Review of Pharmacology - 9E (2015)

Autonomic Nervous System
Lipid Insoluble β-Blockers
These agents are mainly excreted by kidney and are therefore contraindicated in renal failure.
Most of these have long duration of action
*Not
*Soluble
– Nadolol (longest acting β blocker)
– Sotalol
*A – Atenolol
– Acebutolol
*B – Betaxolol
Beta blockers contra-indicated
in renal failure
A – Atenolol
N – Nadolol
S – Sotalol
– Bisoprolol
* C – Celiprolol
Other β blockers are metabolized mainly by liver and are short acting (shortest acting β
blocker is esmolol)
Note: Acebutolol possesses all activities i.e. cardioselectivity, ISA, membrane stabilizing action and
lipid insolubility.
Third Generation b-Blockers
These drugs possess additional vasodilatory property. It may be due to α blockade (labetalol,
carvedilol), β 2
agonism (celiprolol, carteolol, bopindolol), release of NO (nebivolol, nipradilol),
opening of K + channels (tilisolol) or inhibition of Ca 2+ channels (carvedilol, bevantolol,
betaxolol).
Autonomic General Pharmacology
Nervous System
Uses of b-blockers
Cardiac (due to b 1
blockade)
Hypertension
Classical angina
Myocardial infarction
Supraventricular arrhythmias
Chronic CHF
Hypertrophic obstructive cardiomyopathy (DOC)
Emergency management of symptoms of TOF
Mitral valve prolapse
Extra cardiac (due to b 2
blockade)
Pheochromocytoma (after α blockade)
Hyperthyroidism
Performance anxiety
Tremors
Akathisia
Prophylaxis of migraine
Glaucoma (timolol and betaxolol)
Alcohol and opioid withdrawal
Prophylaxis of bleeding in portal
hypertension
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