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Beta blockers or beta-adrenergic blocking agents are a class of drugs used to treat a variety of cardiovascular conditions and some other diseases.

Operation

Beta blockers block the action of epinephrine and norepinephrine on the β-adrenergic receptors in the body (primarily in the heart, peripheral blood vessels, bronchi, pancreas, and liver). The hormones and neurotransmitters stimulate the sympathetic nervous system by acting on these receptors.

There are three types of beta receptors: β₁-receptors located mainly in the heart, and β₂-receptors located all over the body, but mainly in the lungs, muscles and arterioles. β₃-receptors are less well characterised, but have a role in fat metabolism.

Activation of β₁-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Drugs that block these receptors therefore have the reverse effect: they lower the heart rate and blood pressure and hence are used in conditions when the heart itself is deprived of oxygen. They are routinely prescribed in patients with ischemic heart disease and hypertension. In addition, beta blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels.

Drugs that block β₂ receptors generally have a calming effect and are prescribed for anxiety, migraine, esophageal varices and alcohol withdrawal syndrome, among others.

Many beta blockers affect both type 1 and type 2 receptors; these are termed non-selective blockers. Propranolol and nadolol are examples. Selective beta blockers primarily affect β₁-receptors. Non-selective beta blockers should generally not be used in patients with asthma or any reactive airway disease. Doing so can precipitate bronchospasm by blocking the β₂ mediated relaxation of the bronchiole muscles.

Selective beta blockers generally only block the type 1 receptor. They gradually become less selective at higher doses. Examples of selective beta₁ blockers in common use include atenolol and metoprolol.

Since they lower heart rate, beta blockers have been used by some Olympic marksmen to provide more aiming time between heart beats. Some musicians use beta blockers to avoid stage fright and tremor during auditions and performances. Beta blockers decrease nocturnal melatonin release, perhaps explaining the impotence side effect through suppression of morning erections.

1. Stoschitzky K, Sakotnik A, Lercher P, Zweiker R, Maier R, Liebmann P, Lindner W. Influence of beta-blockers on melatonin release. Eur J Clin Pharmacol. 1999 Apr;55(2):111-5. PMID 10335905

Beta Blockers at a Glance

By receptor type:

Beta 1 selective (Cardio selective): Atenolol, Acebutolol, Betaxolol, Bisoprolol, Esmolol, Metoprolol, Nebivolol.

• Preferable in points with bronchospastic disease, diabetes, peripheral vascular ds. e.g. Raynaud’s phenomenon (bronchoconstriction, inhibition of glycogenolysis, vasoconstriction are due to β₂ blockade)

Beta 2 selective—Butoxamine

• Additional a1 antagonistic activity: Bucindolol, Carvedilol, Labetolol, Medroxolol
• Potentially advantageous in points with hypertension, occlusive peripheral artery ds. (promote vasodilatation)

Partial agonist (intrinsic sympathomimetic) activity: Acebutolol, Bopindolol, Carteolol, Celiprolol*, Labetolol, Oxiprenolol, Penbutolol, Pindolol (Beta 1 selective antagonist with β₂-agonist activity; also has non-adrenergic receptor-mediated vasodilating property.)

• Potentially advantageous in points with hypertension, occlusive peripheral artery ds. (Promote vasodilatation)

• Less likely to cause bradycardia, bronchoconstriction, lipid abnormalities.

Local anaesthetic action (membrane stabilizing property/ Na channel blockade): Acebutolol, Propranolol, Propafenone; slight activity: Betaxolol, Labetolol, Metoprolol, Pindolol

By lipid solubility:

High: Propranolol, Penbutolol

• Readily cross BBB—central effects, large volume of distribution

Low: Atenolol, Esmolol, Nadolol

• Don’t cross BBB—no central effects

By half-life:

Long: Betaxolol, Nadolol (14–22 hours)

• OD dosing.

Shortest: Esmolol (8–10 minute)

• Hydrolyzed by esterases in erythrocytes)
• Given as intravenous infusion in urgent settings.

Intermediate: between 3 and 12 hours

By oral bioavailability:

High: Betaxolol, Pindolol, Penbutolol, and Sotalol

Low: Carvedilol, Esmolol, Labetolol, Nadolol, Propranolol

Miscellaneous:

No effect on plasma rennin activity: Pindolol

Anti-oxidant activity: Carvedilol

Antiarrythmic action (independent of β-blocking action): Sotalol

Uses

• Hypertension
• Prophylaxis of angina
• Prophylaxis of MI—Metoprolol, Propranolol, Timolol
• Mild-moderate CHF (Contraindicated in compensated heart failure) – Bisoprolol, Bucindolol, Carvedilol, Metoprolol
• Hypertrophic obstructive cardiomyopathy – esp. Propranolol
• Pheochromocytoma (a blocker given before β-blocker)
• Acute dissecting aortic aneurysm
• Marfan’s syndrome (Chr. Tt. with Propran. slows progression of aortic dilatation and its complications)
• Hyperthyroidism
• Prophylaxis of Migraine — Metoprolol, Propranolol, Timolol
• Somatic manifestations of anxiety (e.g. tremors) — Propranolol
• Glaucoma (↓ aqueous production) — Betaxolol, Carteolol, Levobunolol, Metipranolol, Timolol
• Prevention of vericial bleeding in portal hypertension -Propranolol, Nadolol

External links

• Musicians using beta blockers
• Better Playing Through Chemistry by Blair Tindall, New York Times, October 17, 2004. (Discussing the use of beta-blockers among professional musicians.)

• Beta blockers
• Scottish inventions