The document outlines the pharmacology and clinical uses of adrenergic blockers, specifically focusing on various generations of beta blockers and their characteristics. It discusses their mechanisms, effects, side effects, contraindications, and drug interactions, emphasizing differences among nonselective and cardioselective beta blockers. It also highlights specific clinical applications for conditions such as hypertension, myocardial infarction, and glaucoma.

1. ADRENERGIC BLOCKERS
ADRENERGIC BLOCKERS

3. ADRENERGIC BLOCKERS
ADRENERGIC BLOCKERS
Receptor Bs
Receptor Bs Neurone Bs
Neurone Bs
1. Synthesis inhibitor
1. Synthesis inhibitor
α
α Bs
Bs 
Bs
Bs 2. Storage inhibitor
2. Storage inhibitor
3. NE Release
3. NE Release
inhibitors
inhibitors
α
α &
& 
 -
- Bs.
Bs.

4. Points to consider
Points to consider
1
1 CNS – entry ?
CNS – entry ?
2
2 Block all the subtypes
Block all the subtypes /
/ selectivity ‘one’ subtype ?
selectivity ‘one’ subtype ?
3
3 Is 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? )
4
4 Any 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 Blockerss
Beta Blockerss

7. First Generation
First Generation BBs.
BBs.
Nonselective BBs
Nonselective BBs
(
(Block both
Block both β
β1 &
1 & β
β2 Receptors)
2 Receptors)
Without ISA
Without ISA
1.
1. Propranolol
Propranolol
2.
2. Sotalol
Sotalol
3.
3. Timolol
Timolol
4.
4. Nadolol
Nadolol
V With ISA
With ISA
1.
1. Pindolol
Pindolol
2.
2. Penbutolol
Penbutolol

8. Second Generation BBs
Second Generation BBs
(cardioselective /
(cardioselective / β
β1 selective )
1 selective )
Without ISA
Without ISA
1.
1. Atenolol
Atenolol
2.
2. Metoprolol
Metoprolol
3.
3. Esmolol
Esmolol
4.
4. Bisoprolol
Bisoprolol
With ISA
With ISA
1.
1. Acebutolol
Acebutolol (LA)
(LA)

9. Third Generation Beta Blockers
Third Generation Beta Blockers
Non Selective
Non Selective
1.
1. Bucindolol
Bucindolol
2.
2. Carvedilol
Carvedilol
3.
3. Carteolol
Carteolol (ISA-
(ISA- β
β2
2+
+
)
)
4.
4. Labetalol
Labetalol (ISA-
(ISA- β
β2
2+
+
)
)
β
β1 selective
1 selective
1.
1. Betaxolol
Betaxolol (LA)
(LA)
2.
2. Celiprolol
Celiprolol (ISA-
(ISA- β
β2
2+
+
)
)
3.
3. Nebivolol
Nebivolol (ISA-
(ISA- β
β3
3+
+
)
)

10. Special Points To Remember:
Special Points To Remember:
1. With Local Anesthetic activity
1. With Local Anesthetic activity:
: ( no ocular use )
( no ocular use )
Propranolol, Pindolol , Acebutolol & Labetalol
Propranolol, 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 & Pindolol
Metoprolol, 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 :
1
1 
 propensity to cause
propensity to cause bronchoconstriction
bronchoconstriction
2
2 
 interference with
interference with CHO-metabolism
CHO-metabolism
3
3 
 incidence of
incidence of cold hands and feet &
cold hands and feet &
precipitation Reynaud's phenomenon
precipitation Reynaud's phenomenon
4
4 No deleterious effect
No deleterious effect on lipid profile
on lipid profile
5
5 Less impairment of
Less impairment of exercise capacity
exercise capacity

12. Lipid Insolubility
Lipid Insolubility
Atenolol, Nadolol, Sotolol
Atenolol, Nadolol, Sotolol
1.
1. Less CNS side effects
Less CNS side effects
2.
2. Incomplete oral absorption
Incomplete oral absorption
3.
3. Longer duration of action
Longer duration of action
4.
4. No 1
No 1st
st
pass effect
pass effect
5.
5. Narrow dose-range
Narrow dose-range

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

14. Pharmacological Actions of Beta Blockers
Pharmacological Actions of Beta Blockers
1.
1. ALL ARE COMPETITIVE BLOCKERS
ALL ARE COMPETITIVE BLOCKERS
2.
2. Non selective
Non selective β
β blockers act on both
blockers act on both β
β1and
1and β
β2
2
receptors
receptors
3.
3. No clinical use for
No clinical use for β
β2 antagonists
2 antagonists
4.
4. All
All β
β blockers lower blood pressure in hypertension
blockers lower blood pressure in hypertension
5.
5. They do not induce postural hypotension
They do not induce postural hypotension
6.
6. Α
Αdrenergic
drenergic α
α receptors remain functional
receptors remain functional

15. First Generation Beta Blockers.
First Generation Beta Blockers.
Nonselective BBs
Nonselective BBs
(Block both
(Block both β
β1 &
1 & β
β2 Receptors)
2 Receptors)
Without ISA
Without ISA
1.
1. Propranolol
Propranolol
2.
2. Sotalol
Sotalol
3.
3. Timolol
Timolol
4.
4. Nadolol
Nadolol
V With ISA
With ISA
1.
1. Pindolol
Pindolol
2.
2. Penbutolol
Penbutolol

16. Propranolol
Propranolol
(
( Prototype )
Prototype )

17. Actions Mediated via
Actions Mediated via 
1
1 – blockade
– blockade
1.
1. CVS:
CVS: 
 Rate,
Rate, 
 FOC,
FOC, 
 CO
CO,
, 
 Cardiac work,
Cardiac work,

 O
O2
2 consumption
consumption
USE:
USE: Angina, SVT, MI, HT
Angina, SVT, MI, HT
ADR
ADR: Heart block, Pptn. of CHF, Bradycardia
: Heart block, Pptn. of CHF, Bradycardia
2. CHO-metabolism
2. CHO-metabolism
Blunting of warning signals of hypoglycemia
Blunting of warning signals of hypoglycemia
Caution –
Caution – Diabetics on drug treatment
Diabetics on drug treatment

18. Actions
Actions Mediated via
Mediated via 
2 blockade
2 blockade
1.
1. Blood vessel
Blood vessel
prevents vasodilatation
prevents vasodilatation 
 unopposed
unopposed α
α1 action
1 action

 VC
VC 
 
 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 prophylaxis
Migraine 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 /
Asthma
Asthma –
– contraindicated
contraindicated
3. CHO-metabolism
3. CHO-metabolism
Correction of hypoglycemia
Correction of hypoglycemia –
– impaired
impaired
(-) glycogenolysis in heart, liver &
(-) glycogenolysis in heart, liver & Ske.muscle
Ske.muscle
caution –
caution – diabetics on treatment
diabetics on treatment
4. Ske. Muscle:
4. Ske. Muscle:
Inhibits adrenergically provoked tremor
Inhibits adrenergically provoked tremor

20. 5. Na
5. Na+
+
reabsorption :
reabsorption :

 BP
BP 
 
 RBF
RBF 
 
 Na
Na+
+
retention
retention

 Blood volume
Blood volume
So, combined with a diuretic
So, combined with a diuretic
6. LIPID metabolism
6. LIPID metabolism

 TG,
TG, 
 LDL,
LDL, 
 HDL
HDL
Blockers with ISA &cardioselective Bs:
Blockers with ISA &cardioselective Bs:
-
- no such effect
no 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 property
but not clinically used because of its irritant property

22. Pharmacokinetics
Pharmacokinetics
• Propranolol
Propranolol WELL ABSORBED
WELL ABSORBED ORALLY
ORALLY
• Low bioavailability due to
Low bioavailability due to high first pass
high first pass
metabolism
metabolism
• Lipophilic ,
Lipophilic , penetrates into brain
penetrates into brain
• Metabolism: liver-
Metabolism: liver- depends on hepatic blood
depends on hepatic blood
flow
flow
• More than 90%
More than 90% plasma protein bound
plasma protein bound

23. Clinical Use
Clinical Use

24. Cardiac Uses
Cardiac Uses
1. Hypertension
1. 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 & AF
AFl & AF
5.
5. Hypertrophic Cardiomyopathy
Hypertrophic Cardiomyopathy
6.
6. Dissecting aortic aneurysm:
Dissecting aortic aneurysm: 
 FOC
FOC
7.
7. Congestive cardiac failure
Congestive cardiac failure
Carvedilol, metoprolol
Carvedilol, metoprolol 
 reduce mortality rate
reduce mortality rate

26. Non Cardiac Uses
Non Cardiac Uses
1.
1. Glaucoma
Glaucoma
Chronic simple & narrow angle
Chronic simple & narrow angle
2.
2. Migraine
Migraine: For Chronic Prophylaxis
: For Chronic Prophylaxis
3.
3. Anxiety :
Anxiety : Controls somatic manifestations
Controls somatic manifestations
4.
4. Pheochromocytoma:
Pheochromocytoma: To control cardiac
To control cardiac
manifestations
manifestations (after an
(after an α
α blocker)
blocker)
5.
5. Thyrotoxicosis
Thyrotoxicosis
To prevent
To prevent T
T4
4 
 T
T3,
3, for symptomatic control
for symptomatic control
6.
6. Essential Tremor
Essential Tremor

27. ADR of BBs
ADR of BBs
Extension of their Pharmacological Actions
Extension 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 CHF
B. Heart block & Precipitation of CHF
B.
B. Worsening of
Worsening of PVD
PVD due to
due to unopposed
unopposed α
α1
1
action on blood vessels
action on blood vessels
C. Exacerbation of
C. Exacerbation of Prinzmetal angina
Prinzmetal angina due to
due to
unopposed
unopposed α
α1 action on coronary vessels.
1 action on coronary vessels.
2.
2. Respiratory:
Respiratory:
Severe bronchospasm
Severe bronchospasm due to bronchial
due to bronchial β
β2 blockade
2 blockade in
in
COPD & Bronchial asthma
COPD & Bronchial asthma

29. 3.
3. CNS:
CNS:
Sleep disturbances,
Sleep disturbances, hallucinations,
hallucinations, mental depression
mental depression
4.
4. Metabolic:
Metabolic:
During Hypoglycemia:
During Hypoglycemia:
Masking of warning signals &
Masking of warning signals & Delayed recovery
Delayed 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 & fatigue
tiredness & fatigue

30. 5.
5. Sexual Dysfunction:
Sexual Dysfunction:
6.
6. Allergic Reactions:
Allergic Reactions:
7.
7. Pregnancy:
Pregnancy:
Hypoglycemia & bradycardia in neonates
Hypoglycemia & 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/ MI
acute angina / HT/ MI &
& even sudden death
even sudden death
HENCE ALWAYS TAPER THE DOSE & STOP
HENCE ALWAYS TAPER THE DOSE & STOP

31. Contraindications to BBs. use
Contraindications to BBs. use
Absolute
Absolute
1. Severe Bradycardia
1. Severe Bradycardia
2. Pre-existing high grade heart
2. Pre-existing high grade heart
block
block
3. Overt untreated LVF
3. Overt untreated LVF
4. Cardiogenic shock
4. Cardiogenic shock
5. Severe bronchospasm
5. Severe bronchospasm
6. Severe depression
6. Severe depression
7. Active Reynaud's disease
7. Active Reynaud's disease
Relative
Relative
1.
1. Prinzmetal angina
Prinzmetal angina
2.
2. Concomitant use of
Concomitant use of
Verapamil / Diltiazem /
Verapamil / Diltiazem /
Digoxin
Digoxin
3.
3. Mild asthma
Mild asthma
4.
4. Diabetic patients on OHA /
Diabetic patients on OHA /
Insulin
Insulin

32. Drug Interactions
Drug Interactions
1. Propranolol + digitalis / verapamil
1. Propranolol + digitalis / verapamil
- Additive depression of SA & AV node conduction
- Additive depression of SA & AV node conduction
2. Propranolol + insulin / oral hypoglycemics
2. 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 + α
α agonists present in cold remedies
agonists present in cold remedies
marked
marked 
 in BP
in BP

33.  In Blood Sugar Level
In 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 BBs
Second Generation BBs
(cardioselective /
(cardioselective / β
β1 selective )
1 selective )
Without ISA
Without ISA
1.
1. Atenolol
Atenolol
2.
2. Metoprolol
Metoprolol
3.
3. Esmolol
Esmolol
4.
4. Bisoprolol
Bisoprolol
With ISA
With ISA
1.
1. Acebutolol
Acebutolol (LA)
(LA)

36. Advantages of cardioselectivity :
Advantages of cardioselectivity :
1
1 
 propensity to cause
propensity to cause bronchoconstriction
bronchoconstriction
2
2 
 interference with
interference with CHO-metabolism
CHO-metabolism
3
3 
 incidence of
incidence of hands and cold feet &
hands and cold feet &
precipitation Reynaud's phenomenon
precipitation Reynaud's phenomenon
4
4 No deleterious effect
No deleterious effect on lipid profile
on lipid profile
5
5 Less impairment of
Less impairment of exercise capacity
exercise capacity

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

38. Pharmacokinetics
Pharmacokinetics
• 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 -
- Bisoprolol
Bisoprolol

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

40. Indications & CI
Indications & CI
• Esmolol
Esmolol ( t
( t ½
½ 10 min)
10 min):
: IV use in
IV use in
-
- Hypertensive emergencies
Hypertensive 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 β
β 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 BBs
Third Generation BBs
Non Selective
Non Selective
1.
1. Bucindolol
Bucindolol
2.
2. Carvedilol
Carvedilol
3.
3. Carteolol
Carteolol (ISA-
(ISA- β
β2
2+
+
)
)
4.
4. Labetalol
Labetalol (ISA-
(ISA- β
β2
2+
+
)
)
β
β1 selective
1 selective
1.
1. Betaxolol
Betaxolol (mild LA)
(mild LA)
2.
2. Celiprolol
Celiprolol (ISA-
(ISA- β
β2
2+
+
)
)
3.
3. Nebivolol
Nebivolol (ISA-
(ISA- β
β3
3+
+
)
)

42. These are drugs with
These are drugs with vasodilating
vasodilating action through:
action through:
1.
1. α
α1 blockade
1 blockade :
: bucindolol , labetalol,
bucindolol , labetalol,
carvedilol
carvedilol
2.
2. ‘
‘NO’ production :
NO’ production : celiprolol, nebivolol, carteolol
celiprolol, nebivolol, carteolol
3.
3. β
β2 agonism :
2 agonism : celiprolol, carteolol
celiprolol, carteolol
4.
4. Ca
Ca2+
2+
entry blockade :
entry blockade : carvedilol & betaxolol
carvedilol & betaxolol
5.
5. K
K +
+
channel opening :
channel opening : tilisolol
tilisolol
6.
6. Antioxidant action :
Antioxidant action : carvedilol
carvedilol

43. Uses
Uses
1.
1. HT:
HT: all agents
all agents
2.
2. CHF:
CHF: Carvedilol, Nebivolol
Carvedilol, 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: Celiprolol
Celiprolol
6.
6. Pheochromocytoma:
Pheochromocytoma: Labetalol
Labetalol
7.
7. Clonidine withdrawal :
Clonidine withdrawal : Labetalol
Labetalol

44. OCULAR BETA BLOCKERS
OCULAR BETA BLOCKERS
Chronic Wide angle glaucoma –
Chronic Wide angle glaucoma – as main drug
as main drug
Acute Narrow angle glaucoma –
Acute Narrow angle glaucoma – as adjuvant drug
as adjuvant drug
• Timolol :
Timolol :
Beta Blocker of choice for topical use.
Beta Blocker of choice for topical use.
• Betaxolol
Betaxolol
• Levobunolol
Levobunolol
• Cartiolol
Cartiolol
• Metipranolol
Metipranolol :
: Exclusively For Topical Use In Eye
Exclusively For Topical Use In Eye

45. Essay
Essay
1.
1. Classify beta blockers. Explain the pharmacological
Classify beta blockers. Explain the pharmacological
actions, uses and adverse effects of propranolol
actions, 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 CHF
Carvedilol in CHF
Write short notes on :
Write short notes on :
1.
1. Cardioselective Beta Blockers
Cardioselective Beta Blockers 2. Propranolol
2. Propranolol
3.
3. Esmolol
Esmolol 4. Atenolol
4. Atenolol 5. Labetalol
5. Labetalol

46. Alpha Blockers
Alpha Blockers
1.
1. α
α1
1 Selective Bs
Selective Bs
Prazosin Terazosin
Prazosin Terazosin
Doxazosin Alfuzosin
Doxazosin Alfuzosin Tamsulosin
Tamsulosin
2. Nonselective
2. Nonselective α
α Bs
Bs
Phentolamine
Phentolamine :
: competitve block
competitve block
Phenoxybenzamine
Phenoxybenzamine :
: non competitive –
non competitive – irreversible
irreversible
3.
3. α
α Blockers
Blockers with
with additional
additional ‘ R ’
‘ R ’ blockade
blockade
Ergotamine & Ergotoxine
Ergotamine & Ergotoxine

47. Effects of Selective blockade
Effects of Selective blockade

48. Actions:
Actions:
1
1 Blood vessels
Blood vessels

 BP, Nasal stuffiness
BP, Nasal stuffiness
2.
2. Eye
Eye
Miosis due to (
Miosis due to (α
α1
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 & H2
2O 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 α
α mediated contraction of vas
mediated contraction of vas
deference & related organs
deference & related organs 
 impaired
impaired
ejaculation
ejaculation 
 impotence
impotence

50. USES
USES
1.
1. Hypertension
Hypertension
2.
2. Benign Prostatic Hypertrophy
Benign Prostatic Hypertrophy
3.
3. Pheochromocytoma
Pheochromocytoma
4.
4. Peripheral vascular disease
Peripheral vascular disease
5.
5. To abort acute migraine attack
To 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 PROFILE
ADR PROFILE
1.
1. Orthostatic hypotension
Orthostatic hypotension
2.
2. Tachycardia:
Tachycardia: (-) of
(-) of α
α 2
2 auto regulation
auto regulation
3. Vertigo :
3. Vertigo : Drugs with good CNS entry
Drugs with good CNS entry
Prazosin, Terazosin
Prazosin, Terazosin
4.
4. Sexual Dysfunction-
Sexual Dysfunction- Inhibits ejaculation
Inhibits ejaculation
5.
5. First dose effect :
First dose effect : Fainting
Fainting
6.
6. Na & H
Na & H2
2O Retention
O Retention
7. Development of tolerance
7. Development of tolerance to anti HT effect
to anti HT effect

52. Tamsulosin
Tamsulosin
α
α1a
1a Selective Blocker
Selective Blocker
Prostate & urinary bladder specific
Prostate & urinary bladder specific
Advantage: -
Advantage: - Less side effects like
Less 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
α
α1a
1a Selective Blocker
Selective Blocker
- Prostate & urinary bladder specific
- Prostate & urinary bladder specific
Advantage:
Advantage:
-
- Less side effects like
Less 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’ Blockade
Alpha Blockers With Additional ‘R’ Blockade
Ergotamine & Ergotoxine
Ergotamine & Ergotoxine
• Potent
Potent α
α block
block
• 5HT ‘R’ blockade
5HT ‘R’ blockade
• DA ‘R’ blockade
DA ‘R’ blockade
• Long lasting vasoconstrictor effect
Long lasting vasoconstrictor effect
Principal use :
Principal use :
- In migraine:
- In migraine: to abort an acute attack
to abort an acute attack

55. Neurone Blockers
Neurone Blockers
Reserpine
Reserpine
- Blocks transport of
- Blocks transport of Biogenic Amines
Biogenic Amines
Limitation
Limitation
- Mental depression,
- Mental depression,
- Parkinsonian syndrome
- Parkinsonian syndrome
Guanethidine
Guanethidine
-
- NE release – blocker,
NE release – blocker,
- 1
- 1st
st
displaces NE
displaces NE 
 ‘mimics’
‘mimics’
Limitation
Limitation
- Impotence
- Impotence
- Postural hypotension
- Postural hypotension

56. ADR of storage & release inhibitors
ADR of storage & release inhibitors
1. Postural hypotension
1. Postural hypotension
2. Impaired ejaculation
2. Impaired ejaculation
3. Nasal congestion
3. Nasal congestion
4. Greater GI activity
4. Greater GI activity
ADR of blockers of central sympathetic outflow
ADR of blockers of central sympathetic outflow
1. Sedation
1. Sedation
2. Na & water retention
2. Na & water retention
3. Rebound hypertension
3. Rebound hypertension
4. Endocrine problems
4. Endocrine problems

57. Essay
Essay
1.
1. Classify beta blockers. Explain the pharmacological
Classify beta blockers. Explain the pharmacological
actions, uses and adverse effects of propranolol
actions, 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 CHF
Carvedilol in CHF
Write short notes on :
Write short notes on :
1.
1. Cardioselective Beta Blockers
Cardioselective Beta Blockers 2. Propranolol
2. Propranolol
3.
3. Esmolol
Esmolol 4. Atenolol
4. Atenolol 5. Labetalol
5. Labetalol
6.
6. Tamsulosin
Tamsulosin 6. Prazosin
6. Prazosin