Absorption
––Distribution
––Metabolism
––Excretion
1. Absorption
••It is the movement of drug from site of administration
to blood.
••Lipid Solubility is the most important factor in
absorption.
Q
When The Medium Is Same, Then The Drug Will Cross
DRUG MEDIUM FORM SOLUBILITY CROSS
Acidic
Basic
Acidic
Basic
Acidic
Basic
Basic
Acidic
Non ionized
Non ionized
lonized
lonized
Lipid Soluble
Lipid soluble
Water Soluble
Water Soluble
x
x
Bioavailability
••It is the fraction of given dose that reaches the
systemic circulation in unchanged form
Factors affecting:
1. Absorption
→ Absorption → ↑ Bioavailability
Chapter - 1 General Pharmacology
↓ Absorption → ↓ Bioavailability
2. First Pass metabolism/Pre systemic metabolism
↑ First Pass metabolism → ↓ Bioavailability
↓ First Pass metabolism → ↓ Bioavailability
Note: If we give a drug by IV route, bioavailability is
100%
Q
Plasma Concentration Vs Time Graph
C
max
Maximum concentration
obtained by a particular
dose
Should lie between MTC
and MEC
T
max
Time in which plasma
concentration becomes
maximum
Tells Rate of absorption
AUC
Total area covered by
graph
Q
Tells Extent of
absorption
2. Distribution
••Distribution is a measure of amount of drug in tissues
after absorption in the systemic circulation
••It depends upon lipid solubility and plasma protein
binding.
Plasma Protein Binding
Q
••Acidic drugs bind to → Albumin
••Basic drugs bind to → a1 Acid Glycoprotein
High PPB drugs have
••Low V
d
••Long duration of action
••More drug interactions
••Dialysis not useful in poisoning
••Less Filtration
3Pharmacology
Volume of Distribution (Vd)
Q
Amount given
Plasma concentration
Vd =
••Volume of Distribution (Vd) ∝ Amount of Drug in
Tissues
More Vd → More distribution
Loading Dose [LD]
Initial high dose given to start the action
LD = Vd x Target Plasma Concentration
Maintenance Dose
Q
Repeated doses given to maintain the plasma concentration.
MD = CL x Target PC
3. Metabolism
Aim of Metabolism → To Make a Drug Water Soluble (Polar)
PHASE I REACTIONS
Q
PHASE II REACTIONS
Q
Mostly catabolic Reactions
Includes
••Oxidation (MC)
••Reduction
••Hydrolysis
••Cyclization
••Deamination
Mostly anabolic reactions
Includes
••Glucuronidation (MC)
••Glutathione conjugation
••Acetylation
••Methylation
••Sulfate conjugation
Purpose of Phase I → Expose the Functional Group on
the drug
Purpose of Phase II → Makes the drug water soluble
Enzymes
••Divided into Microsomal and Non-microsomal
Microsomal Non-microsomal
Present in smooth
endoplasmic reticulum
Present outside SER
Can be induced or
inhibited
Cannot be induced or
inhibited
Enzyme Inducers
Q
Enzyme inhibitors
Q
G -Griseofulvin
P -Phenytoin
R -Rifampicin
S -Smoking
Cell -Carbamazepine
Phone -Phenobarbitone
Vit -Valproate
K -Ketoconazole
Can’t -Cimetidine
Cause -Ciprofloxacin
Enzyme -Erythromycin
Inhibition -Isoniazid
Cytochrome p450 Enzymes
These are one type of microsomal enzymes.
CYP3A4 CYP2D6 CYP2C19
Q
C : Cyclosporine
T : Tacrolimus
S : Statins
C : CAT
(Cisapride,
Astemizole,
Terfenadine)
A :Amiodarone
N :Navirs
2 : b-Blockers
D : Anti-Depressants
6 : Anti-Anthythmies
(except amiodarone)
Clopidogrel
CYP2C9
Q
Warfarin
Phenytoin
Clopidogrel
CYP2C19 PPI
–
Active
Therefore, PPIs are avoided with clopidogrel
4. Excretion
4Cerebellum Quick Revision Notes
Glomerular Filtration
••Lipid soluble as well as water soluble drugs can be
filtered
••Filtration is inversely proportional to Plasma Protein
binding
Tubular Reabsorption
••99% of GFR is reabsorbed
––Lipid soluble drugs reabsorbed
––Water soluble drugs excreted
Tubular Secretion
••Due to pumps/transporters in proximal tubules
••These transporters are Saturable (One drug can be
transported at one time)
••Probenecid prolongs action of penicillins by inhibiting
tubular secretion
Kinetics of Elimination
Half Life [t
1/2
]
••It is the time in which plasma concentration of a
drug becomes half.
••Half-life is constant in first order kinetics.
Question: t1/2= 6hrs, after 1 day
••How much drug remains in body → 6.25%
••How much drug eliminated from body
→100-remaining→ 93.75%
Importance of t ½:
••Dose cannot be calculated
••Dosing Interval/ Frequency can be known
Formula of Half-life:
t
K
1
2
0693
=
.
(where, K is elimination rate constant)
As
So,
K
CL
Vd
=
tX
Vd
CL
1
2
0693=.
Order of Kinetics
First order kinetics Zero order kinetics
Q
→ Fraction is constant→ Amount is constant
R a PC
CL = Constant
t½ = Constant
R = Constant
CL a 1/ PC
t½ a PC
••Majority of drugs follow First Order Kinetics
Drugs Following Zero Order Kinetics are
Q
Zero → Zero order Kinetics
W → Warfarin
A → Alcohol/Aspirin
T → Theophylline
T → Tolbutamide
Power → Phenytoin
PHARMACODYNAMICS:
It deals with action of a drug as well as the mechanism
of action
Major mechanism of action of a drug are through
enzymes or through receptors.
Enzyme inhibition
Q
Km V
max
Competitive ↑ -
Non competitive - ↓
Lineweaver Burke Plot:
••Also known as double reciprocal plot
••Graph between 1/S (on X-axis) and 1/V (on Y-axis)
5Pharmacology
••X-axis tells K
m
and Y-axis tells V
max
••If lines intersect at X-axis, it is non-competitive
inhibition
••If lines intersect at Y-axis, it is competitive
inhibition
Classification of Drugs
Q
Drug Intrinsic Activity
Agonist Maximum [+1]
Partial Agonist Submaximum [0 to 1]
Inverse Agonist Opposite action [-ve]
Antagonist No action of itself but interfere
with action of other drugs [0]
Classification of Receptors
1. lonotropic Receptors
••The receptors present on ion channels are known as
ionotropic receptors.
••Fastest acting receptors
2. Enzymatic Receptors
••These are present on cell membrane with intracellular and extracellular ends.
••Drug binds outside and enzyme is activated inside and action is produced
••Aka Tyrosine Kinase Receptors
3. G-Protein Coupled Receptors [GPCR]
Works by one out of the 3 mechanisms
••By changing the level of cAMP
••Can act through Ca
2+
••Can open the ion channels
6Cerebellum Quick Revision Notes
Types of G proteins
Type Mechanism
Second/Third
messenger
G
S
Stimulate adenylate cyclase ↑ cAMP
G
i
Inhibit adenylate cyclase ↓ cAMP
G
q
Convert PIP2 to IP3 and DAG
IP3
DAG
Calcium
4. Intracellular Receptors
A. Cytoplasmic Receptors
B. Nuclear Receptors
••Only Lipid soluble drugs acts through these
receptors
••Thus, whether a drug binds the cytoplasmic receptors or the nuclear receptors, it will finally work through DNA (nuclear mechanism)
••These are also called nuclear recetor superfamilty
••These are slowest acting receptors.
Receptors Examples
1. IonotropicGABA
A
, NMDA, N
N
, N
M
, 5HT
3
2. Enzymatic Cytokines, Prolactin, Insulin, GH
3. Intracellular
A. Cytoplasmic
B. Nuclear
Vit D, Glucocorticoids,
Mineralocorticoids
Vit A, Thyroid hormones, Sex
hormones
4. GPCR Most others
Log Dose Response Curve (Log DRC)
••S-shaped curve [Sigmoid Curve)
••Clinically more useful than DRC
••3 important parameters obtained from log DRC:
1. Potency
2. Efficacy
3. Slope
Potency
••To produce a similar response if a drug is required in
lesser dose, it is more potent
••On log DRC, left-sided curve is more potent drug
whereas right-sided curve is less potent
Efficacy
••Relates to maximum effect of a drug regardless of
dose
••Higher the curve, more is efficacy
H - Height tells about
Q
E - Efficacy
L - Left side drugs are more
P - Potent
C → Most efficacious (Highest curve)
D → Least efficacious (Lowest curve)
D → Most potent (Most left)
B → Least potent (Most right)
7Pharmacology
Quantal DRC
••For All or None phenomenon, where grade of response
cannot be plotted.
••Percentage of subjects responding are kept on Y-axis
••Tells about effect of a drug in population
i) If 50% respond to a particular dose → Then it is
called ED
50
(Median Effective dose)
ii) If 50% of animals die after receiving a particular
dose it is median lethal dose (LD
50
).
Therapeutic index = LD
50
/ED
50
Q
••Therapeutic index is margin of the safety of a drug
The Drugs and Cosmetics Act
––An act to regulate the import, manufacture,
distribution and sales of drugs.
••Spurious drug: Imitation of or substitute of
another drug in a manner likely to deceive the name
of another drug. The less known pharmaceutical
company try to take advantage of reputation of a
well-known company.
••Misbranded drug: If a drug is not labelled in
prescribed manner or its label contains any
statement which makes any false claims for the
drug.
••Adulterated drug: If it contains filthy, patrid or
decomposed substances.
Clinical Trials
Testing of drugs in humans is called clinical trials
••Licensing Authority to give approval for a new drug
in USA is FDA whereas in India it is DCGI (Drug
Controller General of India)
Q
Q
Q
Phase Zero Clinical Trials
••Micro-dosing study
••It is conducted on humans
••Maximum amount of drug given is 100 mcg or
(1/100)th of Human Equivalent Dose, whichever is
lower
••Radiolabeled substances are added with this
sub therapeutic dose to know the Pharmacokinetics
of the drug.
••It is not mandatory
Q
8Cerebellum Quick Revision Notes
Pregnancy Categories:
Drugs are categorized into 5 groups according to safety
in pregnancy
Category Special points
A Safest in pregnancy
B
C
D
X Contra-indicated in pregnancy e.g. Thalidomide
Q
Note:
••Schedule X drugs and category X drugs are totally
different.
••Schedule X include narcotic and psychotropic drugs
e.g. ketamine.
••Category X contain teratogenic drugs like thalidomide
••Schedule H drugs require prescription of a RMP.
SAFE AND UNSAFE DRUGS IN PREGNANCY
Condition Drugs safe in
Pregnancy
Drugs to be
Q
avoided in
Pregnancy
Hypertension Labetalol,
Methyldopa
ACE Inhibitors and
ARBs
Anti-coagulantsHeparin Warfarin
Bipolar disordersAnti-psychoticsValproate (Contra-
indicated)
Lithium (Avoid)
Anti-thyroid PropylthiouracilCarbimazole (1st
trimester)
Anti-microbialsPenicillins,
Cephalosporins
Macrolides
Tetracyclines
Quinolones
Aminoglycosides
Anti-EpilepticsLevetiracetam
Lamotrigine
Valproate
Enteric Coating of Drugs:
••This is a coating that dissolves in alkaline medium
only.
••It can be used for
––Protecting the acid labile drugs from gastric
acid, e.g., proton pump inhibitors.
––It can protect gastric mucosa from irritant
drugs e.g. NSAIDS
––It increases the absorption of drugs that are
preferentially absorbed distal to stomach.
Fixed Dose Combinations (FDC):
When two or more drugs are combined to-
gether in a particular ratio.
Advantages:
••Compliance
improves
••One drug may
reduce the adverse
effects of the
other drug
••Efficacy may
increase
••Cost may decrease
Disadvantages:
••May be used irrationally.
••If adverse effect occurs, it
cannot be ascribed to one drug.
••Drugs with different
pharmacokinetics cannot be
combined.
••Dose of one drug cannot be
altered independently as per
requirement.
Prescription Writing
Prescription is the written order by the doctor to the
pharmacist to dispense some medication.
Q
Note:
••Without date and signature (initials), the prescription is invalid.
••Drug name should never be written in short form (e.g., write paracetamol, not PCM)
••Abbreviations like OD, BD, HS should not be used
Q
••In dose of drug
––Leading zeros should always be mentioned (e.g., 0.5 mg is correct but .5 mg is wrong)
––Trial zeros should never be mentioned (e.g., 5 mg is correct but 5.0 mg is wrong)
––Microgram should be written as mcg not μg.
Q
9Pharmacology
Q8. Which of the following drugs follow zero order
kinetics?
A. Phenytoin B. Diclofenac
C. Morphine D. Propranolol
Q9. Identify the type of inhibition from the given graph
A. Competitive B. Non-competitive
C. Un-competitive D. Allosteric
Q10. True about non-competitive inhibition is
A. Km remains same, Vmax decreases
B. Km increases, Vmax remains same
C. Km decreases, Vmax increases
D. Km increases, Vmax increases
Q11. Identify the missing substance X marked in the
box in the given diagram
A. G protein B. Protein C
C. Cyclic AMP D. Calcium
Previous Years Questions
Q1. Which of the following factor in PC vs time graph is
a measure of extent of drug absorption of a drug?
A. Area under the curve B. Half life
C. Cmax D. Tmax
Q2. Rate of administration of a drug is equal to rate
of elimination. How will you calculate the dosing rate of
the drug to maintain steady state concentration?
A. Dosing rate = Vd x target plasma concentration
B. Dosing rate = CL x target plasma concentration
C. Dosing rate = Vd/target plasma concentration
D. Dosing rate = CL/target plasma concentration
Q3. Anionic and slightly acidic drugs usually bind to
A. Albumin B. Alpha acid glycoprotein
C. Ceruloplasmin D. Globulin
Q4. High plasma protein binding of a drug results in:
A. Decreased glomerular filtration
B. High volume of distribution
C. Lowers duration of action
D. Less drug interaction
Q5. A patient with stroke was started on clopidogrel.
He developed another episode of stroke 6 months later.
Which of the following is the likely cause?
A. Rapid metabolism by CYP 1A2
B. Poor metabolism by CYP 2C19
C. Poor metabolism by CYP 2D6
D. Poor metabolism by CYP 2E1
Q6. Which of the following treatment option is utilized
in salicylate poisoning?
A. Alkalinization of urine
B. Acidificaition of urine
C. Alkalinization of blood
D. Acidification of blood
Q7. Elimination rate constant of a drug is 0.05/hr.
What is its half life?
A. 6.5 hr B. 20 hr
C. 13.9 hr D. 8 hr
Answers
1. - A
2. - B
3. - A
4. - A
5. - B
6. - A
7. - C
8. - A
9. - A
10. - A
11. - C
10Cerebellum Quick Revision Notes
Q12. Which of the following statement is correct
regarding the given graph?
A. Drug A is agonist and Drug B represents inverse
agonist
B. Drug C represents agonist and Drug D is inverse
agonist
C. Drug A is agonist and Drug D is inverse agonist
D. Drug B is partial agonist and Drug C is inverse
agonist
Q13. Type of stimulatory G protein in PIP2-Phospholipase
activation pathway is
A. Gs B. Gi
C. Gq D. Go
Q14. Drug acting via tyrosine kinase receptor is
A. TRH B. TSH
C. Insulin D. MSH
Q15. Which of the following drugs act through
intracellular receptors?
A. Thyroxin B. Glucagon
C. Epinephrine D. Parathyroid hormone
Q16. Find therapeutic index of a drug from the
information given below in the graph
A. 1 B. 2
C. 4 D. 8
Q17. What does LD50 signifies
A. It is the dose at which 50% of animals will die
B. It is the dose at which 50 animals will die
C. It is the dose at which 50% patients will get the
desired response
D. It is drug that will be effective at 50% dose
Q18. Which of the following statements about these
drugs is true?
A. Drug A is most potent
B. Drug A and B have equal efficacy but B is more
potent than drug A
C. Drug C is least potent
D. Drug B has more potency but less efficacy than drug A
Q19. Which of the following statement is correct about
clinical trials?
A. New drug application is filed with Phase 2 clinical
trials
B. Phase 0 clinical trials is for checking the pharma-
cokinetics of the drug
C. In Phase 3, open label studies are done
D. Phase 2 is post marketing surveillance.
Answers
12. - C
13. - C
14. - C
15. - A
16. - C
17. - A
18. - A
19. - B
11Pharmacology
Q20. New drug application is filed after which phase of
clinical trials?
A. Phase 1 B. Phase 2
C. Phase 3 D. Phase 4
Q21. Manufacturer of a drug company labels the drug
contains 500 mg paracetamol. On quantitative analysis
by the authorities, it was found to contain only 200 mg
of drug. According to drugs and cosmetics act 1940,
this type of drug is known as?
A. Spurious drug B. Adulterant drug
C. Unethical drug D. Misbranded drug
Q22. Identify the true statement regarding Clinical
Trials:
A. Phase 1 is done to determine efficacy in patients
B. Healthy volunteers are recruited for the first time
in Phase II
C. Randomized Controlled Trials in patients is done in
Phase III
D. Phase IV is Pharmacokinetics study in animals
Q23. All of the following are advantages of enteric
coated tablets except
A. It increases the half-life of the drug
B. It protects acid labile drugs from gastric pH
C. It increases the absorption of drugs that are
preferentially absorbed distal to stomach.
D. It protects stomach from irritant drugs
Q24. Category A, B, C, D, X division of drugs is based
on
A. Safety in pregnancy
B. Dose adjustment in renal failure
C. Therapeutic index and safety
D. Over the counter use of drug
Q25. Variation in drug responsiveness to a particular
dose of the drug in different individuals can be obtained
from:
A. Graded Dose Response Curve
B. Efficacy
C. Potency
D. Quantal Dose Response Curve
Q26. Which of the following statement is true regarding
Fixed Dose Combination of drugs?
A. Adverse effect of one drug may be reduced by the
other drug
B. Two drugs with different pharmacokinetics can be
combined easily
C. Dose of one drug can be altered independently as
per requirement
D. Adverse effect can be ascribed to a single drug
Q27. Which of the following drug must be sold by
retail only production of a prescription by a registered
medical practitioner?
A. Schedule H B. Schedule G
C. Schedule X D. Schedule M
Q28. As an Indian medical intern, which of the following
is the correct format for prescription of alprazolam?
A. Tablet alprazolam 0.5 mg once a day before
bed time for 7 days
B. Tablet alprazolam 0.5 mg HS for 7 days
C. Tablet alprazolam 500 mcg one tablet OD
for 7 days
D. Tablet alprazolam ½ mg tablet HS daily
Answers
20. - C
21. - D
22. - C
23. - A
24. - A
25. - D
26. - A
27. - A
28. - A
Location Neurotrans-
mitter
Preganglionic parasympathetic
Preganglionic sympathetic
Postganglionic parasympathetic
Postganglionic sympathetic
••At all places
••At sweat glands
ACh
ACh
ACh
NA
ACh
Actions:
Location Parasympathetic Sympathetic
Heart
Bronchus
GIT
Bladder
Glands
Pupil
Sexual system
↓↓
Bronchoconstriction
Diarrhea
Contract
↑ Secretions
Miosis
Erection
+ + +
Bronchodilation
Constipation
Relax
↓ Secretions
Mydriasis
Ejaculation
PARASYMPATHETIC SYSTEM
Major neurotransmitter is ACh
It works on cholinergic receptors
Cholinergic Receptors
Nicotinic Receptor Muscarinic Receptor
N
N
→ Ganglia
N
M
→ NMJ (require
optimal stimulation)
M1 → Stomach: ↑HCl
M2 → Heart: ↓ HR, ↓ Conduction
M3 → Bronchus : BC
GIT : ↑ Peristalsis
Bladder : ↑ Contraction
Glands : ↑ Secretions
Pupil : Miosis
Chapter - 2 Autonomic Nervous System
Origin:
Neurotransmitters:
13Pharmacology
CHOLINERGIC DRUGS:
Drugs stimulating the parasympathetic system can be:
Directly Acting Cholinergic Drugs:
DRUG ACTS ON ACTION INDICATION
Pilocarpine Pupil [M3] Miosis Angle closure
glaucoma
Q
Indirectly Acting Cholinergic Drugs:
••These drugs act by inhibiting AChE.
••These may be reversible or irreversible AChE
inhibitors.
••Reversible AChE inhibitors are used clinically
whereas irreversible AChE inhibitors are toxic.
Reversible AChE Inhibitors:
Uses of Neostigmine
Q
Irreversible AChE Inhibitors
Include
Organophosphates - Malathion
Parathion
Carbamates - Carbaryl
Propoxur
Organophosphate Poisoning:
Clinical features:
Receptor
stimulated
Feature
M1 Aciditiy
M2 Bradycardia and Hypotension
M3••Pin point pupil
••↑ Secretions
••Diarrhea
••Urination
••Bronchoconstriction
M1, M2, M3 Coma
N
M
Muscle weakness
N
N
Tachycardia and Hypertension
Note:
••Nicotinic symptoms (N
N
) are extremely rare.
••If pin point pupil with increase in secretions are
present, diagnosis of OP poisoning is almost sure.
Treatment
1. Atropine
Q
••DOC For OP and Carbamate poisoning
••Given by iv route (every 5 min) till signs of
atropinization occur.
••Atropine cannot reverse muscle weakness
Signs of Atropinization
••↓ Secretions → Most reliable (Most specific) sign
••Mydriasis
→ Most commonly used sign
••Tachycardia
→ HR > 100 bpm
Note: Atropine is not used in organochlorine
(endrin) poisoning.
2. AChE Reactivators (Oximes)
Q
Pralidoxime [PAM]
Di Acetyl Monoxime [DAM]
••Not DOC
••Only effective in OP Poisoning
••PAM acts only peripherally, DAM has both central
as well as peripheral actions.
EYE M3
Atropine
Homatropine
Cyclopentolate
Tropicamide
Longest acting: Atropine
Shortest acting: Tropicamide
Fundoscopy
Refraction testing
Iridocyclitis
DOC in children–Atropine eye ointment
ATROPINE POISONING:
(ANTICHOLINERGIC POISONING)
••Patient has a history of taking some wild fruit
(Dhatura/Belladona) and presents with
Q
D – Dry mouth, Delirium
H – Hyperthermia
A – Agitation
T – Tachycardia
U – Urinary
R – Retention
A – Accommodation lost (Blurred vision, Photophobia)
••DOC for treatment of atropine poisoning is
physostigmine.
Q
SYMPATHETIC NERVOUS SYSTEM
••Major neurotransmitter is nor-adrenaline
Adrenergic Receptors
a
1
a
2
Location Action Presynaptic
receptor
→ Acts like brake to
sympathetic system
Blood vesselsVasoconstriction
Eye Mydriasis
Prostatic
urethra
↓ Outflow
15Pharmacology
b
1
b
2
b
3
Location Action Location Action Location Action
Heart ↑ HR, BP Lungs Bronchodilation Fat Lipolysis
JG cellsRenin secretionGIT Constipation Bladder Relax
Bladder ↓ Out flow
Glands ↓ Secretions
Uterus Tocolytic
Blood vessels Vasodilation
Skeletal muscle
spindle
Tremors
Liver ↑ Blood sugar
Effect on blood vessels
A1 -> C α1 – Cause vasoconstriction
Q
B2 -> D β2 – Cause vasodilation
Effect on metabolism:
••Sympathetic system protects from hypoglycemia by
two mechanisms:
Warning symptoms Hypoglycemia reversal
••Tachycardia (b
1
)
••Palpitations (b
1
)
••Tremor (b
2
)
••Sweating (M
3
)
••By changing metabolism (b
2
)
- ⊕ Gluconeogenesis
- ⊕ Glycogenolysis
- ⊝ Glycogenesis
••Beta Blockers cause (in diabetic patients)
1. Masking of warning symptoms
2. Prevent reversal of hypoglycemia
••So, b blockers are contraindicated in diabetic
patients.
••Sweating is only reliable symptom of hypoglycemia
in diabetics on b blocker medication.
Q
ADRENERGIC DRUGS:
These can be divided into:
••Indirectly Acting Drugs
••Directly Acting Drugs
Indirectly Acting Drugs
COCAINE - It acts by inhibiting reuptake of NA
Q
••It is a local anaesthetic
––All LA cause vasodilation except cocaine
––Cocaine cause vasoconstriction and hypertension
••It is an addictive drug
––Shows tactile hallucinations (cocaine bugs): Scratching of skin
––Cause palatine perforation
––Overdose characterized by
Agitation
Ulcers or scratch marks on skin
Sympathetic symptoms (Tachycardia,
Mydriasis, Hypertension, MI)
Note: Cocaine does not cause bradycardia since it is a
sympathetic drug.
Directly Acting Drugs
1.CATECHOLAMINES
– Not effective orally
Endogenous Exogenous
Adrenaline (a1, a2, b1, b2)
NA (a1, a2, b1)
Dopamine (D1, b1, a1)
Dobutamine (b1)
Isoprenaline (b1, b2)
Fenoldopam (D1)
Uses of Catecholamines
Adrenaline
1. Anaphylactic Shock
••DOC is Adrenaline
••Route of choice is I.M. or S.C.
••Concentration is 1:1000 (0.5 ml)
Q
2. Cardiac Arrest
••CPR is done first
••Adrenaline is useful
••Concentration is 1:10,000
Q
••Preferred routes are IV > Intraoseous > ET
16Cerebellum Quick Revision Notes
Nor-Adrenaline
••DOC for septic shock
••Effect is monitored by checking mean blood pressure
Dopamine
Acts on
Q
Receptors Dose (mcg/
kg/min)
Organ Action
D1 < 2 Blood
vessels
Vasodilation (Max
in Renal BV)
b
1
2-10 Heart Stimulation
a
1
> 10 Blood
vessels
Vasoconstriction
Uses
1. CHF
2. Shock + Oliguria [DOC]
Dobutamine
••Mainly b
1
agonist
••Used for CHF
Fenoldopam
••Only D
1
agonist
••Used for hypertensive emergencies
Isoprenaline
••↑ SBP but ↓ DBP
Q
••Maximum increase in pulse pressure
2. NON-CATECHOLAMINES
StimulatesDrugs Action
a
1
Phenylephrine
eye drops
Mydriasis without
cycloplegia
Methoxamine
Mephentermine
→ Vasoconstriction → Used
in shock
Xylometazoline
Oxymetazoline
Naphozoline
→ Nasal decongestants
a
2
Clonidine
Methyldopa
→ Brake for sympathetic system
→ Used for hypertension
b
2
Salbutamol
Terbutaline
Salmeterol
Formoterol
→ Bronchodilation
→ Used for asthma by
inhalational route
Ritodrine
Isoxsuprine
→ Tocolytic
→ Used for preterm labour
b
3
Mirabegron Overactive bladder
Note: Beta-2
agonists can cause following adverse
effects:
––T - Tremors
––T - Trachycardia
––T - T-wave changes in ECG (due to hypokalemia)
––Pulmonary edema - by ritodrine
––However,
b
2
agonists do not cause
hypoglycemia.
Q
ANTI - ADRENERGIC DRUGS
These may be alpha blockers or b - Blockers.
ALPHA BLOCKERS
These can be non-selective (α
1
+ α
2
) blockers or selective
α
1
blockers
Non-selective α blockerα
1
Blocker
1. Used in severe
hypertension
2. Can cause severe
tachycardia
1. Used in mild to
moderate hypertension
2. Cannot cause severe
tachycardia
Non-Selective α Blockers
Irreversible Reversible
Phenoxybenzamine Phentolamine, Tolazoline
Used for
– Pheochromocytoma
Used for
– Cheese Reaction
– Clonidine withdrawal
Selective α
1
Blockers
••Prazosin
••Terazosin
••Doxazosin
••Alfuzosin
Uses
••BPH (Due to a1A blockade)
••Scorpion sting (D.O.C is Prazosin)
Adverse Effect
First Dose (Postural) Hypotension
→ a1 blockers always started at bed-time.
Q
Types of α
1
receptors
α
1A
α
1B/1D
On Prostatic Urethra On Blood Vessels
TAMSULOSIN
SILODOSIN
••No postural hypotension
••DOC for normotensives with BPH
17Pharmacology
Benign Prostatic Hyperplasia: (BPH)
α
1A
blockers
••Tamsulosin - Stops the dynamic component and do
not affect the size of prostate i.e they are only for
the symptoms of BPH but do not stop the growth
of prostate.
5-α reductase inhibitors:
••Finasteride - Stops the conversion of Testosterone
to DHT which control/stops the growth of Prostate
in BPH (Static Component).
2. BETA (β) BLOCKERS
Beta-1 + Beta-2 # (First
Generation)
Beta-1 # (Second
Generation)
Cardiac and non-cardiac
uses
Contraindicated in Asthma,
DM and PVD
Only cardiac uses
Relatively safe
1. Beta-1# or Cardio-Selective or 2nd
Generation Beta #
New → Nebivolol
Beta → Betaxolol
Blockers → Bisoprolol
Act → Acebutolol
Exclusively → Esmolol
At → Atenolol
Myo → Metoprolol
Cardium → Celiprolol
→ These are relatively safe in Asthma, PVD & DM
2. Intrinsic Sympathomimetic Activity [ISA] or
Partial Agonists
→ Less chances of causing severe bradycardia
Q
Contain → Celiprolol
Partial → Pindolol
Agonist → Alprenolol
Activity → Acebutolol
Indications
Cardiac Uses
1. Hypertension
2. Classical Angina [C/I in Variant angina]
3. MI
4. Chronic CHF [C/I in acute CHF]
5. Arrhythmia
Non-Cardiac Uses
Play - Performance anxiety (DOC : Propranolol)
The – Thyrotoxicosis (DOC : Propranolol)
G – Glaucoma (Timolol is used)
A – Akathisia (DOC : Propranolol)
M – Migraine prophylaxis (DOC : Propranolol)
E – Essential tremors (DOC : Propranolol)
Adverse Effects and Contra-indications
Due to β
1
Blockade
1. ↓ Rate → Bradycardia (C/I in Sick sinus syndrome)
2. ↓ Conduction → AV Block
3. ↓ Contractility → Acute CHF
Due to β
2
Blockade
1. Asthma
2. Peripheral vascular Disease
3. Diabetes mellitus
4. Variant angina.
GLAUCOMA
→ Glaucoma is characterized by ↑ IOP: It may be due
to
––↑ Aqueous humor production
––↓ Aqueous humor drainage
––Pigmentation of Iris (Heterochromia Iridis)
––Growth of eyelashes (Hypertrichosis)
––Fluid in macula (Macular edema)
––Contra-indicated in uveitis
ApracLonIDine
Q
––Lid retraction
Brimonidine
Q
––Causes Brain suppression in Infants (Leads to
Apnea)
––C/l in children < 2yrs
Netarsudil (Rho-kinase inhibitor)
Q
––Cornea verticillata.
ANS PRACTICALS
1. Ileum graph
Q
19Pharmacology
2. Dog Blood Pressure Experiment
Q
A: Adrenaline
B: Nor-adrenaline
C: Isoprenaline
Biphasic Response → Effect of high dose of adrenaline
→ Dog is given Phentolamine → α-blocker → BP → → Then, Epinephrine (high dose) is given → BP ↓ →No
Biphasic Response produced → Called Vasomotor Reversal of Dale
→ Dog is given Atropine first → HR ↑ → After this, a high dose of ACh given → BP & HR ↑ → Nicotinic action appear → Stimulate sympathetic ganglia
→ Ephedrine given → BP ↑ → Same dose is repeated → Less ↑ in BP → Called Tachyphylaxis
20Cerebellum Quick Revision Notes
Previous Years Questions
Q1. Which of the following action is expected on
stimulation of muscarinic receptors?
A. Erection
B. Ejaculation
C. Increased contraction of cardiac muscles
D. Bronchodilation
Q2. A farmer presented with pin point pupil and increase
in secretions. Likely poisoning is
A. Organophosphate poisoning
B. Dhatura poisoning
C. Opioid poisoning
D. Atropine poisoning
Q3. Topical antiglaucoma drug dorzolamide act by which
of the following mechanism of action?
A. Carbonic anhydrase inhibition
B. Beta blockade
C. Alpha agonist
D. Prostaglandin analog
Q4. A patient with history of snake bite presented in
emergency with symptoms of fatigue and irritability.
Ten vials of antivenom were administered intravenously
but the patient is still having difficulty in swallowing,
ptosis and respiratory distress. What should be the
next line of management?
A. Atropine and neostigmine
B. Nebulizer with salbutamol
C. IV hydrocortisone
D. Antihistamines
Q5. A patient on treatment of myasthenia gravis
presents with increasing muscle weakness. Which of
the following drug is used to differentiate myasthenia
gravis from cholinergic crisis?
A. Edrophonium B. Pilocarpine
C. Atropine D. Pyridostigmine
Q6. A 20 year old boy was brought to emergency room
after consuming some unknown substance. The patient
was sweating profusely, saliva was drooling from mouth
and tears were present. The boy had involuntary
urination and diarrhea. On examination, the heart rate
was 58 beats per minute and blood pressure was 80/60
mm Hg. Which of the following is the drug of choice for
treatment of this patient?
A. Atropine
B. N-acetylcysteine
C. Naloxone
D. Physostigmine
Q7. A study was conducted to see the effect of
different drugs on isolated mammalian intestinal tissue
in Dale’s organ bath. The following graph is obtained.
Which of the following is the likely drug?
A. Acetylcholine
B. Barium chloride
C. Adrenaline
D. KCl
Q8. An experiment on dog blood pressure was done
by adding different drugs. The drugs added and the
effects are as shown in the given figure. This experiment
is done to demonstrate the
Answers
1. - A
2. - A
3. - A
4. - A
5. - A
6. - A
7. - C
8. - B
21Pharmacology
Answers
19. - B
20. - C
A. Muscarinic action of ACh
B. Nicotinic action of ACh
C. Potentiation of ACh
D. Antagonistic action of ACh
Q9. After eating an unknown plant, A child presented to
emergency in comatose state. The pupils were dilated
and skin was dry. Body temperature is raised and heart
rate is high. These signs and symptoms can occur with
the intake of which of the following substance?
A. Dhatura B. Poppy seeds
C. Mushroom D. Cannabis
Q10. Topical atropine is not given in
A. Acute congestive glaucoma
B. Corneal ulcer
C. Malignant glaucoma
D. Acute anterior uveitis
Q11. All of the following are Side effects of Ritodrine
except?
A. Hypoglycemia B. Tachycardia
C. Hypotension D. Pulmonary edema
Q12. Which of the following is the action of dopamine
at low doses?
A. It increases renal blood flow
B. It causes vasoconstriciton
C. It has positive chronotropic action
D. It causes hypotension
Q13. A lady was stung by many bees. She developed
breathing difficulty and hypotension. Drug used for
treatment of this condition is?
A. Adrenaline B. Nor-adrenaline
C. Dopamine D. Isoprenaline
Q14. A drug addict patient presented with agitation
and ulceration on skin. The patient had severe itching
and scratch marks on the body. On examination there is
presence of tachycardia, mydriasis and hypertension.
Likely substance responsible for these symptoms is?
A. Cocaine B. Cannabis
C. LSD D. Heroin
Q15. Which dose of dopamine act preferably on beta-1
receptors?
A. Less than 2 mcg/kg/min
B. 2-10 mcg/kg/min
C. 10-20 mcg/kg/min
D. More than 20 mcg/kg/min
Q16. A patient was on metoprolol therapy for
hypertension. He was also administered verapamil.
Which of the following is likely to happen with above
combination therapy?
A. Torsades de pointes
B. Ventricular tachycardia
C. Ventricular fibrillation
D. Bradycardia with AV block
Q17. A 65 years old patient presented with dribbling of
urine with urgency. He was started on prazosin therapy
but the patient developed postural hypotension. Which
of the following is the better alternative drug for this
patient?
A. Terazosin B. Tamsulosin
C. Timolol D. Phenoxybenzamine
Q18. Beta blockers are avoided in all of the following
conditions except
A. Glaucoma
B. Peripheral vascular disease
C. Diabetes mellitus
D. COPD
Q19. Hypertension and pulmonary edema associated
with scorpion sting is managed by:
A. Carvedilol B. Prazosin
C. Spironolactone D. Phentolamine
Q20. Which of the following is a contraindication to the
use of Beta Blockers?
A. Glaucoma B. Tachycardia
C. Bronchial asthma D. Hypertension
9. - A
10. - A
17. - B
18. - A
11. - A
12. - A
13. - A
14. - A
15. - B
16. - D
22Cerebellum Quick Revision Notes
Q21. A known patient of bronchial asthma was started
on treatment with an anti-glaucoma drug. During the
course of treatment, asthma worsened. Which drug is
likely responsible for these symptoms?
A. Timolol B. Brimonidine
C. Latanoprost D. Pilocarpine
Q22. A patient had symptoms of redness and
photophobia. On examination, cells were present in
anterior chamber with keratic precipitates. Intraocular
pressure was measured to be 38 mm Hg. Which of the
following anti-glaucoma drug should be avoided?
A. PG analogues
B. Beta blockers
C. Mannitol
D. Carbonic anhydrase inhibitors
Q23. Drug capable of causing ocular hypotension with
apnoea in infants is:
A. Acetazolamide B. Latanoprost
C. Brimonidine D. Apraclonidine
Q24. Anti-glaucoma drug that acts by increasing
uveoscleral outflow is
A. Latanoprost B. Timolol
C. Pilocarpine D. Dorzolamide
Q25. A patient with bronchial asthma presents with
raised intraocular pressure. Treatment of open angle
glaucoma in this patient is
A. Latanoprost B. Alprostadil
C. Gemeprost D. Carboprost
Q26. Which anti-glaucoma drug acts by increasing
trabecular outflow?
A. Netarsudil B. Timolol
C. Acetazolamide D. Brimonidine
Answers
21. - A
22. - A
23. - C
24. - A
25. - A
26. - A
Chapter - 3 Autacoids
- Have autocrine effects [Local effects]
- Based on chemical Structure
Peptide Autacoids
→ Angiotensin
→ Bradykinin
Amine Autacoids
→ Histamine
→ 5-HT
Lipid Autacoids
→ Prostaglandins
→ Leukotrienes
→ Thromboxane
HISTAMINE
Receptors
Location Action Blockers
H1CNS
Bronchus
Allergy
Stimulates RAS
Promote
wakefulness
First and
second
Generation
Drugs
H2Stomach Secrete Acid Ranitidine
Cimetidine
H3PreSynapticBRAKE H3 Inverse
Agonist
Tiprolisant
[Pitolisant]
Used for
Narcolepsy
H4WBC Chemotaxis
H
1
Blockers
1
st
Generation 2
nd
Generation
Cross BBB, cause sedation Do not cross BBB, no
sedation
Have Anti-cholinergic action
→ Anticholinergic S/E occur
No Anti-cholinergic action
Useful for allergy and
Possess : Prophylaxis of
motion sickness
Anti : Akathisia
Cholinergic : Common Cold
Property : Parkinsonism
(Drug induced)
Useful only for allergy
Promethazine Fexofenadine
Q
••Terfenadine metabolite
Loratidine
Cetirizine
5-HT (SEROTONIN)
Serotonin Receptors
Location Action Drugs Example Uses
5HT1A Presynaptic Brake AgonistBuspirone
Q
Anxiety
5HT1B/ID BV of Brain VasoconstrictionAgonistSumatriptan Naratriptan
Eletriptan Rizatriptan
DOC for
Acute Severe Migraine
5HT2A/2C Brain BlockersClozapine , Olanzapine Atypical Antipsychotics
5HT3 CTZ Emesis BlockersOndansetron Granisetron
Tropisetron Dolasetron
Palonosetron
Q
DOC for vomiting due to
Chemotherapy
Radiotherapy
Post-operative
Q
5HT4 GIT Prokinetic Agonist Cisapride , Mosapride,
Prucalopride
As prokinetics for GERD
24Cerebellum Quick Revision Notes
MIGRAINE:
Q
→ Drug of choice for mild to moderate headache – NSAIDs (Paracetamol, Diclofenac)
→ Drug of choice for Acute severe attack – Triptans
→ Other drug for Acute severe migraine – Ergotamine
→ DOC for prophylaxis of migraine – Propranolol
New Drugs for Migraine:
1. Lasmiditan (DITANS)
Q
••Stimulates 5HT
1F
receptor and decreases CGRP
release.
••This prevents the vasodilation and neuronal
inflammation.
••Effective orally.
••It is recently approved for acute attacks of
migraine.
••Advantage over triptans is that it does not induce
peripheral vasoconstriction.
2. Monoclonal Antibodies Against CGRP
••Approved for prophylaxis of migraine.
••Given by injectable route.
––Erenumab
––Fremanezumab
––Galcanezumab
––Eptinezumab
3. CGRP Antagonist: (GEPANTS)
Q
••Used for acute attack
••Effective orally
••Drugs are
––Olcegepant
––Rimegepant
––Ubrogepant
PROSTAGLANDINS
1. General Effects
••Fever
••Pain
••Inflammation
2. Platelets
••TXA2 → Aggregation
••PGl2 → Inhibition of aggregation
3. Heart
••Ductus Arteriosus is kept open by PGE
1
••PDA [Patent ductus Arteriosus] is treated by NSAIDs like
––Aspirin
––Indomethacin
––Ibuprofen (DOC)
4. Uterus
••PGs Contract upper segment of uterus
••Used for abortion (Misoprostol is used)
5. Stomach
••PGE2 protect the stomach from peptic ulcer disease
••For NSAID Induced Peptic Ulcer Disease
––Most specific drug is Misoprostol
Q
––DOC is proton pump inhibitors
6. Eye
PGF2α
→ ↑ Uveo scleral outflow
→ Latanoprost
→ DOC for Primary Open Angle Glaucoma
Q
25Pharmacology
NON-STEROIDAL ANTI-
INFLAMMATORY DRUGS (NSAIDs)
COX 1 COX-2
Constitutive Enzyme
Present normally at most
places
Inducible enzyme
Present normally in
••Kidney
••Endothelium
••CNS
NSAIDS act by inhibiting COX. These may be:
Non-Selective COX InhibitorsSelective COX-2 Inhibitors
↑ Risk of PUD Less risk of PUD
Non-Selective COX Inhibitors
Drugs
- Aspirin : Irreversible COX inhibitor
(Antiplatelet), ↑Uric acid
- Paracetamol : COX - 3 inhibitor, safe in CKD
- Ibuprofen : DOC for PDA
- Diclofenac : Partial COX-2 selective
- Indomethacin : Sedation is adverse effect
- Piroxicam : Longest acting NSAID
- Nimesulide : Not used in children (hepatotoxic)
- Ketorolac : Given IV
Selective COX 2 Inhibitors
Drugs
- Celecoxib
- Rofecoxib
- Valdecoxib
- Parecoxib
- Lumiracoxib
••These have lesser risk of causing PUD
••These increase the risk of MI and stroke
- Etoricoxib Longest acting
- Rofecoxib and ValdecoxibWithdrawn because of MI
and stroke
- Parecoxib is given by Parenteral route
- Lumiracoxib is withdrawnDue to Liver toxicity
GOUT
It is characterized by increase in serum uric acid.
Acute Gout
1. DOC : NSAIDs (except aspirin and paracetamol)
2. Steriods : If NSAIDs do not work
3. Colchicine (Most effective drug):
Q
- Can cause myopathy and diarrhea
- Inhibit granulocyte migration
Chronic Gout
Three types of drugs can be used in chronic gout.
– Drugs decreasing production of uric acid
– Drugs increasing excretion of uric acid
(Uricosuric agents)
– Drugs increasing metabolism of uric acid
Proteins / Purines
Xanthine
Uric acid Excretion
1
2
3
Allantoin
Uricase
In birds
Xanthine oxidase
26Cerebellum Quick Revision Notes
1. ↓ Formation 2. ↑ Excretion
Allopurinol
Q
••Inhibit xanthine oxidase
••DOC for chronic gout
Febuxostat
••Inhibit xanthine oxidase
Probenecid
Sulfinpyrazone
Lesinurad
→ Plenty of fluids should
be taken
3.↑ Metabolism
Rasburicase → Recombinant uricase
Pegloticase → Long acting uricase
These are fastest urate lowering agents for tumor
lysis syndrome
Q
RHEUMATOID ARTHRITIS
NSAIDs and Steroids DMARDs or SAARDs
••↓ Pain and lnflammation
••No effect on disease
Progression
••Fast acting
••Slow down the disease
progression
••Slow acting
1. Conventional DMARD:
Cute andChloroquine
DMARD of choice in
pregnancy
p Penicillamine
Used for Cu poisoning/
Wilson’s disease
A Azathioprine
G Gold salts
L LeflunomideFastest acting DMARD
Q
I
Inhibitors of
JAK
Tofacitinib
Baricitinib
Malika Methotrexate
DOC, Needs LFT
Monitoring
SherawatSulfasalazine
DOC for ulcerative
colitis
2. Biological DMARDs:
i. Drugs Inhibiting TNF-a:
Q
- All are injectable
A Adalimumab
C Certolizumab
E Etanercept
Inhibitor lnfliximab
Goli Golimumab
→ ↑ Risk of infections.
→ Contra-indicated in T.B. and Hepatitis B
→ Apart from R.A., these drugs can be used for Crohn’s
disease as well as Psoriasis
ii. IL - 1 Receptor Antagonist:
Q
ANAKINRA
––A - 1st letter
––KIN - Interleukin
––R - Receptor
––A - Antagonist
iii. IL - 6 Receptor Antagonists:
Q
Tocilizumab
→ 1
st
IL- 6 targeted monoclonal Antibody.
→ Approved for treatment of cytokine release
syndrome also.
Sarilumab
→
Used for rheumatoid arthritis
S - Six
AR -
R.A.
MAB - Monoclon al antibodyiv. Co-stimulation Inhibitors
Q
•• Abatacept
•• Inhibit the interaction of T-cell and Antigen
Presenting Cells (APC).
27Pharmacology
Previous Years Questions
Q1. Most specific antiemetic for Chemotherapy induced
vomiting is:
A. Doxylamine B. Tegaserod
C. Granisetron D. Domperidone
Q2. Buspirone is a drug used in chronic anxiety. It
produce its action by acting on which of the following
receptors?
A. 5HT1A B. 5HT1B
C. 5HT2 D. 5HT3
Q3. A boy is planning to travel by bus. Which of the
following drug can be used to prevent motion sickness
in this person?
A. Promethazine B. Cetrizine
C. Loratidine D. Fexofenadine
Q4. Drug of choice for prophylaxis of migraine is
A. Propranolol B. Imipramine
C. Flutamide D. Flunarizine
Q5. A young female presented with left sided severe
throbbing headache associated with nausea, vomiting,
photophobia and phonophobia. Which of the following
drug can provide immediate relief to this patient?
A. Propranolol B. Sumatriptan
C. Topiramate D. Flunarizine
Q6. Drug of choice in paracetamol overdose is
A. N-acetylcysteine B. Dopamine
C. Hydralazine D. Furosemide
Q7. A 34 week pregnant female with polyhydramnios
presents with labour pain. She was treated with
indomethacin earlier. Which of the following can be
likely outcome in the baby if delivery occurs at this
time?
A. Patent ductus arteriosus
B. Premature closure of ductus arteriosus
C. Patent ductus venosus
D. Premature closure of ductus venosus
Q8. A 60 year old female with renal disease was
admitted for pyelolithotomy. Post operative analgesic
of choice in this patient is?
A. Diclofenac B. Indomethacin
C. Naproxen D. Acetaminophen
Q9. Which of the following is the fastest urate
lowering therapy in tumor lysis syndrome to prevent
renal damage?
A. Allopurinol B. Febuxostat
C. Rasburicase D. Furosemide
Q10. A female patient presented with pain and redness
in great toe. Serum uric acid level is 9.6 mg/dL. Apart
from prescribing analgesics for relieving pain, the
physician prescribed a drug which can decrease the
formation of uric acid. Which of the following enzyme
is likely to be inhibited by this drug?
A. Xanthine oxidase
B. Thymidylate synthase
C. Phosphpribosyl transferase
D. DHFR
Q11. Drug inhibiting granulocyte migration is:
A. Montelukast B. Cromoglycate
C. Colchicine D. Felbamate
Q12. Pegloticase is used for treatment of :-
A. Ankylosing spondylosis
B. CPPD
C. Chronic tophaceous gout
D. Refractory Rheumatoid arthritis
Answers
1. - C
2. - A
3. - A
4. - A
5. - B
6. - A
7. - B
8. - D
9. - C
10. - A
11. - C
12. - C
28Cerebellum Quick Revision Notes
Q13. A patient diagnosed with Rheumatoid arthritis was
on medications. After 2 years, he developed blurring
of vision and was found to have corneal opacity. Which
drug is most likely to cause this?
A. Sulfasalazine B. Chloroquine
C. Methotrexate D. Leflunomide
Q14. Tocilizumab is an immunosuppressive drug used
for Rheumatoid arthritis. It is a monoclonal antibody
against
A. IL-6 B. IL-12
C. IL-2 D. IL-3
Q15. A 40 year old male patient presents to hospital
with pain in great toe. It was diagnosed to be a case
of gout. Which of the following drug increases the
excretion of uric acid in urine?
A. Colchicine B. Probenecid
C. Allopurinol D. Febuxostat
Answers
15. - B13. - B
14. - A
Diuretics → Cause loss of Na
+
& H
2
O in urine
Classification Based On Site of Action
1. OSMOTIC DIURETICS
→ Includes mannitol
Uses:
••Acute Congestive Glaucoma
Q
••Cerebral edema
Contra-Indications:
••Cerebral hemorrhage
••Pulmonary edema
2. CARBONIC ANHYDRASE INHIBITORS
→ Acts on Proximal tubule
→ Include:
Acetazolamide – Given orally or IV
Brinzolamide
Dorzolamide
Indications:
Glaucoma (Angle closure glaucoma)
Mountain Sickness [DOC]
Q
Given as eye drops
3. LOOP DIURETICS
→ Act on thick ascending limb of loop of Henle
→ Inhibit Na
+
K
+
2Cl
–
symporter
→ Include
Furosemide
Torsemide
Bumetanide
→ High ceiling diuretics [High efficacy Diuretics]
Q
→ Effectve in renal failure
4. THIAZIDES
→ Act on early distal tubule
→ Inhibit Na
+
– Cl
–
symporter
Include
Thiazides Thiazide-like diuretics
Chlorothiazide
Methiazide
Polythiazide
Indapamide
Metolazone
Uses
••Hypertension (DOC)
Q
––Metolazone is effective in renal failure unlike
other thiazides
••Recurrent renal calcium stones
••Diabetes insipidus
••Osteoporosis
••Recurrent renal calcium stones
S/E of both Thiazides and Loop diuretics
↓ Na
+
↑ Glucose
↓ K
+
↑ Uric Acid
↓ Mg
2+
↑ Lipids
↓ H
+
Note: Loop diuretics cause hypocalcemia whereas
thiazides leads to hypercalcemia
5. K
+
SPARING DIURETICS
→ Act on collecting ducts
(1) Aldosterone Receptor Antagonists
––Spironolactone
––Epleronone
Chapter - 4 Diuretics
30Cerebellum Quick Revision Notes
Previous Years Questions
Q1. Which of the following drug is a carbonic anhydrase
inhibitor?
A. Acetazolamide B. Hydrochlorthiazide
C. Furosemide D. Mannitol
Q2. A 25 year old male presented to emergency with
head trauma due to road traffic accident. In hospital,
the patient developed seizures. Emergency CT scan
revealed widespread cerebral edema. Which of the
following is diuretic of choice for cerebral edema in
this patient?
A. Mannitol B. Spironolactone
C. Furosemide D. Hydrochlorthiazide
Q3. A 28 year old male went to Ladakh. He developed
shortness of breath. Which of the following drug will
you use for the treatment of mountain sickness at high
altitude?
A. Acetazolamide B. Furosemide
C. Epleronone D. Salbutamol
Q4. Hydrochlorothiazide works by inhibiting
A. Na
+
Cl
-
pump in DCT
B. Na
+
Cl
-
pump in PCT
C. Na
+
K
+
2 Cl
-
pump in descending limb of loop of
Henle
D. Na
+
K
+
2 Cl
-
pump in ascending limb of loop of Henle
Q5. At a high altitude of 3000m, a person complains
of breathlessness. All of the following can be used for
management of this person except
A. Intravenous digoxin
B. Oxygen supplementation
C. Immediate descent
D. Acetazolamide
Q6. Mannitol is used in the management of:
A. Congestive Cardiac Failure
B. Acute Congestive Glaucoma
C. Acute Renal Failure
D. Pulmonary edema
Q7. A patient of chronic liver cirrhosis presents with
ascites. Which of the following is the best diuretic to
be used in this patient?
A. Eplerenone B. Chlorthiazide
C. Furosemide D. Triamterene
Q8. Which of the following diuretic acts on the site X
shown in the figure?
A. Furosemide B. Hydrochlorthizide
C. Spironolactone D. Acetazolamide
Answers
1. - A
2. - A
3. - A
4. - A
5. - A
6. - B
7. - A
8. - B
(2) Epithelial Na
+
channel Blockers
––Triamterene
––Amiloride
These drugs cause
↓ Na
+
& H
2
O → Diuresis
↑ K
+
→ Hyperkalemia
↑ H
+
→ Metabolic Acidosis
Q
P → Potassium sparing Diuretics
A → Amiloride
S → Spironolactone → Cause Gynaecomastia
T → Triamterene
E → Epleronone → Do not cause Gynaecomastia
Uses:
- DOC for Conn’s Syndrome
- DOC for Edema in Cirrhosis
- DOC for Resistant hypertension
Chapter - 5 Cardiovascular System
CONGESTIVE HEART FAILURE
In low output CHF, heart is not able to pump enough
blood. It results in accumulation of fluid in various parts
of body.
ACUTE (DECOMPENSATED) CHF
Aim of treatment of Acute CHF
1. ↓ FLUID → Loop Diuretics
2. ↑ PUMPING → Inotropics
A. b1 Agonists
••Dopamine
••Dobutamine
••Nor-adrenaline
••Isoprenaline
B. Phosphodiesterase Inhibitors
[Inodilators]
••Inamrinone
••Milrinone
CHRONIC CHF (COMPENSATED)
Aim of Treatment in Chronic CHF
1. ↓ Work
2. ↓ Fluid
3. ↓ LVH [Cardiac Remodeling]
4. Inotropic action
Drugs Used In Chronic CHF
→ 4’D’ are used
Diuretics
Dilators
Decrease LVH
Digoxin
1. ↓ Work → Vasodilators
VenodilatorsArteriolar
dilators
Veno + Arteriolar
Dilators
↓ Preload
Nitrates
↓ Afterload
Hydralazine
↓ Preload and ↓
Afterload
Na Nitroprusside
ACE inhibitors
Angiotensin receptor
blockers
2. ↓ Fluid → Loop Diuretics
3. ↓ LVH [Cardiac Remodeling]
It results due to excessive aldosterone
→ These drugs decrease mortality in CHF
Q
A. Beta Blockers
B. ACE inhibitors
C. Angiotensin Receptor Blockers
D. Aldosterone Antagonists
32Cerebellum Quick Revision Notes
4. Contractility (Ionotropics)
DIGOXIN
→ Only inotropic drug that can be given Orally
MOA in CHF
→ Inhibit Na
+
- K
+
pump that ↑ intracellular calcium
and thus inotropic action.
MOA in Atrial Fibrillation
→ Vagomimetic effect lead to ↓ AV conduction
Q
Adverse Effects
1. Nausea, Vomiting [MC]
2. Arrhythmias
MC arrhythmia → Ventricular bigeminy
Q
Most specific → NPAT with AV Block
Q
3. Xanthopsia / Yellow Vision
Q
4. Gynaecomastia
Drugs Causing Gynaecomastia
DI : DIgoxin
S : Spironolactone
C : Cimetidine
K : Ketoconazole
O : Oestrogens
Factors ↑ Digoxin Toxicity
Metabolic Drugs
↑ Ca
2+
↓ K
+
↓ Mg
2+
Quinidine
Verapamil
Amiodarone
Thiazides and Clarithromycin
Mx of Digitalis Toxicity
Q
1. Correct the cause
2. DOC for Digitalis induced arrhythmias →
Lignocaine
3. Digibind for Severe poisoning
ANGINA PECTORIS
Drugs for Angina Pectoris
I. Nitrates
II. Calcium Channel Blockers
III. Beta Blockers
IV. Potassium Channel Openers
I. Nitrates
Mechanism of action:
Nitrates
↓
Nitric oxide
↓
Guanylate cyclase
↓
↑ cGMP
↓
Vasodilation (Veins >> Arteries)
→ MOA of nitrates in classical angina - ↓ Preload
→ MOA of nitrates in variant angina → Dilation of
coronary arteries
Q
Drugs
••Glyceryl Trinitrate / Nitroglycerine [GTN/ NTG]
••Isosorbide Dinitrate [IDN]
••Isosorbide Mononitrate [IMN]
••Penta Erythrital Tetra Nitrate [PETN]
••Amyl Nitrite [AN]
Nitrates
↓
NO
↓
↑ cGMP Degraded
↓
VD
↓
Hypotension
Nitrates should not be given with Sildenafil
[Risk of Severe hypotension]
Q
Sildenafil
PDE
33Pharmacology
GTN/NTG and IDN
••DOC for acute attack of angina
••Have high 1
st
pass metabolism
••Sublingual route preferred
→ IMN has minimum 1
st
pass metabolism
→ Longest acting → PETN
→ Shortest acting → AN
→ Amyl nitrite is used in cyanide poisoning as an antidote
→ Tolerance occurs, if nitrates are continuously
present in blood
→ To avoid tolerance, 6-8 hours of Nitrate Free
Period should be maintained
Q
ll. L-Type Calcium Channel Blockers
→ DOC for variant angina - CCB like verapamil
and diltiazem
→ Dipines are not used because they can worsen
angina due to reflex tachycardia
Q
III. Potassium Channel Opener
NICORANDIL
→ NO Releaser + K
+
channel opener
Q
IV. Beta Blockers
––Useful in classical angina (Act by ↓ HR)
––Contra-indicated in variant angina
New Drugs for Angina Pectoris
1. Bradycardiac Agent → Ivabradine
Q
Ivabradine inhibit Na
+
channel [Funny current] in SA
node
→ S/E → ↓ Visual acuity (Phosphenes)
2. Rho Kinase Inhibitor → Fasudil
Q
3. Metabolic Modulators
→ Fatty Acids require more oxygen for same energy
production than glucose
→ Metabolic Modulation → Making heart to utilize
glucose instead of fatty acids
Drugs
Q
1. Trimetazidine
2. Ranolazine
→ Main mechanism of ranolazine is now assumed to be
inhibition of Late Inward Na channels.
MYOCARDIAL INFARCTION (MI)
Non-STEMI
M → Morphine
O → Oxygen
N → Nitrates
A → Aspirin
STEMI
S → Streptokinase
O → Oxygen
N → Nitrates
A → Aspirin
M → Morphine
HYPERTENSION
1. First Line Drugs for Hypertension without any
compelling Indications are:
A – ACE inhibitors and ARB
Q
B – Beta Blockers (Not considered first line
drugs now)
C – Calcium channel blockers
D – Diuretics
ACE Inhibitors
••Name ends with pril
C → Cough
A → Angioedema
P → Prodrugs except captopril & Lisinopril
T → Taste alteration [Dysgeusia]
O → Orthostatic / Postural hypotension [max
with captopril]
Q
P → C/l in Pregnancy
R → C/lin B/L Renal Artery Stenosis
Q
I → C/I in Increased K
+
L → Lower the risk of Diabetic Nephropathy
ARBs [Angiotensin (AT1) Receptors Blockers]
- Name ends with ‘SARTAN‘
- All points about ACE inhibitors apply to ARB
also, except that these do not cause cough and
angioedema and ARB are not pro-drugs.
- Telmisartan is a PPAR-g agonist and can reverse
insulin resistance
Q
34Cerebellum Quick Revision Notes
2. DOC in special situations
Q
Condition DOC
HTN in pregnancy Oral Labetalol > Methyldopa
HTN Emergency in
pregnancy
IV Labetalol
HTN Thiazides
HTN Emergency Nicardipine > Nitroprusside
Resistant
Hypertension
(Resistant to
minimum 3 drugs
including thiazides)
Spironolactone
PULMONARY HYPERTENSION
Intravenous Vasodilator Testing (on giving IV CCB,
pulmonary artery pressure decreases)
→ If positive, DOC → CCB
Q
→ If negative, DOC → Endothelin antagonist
Q
DRUGS USED IN PULMONARY HYPERTENSION
1. Calcium channel blockers:
DHPs like amlodipine are DOC if IV vasodilator testing
is positive (in < 5% cases)
2. Endothelin antagonists:
Bosentan, ambrisentan like drugs are DOC for pulmo-
nary hypertension
3. PDEI [Phosphodiesterase Inhibitors]
→ Sildenafil, Tadalafil
4. Prostaglandins
PGI
2
→ lloprost
5. Selexipag
→ Prostacylin agonist
→ Can be given orally
SELE → Selective
XI → Non injectable [Oral]
P → PGI2
AG → Agonist
ANTI-ARRHYTHMIC DRUGS
Vaughan Williams Classification
→ Based on predominant mechanism of action
Class I → Na
+
Channel Blockers
Class II → b Blockers
Class III → K
+
channel blockers
Class IV → Ca
2+
Channel Blockers
Class V → Others
Class I Drugs
Q
→ Na
+
Channel blockers
→ ↓ Slope of Phase 0
ClassEffect on K
+
channelEffect on APDQT interval
1a Blocker ↑ ↑QT
1b Opener ↓ ↓QT
1c No effect - No effect
Class 1a Drugs Class 1b Drugs Class 1c
Drugs
Quinidine
Procainamide
Lignocaine
Phenytoin
Tocainide
Encainide
Flecainide
Cause QT Prolon-
gation
Used only for Ven-
tricular arrhythmia
Class II
→ Beta Blockers
Q
→ Used in Tachyarrhythmias
Class III
→ K
+
Channel Blockers
B → B retylium
I → I butilide
N
D → D ofetilide, Dronedarone
A → A miodarone
S → S otalol
→ Sotalol has both Class III [Major] & class II Actions
35Pharmacology
AMIODARONE
→ Longest acting [t1/2 → > 3wks] anti arrhythmic drug
→ MOA
1. Na
+
channel Blocker
2. Beta-Blocker (Non-competitive)
3. K
+
channel Blocker [Main action]
4. Calcium channel blocker
→ Adverse effect of amiodarone
Q
The Thyroid (hypo/hyper) (40% iodine is
present in amiodarone)
Periphery ofPeripheral neuropathy
My Myocardial depression
Lung Lung fibrosis
Liver Liver toxicity
Cornea is Corneal deposits
PhotosensitivePhotosensitivity (Rash on exposure
to sun)
(Bluish: Blue man syndrome)
Class IV
→ L-Ca
2+
Channel Blockers
––Verapamil
––Diltiazem
––DHPs [Not Used]
→ Used in Tachyarrhythmias
→ Should not be combined with β blockers [Risk of Severe
Bradycardia and AV Block]
Class V
Digoxin - Used for AF (in patients with CHF)
Atropine - DOC for Bradycardia & AV block
Adenosine - Shortest acting antiarrhythmic drug (t1/2
< 10s)
- DOC for PSVT
Q
ANTI-DYSLIPIDEMIC DRUGS
1. Statins
MOA
1. Inhibit HMG-COA Reductase (Rate limiting enzyme
in cholesterol synthesis)
Q
2. Compensatory ↑ of LDL - R
3. Cholesterol is taken from blood
4. ↓ Serum cholesterol
Examples
––Atorvastatin
––Rosuvastatin [Longest Acting]
––Pravastatin
––Simvastatin
Important Points
A. Statins have maximum LDL – Cholesterol lowering
potential
B. Given at late evening/night
••Atorvastatin & Rosuvastatin are long acting, can be
given at anytime of the day
••Rosuvastatin is longest acting statin.
Q
C. Adverse Effects
Q
––Myopathy → Risk further ↑ with Fibrates
and enzyme inhibitors like clarithromycin and
erythromycin.
––Hepatotoxicity
––Hyperglycemia: ↑ Risk of new onset DM.
D. Pleiotropic Effects
Q
These are additional benefits apart from improving
lipid profile.
PL → Plaque Stabilization
E → ↓ Endothelial dysfunction
I → ↓ Inflammation
O → ↓ Oxidative Stress
TR → ↓ Thrombosis
Opic
36Cerebellum Quick Revision Notes
2. Other Drugs
Fibrates Clofibrate
Fenofibrate
• Max TG lowering potential
• S/E → Gall Stones
Q
Ezetimibe Inhibit absorption of cholesterol from intestineUsually combined with statins
BABA Cholestyramine
Colestipol
DOC in pregnancy and children
S/E → ↑ TG
Niacin Vitamin B3 Max. HDL - C increasing potential
Compliance limiting S/E → Itching & flusing
Hyperuricemia
Q
Hepatotoxicity
3. New Drugs
A. PCSK - 9 (Pre Protein ConvertinSubtilisinKexin Type 9) Inhibitors
Q
••PCSK-9 binds to LDL - receptors and take it to lysosomes that result in breakdown of LDL receptors.
••Thus PCSK 9 inhibitors prevent breakdown of LDL receptors. When more LDL receptors are present, they can
take up more LDL-cholesterol from blood.
••So, we can use these drugs as hypolipidemic drugs.
••Alirocumab and Evolocumab are monoclonal antibodies against PCSK-9
B. MTP (Microsomal Triglyceride Triglyceride Transport Protein) Inhibitors
••Triglycerides are packed in VLDL by MTP
••Drug inhibiting MTP is Lomitapide
C. Evinacumab
••Monoclonal antibody against ANGPTL1 (Angiopoietin Like Protein 3)
••It acts independent of LDL-receptor density.
37Pharmacology
Previous Years Questions
Q1. A hypertensive patient has grade 4 renal failure
and GFR less than 30 mL/min. The physician wants to
prescribe a thiazide diuretic. Which is the best drug
for this patient?
A. Hydrochlorthiazide
B. Chlorthalidone
C. Metolazone
D. Indapamide
Q2. A patient with chronic stable angina presents with
pedal edema, breathlessness and other symptoms of
heart failure. Which of the following drug can increase
longevity in this patient?
A. Nifedipine B. Digoxin
C. Lisinopril D. Torsemide
Q3. Drug of choice for treatment of digoxin induced
ventricular arrhythmias is?
A. Atropine B. Lidocaine
C. Amiodarone D. Procainamide
Q4. A patient on digoxin therapy accidently consumed
8 tablets of digoxin 0.25 mg. Two hours later, he
presented to emergency with heart rate of 54 bpm and
ECG evidence of third-degree AV block. What is the
immediate management of this patient?
A. Digoxin immune Fab
B. Lignocaine
C. Phenytoin
D. DC cardioversion
Q5. A patient on digoxin therapy and had a level of 1 ng/
ml. He was receiving several other drugs and presented
2 months later with flattening of T waves in ECG. Now
the plasma level of digoxin is 3.8 ng/ml. Which of the
following drug is likely to be responsible?
A. Triamterene B. Atenolol
C. Clarithromycin D. KCl
Q6. All of the following drugs are indicated in the
treatment of NSTEMI except
A. Clopidogrel B. Aspirin
C. Streptokinase D. Prasugrel
Q7. Which of the following is a K
+
Channel Opener?
A. Ranolazine B. Nicorandil
C. Verapamil D. Quinidine
Q8. Which of the following is a late inward sodium
channel blocker?
A. Ivabradine B. Ranolazine
C. Trimetazidine D. Fasudil
Q9. Which of the following drug acts at the site marked
by arrow as shown in the diagram
A. Aliskiren B. Ramipril
C. Losartan D. Spironolactone
Answers
1. - C
2. - C
3. - B
4. - A
5. - C
6. - C
7. - B
8. - B
9. - B
38Cerebellum Quick Revision Notes
Q10. Which of the following antihypertensive drug is
avoided in patients with high serum uric acid levels?
A. Hydrochlorothiazide
B. Enalapril
C. Prazosin
D. Atenolol
Q11. A 34 weeks pregnant lady presented with seizures.
Her blood pressure is 200/110 mm Hg. Which drugs
should be used for the treatment of this patient?
A. Oral Labetalol
B. IV labetalol plus magnesium sulphate
C. IV Lorazepam
D. IV Enalapril
Q12. Drug used for treatment of pregnancy induced
hypertension is
A. Alpha methyl dopa B. Lisinopril
C. Hydralazine D. Telmisartan
Q13. A 56 year old patient who is a known case of
hypertension was being treated with antihypertensive
drugs. He is having chronic cough since 2 weeks. He was
started on antimicrobials but cough did not resolve.
Which of the following antihypertensive drug may
induce chronic cough in this patient?
A. Lisinopril B. Minoxidil
C. Propranolol D. Amlodipine
Q14. A 26 year old female came to hospital for pre-
conceptional counselling. Patient is a known hypertensive
compliant to drug therapy. Which of the following drugs
will you advise to stop?
A. Methyl dopa B. Labetalol
C. Lisinopril D. Nifedipine
Q15.Identify the correct match regarding the drug and
its adverse drug reaction?
A. Hydralazine: Heart failure
B. Verapamil: Constipation
C. Aliskiren: Hypokalemia
D. Atenolol: Hemolytic anemia
Q16. Resistant hypertension is defined as inability to
attain goal blood pressure inspite of the concurrent
use of 3 antihypertensive agents of different classes
prescribed at optimal doses including
A. Alpha blockers B. Diuretics
C. Reserpine D. Alpha methyl dopa
Q17. A 45 year old patient presented with the symptoms
shown in image below. Patient is a known hypertensive
and was taking some antihypertensive drug. Which of
the following drug is the likely cause of this condition?
A. Lisinopril B. Clonidine
C. Nifedipine D. Timolol
Q18. Which of the following drug should be stopped in a
patient with hyperkalemia?
A. Losartan B. Furosemide
C. Amlodipine D. Hydrochlorthiazide
Q19. A patient presents with grade 2 pulmonary artery
hypertension. Vaso-reactive stimulation test is negative.
Which is the most preferred initial management of this
patient?
A. Epoprostenol B. Amlodipine
C. Alprostadil D. Ambrisentan
Answers
10. - A
11. - B
12. - A
13. - A
14. - C
15. - B
16. - B
17. - A
18. - A
19. - D
39Pharmacology
Q20. A 65-year-old man comes to OPD with history of
fall. He is hypertensive with history of atrial fibrillation
and is presently on captopril, atenolol, aspirin and
amiodarone. He presents with the following finding as
shown in the image. What is the most probable diagnosis?
A. Silver toxicity
B. Lupus pernio
C. Amiodarone induced skin lesion
D. Captopril toxicity
Q21. Which of the following antiarrhythmic drug
is contraindicated in a patient with interstitial lung
disease?
A. Amiodarone B. Sotalol
C. Quinidine D. Lignocaine
Q22. The figure below shows the effect of a drug on
the action potential of heart as shown by arrow. Which
of the following drug is likely to produce this effect on
action potential?
A. Quinidine B. Lignocaine
C. Esmolol D. Tocainide
Q23. Which of the following drug should be avoided in
a patient on rosuvastatin therapy?
A. Clarithromycin B. Oxycodone
C. Rivaroxaban D. Adalimumab
Q24. Which of the following hypolipidemic drug acts by
inhibition of PCSK-9?
A. Atorvastatin B. Evolocumab
C. Ezetimibe D. Lomitapide
Q25. Which of the following anti-dyslipidemic drugs
can result in gall stones?
A. Statins B. Bile acid sequestrants
C. Niacin D. Fibrates
Answers
20. - C
21. - A
22. - A
23. - A
24. - B
25. - D
PITUITARY HYPOTHALAMIC SYSTEM
Anterior Pituitary Hypothalamic control
Growth Hormone [GH]
GHRH [GH Releasing Hormone]
GHIH [GH Inhibiting Hormone]
Thyroid Stimulating HormoneThyrotropin Releasing Hormone
Adreno corticotropic HormoneCorticotropin Releasing Hormone
Gonadotropins GnRH [Gn Releasing Hormone]
Prolactin Prolactin Inhibiting Hormone
1. Growth Hormone Inhibiting Hormones [GHIH]
––It is also known as Somatostatin
SOMA TOSTATIN USES
Q
S → Secretory Diarrohea (Carcinoid syndrome, VIPoma)
O → Oesophageal Varices
M → Malignancy [Insulinoma, Glucagonoma]
A → Acromegaly
→ Any drug ending with “tide” is peptide.
→ Any endogenous substance ending with “in” is a
peptide
e.g; Somatostatin
Vasopressin
Oxytocin
→ Peptides cannot be given orally
Somatostatin → Short acting therefore not used
Octreotide → Long-acting somatostatin derivative
→ Given by SC route
2. Prolactin Inhibiting Hormone [PIH] =
Dopamine [DA]
→ DA acts through D2 Receptors
→ Dopamine D2 Agonists decrease prolactin
Examples
Bromocriptine
Cabergoline [Long acting]
Uses of Dopamine Agonists
Q
1. Leuprolide
2. Nafarelin (nasal route)
3. Goserelin
4. Busurelin
5. Histarelin
→ Not effective orally (Mostly given by subcutaneous
route)
→ Flare up Reaction: When these are given in continuous
Chapter - 6 Endocrine system
41Pharmacology
manner, for initial few days, there is aggravation of
disease
GnRH Antagonists
Q
1. Cetrorelix
2. Ganirelix
3. Aba relix
4. Dega relix
→ No Flare up reaction
→ But they do not ↑ sex hormones (Used only to ↓ sex
hormones)
→ Not effective orally
ELAGOLIX
→ Recently approved oral GnRH antagonist
→ Approved for pain due to Endometriosis
POSTERIOR PITUITARY
→ Secretes two main hormones
••Oxytocin
••Vasopressin
Oxytocin
––Main function is to contract the uterus
••DOC for augmentation of labour
••DOC for postpartum hemorrhage
––Other function is ejection of milk
••DOC for Breast engorgement
Vasopressin
––Also known as anti diuretic hormone (ADH)
Vasopressin Receptors
V
1
Receptor
––Present on BV
––Cause vasoconstriction
V
2
Receptor
––Present on kidney
––↓ Urine.
Vasopressin Receptor Agonists
––V
1
agonist is terlipressin
••DOC for esophageal varices
Q
––V
2
agonist is desmopressin
••DOC for neurogenic (central) diabetes
insipidus (Given by nasal route)
Q
Vasopressin Receptor Antagonists
––VAPTANS: VAsoPressin ANTagonists
Q
––Examples
Coni vaptan - Given via Intravenous route
Tol vaptan - Given via Oral route
––Used for SIADH
THYROID
Hypothyroidism
––DOC is L-thyroxine (T4)
––Started at 25 mcg daily
––Gradually the dose is increased
Hyperthyroidism
1. Thyroid Peroxidase Inhibitors (Thioamides)
Carbimazole (Prodrug)
Methimazole (Active)
Propyl Thio Uracil (PTU)
→ Crosses placenta easily→ Less crossing of Placenta
→ DOC for all patients
except in 1st trimester
of pregnancy
→ DOC in 1st trimester
Q
→ Can cause choanal
atresia and aplasia cutis
in developing fetus
Q
→ Lesser chance
2. Secretion Inhibitors
• Nal
• Kl
• Lugol’s Iodine
→ Fastest acting anti-thyroid drugs.
→ Given preoperatively:
––To make the gland small, firm and less vascular
––To reduce the blood loss during surgery.
42Cerebellum Quick Revision Notes
3. Radioactive iodine or I
131
→ C/I in pregnancy
Q
→ Cause irreversible hypothyroidism
→ Physical t ½ is 8 days
– Acts by stimulating
glucagon receptors on
heart
INSULIN
Indications
1. All patients of type 1 DM
2. Uncontrolled patients of type 2 DM
3. Diabetes in pregnancy
4. Diabetic Ketoacidosis
Routes of Administration
1. Sub - cutaneous route:
––MC route (because self-administration is
possible with this route)
––All insulin preparations can be given by
subcutaneous route.
––Site of administration
••Entire abdomen except area around umbilicus
(thickness of skin is not uniform, so insulin
absorption is affected)
••Anterior thigh
••Lateral thigh
••Arm
2. Intravenous route:
••Only regular insulin can be given
••So, insulin of choice in diabetic Ketoacidosis
→ Regular insulin
3. Inhalational route:
Afreeza → Short acting insulin → So, should be
given before every meal
INSULIN ANALOGUES
Rapid acting Ultra-Long Acting
••LISPRO
••ASPART
••GLULISINE
••GLARGINE
••DETEMIR
••DEGLUDEC (Longest Acting)
Q
- These are peakless insulins
- These have low risk of hypoglycemia
Side Effects
1. Hypoglycemia
2. Hypokalemia
Q
ORAL ANTI DIABETICS DRUGS
1. Insulin Secretagogues (Act by ↑ Insulin secretion)
Q
––These drugs secrete insulin and thus can cause
hypoglycemia
Sulfonylureas Meglitinides
1
st
Generation Nateglinide
Repaglinide
Chlorpropamide
Tolbutamide
2
nd
Generation
Glipizide
Gliclazide
Glibenclamide
Drugs ending with “IDE” can cause - hypoglycemia
Q
43Pharmacology
2. Drugs Acting by Other Mechanisms
A. Metformin
Adverse effects
1. Megaloblastic Anemia
2. Lactic acidosis
Risk of lactic acidosis further ↑, if there is
Q
––Liver disease (Gluconeogenesis cannot occur)
––Renal disease (Lactic acid produced cannot be
excreted)
––Any condition predisposing to hypoxia (e.g.;
Shock, COPD)
Thus, metformin is C/I in these patients.
Indications
→ Metformin is DOC for Type 2 DM because:
––No risk of hypoglycemia
––Max. reduction in HbA1c
Q
––Can cause weight loss or weight neutral (No weight gain)
B. Glitazones
E.g. Troglitazone
Rosiglitazone
Pioglitazone
Mechanism
Act by stimulating PPAR-ꝩ→Reversal of Insulin Resistance
Adverse Effects
1. Hepatotoxic
→ Max. hepatoxicity → Troglitazone [withdrawn]
Q
→ Rosiglitazone and Pioglitazone require LFT
monitoring
Q
2. Na
+
and water Retention → Avoid in CHF and HTN
Q
3. Predispose to osteoporotic fractures.
4. ↑ Risk of Ml by rosiglitazone
5. ↑ Risk of urinary bladder carcinoma by Pioglitazone
Q
C. Acarbose
→ Act by inhibiting the intestinal absorption of
carbohydrates (blood sugar decreases)
→ Does not cause hypoglycemia
→ Flatulence → MC side effect
→ C/I in lnflammatory bowel disease
Q
••Ulcerative colitis
••Crohn’s disease
NEW ANTIDIABETIC DRUGS
1. Incretin – Mimetics
→ Incretins are normal physiological substances
which are released in GIT after food intake that
stimulate the release of insulin.
→ Most important endogenous incretins are GLP
(Glucagon like peptide) and GIP (Glucose
stimulated insulinotropic polypeptide)
→ Functions of Incretins:
––Increase insulin release
––Decrease gastric motility
→ GLP is metabolized by DPP-4 and becomes inactive
A. GLP analogues:
→ Given subcutaneously (Cannot be given orally since these are peptides)
GLP-1 analogues : Used for type 2 DM
Q
––Exenatide
––Liraglutide
GLP-2 analog : Used for short bowel syndrome
Q
––Teduglutide
Side effects
––Acute pancreatitis (Major side effect)
––Increased risk of Medullary carcinoma of Thyroid
44Cerebellum Quick Revision Notes
B. DPP - 4 inhibitors:
a. Sitagliptin
b. Vildagliptin
c. Alogliptin
d. Linagliptin
→ Gliptins are oral anti - diabetic drugs.
––Pancreatitis is the major adverse effect
––Gliptins are contraindicated in renal failure
except Linagliptin which is safe in renal failure
2. SGLT-2 Inhibitors:
→ Glucose is freely filtered by glomerulus but the
clearance of glucose in urine is negligible.
→ Because the reabsorption takes place in proximal
tubule by sodium glucose transporter (SGLT-2)
→ SGLT-2 inhibitors stop the reabsorption of glucose
in PT resulting in glucosuria.
Drugs are
Q
––Canagliflozin
––Dapagliflozin
––Empagliflozin
––Ertugliflozin
––Most common side effect of SGLT-2 Inhibitors
is Urinary Tract infections
––SLGT-2 inhibitors provide cardiovascular benefits.
These are approved for treatment of CHF.
3. Amylin Analogs:
→ Amylin is secreted form β - cells of pancreas.
→ Function of amylin is to ↓ blood sugar.
→ Pramlintide is an amylin analogue
→ It is approved for both type 1 and 2 diabetes.
4. Bromocriptine
Q
→ Decreases insulin resistance and it has been
recently approved for type 2 diabetes treatment.
→ Given in small dose and taken at early morning
on awakening.
ADRENAL
Adrenal Medulla Adrenal Cortex
→ Secretes
––Adrenaline
––Nor-Adrenaline
––Dopamine
→ Secretes
––Glucocorticoids
––Mineralocorticoids
Mineralocorticoids
Aldosterone → Major endogenous Mineralocorticoid
Actions
– Retain Na+ and water
– Remove K
+
and H
+
Glucocorticoids
Hydrocortisone → Major endogenous Glucocorticoid
CLASSIFICATION OF DRUGS
Glucocorticoids Mineralocorticoids
Short Acting (<12 hours)
Cortisone
Hydrocortisone
Aldosterone
Fludrocortisone
DOCA
Intermediate Acting (12-36 hours)
Prednisone
Prednisolone
Triamcinolone
Long Acting (> 36 hours)
Dexamethasone
Betamethasone
Paramethasone
Special Points
Q
Property Drug
Maximum G activity Dexamethasone
Maximum M activity Aldosterone
G with max M activity Hydrocortisone
M with max G activity Fludrocortisone
Selective G
Triamcinolone
Dexamethasone
Betamethasone
45Pharmacology
Selective M DOCA
Note: G means glucocorticoid (anti-inflammatory)
M means mineralocroticoid (Na
+
and H
2
O retaining)
Uses of Corticosteroids
Antenatal Replacement Other Uses
Dexa /
Betamethasone
for fetal
lung maturity
(Glucocorticoids
increase
surfactant
production)
Acute Adrenal
insufficiency /
Addisonian crisis
[by IV]
Chronic Adrenal
lnsufficiency /
Addison’s disease
[by oral]
Inflammation
Auto immune
diseases
Transplantation
Anticancer therapy
Asthma
Ante Natal Steroids Total dose Total duration
Betamethasone → IM 12 mg
every 24 hrs. x 2 Doses
Q
24 mg 48 hrs.
Dexamethasone → IM 6 mg
every 12 hrs. x 4 Doses
24 mg 48 hrs
Hypothalamo-Pitutary-Adrenal Axis [HPA Axis]
HPA Axis Suppression
→ Occurs when corticosteroids are given continuously
for > 2wks
Preventive Measures
1. Stop unnecessary use of steroids
2. If indicated, prescribe them for minimum period
preferably < 2wks
3. If indicated for long periods, prescribe them on
alternate day
––Long-acting steroids (dexa, beta and
paramethasone) are avoided
4. If indicated daily and for longer periods
––Don’t Stop Abruptly
––Tapering should be done
Adverse effects
Major adverse effect is Cushing syndrome
OSTEOPOROSIS
Nutritional
factors
– Calcium
– Vitamin D
Inhibit
osteoclast – Calcitonin – Estrogens – SERMs – Denosumab – Cinacalcet Stimulate osteoblast – PTH
1-34
Drugs used in Osteoporosis
Dual action – Strontium – Romosozumab
Nutritional Factors
––Calcium is given at a dose of 1200 mg/day (It
includes dietary calcium)
––Vitamin D should be given as 800 IU per day
Drugs Inhibiting Osteoclast
1. Calcitonin: Given Intranasally
2. Bisphosphonates
Q
Alendronate
Risedronate
Zoledronate
––Inhibit osteoclasts
––DOC for Osteoporosis [Osteoporosis due to any
reason]
46Cerebellum Quick Revision Notes
––These are indicated for a period of maximum 10
years
––Highly toxic to esophagus
Prevention of Oesophagitis
Q
– Take empty stomach
– Take with full glass of water
– Remain upright for 30 min
3. Estrogen and SERM
Decreased estrogen is responsible for post-
menopausal osteoporosis
Actions of Estrogen
Bone → Prevent resorption
Blood → ↑ HDL/LDL Ratio
Breast → ↑ Risk of Carcinoma
Endometrium → ↑ Risk of Carcinoma
Liver → ↑ Clotting Factors → Thromboembolism
→ Not preferred for Rx of PM Osteoporosis
Raloxifene
Q
––It is selective estrogen receptor modulator
––It has agonist action on ER in bone, blood and
liver whereas antagonistic action on breast and
endometrium
––Used in post menopausal osteoporosis
––Additional Benefits
••↑ HDL
••↓ Breast and Endometrial carcinoma risk
––Major S/E → Thromboembolism
4. Denosumab
DRUGS STIMULATING OSTEOBLASTS
1. Teriparatide
––Parathyroid hormone contains 84 amino acids
(i.e., PTH1-84).
––Full molecule stimulates osteoclast and induces
osteoporosis by resorption of bone.
––Teriparatide is a fraction of parathyroid (PTH
1-34) that stimulates Osteoblast and is used for
osteoporosis treatment.
Q
––Route of administration - Not effective orally
(given subcutaneously)
––PTH
1-34
is recommended for maximum 2 years.
––Treatment with PTH
1-34
should be followed by
bisphosphonates. DRUGS WITH DUAL ACTION
Q
––These have dual activity of stimulating osteoblast and inhibiting osteoclast
––Strontium ranelate and romosozumab act by
dual mechanism
––Romosozumab is a monoclonal antibody against
sclerostin
ANDROGENS
––5α reductase converts testosterone into
Dihydrotestosterone (DHT) which works on
androgen receptors. Testosterone also can
directly work on androgen receptors.
––In treatment of prostatic cancer androgen
receptor blockers are commonly used.
––In treatment of BPH and androgenital alopecia
(Male pattern baldness): 5 α-reductase inhibitors
like finasteride are used.
––On the surface of osteoclast cells, RANK
receptors are present. When ligand binds to
RANK receptors, it stimulates the resorption of
bone.
––Denosumab is a monoclonal antibody against
RANK ligand. It inhibits the osteoclastic activity
and resorption of bone.
Q
47Pharmacology
––Both the class of drugs can cause impotence as an
adverse effect
ORAL CONTRACEPTIVES
1. COMBINED ORAL CONTRACEPTIVE PILLS
→ Drugs
••Estrogen - Ethinyl Estradiol
••Progesterone - Levonorgestrel
→ Dosage
••1 tablet daily for 21 days from 1st day of
menstrual cycle
••No tablet for next 7 days
••To ↑ compliance: 28 tablets strip with 1st
21 tablets contains drug and next 7 tablets
contains iron
→ Missed Tablets
If one tablet is missed Take 2 tablet on next day
If 2 or more tablets
missed
••Discard remaining tablets
••Practice other method of
contraception with it.
••Start a fresh from next
cycle
2. POP / MINIPILLS
––Used where Combined OCPs cannot be used
––Contains LNG
––OCP of choice in lactation
Q
3. EMERGENCY CONTRACEPTIVES
A. Combined Oral Contraceptives
B. Progesterone Only Pills [LNG]
C. Mifepristone
Above 3 drugs should be used with in 72 hrs. of
unprotected intercourse.
D. Ulipristal
→ Can be used within 120 hours of unprotected
intercourse
NON CONTRACEPTIVE BENEFITS
OF OCPs
Other → ↓ Ovarian cyst [DOC for PCOD]
B → ↓ Benign Breast Disease
E → ↓ Endometriosis
N → ↓ Neoplasia [Endometrial and ovarian cancers]
E → ↓ Ectopic pregnancy
F → ↓ Fibroid
I → ↓ Iron deficiency Anemia
T → ↓ Premenstrual Tension Syndrome
S → ↓ Skeletal Disease [Osteoporosis]
↑ Risk of
––Cervical Ca
––Breast Ca
↓ Risk of
––Endometrial Ca
––Ovarian Ca
OCPs
POLYCYSTIC OVARIAN DISEASE
(PCOD)
––OCPs are DOC for regulating the menstrual
cycle in PCOD
––Metformin is used to reverse insulin resistance
––Ovulation inducers are used to induce ovulation
Q
••Aromatase inhibitors e.g. letrozole is DOC
••Clomiphene citrate can also be used.
48Cerebellum Quick Revision Notes
Q6. A 28 year old female with Graves’ disease was taking
medication for hyperthyroidism during pregnancy.
She delivered a child with congenital anomaly ‘aplasia
cutis congenita’. Most likely drug implicated for this
teratogenic effect is?
A. Carbimazole B. Levo-thyroxine
C. Methylthiouracil D. Liothyronine
Q7. Drug of choice for hyperthyroidism in third
trimester of pregnancy is
A. Carbimazole B. Propylthyouracil
C. Sodium iodide D. Radioactive iodine
Q 8. A 30 year old female presented with weight gain
and cold intolerance. On investigations Value of T3 is
70 ng/dl (reference value 100-200 ng/dl),T4 is 3 mcg/
dl (reference value 5-12 mcg/dl) and TSH is 20 mIU/L
(reference value 0.5-5 mIU/L). Which of the following
statement is correct regarding the management of this
patient?
A. Measure T3, T4 and TSH after one month
B. Start L-thyroxine (T4) treatment 100 mcg once
daily
C. Start L-thyroxine (T4) treatment 25 mcg daily and
gradually increase
D. Start daily L-thyroxine (T4) 100 mcg with Liothy-
ronine (T3) 5 mcg
Q 9. What is the Drug of choice for Hyperthyroidism in
first trimester of Pregnancy?
A. Lugol’s iodine B. Methimazole
C. Propylthiouracil D. Carbimazole
Q 10. Which of the following drug is given pre-operatively
to decrease the risk of intraoperative bleeding in a
hyperthyroid patient planned for thyroidectomy?
A. Potassium iodide B. Propranolol
C. Propylthiouracil D. Methimazole
Previous Years Questions
Q1. A patient was operated for prostate carcinoma and
during surgery local metastasis was noted. Which of the
following drug this patient should receive?
A. Leuprolide B. Desmopressin
C. Octreotide D. Tamsulosin
Q2. Tolvaptan is used for:
A. SIADH
B. Central Diabetes Insipidus
C. Von Willebrand Disease
D. Catecholamine resistant Shock
Q3. A patient presents with pituitary tumor that
overproduces growth hormone. surgical removal of the
tumor was incomplete. What is the first line treatment
of this patient?
A. Leuprolide B. Octreotide
C. Nafarelin D. Goserelin
Q4. A 40 year old male presents with protrusion of chin,
excessive sweating, impaired glucose tolerance and
enlargement of hands and feet? Which of the following
drugs is a growth hormone receptor antagonist used to
treat this condition?
A. Pegvisomant B. Octreotide
C. Cabergoline D. Olcegepant
Q5. A female presented with galactorrhea. Her urine
pregnancy test was negative. MRI of head revealed
a large pituitary tumor. Patient refused to undergo
surgery for the tumor. Which of the following is the
best drug for the treatment of this patient?
A. Octreotide B. Bromocriptine
C. Promethazine D. Clozapine
Answers
1. - A
2. - A
3. - B
4. - A
5. - B
6. - A
7. - A
8. - C
9. - C
10. - A
49Pharmacology
Q 16. Which of the following drug is given to mother
delivering premature baby for fetal lung maturation?
A. Aspirin
B. Dexamethasone
C. Magnesium sulfate
D. Depot medroxy progesterone acetate
Q 17. A patient presented with the following features
after chronic intake of a drug for several years. Which
is the likely drug person has consumed?
A. Paracetamol B. Prednisolone
C. Phenytoin D. Metformin
Q 18. What is the prenatal dose of dexamethasone
given for lung maturation in premature infants ?
A. 6 mg 2 doses 12 hours apart
B. 12 mg 2 doses 24 hours apart
C. 6 mg 4 doses 12 hours apart
D. 6 mg 4 doses 24 hours apart
Q 11. A 70 year old patient has diabetes mellitus and
hypertension. He presents with late stage chronic
kidney disease. Which of the following anti-diabetic
drugs require least dose modification in renal disease?
A. Sitagliptin B. Vildagliptin
C. Linagliptin D. Saxagliptin
Q 12. A 50 year old patient of type 2 diabetes mellitus
was controlled on oral hypoglycemic drugs. This patient
presented to hospital with profuse sweating and
dizziness. There was presence of hypoglycemia. Which
among the following drugs can result in hypoglycemia in
this patient?
A. Metformin B. Voglibose
C. Vildagliptin D. Glipizide
Q 13. Which of the following anti-diabetic drugs is
associated with increased risk of fractures in a female
with osteoporosis?
A. Canagliflozin B. Rosiglitazone
C. Voglibose D. Rapaglinide
Q 14. Mechanism of action of exenatide in diabetes
mellitus is
A. It is analogue of GLP released from gut and in-
crease glucose dependent insulin secretion
B. It is DPP-4 inhibitor and result in decreased
breadkdown of GLP
C. It inhibits SGLT-2 and cause glucosuria
D. It is amylin analogue and decrease glucagon
Q 15. To minimize the risk of HPA axis suppression,
what is the correct method of administration of
prednisolone?
A. Give at night just before bedtime
B. Divide in three doses and give small doses 8 hourly
C. Give on alternate day
D. Replace with betamethasone
Answers
11. - C
12. - D
13. - B
14. - A
17. - B
18. - C
15. - C
16. - B
50Cerebellum Quick Revision Notes
Q 19. Which of the following is not used in treatment of
polycystic ovarian disease?
A. Letrozole
B. Clomiphene citrate
C. Ulipristal
D. Combined oral contraceptives
Q 20. Combined oral contraceptive pills act by all of the
following mechanisms except?
A. Inhibit implantation by bringing change in the uterus
B. Inhibit ovulation
C. Makes cervical mucus thick and hostile
D. Increase gonadotropin secretion
Answers
19. - C
20. - D
21. - A
22. - A
Q 21. A 22 year old female presents 8 hours after
sexual assault. It is the 13
th
day of her menstrual cycle.
Which emergency contraceptive should be prescribed
to her?
A. Levonorgestrel 1.5 g single tablet
B. Injection DMPA
C. OCP from day 1 of next cycle
D. Misoprostol
Q 22. Which of the following is not used as emergency
contraceptive?
A. Danazol
B. Levonorgestrel
C. Mifepristone
D. IUCD
Chapter - 7 Central Nervous System
NEURODEGENERATIVE DISEASES
These occur due to age related degeneration of neurons
ALZHEIMER’S DISEASE
––It occurs due to age related degeneration of
cholinergic neurons in basal nucleus of Meynert.
––Aβ-amyloid deposition is the underlying cause of
neuronal degeneration.
––It is characterized by loss of memory (Dementia)
DRUGS USED
1. AChE inhibitors:
Q
Lipid soluble drugs which have very high entry in the
brain are preferred.
Donepezil
Rivastigmine
These are DOC for
Alzheimer’s dementia
Gallantamine
2. NMDA receptor antagonist:
––Memantine is an NMDA receptor antagonist.
Q
3. Monoclonal Antibody against Aβ-amyloid:
––Aducanumab targets the underlying cause
i.e., Aβ-amyloid
PARKINSONISM
––In Parkinsonism, there is deficiency of
dopaminergic activity in basal ganglia of brain
––Normally, there is balance b/w dopaminergic (DA)
and cholinergic (ACh) neurons
––In Parkinsonism, this balance is lost [Relative
cholinergic excess]
Two ways to treat Parkinsonism
A. Increase dopamine
B. Decrease Ach
A. DOPAMINERGIC DRUGS
1. Levo-dopa
Peripheral DOPA decarboxylase convert L-dopa to
Dopamine. So if given alone:
→ Less efficacious due to less entry in brain.
→ DA produced outside the brain causes peripheral
side effects like
52Cerebellum Quick Revision Notes
Carbidopa
Benserazide
↓
↑ Efficacy
↓ Peripheral S/E
Psychosis
––Dyskinesia
––Abnormal behavior
→ Psychosis can occur due to excessive DA in brain
––Central S/E of levodopa cannot be prevented
by carbi-dopa
→ Central S/E of levopa cannot be prevented by carbi-dopa
2. Amantadine
Q
––Acts by releasing DA from vesicle
––Can Cause ankle edema (reversible) and Livedo
reticularis (Pinkish pigmentation of skin in form
of meshwork)
––Recently approved for treating Levo-dopa
induced Dyskinesia as Amantadine acts as a
NMDA Antagonist (Only anti Parkinsonian drug
to treat dyskinesia)
3. Metabolism Inhibitors
Selective MAO-B Inhibitors : Selegiline
COMT Inhibitors : Entacapone
4. Dopamine Agonists
→ Directly works on dopamine receptors
––Pramipexole and ropinirole are DOC for
Parkinsonism
B. ANTI-CHOLINERGIC DRUGS
→ These are DOC for Drug Induced Parkinsonism
Peripheral DOPA Decarboxylase
inhibitors
Two groups:
1. Central Anti-cholinergics: Benzhexol [Trihexyphenidyl]
2. First Generation Anti-histaminic drugs: Promethazine
MULTIPLE SCLEROSIS
––Demyelinating disease
Condition DOC
Acute Episode
Relapsing Remitting (RRMS)
Primary Progressive (PPMS)
Intravenous Steroids
β-IFN
Ocrelizumab
EPILEPSY
Q
Seizure
Special
Feature
First Line Drug
GTCS Valproate, Lamotrigine
Absence
EEG shows
3 spike
/ wave
pattern
Valproate, Ethosuximide
Focal
Temporal
lobe
Carbamazepine (DOC)
Oxcarbazepine
Levetiracetam, (DOC in elderly)
Myoclonic Valproate
Atonic Valproate
Lennox
Gastaut
Syndrome
Valproate, Rufinamide
Febrile
seizures
Diazepam
Status
Epilepticus
Lorazepam
Infantile
spasms
Also called
Salaam
seizures
Seen in
West
syndrome
ACTH (DOC), Vigabatrin
Eclamptic
seizures
Due to
high BP in
pregnancy
MgSO
4
(DOC)
••First sign of toxicity is loss
of deep tendon reflexes like
patellar reflex
Epilepsy in
pregnancy
-
••Don’t change drug if female is
already controlled on any AED
••Least teratogenic are
lamotrigine and levetiracetam
––Hypotension
––Arrhythmias
––Hypertension
––Vomiting
53Pharmacology
Lamotrigine
––DOC for focal seizures in elderly (along with
levetiracetam)
––Side effects:
••Steven Johnson Syndrome
Q
••Toxic Epidermal Necrolysis
These side effects can be avoided by gradually
increasing the dose.
Sodium Valproate
It can cause adverse effects like:
––Liver damage
––Pancreatitis
Q
––PCOD
Phenytoin
Adverse Effects
H - Hirsutism, Hypertrophy of gums
O - Osteomalacia
T - Teratogenicity [Fetal Hydantoin syndrome]
M - Megaloblastic Anemia [↓ Folate]
Q
A - Arrhythmia [Only in overdose]
L - Lymph node enlargement
I - ↓ insulin (avoided in DM)
Q
K - ↓ Vitamin K
A - Ataxias, vertigo [cerebellar symptoms] [only at high dose]
Topiramate
––Can cause renal stone
––Other uses of Topiratmate (COMB)
––Craving of Alcohol
––Obesity
––Migraine prophylaxis
––Bipolar disorder
Vigabatrin
Retigabine
––Used or Focal seizures
––Does not act on GABA
––Can cause retinitis as side-effect.
Other uses of AEDs
Bipolar disorder CBZ, Valporate, Topiramate
Migrane prophylaxis Topiramate, Valproate
Neuropathic pain Gabapentin, Pregabalin, CBZ
Restless leg syndrome Gabapentin (DOC)
Arrhythmias Phenytoin
ANTI-PSYCHOTIC DRUGS
––Psychosis occurs due to excessive dopamine in brain.
––Anti-phychotics drug can be divided into:
1. Typical Anti Psychotics [D2 Blockers]
2. Atypical Anti Psychotics [any other mechanism;
mainly 5HT2 Blockers]
Typical Antipsychotics
1. Strong D2 #
––Haloperidol [Highest risk of EPS]
2. Weak D2 #
––Chlorpromazine
Side effects
1. Extra Pyramidal Symptoms [EPS]
Extra Pyramidal Symptom Drug of choice
1. Dystonias [Earliest]
Q
Benzhexol
2. Akathisia [MC]
Q
Propanolol
3. Parkinsonism Benzhexol
4. Tardive dyskinesia [Very late to appear]
Q
Valbenazine
5. Malignant Neuroleptic Syndrome Dantrolene
2. Hyperprolactinemia
––Dopamine ↓ prolactin by stimulating D2
receptors. Therefore, antipsychotics can cause
hyperprolactinemia due to D2 blockade.
––Hyperprolactinemia can result in galactorrhea
and infertility
54Cerebellum Quick Revision Notes
Atypical Anti Psychotics
Advantages
1. Lesser risk of EPS and hyperprolactinemia
2. Effective against both Positive as well as negative
symptoms
Side effects
– Cause lipodystrophy syndrome characterized
by
••↑ Glucose
••↑ Lipids
••Weight gain
••Insulin Resistance
– Risk is highest with clozapine
Clozapine
→ DOC for resistant Schizophrenia
→ Adverse effects are:
––Agranulocytosis [Dose independent]
Q
––Seizures [Dose dependent]
––Myocarditis
––Sedation (Most common adverse effect)
–– Sialorrhea (MC side effect)
Q
ACUTE MANIA
––Patient is usually aggressive and violent
––Rx of Acute Episode: Sedatives [Antipsychotics/
BZD] + Lithium
––Prophylaxis: Lithium is DOC.
––Bipolar disorder: DOC is lithium
Q
Lithium
Pharmacokinetics
––Half-life is 24 hours
––Narrow Therapeutic Index
––Given thrice a day
Therapeutic drug monitoring
Interactions
Drug increasing toxicity are:
––Lisinopril
––Indomethacin
––Thlazides
Toxicity (DAT)
––Diarrhea
––Agitation & Incordination
––Tinnitis
Actions of Lithium
Q
L - Leucocytes
I - Increase
T - Tremors [MC]
H - Hypothyroidism
I - Increase
U - Urine
M - Avoided in Mothers [Lithium in pregnancy
→ Ebstein anomaly]
DEPRESSION
––Earlier it was believed, decrease in Monoamines
(5-HT > NA» DA) causes depression.
––Later it was linked with decrease in BDNF i.e.,
when ↑ Monoamines
––↑ BDNF → ↑ Neuro Plasticity → ↓ Depression
ANTI DEPRESSANTS
––Typical Anti-Depressants → Act by ↑ 5HT
––Atypical Anti-Depressants → Act by other
mechanisms
Typical Antidepressants
These may be:
1. MAO - A Inhibitors
––Moclebemide
–– Reversible inhibitors of MAO-A]
Q
Leukocytosis
Polyuria
––For measuring plasma concentration: Sample
taken at 12 hours after last dose.
––Plasma concentration of Lithium
Q
••Acute mania → 0.8-1.2 mEq/L
••Prophylaxis → 0.5-0.8 mEq/L
55Pharmacology
2. Reuptake Inhibitors
Non Selective Selective
••Inhibit reuptake of 5HT
and NA
••Avoided in cardiac
patients
••Indicated For severe
depression
••Inhibit reuptake of 5HT
••Can be used in cardiac
patients
••Indicated for mild to
moderate depression
A. Non-Selective Reuptake Inhibitors
––Inhibit the reuptake of both 5HT and NA
––Two classes: TCA and SNRI
(i) TCA [Tricyclic antidepressants]
––Imipramine
––Desipramine
––Clomipramine
––Amitriptyline
––Nortriptyline
→ Adverse Effects:
••ACh#: Dry mouth, blurred vision, C/I in glaucoma
••α #: Postural hypotension
••H1 #: Sedation
••Seizures
••Arrhythmias
••Metabolic acidosis
→ Treatment of TCA poisoning:
••NaHCO
3
to correct metabolic acidosis and reverse
arrhythmias
Q
(ii) SNRI [Serotonin Noradrenaline Reuptake Inhibitors]
––↑ 5 HT and ↑ NA
––Lesser adverse effects than TCAs.
––DOC for severe depression
→ Drugs
––Venlafaxine
––Duloxetine
––Milnacipran
––Desvenlafaxine
––Levo-Milnacipran
B. Selective Serotonin Reuptake Inhibitors
→ Drugs
––Fluoxetine
––Paroxetine
––Fluvoxamine
––Sertraline
––Citalopram
––Es-Citalopram
––Dapoxetine → For premature ejaculation
Q
Indication of SSRI
••SSRI are DOC for mild-moderate depression
••SSRI are DOC for all neurotic disorders like
––GAD
––OCD
––Bulimia
––Phobia
––PTSD
––Impulse control disorders
Adverse Effects of SSRI
––Nausea (Most common)
––Anxiety (Due to up-regulation of 5HT2
receptors)
––CNS: Headache, bad dreams
––Sexual:
Q
••Due to 5HT2 receptor stimulation
••Include
○○Anorgasmia
○○Delayed ejaculation (Dapoxetine used for
Pre mature ejaculation)
••Discontinuation syndrome (Least with
Fluoxetine)
Q
56Cerebellum Quick Revision Notes
Atypical Anti-Depressants
––Less sexual side effects
→ Drugs
––Bupropion - Anti-Smoking drug
Q
––Amineptin - ↑ Reuptake of 5-HT
––Tianeptin - ↑ Reuptake of 5-HT
––Vortioxetine
––Vilazodone
––Esketamine
––Brexanolone
Esketamine
––Acts by blocking NMDA receptors of Glutamate
––Used as a Nasal spray for treatment resistant
depression
Brexanolone/ Allopregnanolone
Approved for Post-partum depression.
DRUG OF ABUSE
Opioids
Morphine
––Acts on µ, K, δ Receptors
––Stimulation of µ, K, δ Receptors cause –
Analgesia
µ Receptor Functions
Q
S - Sedation
A – Analgesia
C – Constipation
R - Respiratory depression
U - eUphoria
M – Miosis
Kappa receptors cause dysphoria
Important Drugs:
Morphine is used to treat pain but it should not be
used to treat Biliary colic because morphine causes
spasm of sphincter of Oddi which increases the
intra biliary pressure that can result in rupture of
bile duct.
Q
Tramadol
→ Two MOA
––Agonist at µ, k, δ receptors (opioid action)
––↑ 5HT and NA in spinal cord (Non-opioid action)
Naloxone cannot completely abolish the analgesic
effect of tramadol and tapentadol
Fentanyl
––Highly lipid soluble drugs
––Used for anesthesia
––Cause Post operative muscle rigidity. It is also
known as Wooden chest syndrome
ANTAGONISTS
→ Drugs
Naloxone - Short acting, given IV
Q
Naltrexone - Long acting, given Orally
DOC for acute Opioid poisoning → Naloxone
DOC for maintenance in opioid poisoning → Naltrexone
Q
57Pharmacology
A. Sedation B. Sudden death
C. Weight gain D. Skin rash
Q 8. Which of the following combination of seizure and
its first line drug is not correct?
A. Generalized seizure -Valproate
B. Myoclonic - Phenytoin
C. Focal – Carbamazepine
D. Absence - Ethosuximide
Q 9. Topiramate is used for the treatment of
A. Lennox Gastaut syndrome
B. Attention deficit hyperkinetic disorder
C. Treatment of migraine
D. Prophylaxis of heat stroke
Q 10. A young boy was brought to hospital with
complaints of few episodes of fast blinking and staring
at something for around 20 seconds. ECG shows spike
and wave pattern. Which of the following drug should
be used for treatment?
A. Phenytoin B. Sodium valproate
C. Diazepam D. Carbamazepine
Q11. ACTH is the treatment of
A. Juvenile myoclonic epilepsy
B. West syndrome
C. Dravet syndrome
D. Lennox Gastaut syndrome
Q 12. Which of the following anti-epileptic drug is used
in treatment of neuropathic pain ?
1. Gabapentin 2. Lamotrigine
3. Carbamazepine 4. Pregabalin
A. 1 and 2 B. 2 and 3
C. 1, 2 and 3 D. 1, 3 and 4
Previous Years Questions
Q 1. An elderly male developed the symptoms of
dementia and was diagnosed as Alzheimer’s disease.
Which neurotransmitter level is reduced in this disease?
A. Dopamine B. Acetylcholine
C. Adrenaline D. Serotonin
Q 2. An elderly patient presented with tremors, rigidity
and bradykinesia. The most likely neurotransmitter
affected in the brain of this patient is?
A. Dopamine B. GABA
C. Adrenaline D. Serotonin
Q 3. Which of the following drug is the only medication
useful in preventing disability progression in a patient
with primary progressive multiple sclerosis?
A. Natalizumab B. Ocrelizumab
C. Siponimod D. Rituximab
Q 4. A patient presents with tremors, rigidity and
bradykinesia. Which of the following drugs can be used
for the treatment of this patient?
A. Selegiline B. Donepezil
C. Fluoxetine D. Haloperidol
Q 5. A patient is on long term anticonvulsant therapy.
There is progressive contractility of visual field. The
likely anti-epileptic drug responsible for this adverse
effect is
A. Vigabatrin B. Ethosuximide
C. Phenobarbital D. Levetiracetam
Q 6. Least teratogenic antiepileptic drug in pregnancy
is
A. Valproate B. Phenytoin
C. Carbamazepine D. Levetiracetam
Q 7. A patient was started on lamotrigine 50 mg daily
for treatment of epilepsy. Gradually, the dose of the
drug is increased every 1-2 weeks to reach the final
dose of 200 mg per day. This step up titration of
lamotrigine dose is done in order to prevent or minimize
the development of
Answers
1. - B
2. - A
3. - B
4. - A
5. - A
6. - D
7. - D
8. - B
9. - A
10. - B
11. - B
12. - D
58Cerebellum Quick Revision Notes
Q 19. A 30 year old patient was started on lithium
carbonate for bipolar disorder. The nurse will gave
instructions on adverse effects of the therapy. The
patient should report back if the following features are
seen:
A. Palpitations, chest pain, raised blood pressure
B. Sedation, constipation, vomiting
C. Tinnitus, severe diarrhea, ataxia
D. Fever, skin rash, bradycardia
Q 20. For plasma level monitoring, lithium estimation is
done?
A. Immediately after the dose
B. 8 hours after last dose
C. 12 hours after last dose
D. 24 hours after last dose
Q 21. A 25 year old female presented with mania.
History revealed that her father is taking medications
for bipolar disorder. Which of the following drug will
you prescribe for this patient?
A. Sodium valproate B. Lithium
C. Carbamazepine D. Lamotrigine
Q 22. Which of the following anti-depressant drug acts
by inhibiting the reuptake of both serotonin and nor-
adrenaline?
A. Fluoxetine B. Venlafaxine
C. Phenelzine D. Nortriptyline
Q 23. A patient had a history of previous child with
down syndrome, currently on lithium therapy present
for antenatal checkup. Which of the following condition
is the fetus at the greatest risk of?
A. Ebstein’s anomaly
B. Down’s syndrome
C. Tetralogy of Fallot
D. Neural tube defect
Q 24. A 30 year old female presented to psychiatry OPD
with symptoms of hypomania. She has a past history of
mania and wants to conceive. Which of the following
drug is most teratogenic?
Q 13. A child born by normal vaginal delivery developed
repeated attacks of flexion of neck over the trunk
and jerks in the hands. EEG shows the presence of
hypsarrhythmia. Anti-epileptic drug of choice for this
patient is?
A. Phenobarbitone B. Phenytoin
C. ACTH D. Levetiracetam
Q 14. First sign of MgSO4 toxicity is
A. Loss of patellar reflex
B. Respiratory distress
C. Cardiac arrest
D. Decrease in urine output
Q 15. Which of the following adverse effect is more
with oxcarbazepine as compared to carbamazepine?
A. Thrombocytopenia
B. Dilutional hyponatremia
C. Rash
D. Hepatotoxicity
Q 16. A patient of psychosis was being treated with
risperidone. He presented to emergency with upward
fixed gaze. What will be the treatment of this patient?
A. Wait and assurance
B. Intramuscular Promethazine
C. Injection Diazepam
D. Injection Lorazepam
Q 17. A patient was recently started on Fluphenazine.
Few weeks later, he developed tremors, rigidity,
bradykinesia and excessive salivation. First line of
management for this patient is
A. Selegiline B. Trihexyphenidyl
C. Pramipexole D. Amantadine
Q 18. A psychotropic drug inhibiting the reuptake
of serotonin is likely to cause which of the following
adverse effect?
A. Visual disturbance B. Constipation
C. Dry mouth D. Sexual dysfunction
Answers
13. - C
14. - A
15. - B
16. - B
19. - C
20. - C
23. - A
24. - A
17. - B
18. - D
21. - B
22. - B
59Pharmacology
Q 30. Which of the following is safe plasma concentration
of lithium for treatment of acute attack and prophylaxis
of migraine?
A. 0.6-1.2 mEq/L B. 0.6-1 mEq/L
C. 2-3 mEq/L D. 1-2 mEq/L
Q 31. A patient suffering from depression has to be
started on anti-depressant drug. Which of the following
is least likely to cause sexual side effects?
A. Venlafaxine B. Escitalopram
C. Imipramine D. Bupropion
Q 32. A 22 year old female with bipolar disorder was
on lithium therapy. Which of the following statements
about the therapy is not correct
A. Hemodialysis is not useful in lithium overdose
B. Lithium decreases thyroid function
C. Lithium toxicity is increased by thiazides
D. Lithium is avoided in pregnancy due to its teratogenic
effects
Q 33. Which of the following drug used for pain relief in
arthritis acts by both opioid and non opioid mechanisms?
A. Paracetamol B. Tramadol
C. Ketorolac D. Diclofenac
A. Valproate B. Lithium
C. Carbamazepine D. Olanzapine
Q 25. Which of the following is a novel antidepressant
drug?
A. Vilazodone B. Asenapine
C. Flibanserin D. Lurasidone
Q 26. Which of the following antidepressant drug should
be avoided in a patient of angle closure glaucoma?
A. Sertraline B. Amitriptyline
C. Mirtazapine D. Venlafaxine
Q 27. A patient on anti-depressant therapy presents with
elevated body temperature, dilated pupil, palpitations
and low blood pressure. ECG shows tachycardia, broad
QRS complex and right axis deviation. Which of the
following interventions must be done immediately?
A. Wait and watch
B. Intravenous sodium bicarbonate
C. Intravenous esmolol
D. DC cardioversion
Q 28. A patient on lithium therapy developed
hypertension. He was started on thiazides for
hypertension. After few days, he developed coarse
tremors and other symptoms suggestive of lithium
toxicity. Explain the likely mechanism of this interaction.
A. Thiazide inhibits the metabolism of lithium
B. Thiazides act as an add on drug to lithium
C. Thiazides increase the tubular reabsorption of
lithium
D. Thiazides cause loss of water thereby increase
lithium levels.
Q 29. A female patient was on lithium therapy for
bipolar disorder for 6 months. She kept the fast for
few days due to religious reasons and presented with
seizures, coarse tremors, confusion and weakness of
limbs. Which of the following should be done to diagnose
her condition?
A. Serum Electrolytes B.Serum lithium levels
C. ECG D. MRI
Answers
25. - A
26. - B
27. - B
28. - C
29. - A
30. - A
31. - D
32. - A
33. - B
DRUGS AFFECTING BLOOD FLOW
ANTI PLATELET DRUGS
Chapter - 8 Hematology
1. Aspirin Inhibit COX → ↓TXA
2
2. Clopidogrel
Ticlopi
dine
Acts on ADP
3. Abciximab
Tirofiban
Eptifibatide
Act on GP IIb/III a
Q
4. Atopaxar
Vorapaxar
Act on PAR-1 receptors of
thrombin
Q
ANTI COAGULANTS
These are divided into oral and parenteral anticoagulants
Oral Anti-Coagulants
••Vitamin K inhibitors
••Direct thrombin inhibitors
••Factor Xa inhibitor
1. Vitamin K inhibitors
→ Includes dicumarol and warfarin
Properties of Warfarin:
1. Oral anticoagulant
2. Inhibit vitamin - K
3. Takes 4-5 days to produce action
4. Mainly used for maintenance purpose
5. Contraindicated in pregnancy
6. Effect of Warfarin is monitored by PT/INR
Warfarin Overdose:
••Overdose of Warfarin causes bleeding
••Active Factors like IIa, VIIa, IXa, Xa (which are Known as Four Factor complex (or) Prothrombin Factor complex) is the Treatment of choice.
Q
••If Four Factor complex is not available, then fresh frozen plasma can be used.
••If the fresh frozen plasma is also not available, whole blood should be given
••But the Treatment of choice for bleeding tendency
due to warfarin is Vitamin K
••Vitamin K is also antidote for Warfarin overdose.
2. Direct Thrombin Inhibitors
••Dabigatran - Can be given Orally and does not
require monitoring
Q
3. Direct factor Xa inhibitors
Drugs are
••Rivaroxaban
••Apixaban
••Edoxaban
••Betrixaban
RIVAR – REVERSIBLE
O – ORAL
XA – XA
B – BLOCKER (OR)
AN – ANTAGONIST
61Pharmacology
Injectable Anti-Coagulants
1. Indirect Thrombin Inhibitors
2. Direct Thrombin Inhibitors
1. Indirect Thrombin Inhibitors [Heparin]
UFH Activate
antithrombin
Inhibit factor IIa = Xa
LMWH Activate
antithrombin
Inhibit factor Xa > lla
Q
FondaparinuxActivate
antithrombin
Only inhibits factor Xa
Q
Heparins
1. Route → S.C. or IV
2. Activate anti-thrombin
3. Immediate Action → Useful in acute conditions
4. Anti-coagulant of choice in pregnancy
5. Monitoring done by a PTT
6. Antidote → Protamine Sulphate
WARFARIN HEPARIN
Route Oral S/C or IV
MOA Inhibit vitamin KActivate AT – III
Onset 4-5 days Immediate
Use Maintenance Acute condition
Pregnancy C/I DOC
Monitoring PT/INR aPTT
Q
Antidote Vitamin K Protamine
2. Direct Thrombin Inhibitors (DTI)
••Bivalirudin, argatroban and melagatran are injectable
DTI.
Q
••Hirudin and lepirudin are not used now
••These are DOC for heparin induced thrombocytopenia
(HIT)
ANTIDOTES OF ANTI-COAGULANTS
Antidote Anticoagulant
Vitamin K
Protamine sulfate
Idarucizumab
Andexanet-Alpha
Warfarin
Heparin
Q
Dabigatran
Q
Factor Xa inhibitors e.g., Apixaban
FIBRINOLYTIC DRUGS
••All drugs in this group are tissue plasminogen
activators.
••tPA converts plasminogen to plasmin that breaks the
thrombus
••These are used for acute MI, acute stroke and acute
DVT
→ Drugs
S – Streptokinase
U – Urokinase
R – Reteplase
A – Alteplase
T – Tenecteplase
Overdose of thrombolytics
→ Leads to bleeding
→ Antidotes:
––Epsilon Amino Caproic Acid [EACA]
––Tranexamic Acid.
DRUGS AFFECTING BLOOD CELLS
••Hematinics
••Growth factors
HEMATINICS
These are nutritional substances which help in formation
of blood. e.g.
1. Iron (Fe)
2. Folic acid (FA)
3. Vitamin B12
Iron Deficiency Anemia
••Treatment of choice is Oral iron.
Oral Iron
••Various preparations like ferrous sulphate, ferrous
fumarate are available.
––For adults, tablets are given
––For children drops are available. These should
be given deep in mouth or else they cause skin
pigmentation
••Earliest response - Reticulocytosis
Q
••If Hb is improving by 0.5 g/dl/week, that means
adequate response
62Cerebellum Quick Revision Notes
••Oral iron treatment is continued for 2-3 months
even after the Hb levels come to normal to replenish
the iron stores in body.
••Factors affecting
––Ascorbic acid : Increase Absorption
––Phytates and oxalates :Decrease Absorption
Injectable Iron
••Preparations of injectable iron are:
––Iron Dextran –Can be given IV as well as IM
––Iron Sorbital citrate (Used IM only)
••Intramuscular iron is given by Z-tract technique to avoid pigmentation
HEMATOPOIETIC GROWTH FACTORS
Cells Growth Factor Drug Indications
RBC Erythropoietin Darbopoietin Anemia due to chronic renal failure
Anemia due to bone marrow suppression
WBC G-CSF
GM-CSF
Filgrastim
Sargramostim
Leukopenia due to bone marrow suppression
Platelets IL-11 Oprelvekin Thrombocytopenia due to bone marrow suppression
Previous Years Questions
Q1. Which of the following is an oral direct thrombin
inhibitor?
A. Dabigatran B. Rivaroxaban
C. Warfarin D. Lepirudin
Q2. What is the mechanism of action of tPA?
A. Fibrinolysis
B. Inhibition of factor V and VII
C. Inhibition of factor III and V
D. Activation of anti-thrombin III
Q3. A female patient was taking warfarin for prosthetic
heart valves. She became pregnant. What advise will
you give regarding use of this drug in early pregnancy?
A. Continue warfarin without any concern
B. Continue warfarin but add vitamin K to the therapy
C. Change warfarin to heparin
D. Terminate the pregnancy
Q4. In the given diagram, identify drug Z marked by
the arrow
A. Clopidogrel B. Heparin
C. Dicumarol D. Alteplase
Q5. A patient presented to hospital with chest pain.
ECG of the patient confirms it to be non ST elevation
myocardial infarction. Which of the following drug useful
in this patient acts by inhibiting platelet aggregation?
A. Clopidogrel B.Streptokinase
C. Low molecular weight heparin D.Warfarin
Answers
1. - A
2. - A
3. - C
4. - C
5. - A
63Pharmacology
Drug A Drug B Drug C
aAspirin Vorapaxar Prasugrel
bDipyridamole Eptifibatide Vorapaxar
cAspirin Eptifibatide Prasugrel
dDipyridamole Prasugrel Eptifibatide
Q10. Which of the following statements is most correct
regarding mechanism of action of dicumarol?
A. It acts as a calcium chelator and reduces the
availability of calcium in coagulation pathway
B. It binds and activates anti-thrombin 3 that
accelerates its interaction with thrombin and factor Xa
resulting in their degradation
C. It acts as a Vitamin K inhibitor that results in
inhibition of activation of clotting factors 2,7,9 and 10
D. It inhibits tissue plasminogen activator resulting in
stoppage of conversion of plasminogen to plasmin
Q11. Vitamin that increases the absorption of iron from
stomach is?
A. Vitamin A B. Vitamin B12
C. Vitamin C D. Vitamin D
Q12. Excessive phytates intake in the diet may lead to
deficiency of
A. Proteins B. Iron
C. Vitamin B12 D. Vitamin D
Q13. Indication for use of Pegylated Filgrastim is in the
correction of:
A. Anaemia B. Neutropenia
C. Thrombocytopenia D. Pancytopenia
Q6. A deep vein thrombosis patient was started on an
anticoagulant therapy. Next day, the patient presented
with the features shown in the diagram below. Likely
drug implicated for this adverse effect is
A. Heparin B. Rivaroxaban
C. Warfarin D. Dabigatran
Q7. Among the following drugs, oral factor Xa inhibitor
is:
A. Dabigatran etexilate B. Rivaroxaban
C. Fondaparinux D. Bivalirudin
Q8. A 45 year old patient being treated with low dose
aspirin since 6 months presented with rectal bleeding.
Inhibition of which of the following substance is likely
to responsible for the bleeding?
A. TXA2 B. LT
C. Bradykinin D. PGI2
Q9. Mechanism of action of some antiplatelet drugs is
shown in the given diagram. Which of the following is
correct match:
Answers
6. - C
7. - B
8. - A
9. - C
10. - C
11. - C
12. - B
13. - B
Chapter - 9 Gastrointestinal Tract
PEPTIC ULCER DISEASE
→ Due to excessive acid in stomach
Treatment
1. ↓ ACID
→ HCl produced by Parietal cell of stomach
→ Proton Pump [H
+
-K
+
-Pump] helps in secretion of acid
––Stimulated by
ACh [M
1
]
Histamine [H
2
]
Gastrin [CCK]
––Inhibited by PGE
2
Drugs ↓ Acid
M1 blockersH2 blockers PGE2 PPI
Pirenzepine
Telenzepine
Cimetidine
Ranitidine
Famotidine
Loxatidine
MisoprostolOmeprazole
Esomeprazole
Pantoprazole
Lansoprazole
Rabeprazole
Most specific drug for NSAID
induced Peptic ulcer
Misoprostol
Q
DOC for NSAID induced Peptic
ulcer
Proton Pump lnhibitors
Q
PPls [Proton Pump Inhibitors]
••Irreversible inhibitors
••Example of Hit and Run Drugs
••Exert systemic effect [Do not work locally]
••Given with acid resistant coating (Enteric coating)
Indications
• DOC for PUD due to any reason
• DOC for GERD
• DOC for Zollinger Ellison Syndrome
Adverse Effects (on long-term use)
••↓ Ca
2+
[Osteoporosis]
••↓ Vit B12 [Megaloblastic anaemia]
Q
••↑ Infections
2. ANTACIDS
→ Fastest pain relievers of PUD
→ Include
––AI [OH]3 → Cause constipation
––Mg [OH]2 → Cause Diarrhoea
→ Given in combination
3. ULCER PROTECTIVE DRUGS
→ Sucralfate
→ Sucralfate acts by Polymerization, requires acidic
pH [<4]
––Should not be combined with antacids
→ Inhibits absorption of several drugs like
phenytoin. So, a gap of minimum 120 minutes
should be kept between two drugs
4. ANTI-H. PYLORI DRUGS
• Amoxycillin
• Metronidazole
• Clarithromycin
Triple Drug Therapy
••Used for H. pylori associated PUD
••PPI + 2AMA used
C → Clarithromycin
A → Amoxycillin
P → PPI
Preferred triple drug therapy
Q
Given for 2 weeks
65Pharmacology
Previous Years Questions
Q1. A patient on phenytoin for seizure disorder
was prescribed sucralfate 4 times a day for peptic
ulcer. What should be the minimum duration between
consumption of two drugs?
A. 30 min B. 60 min
C. 90 min D. 120 min
Q2. A female with ovarian cancer was on cisplatin
therapy. He presented to hospital with several episodes
of vomiting. After giving an antiemetic drug, the patient
developed dystonia. The anti-emetic drug most likely to
be responsible for these features is
A. Metoclopramide B. Meclizine
C. Ondansetron D. Scopolamine
Q3. Which of the following is not a prokinetic?
A. 5HT4 agonist B. D2 blocker
C. Macrolides D. Diphenoxymethane
Q4. A patient presented to hospital with three bouts
of vomiting and treated with anti-emetic drug. Vomiting
subsided but after sometime, he developed abnormal
movements. Which of the following drug is used for
treatment of these motor symptoms?
A. Benzhexol B. Cyproheptadine
C. L-dopa D. Hyoscine
Q5. A patient is planned to receive chemotherapy with
cisplatin. Which of the following drugs are used for
the treatment of chemotherapy induced nausea and
vomiting
A. Granisetron, aprepitant and dexamethasone
B. Metoclopramide, dexamethasone and domperidone
C. Prochlorperazine, granisetron and domperidone
D. Promethazine, doxylamine and metoclopramide
Answers
1. - D
2. - A
3. - D
4. - A
ANTI-EMETIC DRUGS
1. Chemotherapy induced nausea and vomiting (CINV):
Type Drug of Choice
Early CINV 5HT3 antagonists
Q
- Ondansetron
- Granisetron
- Palonosetron
Delayed CINV Substance P antagonists
Q
- Aprepitant
- Rolapitant
2. D2 Blockers
Metoclopramide Domperidone
Q
Cross BBB Do not cross BBB
Can cause dystonia Do not cause dystonia
DOC for Levodopa induced vomiting
PROKINETIC DRUGS
→ Used in GERD
→ Drugs are
1. D2 Blockers
••Domperidone
••Metoclopramide
2. 5HT4 Agonist
••Mosapride
••Prucalopride
3. Motilin Receptor Agonist
••Erythromycin
5. - A
BRONCHIAL ASTHMA
1. Bronchodilators
A. Sympathomimetics
b2 Agonists
Salmeterol → Slow acting → Only used for prophylaxis
Formoterol → Fast acting → Used for acute attacks also
Adverse Effects of b2 Agonists
T - Tachycardia
T - Tremors (Most common side effect)
T - Tolerance (Mainly with long-acting beta 2 agonists)
T - T wave changes (Because of hypokalaemia)
These drugs can cause hyperglycaemia (but never
hypoglycemia)
B. Parasympatholytics
M3 Blockers
••Ipratropium
••Tiotropium
→ Given by inhalational route
C. Phosphodiesterase Inhibitors
••Include theophylline and aminophylline
••Given orally or by intravenous route (not available by
inhalational route)
Chapter - 10 Respiratory System
Mechanism
→ Inhibit PDE (thereby ↑ cAMP)
→ Adenosine A1 receptor antagonist
Q
Adverse effects
Due to PDE inhibition Due to ADEnosine A1 an-
tagonism
Q
Nausea, Vomiting, DiarrheaArrhythmias
Headache Diuresis
Arrhythmias Epileptic seizures
→ Theophylline is metabolized by microsomal enzymes,
so prone to drug interactions
••Enzyme inducers (like smoking) decrease the effect,
therefore smokers require higher doses
••Enzyme inhibitors (like ciprofloxacin, clarithromycin
and erythromycin) can result in toxicity (seizures,
arrhythmias etc.)
Q
2.Drugs affecting LTs
A. Steroids
→ DOC for prophylaxis
→ Also used in acute attack along with bronchodilators
Function in acute attack of asthma is to ↑ the
sensitivity of b2 agonists.
→ Preferred by inhalational route
––MC side effect is oropharyngeal candidiasis
––Topical Nystatin or clotrimazole is used to treat
candidiasis
––Gargling after every dose will prevent this
adverse effect
67Pharmacology
Previous Years Questions
Q1. A patient was taking theophylline for bronchial
asthma. After starting another drug, symptoms of
theophylline toxicity started appearing. Which is the
likely drug started?
A. Erythromycin
B. Phenytoin
C. Griseofulvin
D. Rifampicin
B. LOX inhibitors
––Zileuton
C. LT Receptor antagonists
––Zafirlukast
––Montelukast
3. Mast Cell Stabilizers
––Sodium Cromoglycate
––Nedocromil
→ Only used for prophylaxis
Q
→ Given by inhalational route
4. Omalizumab
→ Monoclonal antibody against IgE
Q
→ Only used for prophylaxis
→ Given subcutaneously
GINA (GLOBAL INITIATIVE FOR
ASTHMA) GUIDELINES
••Drug of choice for treatment of acute attack
of asthma (rescue therapy) is combination of
inhalational formoterol and low dose inhaled
corticosteroids.
Q
••Drug of choice for maintenance therapy in asthma
is also the same combination (Formoterol + Low
dose ICS).
Q
Q2. A patient with COPD was given intravenous
aminophylline therapy following which the patient
developed diuresis. This is due to action on which
effector?
A. Adenosine receptors
B. Beta 2 adrenergic receptors
C. IL-10
D. Histone deacetylase
Answers
1. - A
2. - A
Chapter - 11 Antimicrobial Agents
These drugs are used to kill or inhibit the growth of micro-organisms
CLASSIFICATION OF ANTIMICROBIALS
Based on activity
CIDAL:
These kill the microoganisms
These must be used to treat infections in
immunocompromised person
BEta lactams
VAncomycin
Fluroquinolones
Aminoglycosides
BE VA F A
STATIC:
These inhibit the growth of microorganisms.
These cannot be relied upon if there is immunosuppression
Based on Mechanism of Action
Cell wall inhibitors
Firmly – Fosfomycin
Bind to – Beta lactans
Bacterial – Bacitracin
Cell – Cycloserine
Vall – Vancomycin
Protein inhibitors
Bind at 30S ribosomes:
Aminoglycosides
Tetracyclines
Bind to 50S ribosomes:
Chloramphenicol
Macrolides
Clindamycin
Quinpristin
Linezolide
Metabolism
inhibitors
– Sulfonamides
– Trimethoprim
– Pyrimethamine
DNA gyrase
inhibitors
– Fluroquinolones
– Nalidixic acid
Drugs acting
on membranes
– Daptomycin
– Polymyxin B
– Polymyxin E
••Vancomycin inhibits transglycosylase and thus chain
elongation step in bacterial cell wall synthesis.
Q
••Beta-lactams inhibit transpeptidase and thus cross-
linking of peptidoglycan chains
Q
CELL WALL SYNTHESIS
INHIBITORS
A. BETA LACTAMS
1. Penicillins
2. Cephalosporins
3. Carbapenems
4. Monobactams
1. Penicillins
Penicillin G (Benzyl Penicillin)
Limitations
1. Not effective orally [Acid labile]
2. Short acting [Due to rapid tubular secretion]
3. Narrow spectrum
4. Resistance
5. Allergy
69Pharmacology
1. Acid Resistant / Oral Penicillins
V → Penicillin V (Phenoxymethyl Penicillin)
O → Oxacillin
D → Dicloxacillin
K → Cloxacillin
A → Ampicillin, Amoxycillin
2. Prolong duration of action
a. Probenecid competes with Penicillin for transporters
in PT → ↑ Duration of action of Penicillin
b. Depot Preparations
••Benzathine Penicillin G → Longest acting Penicillin
•• Procaine Penicillin G
––Depot preparations are given by IM route only
3. Spectrum of Penicillins
••Mainly against gram positive bacteria.
••Not effective against most gram negative bacilli.
Extended (Wide) Spectrum Penicillins
Q
A → Ampicillin, Amoxycillin
Ci → Carbenicillin
Ty → Ticarcillin
M → Mezlocillin
A → Azlocillin
P → Piperacillin––All of these are effective against Pseudomonas
except ampicillin and amoxycillin
4. Solving problem of resistance
A. b Lactamase Inhibitors
••β-lactams break the structure of penicillin at
β-lactam ring
••Clavulanic acid, sulbactam and tazobactam inhibit
these enzymes and prevent resistance
••Combinations are:
––Clavulanic Acid + Amoxycillin
––Sulbactam + Ampicillin
––Tazobactam + Piperacillin
B. Penicillinase Resistant Penicillins
C → C loxacillin
O → Oxacillin
N → Nafcillin
D →
Dicloxacillin
O
M
→ Methicillin [Most resistant]
MRSA [Methicillin Resistant staph. aureus]
- Resistance is due to altered Penicillin Binding
Proteins
- All β-lactams are ineffective except 5
th
gen
cephalosporins
5. Allergy
••Skin testing done by intradermal injection of drug
••Cross Allergy → If allergic to one penicillin, all β
lactams can cause allergy except monobactam
Indications of Penicillins
Penicillins are First Line Drugs in
Q
L → Listeria (DOC is ampicillin)
A → Actinomycosis
S
→ Syphilis
T → Tetanus
M → Meningococcus
AN → Anthrax
2. Cephalosporins
1
st
Gen 2
nd
Gen 3
rd
Gen 4
th
Gen5
th
Gen
Cefazolin
Cefalexin
Cefadroxil
Cefuroxime
Cefoxitin
Cefaclor
Cefixime
Cefotaxime
Ceftizoxime
Cefpodoxime
Ceftazidime
Cefoperazone
Ceftriaxone
Ceftibuten
Cefepime
Cefpirome
Ceftibiprole
Ceftaroline
••Cefazolin is DOC for surgical prophylaxis
••5th generation are effective against MRSA
A. Cephalosporins secreted in bile
••Safe in renal failure
••Include
––Cefoperazone
––Ceftriaxone
70Cerebellum Quick Revision Notes
Antimicrobial Agents That are Secreted in Bile
Cef in --- Cefoperazone,
Q
Ceftriaxone
The --- Tigecycline
R --- Rifampicin
E --- Erythromycin
N --- Nafcillin
A --- Ampicillin
L --- Lincosamides [Clindamycin]
Disease --- Doxycycline
B. Anti-Pseudomonal Cephalosporins
→ Include:
––Cefepime
––Cefpirome
––Cefoperazone
––Ceftazidime [ Most effective anti-Pseudomonal
cephalosporin]
Q
C. Disulfiram Like Reaction
→ Should not be given with alcohol
→ Include:
••Cefoperazone
Q
••Moxalactam
D. Hypoprothrombinemia (↓ Prothrombin)
→ ↑ Bleeding tendency
→ ↑ Risk of bleeding with warfarin
→ Avoided in hemophilia patients
→ Include:
••Cefoperazone
••Moxalactam
3. Carbapenems
Imipenem:
••Effective against Gram (+), Gram (-) and Anaerobes
••Always given with Cilastatin because if given alone
it is broken down by dehydropeptidase enzyme in
the Kidney
••Imipenem is a broad spectrum antibiotic, it is also
effective against Pseudomonas.
Side effect : Seizures
Contraindication : Epileptic patients
Q
Other Carbapenems:
Meropenem
Ertapenem
Doripenem
Faropenem
4. Monobactam
Only drug in the group is Aztreonam
Q
→ Do not show cross allergy
→ Effective only against Gm -ve bacteria including
Pseudomonas
B. VANCOMYCIN
→ It is not effective orally [Not Absorbed]
Adverse Effects:
••When given by IV route → releases Histamine - Red man syndrome
Q
••Nephrotoxic
••Ototoxic
Indications
••DOC for MRSA infections
••Can be used for Pseudomembranous Colitis (Now DOC is fidaxomicin)
••Not effective against Pseudomonas
Q
DOC for MRSA : Vancomycin
DOC for VRSA : Daptomycin
DOC for VRSA pneumonia : Linezolide
PSEUDOMEMBRANOUS COLITIS
••It is a type of superinfection
••MC bacteria involved: Clostridium difficile
••MC antimicrobials implicated are:
––3rd Gen. Cephalosporins > Clindamycin > Ampi or Amoxycillin > FQ
Q
Treatment:
DOC : Fidaxomicin (Low chances of relapse)
Q
Alternative : Oral vancomycin, Metronidazole
Monoclonal Ab against toxin : Bezlotoxumab
Cilastatin not required
Lesser risk of seizures
71Pharmacology
PROTEIN SYNTHESIS INHIBITORS
→ Drugs inhibit protein synthesis by binding to 30S or
50S
→ It is rememberred as buy AT - 30, SELL @ 50
––Aminoglycosides and Tetracyclines bind at 30S
ribosomes
––Rest all (streptogramins, Erythromycin group,
Linizolid and Lincosamides) bind at 50S ribosomes
Aminoglycosides
Drugs
––Streptomycin
––Gentamicin
––Amikacin
General Properties
••Not effective orally [Not absorbed]
••Active mainly on Gm -ve [Including Pseudomonas]
••Not effective on anaerobic bacteria
••Cidal drugs (Only protein synthesis inhibitors which
are cidal)
••These are nephrotoxic, ototoxic and can cause
neuromuscular blockade
Tetracyclines
- Demeclocycline
- Doxycycline
- Minocycline
Adverse Effects
K – Kidney Failure – All are C/I except Doxycycline
A - Anti-anabolic
P – Phototoxic
I –
Insipidus diabetes (Inhibit ADH release)
L –
Liver Failure C/I
D – Dentition and Bone problems
(C/I in pregnancy and children < 8 years)
Q
E – Not to be given after Expiry
[Risk of Fanconi Syndrome]
V –
Vestibular dysfunction
Uses
S – SIADH [Demeclocycline]
R – Rickettsia [DOC ]
I – Granuloma lnguinale
L – LGV
A – Atypical pNeumonia [DOC – Macrolides]
N
K – Cholera [DOC]
A – Luminal Amoebiasis [DOC For amoebiasis →
Metronidazole]
Resistance:
••Due to development of efflux pumps
Streptogramins
→ Quinpristin + Dalfopristin
→ Can be used for VRSA
Macrolides
––Erythromycin
––Clarithromycin
––Roxithromycin
––Azithromycin
Indications
DOC for
Q
C: Chancroid, C orynebacterium
L: Legionella
A: Atypical Pneumonia
P: Pertussis
Linezolide
••DOC for VRSA pneumonia
Q
••Now approved for TB also
••It is a static drug, so not reliable in immunocompromised
patients
Lincosamides (Clindamycin)
••Secreted in Bile, so safe in renal failure
••Causes Pseudo membranous colitis
••Used in anaerobic bacterial infections
••DOC for lung abcess and brain abscess
Q
72Cerebellum Quick Revision Notes
ANTIMETABOLITES
A. Sulfonamides/Sulfa Drugs
––Sulfadoxine
––Sulfasoxazole
––Sulfamethoxazole
––Sulfadiazine
––Dapsone
Adverse Effects
A – Aplastic anemia
B - Bilirubin displacement →Cause Kernicterus in
newborn
Q
C - Crystalluria
R - Rash
A – Acetylation
S – SLE
H – Hemolysis in G6PD deficiency
••Sulfonamides are structural analogs of PABA, which
is essential for synthesis of folic acid. Therefore,
sulfonamides are competitive inhibitors of FA
synthase enzyme.
••In any infection, where pus is present, which usually
contains PABA, Sulfonamides are unlikely to be
effective.
B. Combinations
1. Cotrimoxazole
Trimethoprim (T) + Sulfamethoxazole (S)
••Ratio for best bactericidal activity → 1: 20 (T:S)
••Ratio in tablet to attain this ratio → 1: 5 (T:S)
Cotrimoxazole is DOC For
P → Pneumocystis jiroveci
N → Nocardia
B → Burkholderia cepacian
2. Sulfadoxine + Pyrimethamine
••Indicated in Parasitic infections → Malaria
→ Toxoplasmosis
DNA GYRASE INHIBITORS
••DNA Gyrase - Introduces negative supercoils and
helps in replication.
••DNA gyrase Inhibitors inhibit replication by
preventing uncoiling.
••The drugs are fluoroquinolones
Fluoroquinolones
Drugs:
••Norfloxacin
••Ofloxacin
••Ciprofloxacin
••Levofloxacin
••Moxifloxacin
General Properties
••Oral cidal drugs
••Wide spectrum [Effective against Gm + ve as well as
Gm -ve]
••C/I in pregnancy and children (<18 yrs) [Cause
cartilage and tendon damage]
Q
••Induce seizures [Avoided in Epilepsy]
••C/I in Renal Failure
Exception
Q
P – Pefloxacin
M – Moxifloxacin
T – Trovafloxacin Safe in renal failure
Avoided in liver disease
Not effective in UTI
Respiratory FQ
Q
O – Ofloxacin
M – Moxifloxacin
G – Gatif loxacin
Levofloxacin [Isomer of Ofloxacin, Long acting]
These are active against respiratory infections caused
by
••Gm +ve bacteria
••Gm -ve bacteria
••Atypical bacteria
••Mycobaterium TB
DRUGS NOT EFFECTIVE AGAINST
PARTICULAR BACTERIA
Bacteria Resistant to DOC
1. Mycoplasma Cell wall inhibitorsMacrolides
2. MRSA Beta lactams Vancomycin
3. PseudomonasVancomycin
Aminoglycoside +
Ceftazidime
4. Enteric feverAminoglycosides Ceftriaxone
5. Anaerobes Aminoglycosides Metronidazole
73Pharmacology
TUBERCULOSIS
FIRST LINE DRUGS
H → Isoniazid
R → Rifampicin [RCIN]
Z → Pyrazinamide
E → Ethambutol
S → Streptomycin (Not first line now)
ActivityBacteriaHepatotoxic Pregnancy
H Cidal Both √ Safe
R Cidal Both √ Safe
Z Cidal i/c √ √ √ Avoided
E StaticBoth X Safe
S Cidal e/c X C/I
lsoniazid (INH)
••INH is activated by catalase peroxidase (formed by
Kat G)
Q
enzyme of mycobacteria. It acts by inhibiting
the formation of mycolic acid.
••Causes pyridoxine (Vitamin B6) deficiency resulting
in peripheral neuropathy. So, pyridoxine is used for
treatment as well as prevention
••Hepatotoxic (INH: lsoniazid causes Neuropathy
and Hepatotoxicity)
Q
Rifampicin
••Act by inhibiting RNA polymerase of mycobacteria
by binding to its β-subunit. It thus inhibits
transcription.
••Should be given on empty stomach
••Secreted in Bile → Safe in renal failure
••Enzyme Inducer
Interactions
Warfarin Heparin
OCP Other contraceptive method
Replace with
Replace with
Other Uses:
••Leprosy
••Effective against Gram positive bacteria (including
MRSA)
••Effective against Gram negative bacteria (including
Pseudomonas)
Other First Line Drugs
••Pyrazinamide causes gout
••Ethambutol causes red-green color blindness (optic
neuritis)
SECOND LINE DRUGS
A. Cidal Drugs
1. FQ
••Ofloxacin
••Moxifloxacin
••Gatifloxacin
••Levofloxacin
2. Injectable
••Capreomycin
••Kanamycin
••Amikacin
••Streptomycin
B. Drugs used for other conditions, now
approved for TB
1. Linezolide – Also used for VRSA
2. Clofazimine – Also used for multibacillary leprosy
C. Other static drugs:
1. Cycloserine – Causes neuropsychiatric adverse effects
2. Ethionamide –
Hepatotoxic
3. PAS – Causes hypothyroidism
4. Thioacetazone – Never given in HIV patients
D. New drugs:
1. Bedaquiline
2. Delamanid
3. Pretomanid
TREATMENT OF TUBERCULOSIS (NTEP)
Drug Sensitive TB:
2HRZE + 4 HRE
74Cerebellum Quick Revision Notes
Drug Resistant TB
Multi drug (MDR) Resistant to H+R
Rifampicin resistanceResistant to R but sensitive to H
Pre-XDR Resistant to H + R + FQ
Extensive (XDR) Resistant to H + R + FQ + One of
Bedaquiline or Linezolide
For TB with HIV
––First start treatment of TB (ATT)
––After 2 weeks, start treatment of HIV (ART)
LEPROSY
Rifampicin600 mgOnce monthly Supervised
Clofazimine300 mgOnce monthly Supervised
Clofazimine50 mg Once daily for
28 days
Unsupervised
Dapsone 100 mgOnce daily for
28 days
Unsupervised
Above regimen is given for
– 12 months in multi-bacillary leprosy
– 6 months in pauci-bacillary leprosy
Lepra Reactions
––DOC for both type 1 and type 2 Lepra reaction
is steroids
––MDT for leprosy should continue
Q
ANTI-HIV DRUGS
1. Fusion Inhibitors
Enfuvirtide Maraviroc
• Binds with GP 41 of Envelope
and Fusion of Virus with T
cell is Inhibited
• Given subcutaneously
• Binds with
CCR-5
• Given orally
2. Reverse Transcriptase Inhibitors(RTI)
→ Inhibit reverse transcriptase (RNA dependent
DNA polymerase)
→ May be competitive (NRTI) or Non-competitive
(NNRTI)
A. Competitive RTI
NRTI (Nucleotide or side RT inhibitors)
Nucleoside RTI Nucleotide RTI
Zidovudine
Lamivudine
Stavudine
Didanosine
Zalcitabine
Emtricitabine
Abacavir
Tenofovir
MI
Aphthous ulcers in mouth
Pigmentation of palms and soles
Maximum risk of pancreatitis
Maximum risk of peripheral neuropa-
thy
B. Non-Competitive RTI (NNRTI)
––Efavirenz
––Nevirapine
––Delavirdine
3. Integrase Inhibitors
→ Can be given orally
→ One of the first line drugs for HIV now.
Q
→ Drugs include
––Raltegravir
––Elvitegravir
––Dolutegravir
4. Protease Inhibitors
••Ritonavir
••Lopinavir
••Amprenavir
••Fosamprenavir
••Atazanavir
••Saquinavir
••Nelfinavir
••lndinavir
Properties of Protease Inhibitors
••Substrates of CYP3A4
••Inhibitors of CYP 3A4
––Strongest is ritonavir
Q
––Boosts the effect of other protease inhibitors
••Cause lipodystrophy syndrome
––↑ Glucose
––↑ Lipids
––Insulin resistance
––Weight gain
CLINICAL MANAGEMENT OF HIV
1. Treatment of HIV
••Called HAART (Highly Active Anti Retro Viral
Therapy)
••Should be given to All HIV positive patients
irrespective of CD4 count
••Given for life long duration
••Minimum 3 drugs (from minimum 2 groups) should
be used
••First line therapy is
––2 NRTI +1 NNRT/ integrase Inhibitors
––Commonly used – T + L + E or T + L + D
Q
[T – Tenofovir, L – Lamivudine, E – Efavirenz, D –
Dolutegravir]
2. Post exposure prophylaxis
→ To prevent development of HIV after exposure
→ Used commonly in health care workers
→ Should be started as early as possible after
exposure (within maximum limit of 72 hours)
→ Should be given for 28 days (4 weeks)
Q
→ All the drugs are given orally
→ Drugs: Tenofovir +Lamivudine + Protease
Q
Inhibitors (or integrase inhibitors)
ANTI-INFLUENZA DRUGS
Uncoating
Inhibitors
Neuraminidase inhibitors
Amantadine
Rimantadine
Inhibit release of virus from cell
••Oseltamivir - Oral
••Zanamivir - Inhalation
••Peramivir - Parenteral
D.O.C for Bird flu (H5N1) and Swine
flu (H1N1)
ANTI-HERPES VIRUS DRUGS
••HSV-1••Mucocutaneous Herpes and Herpes
Encephalitis
••HSV-2••Genital Herpes
••VZV••Chicken pox
••DOC for all of them is ACYCLOVIR
••Ganciclovir is DOC for CMV.
76Cerebellum Quick Revision Notes
ANTI-HEPATITIS VIRUS DRUGS
Hepatitis B
L : Lamivudine
E : Emtricitabine
T : Tenofovir (DOC)
Hepatitis C
→ Previously treated with interferon and ribavirin
→ Treatment was very toxic
→ Now all oral treatment is used
New Oral Drugs for Hepatitis C
Protease
Inhibitors
NS 5A InhibitorsNS 5B Inhibitors
Previrs Asvirs Buvirs
Telaprevir Elbasvir Sofosbuvir
Simprevir Ledipasvir Dasabuvir
Boceprevir Daclatasvir Beclabuvir
Grazoprevir Ombitasvir
Paritaprevir Pimbrentasvir
DRUGS FOR COVID-19
••Caused by Novel corona virus
••Most cases are self-limiting
Important drugs
1. Steroids
••Only life saving drugs in COVID-19 pneumonia.
••Safe in children
••Increase the risk of infections like mucormycosis
2. Remdesivir
••Inhibit RNA dependent RNA polymerase.
Q
••Given intravenously.
••Effective in first 10 days of illness only.
••Given with steroids (or baricitinib).
••Only US-FDA approved drug for COVID-19
pneumonia.
3. Monoclonal antibodies against spike protein
••Drugs include Bebtelovimab
••Indicated for OPD treatment
••Decrease risk of hospitalization.
ANTIFUNGAL DRUGS
1. TOPICAL ANTIFUNGAL DRUGS:
→ Used for dermatopytosis e.g. azoles
→ Used for steroid induced oropharyngeal candidiasis
e.g. nystatin, clotrimazole
Drugs:
C : Ciclipirox olamine
A : Azoles, Amorolofine
T : Terbinafine
Sertaconazole (Has anti-inflammatory and
anti-pruritic activity)
2. SYSTEMIC ANTIFUGAL DRUGS
DRUG MECHANISM USE
Azoles
Inhibit
lanosterol
14-a-
demethylase
DOC for Candidasis
is fluconazole
DOC for Aspergillosis
is voriconazole
Q
Amphotericin
-B
Bind to
ergosterol
and create
pores
Mucormycosis (DOC)
Cryptococcal
meningitis (DOC)
Kala azar (DOC)
Terbinafine
Inhibit
squalene
epoxidase
Dermatophytosis
(DOC)
Griseofulvin
Inhibit
mitotic
spindle
Dermatophytosis
5-Flucytosine
Inhibit DNA
Polymerase
With AMB for
cryptococcal
meningitis
Caspofungin
Cell wall
inhibitor
Q
Candidasis
Aspergillosis
Note: AMB is nephrotoxic but Liposomal AMB is less
nephrotoxic
77Pharmacology
ANTI-PARASITIC DRUGS
MALARIA
••Caused by Plamodium
••Transmitted by female Anopheles
Treatment of Malaria
Type of Malaria DOC
DOC in 1st
Trimester
P. vivax malaria ChloroquineChloroquine
P falciparum malariaACT Quinine
Complicated or
severe or cerebral
Malaria
IV
Artesunate
IV Artesunate
Artemisinin Combination Therapy [ACT]
••Artemisinin + Long acting drug
••DOC for chloroquine resistant malaria
••Given orally
••Lumefantrine + Artemether: DOC in North Eastern
States
••Artesunate + Sulfadoxine - Pyrimethamine : DOC for
rest of India
Radical Cure
••For P.vivax Malaria
••DOC is primaquine
••Given for 14 days
••C/I in G-6-PD deficiency, pregnancy and infants
••Tafenoquine is single dose radial cure of P.vivax malaria
AMOEBIASIS
Drug of Choice
Luminal amoebiasis
(Carrier state)
Diloxanide Furoate (or
Paromomycin)
Q
Intestinal and Hepatic
amoebiasis
Nitroimidazole (Nidazole) e.g.
Metronidazole, Tinidazole,
Secnidazole, Ornidazole,
Satranidazole
*Nidazoles can cause disulfiram like reaction, so are
C/I in alcoholics
USES OF METRONIDAZOLE:
Q
G - Giardiasis, Gardnerella vaginalis (bacterial
vaginosis)
U - Ulcer (Peptic ulcer)
P - Pseudomembranous colitis
T - Trichomoniasis
A - Amoebiasis, Anaerobic bacterial infections
78Cerebellum Quick Revision Notes
Answers
1. - D
2. - A
3. - A
4. - A
5. - C
Previous Years Questions
Q1. The given diagram shows the steps in formation of bacterial cell wall. Identify the site of action of beta
lactam antimicrobials:
Q2. Which of the following cephalosporins can increase
the effect of warfarin resulting in raised INR and
increased risk of bleeding?
A. Cefoperazone B. Cefixime
C. Ceftibiprole D. Ceftazidime
Q3. Carbapenem with maximum seizure risk is:
A. Imipenem B. Meropenem
C. Ertapenem D. Doripenem
Q4. Cilastatin is given in combination with Imipenem
because:
A. Cilastatin prevents degradation of Imipenem in kidney
B. Cilastatin increases absorption of Imipenem
C. Inhibits the enzymes that digest Imipenem in stomach
D. Reduces side effects of Imipenem.
Q5. Mechanism of resistance to penicillins via beta
lactamase is
A. Altered penicillin binding proteins
B. Drug efflux
C. Breaks drug structure
D. Alteration in 50S ribosome structure
79Pharmacology
Answers
6. - C
7. - C
8. - A
9. - B
10. - C
11. - A
12. - B
13. - B
14. - B
15. - A
16. - A
17. - B
Q6. A patient presented with hospital acquired
pneumonia. On testing he was found to be allergic to
penicillin G. Which of the following drug is likely to be
safe in this patient?
A. Ceftriaxone B. Ampicillin
C. Aztreonam D. Imipenem
Q7. Mechanism of action of doxycycline is
A. DNA gyrase inhibitor
B. Cell wall synthesis inhibitor
C. Protein synthesis inhibitor
D. DNA dependent RNA polymerase inhibitor
Q8. Drug of choice for Legionnaire’s disease is:
A. Azithromycin B. Tigecycline
C. Streptomycin D. Amoxycillin
Q9. Which of the following antimicrobials is
contraindicated in a patient with seizure disorder?
A. Ampicillin B. Ofloxacin
C. Doxycycline D. Cefixime
Q10. A pregnant female with urinary tract infection took
antimicrobials for the same. The baby of this female
developed tendon rupture and arthropathy. What is
the likely mechanism of action of the antimicrobial
consumed by the pregnant female?
A. Folic acid synthesis inhibitor
B. Mycolic acid synthesis inhibitor
C. DNA gyrase inhibitor
D. DNA inhibitor
Q11. Drug of choice for prophylaxis against Diphtheria
is
A. Erythromycin B. Rifampicin
C. Cloxacillin D. Ciprofloxacin
Q12. Fluoroquinolone contraindicated in liver disease is
A. Levofloxain B. Pefloxacin
C. Ofloxacin D. Lomefloxacin
Q13. Which of the following is a second line anti-
tubercular drug?
A. Rifampicin B. Ethionamide
C. Vancomycin D. Acyclovir
Q14. All of the following are bactericidal drugs against
Mycobacterium except
A. Kanamycin B. Thioacetazone
C. Rifapentine D. Isoniazid
Q15. Which of the following drug will you omit from
the prescription of a patient with XDR tuberculosis in
pregnancy?
A. Kanamycin
B. Ethambutol
C. Moxifloxacin
D. Amoxycillin-clavulanic acid
Q16. From the given diagram, identify the mechanism
of action of isoniazid.
A. Drug A B. Drug B
C. Drug C D. Drug D
Q17. A 48 year old patient presented to OPD with
tingling and numbness of fingers. The patient is chronic
alcoholic and was recently started on antitubercular
treatment. What should be the treatment of this
patient?
A. Vitamin B3 B. Vitamin B6
C. Vitamin B1 D. Vitamin B12
80Cerebellum Quick Revision Notes
Answers
18. - B
19. - A
20. - C
21. - D
22. - C
23. - A
24. - B
25. - A
26. - A
27. - C
Q18. In MDR tuberculosis, which of following drug
combinations show resistance?
A. Rifampicin and Fluoroquinolones
B. Isoniazid and rifampicin
C. Isoniazid and Pyrazinamide
D. Rifampicin and kanamycin
Q19. Which of the following drug acts by inhibiting the
transcription of DNA to RNA?
A. Rifampicin B. Nitrofurantoin
C. Ciprofloxacin D. Novobiocin
Q20. A female taking oral contraceptives acquired
tuberculosis. After prescribing anti-tubercular
therapy, physician advised the patient for alternative
contraception. What is the probable reason of this
advise?
A. Rifampicin causes teratogenicity
B. Isoniazid is teratogenic
C. Rifampicin increases the metabolism of oral contraceptives
D. Oral contraceptives decrease the efficacy of ATT
Q21. A patient of borderline leprosy received multi
drug therapy. He developed skin lesions as shown in the
figure below. How should this patient be managed?
A. Stop MDT and give thalidomide
B. Continue MDT and give thalidomide
C. Stop MDT and give steroids
D. Continue MDT and give steroids
Q22. A patient developed COVID-19 pneumonia and
was treated. Few months later, patient presented with
nasal congestion and swelling of face. There were black
lesions on the nose bridge. A diagnosis of mucormycosis
was made. What is the drug of choice for this condition?
A. Fluconazole B. Dexamethasone
C. Amphotericin B D. Azithromycin
Q23. Mechanism of action of Triazoles anti-fungal
drugs is:
A. Inhibits ergosterol biosynthesis
B. Inhibits tubulin
C. Inhibits glucan synthesis
D. Inhibits cell wall synthesis
Q24. Drug of choice for invasive aspergillosis is
A. Posaconazole B. Voriconazole
C. Liposomal AMB D. Caspofungin
Q25. An HIV patient presents with seizures and neck
rigidity. The CSF examination shows the presence of
organisms on India ink and a diagnosis of cryptococcal
meningitis is made. Which of the following anti-fungal
drug is used for initial treatment of this meningitis?
A. Liposomal amphotericin B
B. High dose fluconazole
C. Fluconazole + 5 Flucytosine
D. Voriconazole
Q26. Which of the following drugs can be used for the
treatment of severe covid-19 pneumonia in children?
A. Steroids B. Remdesivir
C. Ivermectin D. All of these
Q27. A newly diagnosed tuberculosis patients was found
to be HIV positive. Which of the following statement is
true about treatment of this patient?
A. Start ATT and ART together
B. ART should be started only if CD4 count is less than 50/mcL
C. ATT should be started first followed by ART 2 weeks later
D. ART should be started first followed by ATT 2 weeks later
81Pharmacology
Answers
28. - A
29. - A
30. - D
31. - A
32. - A
33 - B
34. - B
35. - A
36. - B
37. - A
38. - A
Q28. Which of the following drugs improves
bioavailability and prolongs duration of action of
Saquinavir?
A. Ritonavir B. Cimetidine
C. Vitamin C D. Remdesivir
Q29. Mechanism of action of Remdesivir is inhibition
of?
A. RNA dependent RNA polymerase
B. DNA dependent RNA polymerase
C. Viral protease enzyme
D. Cell wall synthesis
Q30. Mechanism of action of Oseltamivir is
A. DNA polymerase inhibition
B. Inhibition of viral mRNA
C. Blocking viral uncoating
D. Neuraminidase inhibition
Q31. Which of the following drug is associated with
causation of pigmentation of hand and soles on chronic
use?
A. Emtricitabine B. Nevirapine
C. Zidovudine D. Abacavir
Q32. A lady has taken medication of ameiobiasis
infection . In a party she drank alcohol. She has nausea
vomiting and dizziness . Which anti-amoebic drug could
have lead to interaction with alcohol to produce these
symptoms?
A. Metronidazole B. Nitazoxanide
C. Paromomycin D. Diloxanide
Q33. A female patient presented with greenish vaginal
discharge. Clue cells were present and Whiff test was
positive in vaginal discharge. What is the drug of choice
for this condition?
A. Doxycycline B. Metronidazole
C. Ceftriaxone D. Fluconazole
Q34. A 30 year old man travelled to Assam. After
coming back he developed fever, chills and rigors and
altered sensorium. The peripheral smear demonstrated
the presence of P. falciparum. What is the treatment
of choice for this patient?
A. Chloroquine, Sulfadoxine pyrimethamine
B. Intravenous Artesunate
C. Quinine
D. Primaquine
Q35. A 25 year old male has frequent visits to rural
areas and need to eat outside food. During one such
visit, he developed loose stools. Which of the following
drug should be used to manage this case?
A. Metronidazole B. Diphenoxylate
C. Loperamide D. Octreotide
Q36. A female patient presented with greenish vaginal
discharge and pruritus. On colposcopy, strawberry
cervix is noted. What is the drug of choice for this
condition?
A. Ceftriaxone B. Metronidazole
C. Acyclovir D. Fluconazole
Q37. The drug kit shown in the diagram below is used
for the treatment of
A. Malaria B. Kala azar
C. HIV D. Syphilis
Q38. Which of the following drug has highest risk
of causing hemolysis in a patient with deficiency of
Glucose-6-Phosphate Dehydrogenase enzyme?
A. Primaquine B. Chloroquine
C. Azithromycin D. Pyrimethamine
Anticancer drugs can be divided into
a. Cytotoxic
b. Targeted
CYTOTOXIC DRUGS
Common Adverse Effects
••BM Suppression
••Alopecia
••Mucositis → Diarrhea
••Hyperuricemia
••Nausea and vomiting (CINV)
1. Alkylating Agents
Drugs:
If – lfosfamide
Bus
– Busulfan
Not – Nitrosoureas
• Carmustine (BCNU)
• Lomustine (CCNU)
• Semustine (Methyl
CCNU)
Present – Procarbazine
Take –
Temozolomide
My
– Melphalan, Mitomycin C
Cycle – Cyclophosphamide
Important Points Regarding Alkylating Agents
Cyclophosphamide Cause Hemorrhagic cystitis
Q
Cause Pulmonary fibrosis
Ifosfamide Cause Hemorrhagic cystitis
Busulfan Cause pulmonary fibrosis
Nitrosoureas Cause Delayed neutropenia
Procarbazine Cause disulfiram-like
reaction
Temozolomide DOC for gliomas
Melphalan Used for multiple myeloma
Mitomycin-C Used topically for
*Subglottic stenosis
Q
*Superficial bladder cancer
Chapter - 12 Anti-Cancer Drugs
Hemorrhagic cystitis
••Caused by cyclophosphamide and ifosmide.
••Metabolite responsible is acrolein
••Prevented by mesna
Q
••Treatment is steroids.
CYCLOphosphamide :
CARmustine :
BUSulphan :
MethoTRUCKsate :
(Methotrexate)
AmioDaRONE :
BLEOmycin :
Drugs Causing Pulmonary Fibrosis
Q
2. Antimetabolites
••These are S Phase Specific
a. Drugs affecting Folic Acid Metabolism
••Example: Methotrexate
••Act by inhibiting dihydrofolate reductase enzyme.
Uses of
Methotrexate:
••Choriocarcinoma - D.O.C
••Rheumatoid arthritis - D.O.C
––Methotrexate toxicity treatment- Folinic acid
(Leucovorin or Citrovorum)
b. Drugs Affecting Purine Metabolism
6-Mercaptopurine Hepatotoxic
6
- Thioguanine Hepatotoxic
Cladribine DOC for Hairy cell Leukamia
Q
Fludarabine DOC for CLL
Q
83Pharmacology
c. Drugs Affecting Pyrimidine Metabolism
5-Fluorouracil
[5-FU]
Cause Hand and foot syndrome
CapecitabineProding
Gemcitabine DOC for Pancreatic carcinoma
Cytarabine Cause cerebellar side effects
3. Drugs Acting on Mitotic Spindle
→ Specific for M-Phase of cell cycle
Formation inhibitors Breakdown inhibitors
Vincristine
Vinblastine
Paclitaxel
Q
S/E → Peripheral neuropathy
SIADH
Vincristine → Marrow sparing anticancer drug
4. Topoisomerase Inhibitors
Topoisomerase I inhibitorsTopoisomerase II inhibitors
Irinotecan
→ Used for colorectal
carcinoma
→ Cholinergic Side
effects
Etoposide
Anthracyclines
••Doxorubicin
••Donorubicin
••Epirubicin
Anthracyclines – Cause Cardiotoxicity
5. Miscellaneous Drugs
a. Bleomycin
••Marrow sparing
••Cause pulmonary fibrosis
••Causes Flagellated pigmentation of skin
Q
b. L-Asparaginase
••Marrow sparing
••Used for ALL
••Cause Allergy
••Cause Acute Pancreatitis
Q
TARGETED ANTICANCER DRUGS
A. SMALL MOLECULES
1. Tyrosine Kinase Inhibitors
DOC for Chronic Myeloid Leukemia – Imatinib
General Properties
1. All end with ‘nib’
2. Orally effective
Important Tyrosine Kinase Inhibitors
For CML
Q
I - Imatinib [DOC]
N - Nilotinib
D - Dasatinib
••Imatinib is DOC for CML and GIST
••Sorafenib is DOC for hepatocellular carcinoma
••Lapatinib is used for breast cancer
Q
84Cerebellum Quick Revision Notes
B. MONOCLONAL ANTIBODIES
→ End with ‘MAB’
→ Injectable Anticancer Drugs
EGFR ANTAGONISTS:
••Cetuximab: Colorectal carcinoma
••Panitumumab: Colorectal carcinoma
MAB AGAINST HER – 2
••Trastuzumab
••Pertuzumab
MAB AGAINST CD20
••Rituximab : For Non-Hodgkin Lymphoma and CLL
• Used for breast cancer
• Cardiotoxic
IMMUNE CHECK POINT
INHIBITORS
••Normally, T-cells are not activated against normal
cells because an interaction between PD-1 (receptor
present on T-cells) and PDL-1 (Ligand present on
normal cells) inhibit T-cells. This is called immune
check point. Tumor cells do not express PDL-1 and
thus can be killed by T-cells.
••Some tumor cells start expressing PDL-1 on their
surface and thus can evade immunity by inhibiting
T-cells.
••Immune check point inhibitors are monoclonal
antibodies against PD-1 or PDL-1 to stop this
interaction. T-cells now can kill cancer cells.
••These drugs can result in auto-immune conditions
like autoimmune hepatitis as adverse effects.
Drugs:
Mnemonic Drug
Q
Use
New
Drugs
Act
At
Immune
Check
Point
Nivolumab
Durvalumab
Avelumab
Atezolizumab
Ipilimumab
Cemiplimab
Pembrolizumab
HL, NSCLC
Multiple cancers including
endometrial cancer
IMMUNOSUPPRESSANTS
1. STEROIDS
2. DRUGS TARGETING THE CALCINEURIN
PATHWAY
a. Cyclosprine and
Tacrolimus
b. Daclizumab and
Basiliximab
c. Sirolimus
a. Cyclosporine and Tacrolimus
Q
••Inhibit formation of IL-2
b. Sirolimus and Everolimus
••Inhibit action of IL - 2
3. BIOLOGICAL AGENTS
Formed by recombinant DNA technology
TNF-α inhibitors
A – Adalimumab
C – Certolizumab
E – Etanercept
INhibitor – INfliximab
GOLI – GOLImumab
85Pharmacology
Previous Years Questions
Q1. Drug of choice for treatment of hairy cell leukemia is?
A. Interferon alpha
B. Fludarabine
C. Pentostatin
D. Cladribine
Q2. Which of the following drug can cause the side-
effect given in the picture?
A. Bleomycin
B. Mitomycin C
C. Doxorubicin
D. Actinomycin D
Q3. A 50 year old female presented to oncologist with
breast lump. On examination and investigations, breast
cancer was diagnosed. Echocardiography of the patient
shows ejection fraction of 25 %. Which of the following
drug will you avoid in this patient?
A. Epirubicin
B. Irinotecan
C. Cyclophosphamide
D. Methotrexate
Q4. A 20 year old boy presented with slow growing mass
on the medial side of thigh. Investigations revealed
it to be osteosarcoma and patient was started on
methotrexate. Mechanism of action of methotrexate
as an anticancer drug is
A. Inhibition of Dihydrofolate reductase
B. Inhibition of N5 tetrahydro folate reductase
C. Inhibition of tyrosine kinase
D. Inhibition of purine metabolism
Q5. Topical application of 400 mcg/ml mitomycin C is
used for
A. Subglottic stenosis
B. Tympanoplasty
C. Rhinocerebral mucormycosis
D. Nasopharyngeal bleeding
Q6. Which of the following is not an immune check point
inhibitor?
A. Cetuximab
B. Pembrolizumab
C. Atezolizumab
D. Nivolumab
Q7. Which of the following is true about Rituximab
A. Anti- CD 20, monoclonal antibody
B. Anti-CD 50, monoclonal antibody
C. Anti-CD 20 polyclonal antibody
D. Anti-CD 50 polyclonal antibody
Q8. What is mechanism of action of Cyclosporine?
A. Calcineurin inhibitor
B. mTOR inhibitor
C. IL-2 receptor antagonist
D. TNF-α inhibitor
Answers
1. - D
2. - A
3. - A
4. - A
5. - A
6. - A
7. - A
8. - A
LOCAL ANAESTHETIC AGENTS
Drugs
Ester Amide
Cocaine Lignocaine
Procaine Bupivacaine
Chlorprocaine Prilocaine
Tetracaine Etidocaine
Benzocaine Ropivacaine
Dibucaine
Special points:
••Only LA causing vasoconstrictionCocaine
Q
••MC used LA Lignocaine
••Shortest acting LA Chlorpropane
••LA causing methemoglobinemia Prilocaine
Q
••Maximum Cardiotoxic Bupivacaine
Q
Local Anaesthetic Systemic Toxicity (LAST):
→ Characterized by
––Arrhythmias
––Cardiovascular collapse
––Seizures
→ Treatment is
––Cardiopulmonary resuscitation
––20% intralipid (DOC)
Q
SKELETAL MUSCLE RELAXANTS
NEUROMUSCULAR BLOCKERS:
These may be depolarizing or non-depolarizing skeletal
muscle relaxants
Depolarizing Muscle Relaxants (DMR)
Non Depolarizing Muscle Relaxants
(NDMR)
••Act by blocking N
M
receptors competitively
••Example is d- Tubocurarine (Curare)
••It does not cause post opeartive muscle pain
••Release Histamine
that causes bronchoconstriction
and hypotension
Q Other NDMR
Curium [Release less
histamine]
Curonium [No histamine
released]
Atracurium
Cis-Atracurium
Mivacurium [Shortest
acting]
Pancuronium
Pipecuronium
Vecuronium
Rocuronium
Rapacuronium
••Cis-atracurium release less histamine than
atracurism
Q
Hoffman’s Elimination
••Shown by Atracurium and Cis-atracurium
••Muscle relaxant of choice in liver and renal disease
Q
Reversal Agents
Used to reverse action of NDMR after surgery
→ Neostigmine: Can cause cholinergic adverse effects
→ Suggamadex: No cholinergic side effects
Q
GENERAL ANAESTHETICS
INDUCING AGENTS (INTRAVENOUS)
••Thiopentone
••Ketamine
••Propofol
••Etomidate
Thiopentone
••Highly lipid soluble
••Very short acting d/t Redistribution
Chapter - 13 Anaesthesia
••Acts by stimulating N
M
receptors
••Example is Succinylcholine (SCh)
Q
Succinylcholine (SCh)
••Shortest acting MR [< 5 min]
••C/I in nerve and muscle injuries [Can cause severe
hyperkalemia]
••Hyperthermia [precipitate malignant hyperthermia]
••Fasciculations: Responsible for post operative muscle
pain
87Pharmacology
Propofol
••Painful
••DOC for day care Surgery
Q
••Avoided in patients with egg allergy
Etomidate
••Agent of choice for CVS surgery
••Causes Adrenal Suppression
Q
Ketamine
K → Agent of choice in kids
E → Emergence Rxn (post operative delirium and
hallucinations)
T → Thalamo - Cortical junction (site of action)
Dissociative Anesthesia
Q
A → Analgesic
M → M eals (can be given in full stomach)
I → ↑ BP/IOP/ ICP (Agent of choice in shock)
N → N MDA Blocker
E → E xcellent bronchodilator
Q
INHALATIONAL AGENTS
N2O Highest MAC (104%)
Q
Halothane Causes hepatitis
Causes malignant hyperthermia
Enflurane Seizures (Maximum risk)
Isoflurane DOC for cardiovascular and
neurosurgery
Sevoflurane DOC for children
Methoxyflurane Nephrotoxic
Q
Desflurane Maximum irritation to respiratory
pathway
Xenon Ideal anaesthetic agent
1. MAC (Minimum Alveolar concentration)
••Minimum Concentration required in alveoli
to produce anaesthesia
Mac a
1
Potency
MAC Potency Drug
Maximum
Minimum
Least
Most
N2O (104%)
Methoxyflurane
2. Blood Solubility
Measured by blood gas partition coefficient (BGPC)
Q
BPGC a
1 speed of onset
BGPC Onset Drug
Highest Slowest Methoxyflurane
Lowest Fastest Xenon
COLORS OF CYLINDERS
N
2
O Blue (NEELA)
CyclopropaneOrange (SANTRI)
O
2
Black and white (Black body and White
shoulder)
Entonox––Blue and White (Blue body and
White shoulder)
––Mixture of 50% N
2
O and 50%
O
2
is Entonox
88Cerebellum Quick Revision Notes
Previous Years Questions
Q1. Mechanism of action of curare like drugs is
A. Competitive, Non depolarizing block at the Nm
cholinergic receptors
B. Non-competitive, Non depolarizing block at the Nm
cholinergic receptors
C. Competitive, Depolarizing block at the Nm cholin-
ergic receptors
D. Non-competitive, Depolarizing block at the Nm
cholinergic receptors
Q2. Reason for preferring cis-Atracurium over Atracurium
is:
A. Equal potency like Atracurium
B. Lesser provocation of histamine release
C. Short fast action
D. Does not undergo Hoffman elimination
Q3. A person was given a muscle relaxant that
competitively blocks nicotinic receptors. Which of the
following drug is used for reversal of muscle relaxation
after surgery?
A. Neostigmine B. Carbachol
C. Succinylcholine D. Physostigmine
Q4. An anesthetist injected bupivacaine in a patient
for axillary nerve block. Later, the patient developed
restlessness, agitation and cardiovascular collapse.
Next best step in the management would be?
A. Cardiac resuscitation + dopamine
B. Cardiac resuscitation + dantrolene
C. Cardiac resuscitation + sodium bicarbonate
D. Cardiac resuscitation + 20 % intralipid
Q5. A patient was admitted for surgery and halothane
is being planned to be used as an anaesthetic agent.
The patient was explained about the adverse effect
of malignant hyperthermia with this drug. Which
of the following drugs may also result in malignant
hyperthermia?
A. Succinylcholine B. D-Tubocurarine
C. Dantrolene D. Baclofen
Q6. Which of the following drug is associated with post
operative delirium and hallucinations?
A. Ketamine B. Thiopentone
C. Fentanyl D. Halothane
Q7. Inhalational anesthetic agent with highest
respiratory irritation is:
A. Desflurane B. Nitrous Oxide
C. Sevoflurane D. Halothane
Q8. Which IV anesthetic does not cause cardiac
depression?
A. Etomidate B. Propofol
C. Methohexitone D. Thiopentone
Q9. Inhalational anaesthetic agent of choice in children is
A. Isoflurane B. Desflurane
C. Sevoflurane D. Halothane
Q10. A patient of COVID-19 requires oxygen therapy.
Which of the following cylinders should be used to
provide oxygen to this patient?
A B C D
Answers
1. - A
2. - B
3. - A
4. - D
5. - A
6. - A
7. - A
8. - A
9. - C
10. - A
ANTI-SMOKING DRUGS
1. Nicotine Replacement Therapy (NRT)
••Most commonly used anti-smoking drugs
••Available as chewing gums and lozenges
••Lozenges have more bioavailabilty than gums
••Do not take tea or coffee for 15 minutes after
taking NRT
2. Bupropion
Q
••Bupropion is anti-smoking whereas buspirone is
anti-anxiety
3. Vareniciline
Q
••Most effective anti-smoking drug
••Can cause CVS and CNS adverse effects
ANTI-OBESITY DRUGS
O – Orlistat
B – Bupropion + Naltrexone
E – Exenatide
S – Semaglutide
I – LIraglutide
Ty – Tirzepatide
Topiramate + Phentermine
••Orlistat is oral lipase inhibitor. It inhibits absorption of fats. Major adverse effect is steatorrhea.
Q
••GLP-1 analogues include exenatide, liraglutide and semaglutide
••Tirzepatide is dual GLP-1 and GIP agonist.
ANTIDOTES
Poisoning Antidote
Beta blocker Glucagon
Q
Organophosphate Atropine
Opioid Naloxone
Q
Methanol Fomepizole
Q
Ethylene glycol Fomepizole
Warfarin Vitamin K
Chapter - 14 Miscellaneous Topics
Heparin Protamine sulfate
Paracetamol N. Acetylcysteine
Q
Atropine Physostigmine
Iron Desferrioxamine
Benzodiazepine Flumazenil
Q
Zolpidem Flumazenil
Cyanide Hydroxocobalamin (or Amyl
nitrite)
Q
Valproate hepatotoxicity L-carnitine
MANAGEMENT OF HYPERKALEMIA
Acute hyperkalemia
Q
1. Drugs increasing intracellular movement of K
+
90Cerebellum Quick Revision Notes
CHELATING AGENTS
••Used for heavy metal poisoning
1. BAL (British Anti Lewisite)/ Dimercaprol
Indications:
B - Bismuth poisoning
A - Arsenic poisoning
L - Lead poisoning
Contra-Indications
Cadmium poisoning
Fe poisoning
2. Ca Na
2
EDTA
Indications
M – Manganese poisoning
I – Iron poisoning
L –
Lead poisoning
K – Cadmium poisoning
3. d- Penicillamine
Used for Cu poisoning and Wilson disease
4. Fe chelating agents
Q
DesferioxamineInjectable
DOC for acute Iron poisoning
Deferipirone Oral
Used for chronic Iron over load
Previous Years Questions
Q1. Which of the following is an adverse effect of
orlistat?
A. Suicidal tendancy
B. Steatorrhea
C. Weight gain
D. Hyperglycemia
Q2. Longest acting phosphodiesterase inhibitor among
the following drugs is?
A. Sildenafil
B. Vardenafil
C. Tadalafil
D. Phentolamine
Q3. Which of the following is FDA-approved drug for
long term treatment of obesity?
A. Sibutramine
B. Liraglutide
C. Metformin
D. Fenfluramine
Q4. An 11-year-old boy presented to emergency with
vom iting. Parents gave history of consuming 10-15
tablets of ferrous sulphate a day before. What is the
antidote of iron for treatment of this patient?
A. Dimercaprol
B. Desferrioxamine
C. d- Penicillamine
D. Activated charcoal
Q5. A patient presented with hyperkalemia. Which of
the following drugs can cause intracellular movement of
and thus decrease in extracellular potassium levels?
A. Atropine
B. Lactic acid
C. Epinephrine
D. Glucagon
Answers
1. - B
2. - C
3. - B
4. - B
5. - C