ADRENERGIC RECEPTOR BLOCKERS

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

-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 : 1selective 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.
2.
3.
4.
5.

Mild to moderate HTN

Pheochromocytoma (with -blocker)
BHP
Raynauds disease
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.

Propranolol (contd)
Blood vessels : Vasoconstriction. No change

in BP. Chronic use reduces plasma renin activity,

thus reducing BP.
Respiratory tract :Bronchoconstriction (2blockade).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.
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Propranolol (contd)
Metabolic effects: Symptomless
hypoglycemic coma in diabetics. C/I in
DM.
Skeletal muscle tremors are blocked.

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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1.
2.
3.
4.

Treatment of beta-blocker overdose

Pace maker
Isoprenaline IV infusion
Atropine IV bolus
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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