ADRENERGIC RECEPTOR BLOCKERS

-BLOCKERS:1.Non-selective (1&2), non-

competitive: Phenoxybenzamine, Dibenamine
2. Competitive, non-selective:Phentolamine,
DHE, DHEtx
3. Competitive, 1-selective:Prazosin,
terazosin, doxazosin, tamsulosin, alfuzosin
4. - and -blockers: Labetolol, carvedilol
5. 2-selective: Yohimbine ( not used clinically)
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 ADRENERGIC RECEPTOR BLOCKERS
(contd)
-blockers:
1. Non-selective (1&2) : Propranolol,
oxprenolol, pindolol,sotalol, nadolol,
timolol
2. Cardioselective (1):Bisoprolol, esmolol,
acebutolol, atenolol, metoprolol,
celiprolol (+ at 2)
3. - and -blockers: Labetolol, carvedilol,
nebivolol, betaxolol 2
 -BLOCKERS
Pharmacological effects:
CVS: 1 blockade : Vasodilatation,
decreased TPR = fall in BP
Decreased force of cardiac contraction =
fall in BP
Postural hypotension (first dose effect)
and reflex tachycardia.
DALES VASOMOTOR REVERSAL
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 -BLOCKERS (CONTD)
Other effects: Sluggish pupil, decreased
adrenergic sweating, nasal stuffiness,
decreased resistance to urine outflow in
males ( BPH).
Phenoxybenzamine: Also blocks H1, Ach
and 5-HT receptors.
ADR: first dose effect, reflex tachycardia,
nasal stuffiness, fatigue, sedation &
nausea.
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 -BLOCKERS (CONTD)
Phentolamine :ADR: Dysrhythmias,
angina pectoris, hyperacidity, diarrhea.
Prazosin, terazosin, doxazosin : 1-
selective blockers. Less reflex tachycardia
postural hypotension and renin release.
Preferred in HTN.
Tamsulosin, alfluzosin :1A-selective
(uroselective): Preferred in BHP.
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 -BLOCKERS: USES
1. Mild to moderate HTN
2. Pheochromocytoma (with -blocker)
3. BHP
4. Raynauds disease
5. To reverse effect of adrenaline + local
anesthetic: Phentolamine infiltration
6. To prevent ischemic necrosis caused by
extravasated vasopressors:
Phentolamine infiltration
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 -blockers
Propranolol :Non-selective -blocker with
membrane stabilizing activity, no intrinsic
sympathomimetic activity.
P.K.E.:25% oral bioavailability. Food enhances
its absorption.
Effects:
C.V.S.:Negative ino-, chrono-, dromo- and
bathmotropic effects.
SA rate and AV conduction decreased
Dysrhythmias, IHD ( except variant angina),
HTN. 7
 Propranolol (contd)

Blood vessels : Vasoconstriction. No change

in BP. Chronic use reduces plasma renin activity,
thus reducing BP.
Respiratory tract :Bronchoconstriction (2-
blockade).C/I in asthmatics.
Eye : IOP decreased by reducing aqueous
humor formation :Timolol, betaxolol,
levbunolol :eye drops.
C.N.S.: Sympathetic tone is reduced :fall in BP.
Sedation, depression, sleep disturbances. 8
 Propranolol (contd)

Metabolic effects: Symptomless

hypoglycemic coma in diabetics. C/I in
DM.
Skeletal muscle tremors are blocked.

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 Cardioselective beta-blockers

Bisoprolol, Esmolol, Acebutolol, Atenolol,

Metoprolol, Celiprolol. Nebivolol.
Relatively safer in asthmatics and
diabetics.
Atenolol does not cross BBB.
They are not effective in controlling
sekletal muscle tremors.

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 Beta-blockers with ISA

Pindolol, Oxprenolol,Acebutolol.
Less myocardial depression and
bradycardia, hence preferred in patients
with low cardiac reserve.
Less likely to cause rebound hypertension
on abrupt withdrawal.

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 ADR of beta-blockers

1. CVS: Bradycardia, heart block, CCF, rebound

HTN on abrupt cessation.
2. RS: Bronchoconstriction.
3. Metabolic: Symptomless hypoglycemic coma
in diabetics.
4. CNS: Lethargy, sleep disturbances, fatigue and
deprression.
5. Others: Nausea, diarrhea and skin rash.

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 Treatment of beta-blocker overdose
1. Pace maker
2. Isoprenaline IV infusion
3. Atropine IV bolus
4. Glucagon IV bolus

C/I for non-selective beta-blockers:

Asthma
Block
CCF
DM
Variant angina
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 blockers- drug interactions
Verapamil, digitalis- SA node and AV
conduction are depressed
Insulin and hypoglycemic drugs
agonists- Hypertensive crisis

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 USES OF BETA-BLOCKERS

1.HTN
2. Angina pectoris
3.MI
4.Cardiac dysrhythmias
5. Fallots tetrology
6. Mitral stenosis with tachycardia
7. Dissecting aortic aneurysm
8. Hypertrophic cardiomyopathy
9.Subaortic stenosis
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 USES OF BETA-BLOCKERS (contd)

10. Pheochromocytoma ( with alpha-blocker)

11. Thyrotoxicosis
12. Migraine Prophylaxis: Propranolol
13. Glaucoma : Timolol, betaxolol, levbunolol
14. Anxiety states
15. Alcohol withdrawal symptoms.
16. CHF: Metoprolol, celiprolol, nebivolol

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THANK YOU

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