1.Rao_Bronchodilators and Xanthines_AHS_20 Mar 2024.ppt

RaosinghRamadoss 82 views 100 slides Apr 24, 2024
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About This Presentation

PPT for Allied health sciences


Slide Content

Bronchodilators &
Xanthines
4/24/2024 1
Dr.R.Rao Prethendhira Singh.
BDS., Msc Med.Pharmacology.PGDCR
Dept.of Pharmacology.

4/24/2024 2

4/24/2024 3

PHYSIOLOGY OF RESPIRATION
•Respiration is the exchange of gases between the tissue of the body and
to outside environment.
4/24/2024 4
Breathing in of an air Respiratory tract
Uptake of oxygen from the lungs
Transport of oxygen through the body in
the blood stream
Utilization of oxygen in the metabolic
activities
Removal of carbon dioxide from the body.

Innervation of respiratory system
Parasympathetic supply
M3 receptors in smooth muscles and glands.
Bronchoconstriction
Increase mucus secretion
No sympathetic supplybut B
2receptors in smooth muscles and
glands.
Bronchodilation
Decrease mucus secretion

Pulmonary Diseases
•Bronchial Asthma
•Acute Severe Asthma
•Chronic Asthma
•Acute bronchitis
•Chronic bronchitis and emphysema
•Chronic obstructive pulmonary disease
•Respiratory failure
•Cough
•α1-Antitrypsin deficiency
•Drug-induced pulmonary disease
4/24/2024 7

Asthma
Asthma is a chronic inflammatory disorder
of airways that result in airway
obstruction in response to external
stimuli.
It’s characterized by activation of mast cell,
infiltration of eosinophil, T2 helper cells,
Innate type 2 lymphocytes.
4/24/2024 8

Bronchial asthma
•Bronchial asthma is characterized by
hyperresponsivenessof tracheobronchial smooth
muscle to a variety of stimuli, resulting in narrowing
of air tubes, often accompanied by increased
secretion, mucosal edema and mucus plugging.
•Symptoms include dyspnoea, wheezing, cough
and may be limitation of activity.
•Infection, irritants, pollution, exercise, exposure to
cold air, psychogenic.
•Extrinsic asthma: It is mostly episodic, less prone
to status asthmaticus.
•Intrinsic asthma: It tends to be perennial, status
asthmaticus is more common.
4/24/2024 9

Bronchial asthma
•Acute Asthma. It is characterized by episodes
of dyspnoea associated with expiratory
wheezing.
•Chronic Asthma. There is continuous wheeze
and breathlessness on exertion; cough and
mucoid sputum with recurrent respiratory
infection are common.
•Status Asthmaticus (Acute Severe Asthma).
When an attack of asthma is prolonged with
severe intractable wheezing, it is known as
acute severe asthma.
4/24/2024 10

Causes
Exogenous chemicals or irritants
Chest infections
Stress
Exercise (cold air)
Pets
Seasonal changes
Emotional conditions
Some drugs as aspirin, β-bockers

Pathophysiology
•Mast cells (present in lungs) and inflammatory cells
recruited as a result of the initial reaction produce a
multitude of mediators by the following processes
•Release of mediators stored in granules (immediate):
histamine, protease enzymes, TNF-a.
•Release of phospholipids from cell membrane followed
by mediator synthesis (within minutes): PGs, LTs, PAF.
•Activation of genes followed by protein synthesis (over
hours): Interleukins, TNFa.
•These mediators together constrict bronchial smooth
muscle, cause mucosal edema, hyperemia and
produce viscid secretions.
•All resulting in reversible airway obstruction.
4/24/2024 12

4/24/2024 13

Airways of the asthmatic patients are characterized
by:
1.Inflammation
•Swelling
•Thick mucus production.
2.Bronchospasm
•constriction of the muscles around the airways,
causing the airways to become narrow.
4/24/2024 14

Airwayhyper-reactivity:abnormalsensitivityoftheairwaystowiderangeofexternal
stimuliaspollen,coldairandtobaccosmoke.
4/24/2024 15

Symptoms of asthma
Asthma produces recurrent episodic attack of
Acute bronchoconstriction (immediate)
Shortness of breath
Chest tightness
Wheezing
Rapid respiration
Cough
Symptoms can happen each time the airways
are irritated.
4/24/2024 16

CLASSIFICATION OF ANTIASTHMATIC DRUGS
1. Bronchodilators
(a) Sympathomimetics
•Selective Beta 2-adrenergic agonists: Salbutamol and terbutaline
(short acting);
bambuterol, salmeterol and formoterol (long acting).
(b) Methylxanthines: Theophylline, aminophylline, etophylline,
doxophylline.
(c) Anticholinergics: Ipratropium bromide, tiotropium bromide.
2. Leukotriene receptor antagonists: Zafirlukast, montelukast,
zileuton.
3. Mast cell stabilizers: Sodium cromoglycate, ketotifen.
4. Glucocorticoids
(a) Inhaled glucocorticoids: Beclomethasone, budesonide,
fluticasone, ciclesonide.
(b) Systemic glucocorticoids: Hydrocortisone, prednisolone,
methylprednisolone.
5. Anti-IgEmonoclonal antibody: Omalizumab.
4/24/2024 17

Anti asthmatic drugs:
1) Quick relief medications:
Bronchodilators used to relieve acute episodic
attacks of asthma.
2) Control therapy (prophylactic drugs):
anti-inflammatory drugs used to reduce the
frequency of attacks, and nocturnal awakenings.

Anti asthmatic drugs
Bronchodilators
(Quick relief medications)
treat acute attack of asthma
•Short acting 2-agonists
•Antimuscarinics
•Xanthine preparations
Anti-inflammatory Agents
(Prophylactic therapy)
reduce the frequency of attacks
•Corticosteroids
•Mast cell stabilizers
•Leukotrienes antagonists
•Anti-IgE monoclonal antibody
•Long acting ß2-agonists

Bronchodilators:
Abronchodilatoris a substance
thatdilatesthebronchiandbronchioles,decreasing
resistance in therespiratory airwayand increasing
airflow to thelungs.
Medicationsadministered for the treatment of
breathing difficulties.
They are most useful inobstructive lung diseases, of
whichasthmaandchronic obstructive pulmonary
diseaseare the most common conditions
4/24/2024 20

Bronchodilators
These drugs can produce rapid relief of
bronchoconstriction.
Bronchodilators:
2 -adrenoreceptor agonists
Antimuscarinics
Xanthine preparations

Sympathomimetics
-adrenoceptor agonists
Classification of agonists
Non selective agonists:
epinephrine -isoprenaline
Selective 2 –agonists (Preferable).
Salbutamol (albuterol)
Terbutaline
Salmeterol
Formeterol

Mechanism of Action
direct 
2stimulation stimulate adenyl
cyclase cAMP bronchodilation.
Increase mucus clearance by (increasing
ciliary activity).
Stabilization of mast cell membrane.

Non selective -agonists.
Epinephrine
•Potent bronchodilator
•Given subcutaneously, S.C.
•rapid action (maximum effect within 15 min).
•Has short duration of action (60-90 min)
•Drug of choicefor acute anaphylaxis (hypersensitivity
reactions).

Disadvantages
Not effective orally.
Hyperglycemia
Skeletal muscle tremor
CVS side effects:
tachycardia, arrhythmia, hypertension
Not suitable for asthmatic patients with hypertension
or heart failure.
Contraindications:
CVS patients, diabetic patients

Selective 2 –agonists
Are mainly given by inhalationby (metered
dose inhaler or nebulizer).
Can be given orally, parenterally.
Short acting ß2 agonists
e.g. salbutamol, terbutaline
Long acting ß2 agonists
e.g. salmeterol, formoterol

Nebulizer Inhaler

Short acting ß
2agonists
Salbutamol, inhalation, orally, i.v.
Terbutaline, inhalation, orally, s.c.
Have rapid onset of action (15-30 min).
short duration of action (4-6 hr)
used for acute attack of asthma (drugs of
choice).

Long acting selective ß
2 agonists
Salmeterol & formoterol
are given by inhalation
Long acting bronchodilators (12 hours) due to
high lipid solubility (creates depot effect).
are not used to relieveacute episodes of asthma
used for nocturnal asthma.
combined with inhaled corticosteroids to control
asthma (decreases the number and severity of
asthma attacks).

Advantages of ß
2agonists
Minimal CVS side effects
suitable for asthmatic patients with
CV disorders as hypertension or heart failure.
Disadvantages of ß
2agonists
Skeletal muscle tremors.
Nervousness
Tolerance (β-receptors down regulation).
Overdose may produce tachycardia due to
β
1stimulation.

Muscarinic antagonists
Ipratropium –Tiotropium
Act by blocking muscarinic receptors .
given by aerosol inhalation
Have delayed onset of action.
Quaternary derivatives of atropine (polar).
Does not diffuse into the blood
Does not enter CNS.
Have minimal systemic side effects
Ipratropiumhas short duration of action 3-5 hr
Tiotropium has longer duration of action (24 h).

Pharmacodynamics
Inhibit bronchoconstriction and mucus secretion
Less effective than β
2-agonists.
No anti-inflammatory action only bronchodilator
Uses
Main choice in chronic obstructive pulmonary
diseases (COPD).
In acute severe asthma combined with β
2agonists
& corticosteroids.
Never use as a rescue medication.

Methylxanthines
Theophylline -aminophylline
Mechanism of Action
are phosphodiestrase inhibitors
cAMP bronchodilation
Adenosine receptors antagonists (A1)
Increase diaphragmatic contraction
Stabilization of mast cell membrane

Bronchodilation
Adenyl cyclase
Phosphodiesterase
ATP
cAMP
3,5,AMP
+ B-agonists
Theophylline

Pharmacological effects :
Bronchial muscle relaxation
contraction of diaphragmimprove ventilation
CVS: ↑ heart rate, ↑ force of contraction
GIT: ↑ gastric acid secretions
Kidney: ↑renal blood flow, weak diuretic action
CNS stimulation
* stimulant effect on respiratory center.
* decrease fatigue & elevate mood.
* overdose (tremors, nervousness, insomnia,
convulsion)

Pharmacokinetics
Theophylline is given orally
Aminophylline, is given asslow infusion
metabolized by Cyt P450 enzymes in liver
T ½= 8 hours
has many drug interactions
Enzyme inducers:
as phenobarbitone & rifampicin
↑ metabolism of theophylline → ↓ T ½.
Enzyme inhibitors:
as erythromycin
↓ metabolism of theophylline → ↑ T ½.

Uses
Second line drug in asthma (theophylline).
For status asthmatics (aminophylline, is given
asslow infusion).
Side Effects
Low therapeutic index(narrow safety margin)
monitoring of theophylline blood level is
necessary.
GIT effects:nausea & vomiting
CVS effects:hypotension, arrhythmia.
CNS side effects:tremors, nervousness,
insomnia, convulsion

Prophylactic therapy
Anti -inflammatory drugs include:
Glucocorticoids
Leukotrienes antagonists
Mast cell stabilizers
Anti-IgEmonoclonal antibody
e.g. omalizumab

Anti -inflammatory drugs:
(control medications / prophylactic
therapy)
↓ bronchial hyper-reactivity.
↓ reduce inflammation of
airways
↓ reduce the spasm of airways

Glucocorticoids
Mechanism of action
Anti-inflammatory action due to:
Inhibition of phospholipase A2
↓prostaglandin and leukotrienes
↓Number of inflammatory cells in airways.
Mast cell stabilization →↓histamine release.
↓capillary permeability and mucosal edema.
Inhibition of antigen-antibody reaction.
Upregulate β
2receptors(have additive effect to B
2
agonists).

Pharmacological actions of glucocorticoids
Anti-inflammatory actions
Immunosuppressant effects
Metabolic effects
–Hyperglycemia
–↑protein catabolism, ↓protein anabolism
–Stimulation oflipolysis-fat redistribution
Mineralocorticoid effects:
–sodium/fluid retention
–Increase potassium excretion (hypokalemia).
–Increase blood volume (hypertension).

Behavioral changes: depression
Bone loss (osteoporosis)due to
•Inhibit bone formation
•↓ calcium absorption from GIT.

Routes of administration
Inhalation:
e.g. Budesonide & Fluticasone, beclometasone
•Given by inhalation (metered-dose
inhaler).
•Have first pass metabolism
•Best choice in asthma, less side effects
Orally:Prednisone, methyl prednisolone
Injection:Hydrocortisone, dexamethasone

Glucocorticoids in asthma
Are not bronchodilators
Reduce bronchial inflammation
Reduce bronchial hyper-reactivity to stimuli
Have delayed onset of action (effect usually attained after
2-4 weeks).
Maximum action at 9-12 months.
Given as prophylactic medications, used alone or
combined with β
2agonists.
Effective in allergic, exercise, antigen and irritant-induced
asthma,

Systemic corticosteroids are reserved for:
•Status asthmaticus (i.v.).
Inhaled steroids should be consideredfor
adults,
children with any of the following features
•using inhaled β
2agonists three times/week
•symptomatic three times/ week or more;
•or waking one night/week.

Clinical Uses of glucocorticoids
1.Treatment of inflammatory disorders(asthma,
rheumatoid arthritis).
2.Treatment of autoimmune disorders(ulcerative
colitis, psoriasis) and after organ or bone marrow
transplantation as immunosuppressants.
3.Antiemetics in cancer chemotherapy.

Side effects due to systemic corticosteroids
•Adrenal suppression
•Growth retardation in children
•Susceptibility to infections
•Osteoporosis
•Fluid retention, weight gain, hypertension
•Hyperglycemia
•Fat distribution
•Cataract
•Psychosis

Inhalation has very less side effects:
•Oropharyngeal candidiasis (thrush).
•Dysphonia (voice hoarseness).
Withdrawal of systemic corticosteroids
•Abrupt stop of corticosteroids should be
avoided and dose should be tapered (adrenal
insufficiency syndrome).

Mast cell stabilizers
e.g. Cromoglycate -Nedocromil
act by stabilization of mast cell membrane.
given by inhalation (aerosol, nebulizer).
Have poor oral absorption (10%)

Pharmacodynamics
areNotbronchodilators
Noteffective in acute attack of asthma.
Prophylacticanti-inflammatory drug
Reduce bronchial hyper-reactivity.
Effective in exercise, antigen and irritant-
induced
asthma.
Children respond better than adults

Uses
Prophylactic therapy in asthma especially in
children.
Allergic rhinitis.
Conjunctivitis.
Side effects
Bitter taste
minor upper respiratory tract irritation
(burning sensation, nasal congestion)

Leukotrienes antagonists
Leukotrienes
synthesized by inflammatory cells found in
the airways(eosinophils, macrophages, mast
cells).
produced by the action of 5-lipoxygenase on
arachidonicacid.
Leukotriene B4: chemotaxisof neutrophils
Cysteinyl leukotrienes C4, D4 & E4:
•bronchoconstriction
•increase bronchial hyper-reactivity
•↑ mucosal edema, ↑ mucus secretion

Leukotriene receptor antagonists
e.g. zafirlukast, montelukast, pranlukast
are selective, reversible antagonists of cysteinyl
leukotriene receptors (CysLT
1receptors).
Taken orally.
Are bronchodilators
Have anti-inflammatory action
Less effective than inhaled corticosteroids
Have glucocorticoids sparing effect (potentiate
corticosteroid actions).

Uses of leukotriene receptor antagonists
Noteffective in acute attack of asthma.
Prophylaxisof mild to moderate asthma.
Aspirin-induced asthma
Antigen and exercise-induced asthma
Can be combined with glucocorticoids (additive
effects, low dose of glucocorticoids can be
used).
Side effects:
Elevation of liver enzymes, headache, dyspepsia

Anti-IgE monoclonal antibody
e.g. Omalizumab
is a monoclonal antibody directed against human
IgE –given by injection (s.c.)
prevents IgE binding with its receptors on mast
cells & basophiles.
↓ release of allergic mediators.
Expensive-not first line therapy.
used for treatment of moderate to severe allergic
asthma which does not respond to high doses
ofcorticosteroids.

Drugs used in chronic obstructive pulmonary
disease (COPD)
•COPDis a chronic irreversible airflow
obstruction, lung damage and inflammation
of the air sacs (alveoli).
•Smoking is a high risk factor but air
pollution and genetic factors can contribute.

4/24/2024 61

Treatment:
•Inhaled bronchodilators
•Inhaled glucocorticoids
•Oxygen therapy
•Antibioticsspecificallymacrolides such
asazithromycinto reduce the number of
exacerbations.
•Lung transplantation

Inhaled bronchodilators in COPD
Inhaled antimuscarinics
Ipratropium & tiotropium.
are superior to β2agonists in COPD
β
2agonists
these drugs can be used either alone or combined
•salbutamol + ipratropium
•salmeterol + Tiotropium (long acting-less dose
frequency).

Summary

Drugs
Adenyl
cyclase
cAMP
–Short acting
–main choicein acute
attack of asthma
–Inhalation
B2 agonists
Salbutamol, terbutaline
Long acting, Prophylaxis
Nocturnal asthma
Salmeterol, formoterol
Blocks M
receprtors
Main drugs For COPD
Inhalation
Inhalation
Antimuscarinics
Ipratropium (Short)
Tiotropium (long)
Inhibits
phosphodi
esterase
cAMP
(orally)
(parenterally)
Xanthine derivatives
Theophylline
Aminophylline
Bronchodilators (relievers for bronchospasm)

Inhalation
Corticosteroids
(Inhibits phospholipase A2)
Dexamethasone, Fluticasone, budesonide
Orallyprednisolone
parenterallyHydrocortisone
Inhalation,
prophylaxis in
children
Mast stabilizers
Cromoglycate (Cromolyn), Nedocromil
orally
Cysteinyl antagonists (CyLT1 antagoist)
Zafirlukast, montelukast
Injection, SCOmalizumab (Anti IgE antibody)
Anti-inflammatory drugs (prophylactic)

Understanding the Common Cold
Most caused by viral infection
(rhinovirus or influenza virus—the “flu”)
4/24/2024
Dr. Nitin Mirgane
Drugs for respiratory system 68

Understanding the Common Cold
Virus invades tissues (mucosa) of upper
respiratory tract, causing upper respiratory
infection (URI).
Excessive mucus production results from the
inflammatory response to this invasion.
Fluid drips down the pharynx into the
esophagus and lower respiratory tract,
causing cold symptoms: sore throat,
coughing, upset stomach.
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Drugs for respiratory system 69

Understanding the Common Cold
Irritation of nasal mucosa often triggers the
sneeze reflex.
Mucosal irritation also causes release of
several inflammatory and vasoactive
substances, dilating small blood vessels in
the nasal sinuses and causing nasal
congestion.
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Drugs for respiratory system 70

Treatment of the Common Cold
Involves combined use of antihistamines,
nasal decongestants, antitussives, and
expectorants.
Treatment is SYMPTOMATIC only, not
curative.
Symptomatic treatment does not eliminate
the causative pathogen.
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Cough:protective reflex which helps
to expel irritant matter from the
respiratory tract
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4/24/2024
Dr. Nitin Mirgane Drugs for respiratory system
Antitussive Agents
Depress the area in CNS which controls the
cough refles
Stimulate the flow of respiratory secretions

Expectorants
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Drugs for respiratory system 74

Expectorants
“Drugsthathelpinremovingsputumfromtherespiratorytract.
-eitherbyincreasingthefluidity(orreducingtheviscosity)of
sputumor
-increasingthevolumeoffluidsthathavetobeexpelledfrom
therespiratorytractbycoughing.”
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Drugs for respiratory system 75

Expectorants: Mechanisms of
Action
Direct stimulation
or
Reflex stimulation
Final result: thinner mucus that is easier to remove
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Drugs for respiratory system 76

Expectorants: Mechanism of
Action
Direct stimulation:
The secretory glands are stimulated directly
to increase their production of respiratory
tract fluids.
Examples: terpin hydrate, iodine-containing
products such as iodinated glycerol and
potassium iodide (direct and indirect
stimulation)
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Drugs for respiratory system 77

Expectorants: Mechanism of
Action
Reflex stimulation:
Agent causes irritation of the GI tract.
Loosening and thinning of respiratory tract
secretions occur in response to this irritation.
Examples: guaifenesin, syrup of ipecac
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Drugs for respiratory system 78

Expectorants: Drug Effects
By loosening and thinning sputum and
bronchial secretions, the tendency to cough
is indirectly diminished.
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Drugs for respiratory system 79

Boththeactionandmechanismofexpectorantshavebeenquestioned
andremaincontroversial.However,thesemayserveaplaceborole
andhelpthepatient
•Ammonium chloride
•Potassium iodide
•Sodium iodide
placebois a simulated or otherwise medically ineffectual treatment for a disease
.
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Drugs for respiratory system
80

Dose related side-effects
•Ifthepatientissensitive,doseofexpectorantishighenough,this
mayinducevomiting(emeticaction).
•Hence,itisadvisabletogivethedosesofexpectorantsthatcouldbe
tolerated(bythepatient)alongwithotherpharmaceuticalaids
(flavours,sweetners,etc.)andcoughsuppressants.
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Drugs for respiratory system 81

Classification of Expectorants
•According the their mechanism of action…
(1) Sedative type
(2) Stimulant type
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Drugs for respiratory system 82

Sedative expectorants
•Thesearestomachirritantexpectorantswhichareabletoproduce
theireffectthroughstimulationofgastricreflexes.
•e.g.
Bitter drugs –Ipecac, Senega, Indian Squill
Compounds –Antimony potassium tartrate,
Ammonium chloride, Sodium citrate,
Potassium iodide, etc.
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Drugs for respiratory system 83

Stimulant type
•Thesearetheexpectorantswhichbringaboutastimulationofthe
secretorycellsoftherespiratorytractdirectlyorindirectly.
•Sincethesedrugsstimulatesecretion,morefluidinrespiratorytract
andsputumisdiluted.
•e.g. -Eucalyptus, lemon, anise
-Active constituents of oil like terpine hydrate,
anethole
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Drugs for respiratory system 84

Ammonium chloride
•Assay:Itwaspreviouslyassayedbyprecipitationtitrationby
usingtheVolhard’smethod.
Now,itisassayedbyacid-basetitrationmethod.
•Uses:
(1)Itactsasmildexpectorantanddiaphoreticwhen
administeredinsmalldoses.
Itdoessoduetolocalirritationwhichproducesincreasing
secretionofrespiratorytract,andmakesthemucusless
viscous.NH
4ClandNH
4HCO
3arethereforeusedincough
preparations.
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Drugs for respiratory system 85

Mucolytes
Mucolyticsare medicines that make the mucus
(sputum) less thick and sticky and easier to
cough up.
They are usually prescribed for people who have
a chronic (long-term) cough.
They work best if they are taken regularly.
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Drugs for respiratory system 86

Anexpectorantincreases bronchial
secretionsand mucolyticshelp loosen thick
bronchial secretions.
Expectorantsreduce the thicknessorviscosity
of bronchial secretions thus increasing mucus
flow that can be removed more easily through
coughing.
Mucolyticsbreak down the chemical structure
of mucus molecules.
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Dr. Nitin Mirgane
Drugs for respiratory system 87

Bronchitis is inflammation or swelling of the
bronchial tubes (bronchi), the air passages between
the nose and the lungs.
More specifically, bronchitis is when the lining of the
bronchial tubes becomes inflamed or infected.
Bronchitis is caused by viruses, bacteria, and other
particles that irritate the bronchial tubes.
Bronchitis
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Dr. Nitin Mirgane
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Acute bronchitis
Acute bronchitisis a shorter illness that commonly follows a
cold or viral infection, such as theflu
Acute bronchitis usually lasts a few days or weeks
Chronic bronchitis
Chronic bronchitisis characterized by a persistent, mucus-
producing cough on most days of the month, three months of
a year for two successive years in absence of a secondary
cause of the cough.
TYPES OF BRONCHITIS
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Dr. Nitin Mirgane
Drugs for respiratory system 89

Bronchial asthma
Types of Asthma based on clinical condition:
Mild episodic asthma:
Seasonal asthma:
Mild chronic asthma:
Moderate asthma with frequent exacerbations:
Severe asthma:
Status asthmaticus/Refractory asthma
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Dr. Nitin Mirgane
Drugs for respiratory system 90

Inflammation or swelling of the bronchi
Coughing
Production of clear, white, yellow, grey, or green mucus
(sputum)
Shortness of breath
Wheezing
Fatigue
Fever and chills
Chest pain or discomfort
Blocked or runny nose
Signs &symptoms of bronchitis
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Dr. Nitin Mirgane
Drugs for respiratory system 91

Antiasthmaticdrugsaremedicinesthat
treatorpreventasthmaattacks.
BRONCHODILATORS:
CORTICOSTEROIDS
1
ST
choice in patients with any degree of persistent asthma
ANTI Ig-E ANTIBODY: In moderate to severe asthma patients who are poorly
controlled with conventional therapy.
 ◦Reduces steriod requirements
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Dr. Nitin Mirgane
Drugs for respiratory system 92

Decongestants
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Dr. Nitin Mirgane
Drugs for respiratory system 93

Nasal Congestion
Excessive nasal secretions
Inflamed and swollen nasal mucosa
Primary causes:
–Allergies
–Upper respiratory infections (common cold)
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Dr. Nitin Mirgane
Drugs for respiratory system 94

Decongestants
Two main types are used:
Adrenergics (largest group)
Corticosteroids
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Dr. Nitin Mirgane
Drugs for respiratory system 95

Decongestants
Two dosage forms:
Oral
Inhaled/topically applied to the nasal membranes
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Drugs for respiratory system 96

Oral Decongestants
Prolonged decongestant effects,
but delayed onset
Effect less potent than topical
No rebound congestion
Exclusively adrenergics
Examples:phenylephrine
pseudoephedrine (Sudafed)
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Dr. Nitin Mirgane
Drugs for respiratory system 97

Topical Nasal Decongestants
Both adrenergics and steroids
Prompt onset
Potent
Sustained use over several days causes
rebound congestion, making the condition
worse
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Drugs for respiratory system 98

Nasal Decongestants:
Mechanism of Action
Site of action: blood vessels surrounding
nasal sinuses
Adrenergics
–Constrict small blood vessels that supply
URI structures
–As a result, these tissues shrink and nasal
secretions in the swollen mucous membranes
are better able to drain
–Nasal stuffiness is relieved
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Drugs for respiratory system 99

Nasal Decongestants: Drug
Effects
Shrink engorged nasal mucous membranes
Relieve nasal stuffiness
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Dr. Nitin Mirgane
Drugs for respiratory system 100
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