Drugs acting on ANS_Alpha & Beta Blockers.ppt

Adrenergic blockers

1. ADRENERGIC BLOCKERSADRENERGIC BLOCKERS

3. ADRENERGIC BLOCKERSADRENERGIC BLOCKERS

Receptor BsReceptor Bs Neurone Bs Neurone Bs
1. Synthesis inhibitor1. Synthesis inhibitor
αα BsBs BsBs 2. Storage inhibitor2. Storage inhibitor
3. NE Release 3. NE Release
inhibitorsinhibitors

αα &&  - - Bs.Bs.

4. Points to considerPoints to consider
11CNS – entry ?CNS – entry ?
22Block all the subtypes Block all the subtypes / / selectivity ‘one’ subtype ?selectivity ‘one’ subtype ?
33Is there any intrinsic sympathetic activity ?Is there any intrinsic sympathetic activity ? (are they (are they
partial agonists of any subtype? )partial agonists of any subtype? )
44Any reflex activity triggered by blockade? Eg. Any reflex activity triggered by blockade? Eg. CVS.CVS.
5.5.Do they have Mb – stabilizing effect ( LA )Do they have Mb – stabilizing effect ( LA )? ?
6.6.Additional mechanism of action other than adrenergic Additional mechanism of action other than adrenergic
blockade?blockade?

5. Beta BlockerssBeta Blockerss

7. First Generation First Generation BBs.BBs.
Nonselective BBsNonselective BBs
((Block both Block both ββ1 & 1 & ββ2 Receptors)2 Receptors)
Without ISAWithout ISA
1.1.PropranololPropranolol
2.2.SotalolSotalol
3.3.TimololTimolol
4.4.NadololNadolol
V With ISAWith ISA
1.1.PindololPindolol
2.2.PenbutololPenbutolol

8. Second Generation BBsSecond Generation BBs
(cardioselective / (cardioselective / ββ1 selective )1 selective )
Without ISA Without ISA
1.1. AtenololAtenolol
2.2. MetoprololMetoprolol
3.3. EsmololEsmolol
4.4. BisoprololBisoprolol
With ISAWith ISA
1.1. Acebutolol Acebutolol (LA)(LA)

9. Third Generation Beta BlockersThird Generation Beta Blockers
Non SelectiveNon Selective
1.1.BucindololBucindolol
2.2.CarvedilolCarvedilol
3.3.Carteolol Carteolol (ISA-(ISA- β β22
++
))
4.4.Labetalol Labetalol (ISA- (ISA- ββ22
++
))
ββ1 selective1 selective
1.1.Betaxolol Betaxolol (LA)(LA)
2.2.Celiprolol Celiprolol (ISA-(ISA- β β22
++
))
3.3.Nebivolol Nebivolol (ISA-(ISA- β β33
++
))

10. Special Points To Remember:Special Points To Remember:
1. With Local Anesthetic activity1. With Local Anesthetic activity:: ( no ocular use )( no ocular use )
Propranolol, Pindolol , Acebutolol & LabetalolPropranolol, Pindolol , Acebutolol & Labetalol
2. Lipid solubility & CNS entry: 2. Lipid solubility & CNS entry: ( CNS - USE / ADR)( CNS - USE / ADR)High-High-
Propranolol, Propranolol, Low – Low – All others.All others.Moderate - Moderate - Timolol, Timolol,
Metoprolol, Carvedilol & PindololMetoprolol, Carvedilol & Pindolol
3. Oral Bioavailability: 3. Oral Bioavailability: Low – Low – Propranolol, Nadolol, Labetal0ol, Propranolol, Nadolol, Labetal0ol,
Carvedilol Carvedilol Moderate – Moderate – Timolol & Betaxolol, Celiprolol, Timolol & Betaxolol, Celiprolol,
Acebutolol Acebutolol High – High – All others. All others.
4. Ocular Use: 4. Ocular Use: (no LA activity)(no LA activity)
Timolol, Levobunolol, Carteolol, Betaxolol, Metipranolol Timolol, Levobunolol, Carteolol, Betaxolol, Metipranolol

11. Advantages of cardioselectivity :Advantages of cardioselectivity :
11 propensity to cause propensity to cause bronchoconstrictionbronchoconstriction
22 interference with interference with CHO-metabolismCHO-metabolism
33 incidence of incidence of cold hands and feet & cold hands and feet &
precipitation Reynaud's phenomenonprecipitation Reynaud's phenomenon
44No deleterious effect No deleterious effect on lipid profileon lipid profile
55Less impairment of Less impairment of exercise capacityexercise capacity

12. Lipid InsolubilityLipid Insolubility
Atenolol, Nadolol, SotololAtenolol, Nadolol, Sotolol
1.1. Less CNS side effectsLess CNS side effects
2.2. Incomplete oral absorptionIncomplete oral absorption
3.3. Longer duration of actionLonger duration of action
4.4. No 1No 1
stst
pass effect pass effect
5.5. Narrow dose-rangeNarrow dose-range

13. Drugs with ISADrugs with ISA
Oxprenolol,Oxprenolol, Alprenolol, Alprenolol, Pindolol Pindolol
AcebutololAcebutolol BetaxololBetaxolol
Advantages:Advantages:
-- Prevents ‘R’ supersensitivityPrevents ‘R’ supersensitivity
- Plasma lipid profile not worsened- Plasma lipid profile not worsened
Disadvantages Disadvantages
- - Not effective in migraine prophylaxisNot effective in migraine prophylaxis

14. Pharmacological Actions of Beta BlockersPharmacological Actions of Beta Blockers
1.1.ALL ARE COMPETITIVE BLOCKERSALL ARE COMPETITIVE BLOCKERS
2.2.Non selective Non selective ββ blockers act on both blockers act on both ββ1and 1and ββ22
receptorsreceptors
3.3.No clinical use for No clinical use for ββ2 antagonists2 antagonists
4.4.All All ββ blockers lower blood pressure in hypertension blockers lower blood pressure in hypertension
5.5.They do not induce postural hypotensionThey do not induce postural hypotension
6.6.ΑΑdrenergic drenergic αα receptors remain functional receptors remain functional

15. First Generation Beta Blockers.First Generation Beta Blockers.
Nonselective BBsNonselective BBs
(Block both (Block both ββ1 & 1 & ββ2 Receptors)2 Receptors)
Without ISAWithout ISA
1.1.PropranololPropranolol
2.2.SotalolSotalol
3.3.TimololTimolol
4.4.NadololNadolol
V With ISAWith ISA
1.1.PindololPindolol
2.2.PenbutololPenbutolol

16. PropranololPropranolol
( ( Prototype )Prototype )

17. Actions Mediated via Actions Mediated via 
11 – blockade – blockade
1.1.CVS: CVS:  Rate, Rate,  FOC,FOC,  COCO, ,  Cardiac work, Cardiac work,
 OO
22 consumption consumption
USE: USE: Angina, SVT, MI, HT Angina, SVT, MI, HT
ADRADR: Heart block, Pptn. of CHF, Bradycardia: Heart block, Pptn. of CHF, Bradycardia
2. CHO-metabolism2. CHO-metabolism
Blunting of warning signals of hypoglycemiaBlunting of warning signals of hypoglycemia
Caution –Caution – Diabetics on drug treatmentDiabetics on drug treatment

18. Actions Actions Mediated via Mediated via 2 blockade2 blockade
1.1.Blood vesselBlood vessel
prevents vasodilatationprevents vasodilatation  unopposed unopposed αα1 action 1 action
 VCVC   blood flow to periphery. blood flow to periphery.
C.I. C.I. - - Reynaud’s disease Reynaud’s disease
- Vasospastic angina- Vasospastic angina
Use: Use: Migraine prophylaxisMigraine prophylaxis
( Blocks vasodilatation in cerebral BVs)( Blocks vasodilatation in cerebral BVs)

19. 2. Bronchi – 2. Bronchi –
Bronchospasm Bronchospasm  respiratory crisis in COPD / respiratory crisis in COPD /
AsthmaAsthma – – contraindicated contraindicated
3. CHO-metabolism3. CHO-metabolism
Correction of hypoglycemiaCorrection of hypoglycemia –– impairedimpaired
(-) glycogenolysis in heart, liver & (-) glycogenolysis in heart, liver & Ske.muscleSke.muscle
caution –caution – diabetics on treatmentdiabetics on treatment
4. Ske. Muscle:4. Ske. Muscle:
Inhibits adrenergically provoked tremorInhibits adrenergically provoked tremor

20. 5. Na5. Na
++
reabsorption : reabsorption :
 BP BP   RBFRBF   NaNa
++
retention retention
 Blood volumeBlood volume
So, combined with a diureticSo, combined with a diuretic
6. LIPID metabolism 6. LIPID metabolism
 TG, TG,  LDL, LDL,  HDLHDL
Blockers with ISA &cardioselective Bs:Blockers with ISA &cardioselective Bs:
-- no such effectno such effect

21. 7.7.Eye –Eye –
- - Reduces the secretion of aqueous humor,Reduces the secretion of aqueous humor,
- IOT is lowered - IOT is lowered
- no effect on pupil size or accommodation- no effect on pupil size or accommodation
8. LA activity:8. LA activity:
• Propranolol is a Potent Local Anaesthetic as Lidocaine Potent Local Anaesthetic as Lidocaine
but not clinically used because of its irritant propertybut not clinically used because of its irritant property

22. PharmacokineticsPharmacokinetics
•Propranolol Propranolol WELL ABSORBEDWELL ABSORBED ORALLY ORALLY
•Low bioavailability due to Low bioavailability due to high first pass high first pass
metabolismmetabolism
•Lipophilic ,Lipophilic , penetrates into brainpenetrates into brain
•Metabolism: liver- Metabolism: liver- depends on hepatic blood depends on hepatic blood
flowflow
•More than 90%More than 90% plasma protein boundplasma protein bound

23. Clinical UseClinical Use

24. Cardiac UsesCardiac Uses
1. Hypertension1. Hypertension
- On prolonged admn. BP gradually falls in Hypertensives. - On prolonged admn. BP gradually falls in Hypertensives.
- Reduced Na release from sympathetic terminals- Reduced Na release from sympathetic terminals
- -  renin release from kidney renin release from kidney  marked fall in BP marked fall in BP
Advantages:Advantages:
- Sodium water retention is rare- Sodium water retention is rare
- cheaper- cheaper
- Long duration of action- Long duration of action

25. 2.2. Myocardial Infarction: Myocardial Infarction:
Acute:Acute: limits infarct size limits infarct size
Prohylactic use :Prohylactic use : mortality & reinfarction mortality & reinfarction
3.3.Angina Pectoris: Angina Pectoris: ( in angina of effort)( in angina of effort)
4.4.Cardiac Arrhythmias: Cardiac Arrhythmias: AFl & AFAFl & AF
5.5.Hypertrophic CardiomyopathyHypertrophic Cardiomyopathy
6.6.Dissecting aortic aneurysm: Dissecting aortic aneurysm:  FOC FOC
7.7.Congestive cardiac failureCongestive cardiac failure
Carvedilol, metoprolol Carvedilol, metoprolol  reduce mortality rate reduce mortality rate

26. Non Cardiac UsesNon Cardiac Uses
1.1.GlaucomaGlaucoma
Chronic simple & narrow angle Chronic simple & narrow angle
2.2.MigraineMigraine: For Chronic Prophylaxis: For Chronic Prophylaxis
3.3.Anxiety : Anxiety : Controls somatic manifestationsControls somatic manifestations
4.4.Pheochromocytoma: Pheochromocytoma: To control cardiac To control cardiac
manifestations manifestations (after an (after an αα blocker) blocker)
5.5.ThyrotoxicosisThyrotoxicosis
To preventTo prevent TT
4 4 
TT
3, 3, for symptomatic controlfor symptomatic control
6. 6. Essential TremorEssential Tremor

27. ADR of BBsADR of BBs
Extension of their Pharmacological ActionsExtension of their Pharmacological Actions

28. 1. Cardiovascular:1. Cardiovascular:
A. A. BRADYCARDIA BRADYCARDIA (STOP BBs if HR is < 60/min)(STOP BBs if HR is < 60/min)
B. Heart block & Precipitation of CHFB. Heart block & Precipitation of CHF
B.B. Worsening of Worsening of PVD PVD due to due to unopposed unopposed αα1 1
action on blood vesselsaction on blood vessels
C. Exacerbation of C. Exacerbation of Prinzmetal anginaPrinzmetal angina due to due to
unopposed unopposed αα1 action on coronary vessels.1 action on coronary vessels.
2.2. Respiratory:Respiratory:
Severe bronchospasm Severe bronchospasm due to bronchial due to bronchial ββ2 blockade2 blockadein in
COPD & Bronchial asthma COPD & Bronchial asthma

29. 3.3.CNS:CNS:
Sleep disturbances, Sleep disturbances, hallucinations, hallucinations, mental depressionmental depression
4.4.Metabolic:Metabolic:
During Hypoglycemia:During Hypoglycemia:
Masking of warning signals &Masking of warning signals & Delayed recoveryDelayed recovery
Adverse Lipid Profile:Adverse Lipid Profile:
Non selective BBs Non selective BBs  HDL and HDL and  TGs & LDL TGs & LDL
5.5.Skeletal muscle:Skeletal muscle:
muscle weakness muscle weakness  tiredness & fatiguetiredness & fatigue

30. 5.5.Sexual Dysfunction:Sexual Dysfunction:
6.6.Allergic Reactions:Allergic Reactions:
7.7.Pregnancy:Pregnancy:
Hypoglycemia & bradycardia in neonatesHypoglycemia & bradycardia in neonates
8.8.Withdrawal Symptoms:Withdrawal Symptoms:
Abrupt withdrawal after chronic use is Abrupt withdrawal after chronic use is dangerous dangerous
due to ‘R’ up regulation. due to ‘R’ up regulation. May precipitate:May precipitate:
- - acute angina / HT/ MIacute angina / HT/ MI & & even sudden deatheven sudden death
HENCE ALWAYS TAPER THE DOSE & STOPHENCE ALWAYS TAPER THE DOSE & STOP

31. Contraindications to BBs. useContraindications to BBs. use
AbsoluteAbsolute
1. Severe Bradycardia1. Severe Bradycardia
2. Pre-existing high grade heart 2. Pre-existing high grade heart
blockblock
3. Overt untreated LVF3. Overt untreated LVF
4. Cardiogenic shock4. Cardiogenic shock
5. Severe bronchospasm5. Severe bronchospasm
6. Severe depression6. Severe depression
7. Active Reynaud's disease7. Active Reynaud's disease
RelativeRelative
1.1.Prinzmetal anginaPrinzmetal angina
2.2.Concomitant use of Concomitant use of
Verapamil / Diltiazem / Verapamil / Diltiazem /
Digoxin Digoxin
3.3.Mild asthmaMild asthma
4.4.Diabetic patients on OHA / Diabetic patients on OHA /
InsulinInsulin

32. Drug InteractionsDrug Interactions
1. Propranolol + digitalis / verapamil1. Propranolol + digitalis / verapamil
- Additive depression of SA & AV node conduction - Additive depression of SA & AV node conduction
2. Propranolol + insulin / oral hypoglycemics2. Propranolol + insulin / oral hypoglycemics
- - delayed recovery from hypoglycemia & masking of delayed recovery from hypoglycemia & masking of
warning signals.warning signals.
3. Propranolol + lignocaine: 3. Propranolol + lignocaine:
 clearance of lignocaine clearance of lignocaine (( hepatic blood flow) hepatic blood flow)
4. Propranolol + 4. Propranolol + αα agonists present in cold remedies agonists present in cold remedies
marked marked  in BP in BP

33.  In Blood Sugar LevelIn Blood Sugar Level

34. 5.5.Propranolol + NSAIDs: Propranolol + NSAIDs:
 in antihypertensive effect of Propranolol.in antihypertensive effect of Propranolol.
6.6.Cimetidine + Cimetidine + Propranolol Propranolol : :
Inhibition of Inhibition of Propranolol metabolism.Propranolol metabolism.
6.6.Propranolol + Propranolol + chlorpromazine :chlorpromazine :
Propranolol Propranolol  t the first pass metabolism of he first pass metabolism of
chlorpromazine chlorpromazine   in its bioavailability in its bioavailability

35. Second Generation BBsSecond Generation BBs
(cardioselective / (cardioselective / ββ1 selective )1 selective )
Without ISA Without ISA
1.1. AtenololAtenolol
2.2. MetoprololMetoprolol
3.3. EsmololEsmolol
4.4. BisoprololBisoprolol
With ISAWith ISA
1.1. Acebutolol Acebutolol (LA)(LA)

36. Advantages of cardioselectivity :Advantages of cardioselectivity :
11 propensity to cause propensity to cause bronchoconstrictionbronchoconstriction
22 interference with interference with CHO-metabolismCHO-metabolism
33 incidence of incidence of hands and cold feet & hands and cold feet &
precipitation Reynaud's phenomenonprecipitation Reynaud's phenomenon
44No deleterious effect No deleterious effect on lipid profileon lipid profile
55Less impairment of Less impairment of exercise capacityexercise capacity

37. Advantages of having ISAAdvantages of having ISA
- Prevents ‘R’ supersensitivity- Prevents ‘R’ supersensitivity
- Plasma lipid profile not worsened- Plasma lipid profile not worsened
Disadvantages of having ISADisadvantages of having ISA
- - Not effective in migraine prophylaxisNot effective in migraine prophylaxis

38. PharmacokineticsPharmacokinetics
•Lipid solubility: Lipid solubility:
- Low with all - Low with all except except metoprolol.metoprolol.
•Absorption: Absorption:
- > 90% for all - > 90% for all except except Esmolol Esmolol (not absorbed)(not absorbed)
•Oral BA: Oral BA:
- Bisoprolol- 80% - Bisoprolol- 80% & & > 50% for all > 50% for all except except Esmolol Esmolol (NIL)(NIL)
•Duration of action:Duration of action:
- - USA-USA- Esmolol Esmolol SA SA - - Acebutalol & Metoprolol Acebutalol & Metoprolol
- - MA MA - - Atenolol Atenolol LA LA - - BisoprololBisoprolol

39. Indications & CIIndications & CI
Metoprolol: Metoprolol:
HT, Angina, Tachycardia, HF, prevention of MI, HT, Angina, Tachycardia, HF, prevention of MI,
migraine prophylaxis, Hyperthyroidismmigraine prophylaxis, Hyperthyroidism
CI:CI: in acute MIin acute MI
Atenolol:Atenolol:
Less CNS effects, & bronchospasmLess CNS effects, & bronchospasm
HT, Angina, Arrhythmias, HF, to prevent cardiac HT, Angina, Arrhythmias, HF, to prevent cardiac
complications following MI, Hyperthyroidismcomplications following MI, Hyperthyroidism
CI:CI: strokestroke

40. Indications & CIIndications & CI
•Esmolol Esmolol ( t ( t
½½ 10 min) 10 min): : IV use in IV use in
- - Hypertensive emergenciesHypertensive emergencies
- for rapid control of ventricular rate in SVT- for rapid control of ventricular rate in SVT
- during surgery to prevent / treat tachycardia, - during surgery to prevent / treat tachycardia,
- - severe postoperative HT,severe postoperative HT,
- - for for ββ blockade of short duration blockade of short duration
- - in critically ill patients when rapid withdrawal of in critically ill patients when rapid withdrawal of
a drug is indicated. a drug is indicated.

41. Third Generation BBsThird Generation BBs
Non Selective Non Selective
1.1.BucindololBucindolol
2.2.CarvedilolCarvedilol
3.3.Carteolol Carteolol (ISA-(ISA- β β22
++
))
4.4.Labetalol Labetalol (ISA- (ISA- ββ22
++
))
ββ1 selective1 selective
1.1.Betaxolol Betaxolol (mild LA)(mild LA)
2.2.Celiprolol Celiprolol (ISA-(ISA- β β22
++
))
3.3.Nebivolol Nebivolol (ISA-(ISA- β β33
++
))

42. These are drugs with These are drugs with vasodilatingvasodilating action through: action through:
1. 1. αα1 blockade1 blockade : : bucindolol , labetalol, bucindolol , labetalol,
carvedilol carvedilol
2.2. ‘ ‘NO’ production : NO’ production : celiprolol, nebivolol, carteololceliprolol, nebivolol, carteolol
3.3. ββ2 agonism : 2 agonism : celiprolol, carteololceliprolol, carteolol
4.4. CaCa
2+2+
entry blockade : entry blockade : carvedilol & betaxololcarvedilol & betaxolol
5.5. KK
+ +
channel opening : channel opening : tilisololtilisolol
6.6. Antioxidant action : Antioxidant action : carvedilolcarvedilol

43. UsesUses
1.1. HT: HT: all agentsall agents
2.2. CHF: CHF: Carvedilol, NebivololCarvedilol, Nebivolol
3.3. Hypertensive emergency: Hypertensive emergency: Labetalol (IV)Labetalol (IV)
4.4. Pregnancy induced HT-crisis: Pregnancy induced HT-crisis: Labetalol Labetalol
(no placental transfer)(no placental transfer)
5.5. Angina: Angina: CeliprololCeliprolol
6.6. Pheochromocytoma: Pheochromocytoma: Labetalol Labetalol
7.7. Clonidine withdrawal : Clonidine withdrawal : Labetalol Labetalol

44. OCULAR BETA BLOCKERSOCULAR BETA BLOCKERS
Chronic Wide angle glaucoma – Chronic Wide angle glaucoma – as main drugas main drug
Acute Narrow angle glaucoma – Acute Narrow angle glaucoma – as adjuvant drugas adjuvant drug
•Timolol : Timolol :
Beta Blocker of choice for topical use.Beta Blocker of choice for topical use.
•BetaxololBetaxolol
•LevobunololLevobunolol
•CartiololCartiolol
•MetipranololMetipranolol : : Exclusively For Topical Use In EyeExclusively For Topical Use In Eye

45. EssayEssay
1.1.Classify beta blockers. Explain the pharmacological Classify beta blockers. Explain the pharmacological
actions, uses and adverse effects of propranololactions, uses and adverse effects of propranolol
Explain the pharmacological basis for the use of :Explain the pharmacological basis for the use of :
1.1.Beta blockers in hypertension Beta blockers in hypertension
2.2.Carvedilol in CHFCarvedilol in CHF
Write short notes on :Write short notes on :
1.1.Cardioselective Beta BlockersCardioselective Beta Blockers2. Propranolol2. Propranolol
3.3.EsmololEsmolol 4. Atenolol4. Atenolol5. Labetalol 5. Labetalol

46. Alpha BlockersAlpha Blockers
1. 1. αα
11 Selective Bs Selective Bs
Prazosin Terazosin Prazosin Terazosin
Doxazosin Alfuzosin Doxazosin Alfuzosin TamsulosinTamsulosin
2. Nonselective 2. Nonselective αα Bs Bs
Phentolamine Phentolamine : : competitve blockcompetitve block
Phenoxybenzamine Phenoxybenzamine : : non competitive – non competitive – irreversibleirreversible
3. 3. αα Blockers Blockers withwith additionaladditional ‘ R ’‘ R ’ blockadeblockade
Ergotamine & ErgotoxineErgotamine & Ergotoxine

47. Effects of Selective blockadeEffects of Selective blockade

48. Actions:Actions:
11Blood vesselsBlood vessels
 BP, Nasal stuffinessBP, Nasal stuffiness
2.2.EyeEye
Miosis due to (Miosis due to (αα
1 1 block) block)
3.3. Intestinal Smooth Muscle Intestinal Smooth Muscle
 Reversal of relaxation Reversal of relaxation   motility motility
4.4.Renal Renal
 RBF RBF   GFR GFR   Na & H Na & H
22O retention O retention
  blood volume. blood volume.

49. 5.5.Urinary Bladder Urinary Bladder
Relaxation of trigone, prostate & prostatic Relaxation of trigone, prostate & prostatic
urethra urethra   urinary flow rate & emptying urinary flow rate & emptying
of bladder. of bladder.
6.6. Genital Tract Genital Tract
Blockade of Blockade of αα mediated contraction of vas mediated contraction of vas
deference & related organs deference & related organs  impaired impaired
ejaculation ejaculation  impotenceimpotence

50. USESUSES
1.1.Hypertension Hypertension
2.2.Benign Prostatic HypertrophyBenign Prostatic Hypertrophy
3.3.PheochromocytomaPheochromocytoma
4.4.Peripheral vascular diseasePeripheral vascular disease
5.5.To abort acute migraine attackTo abort acute migraine attack
6.6.Secondary shock Secondary shock
- Acts by reversing Reflex VC.- Acts by reversing Reflex VC.
(To be given only after fluid replacement) (To be given only after fluid replacement)

51. ADR PROFILEADR PROFILE
1.1. Orthostatic hypotension Orthostatic hypotension
2.2. Tachycardia: Tachycardia: (-) of (-) of αα
2 2 auto regulation auto regulation
3. Vertigo : 3. Vertigo : Drugs with good CNS entryDrugs with good CNS entry
Prazosin, TerazosinPrazosin, Terazosin
4.4. Sexual Dysfunction- Sexual Dysfunction- Inhibits ejaculation Inhibits ejaculation
5.5. First dose effect : First dose effect : FaintingFainting
6.6. Na & HNa & H
22O RetentionO Retention
7. Development of tolerance 7. Development of tolerance to anti HT effectto anti HT effect

52. Tamsulosin Tamsulosin
αα
1a1a Selective Blocker Selective Blocker
Prostate & urinary bladder specificProstate & urinary bladder specific
Advantage: - Advantage: - Less side effects likeLess side effects like
- Hypotension, Dizziness, Impotence- Hypotension, Dizziness, Impotence
- Drug interaction- Drug interaction
Use: Use: - Drug preferred for treating BPH- Drug preferred for treating BPH
- Not Used As Antihypertensive- Not Used As Antihypertensive

53. Tamsulosin Tamsulosin
αα
1a1a Selective Blocker Selective Blocker
- Prostate & urinary bladder specific- Prostate & urinary bladder specific
Advantage:Advantage:
- - Less side effects likeLess side effects like
- Hypotension, Dizziness, Impotence- Hypotension, Dizziness, Impotence
- Drug interaction- Drug interaction
Use :Use :
- Drug preferred for treating BPH- Drug preferred for treating BPH
- NOT USED AS ANTIHYPERTENSIVE- NOT USED AS ANTIHYPERTENSIVE

54. Alpha Blockers With Additional ‘R’ BlockadeAlpha Blockers With Additional ‘R’ Blockade
Ergotamine & ErgotoxineErgotamine & Ergotoxine
• Potent Potent αα block block
• 5HT ‘R’ blockade5HT ‘R’ blockade
• DA ‘R’ blockade DA ‘R’ blockade
• Long lasting vasoconstrictor effectLong lasting vasoconstrictor effect
Principal use : Principal use :
- In migraine: - In migraine: to abort an acute attackto abort an acute attack

55. Neurone BlockersNeurone Blockers
ReserpineReserpine
- Blocks transport of - Blocks transport of Biogenic AminesBiogenic Amines
LimitationLimitation
- Mental depression,- Mental depression,
- Parkinsonian syndrome- Parkinsonian syndrome
GuanethidineGuanethidine
- - NE release – blocker, NE release – blocker,
- 1- 1
stst
displaces NE displaces NE  ‘mimics’ ‘mimics’
LimitationLimitation
- Impotence- Impotence
- Postural hypotension- Postural hypotension

56. ADR of storage & release inhibitorsADR of storage & release inhibitors
1. Postural hypotension1. Postural hypotension
2. Impaired ejaculation2. Impaired ejaculation
3. Nasal congestion3. Nasal congestion
4. Greater GI activity4. Greater GI activity
ADR of blockers of central sympathetic outflowADR of blockers of central sympathetic outflow
1. Sedation1. Sedation
2. Na & water retention2. Na & water retention
3. Rebound hypertension3. Rebound hypertension
4. Endocrine problems4. Endocrine problems

57. EssayEssay
1.1.Classify beta blockers. Explain the pharmacological Classify beta blockers. Explain the pharmacological
actions, uses and adverse effects of propranololactions, uses and adverse effects of propranolol
Explain the pharmacological basis for the use of :Explain the pharmacological basis for the use of :
1.1.Beta blockers in hypertension Beta blockers in hypertension
2.2.Carvedilol in CHFCarvedilol in CHF
Write short notes on :Write short notes on :
1.1.Cardioselective Beta BlockersCardioselective Beta Blockers2. Propranolol2. Propranolol
3.3.EsmololEsmolol 4. Atenolol4. Atenolol5. Labetalol 5. Labetalol
6. 6. TamsulosinTamsulosin6. Prazosin6. Prazosin