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2.4 Beta-adrenoceptor blocking drugs

*Atenolol tablets, syrup, injection
Labetalol tablets, injection
*Metoprolol tablets, injection.
Propranolol tablets, syrup, injection
Timolol tablets
*Carvedilol tablets
*Bisoprolol tablets
Esmolol

Relatively cardioselective agents are marked* although even these have been associated with bronchospasm.

Notes:

1. Propranolol is also included in the Guideline for anxiety and migraine prophylaxis.

2. Carvedilol and bisoprolol are consultant use only-see shared care guidelines for use in stable heart failure.

3. Esmolol: once control has been achieved consideration should be given to converting to an alternative longer acting beta-blocker.

Pharmacological Properties of Beta Blockers

Plasma half-life of the drug, although important, is less relevant than the biological half-life which depends on the mode of action in the condition being treated. For example for the treatment of angina, which depends critically on beta-1 blockade, propranolol must be given 3-4 times daily; once or twice daily is adequate for hypertension.

Lipid soluble beta-blockers (propanolol, metoprolol) are rapidly absorbed and extensively metabolised in the liver and most have short half-lives. They cross the blood-brain barrier readily and may cause CNS side effects, e.g bad dreams, headache. Topical formulations of lipid-soluble beta-blockers (e.g. timolol eye drops) are also well absorbed and may cause systemic effects.

Water soluble beta-blockers (atenolol, sotalol) are less well absorbed, excreted virtually unchanged by the kidney and have longer plasma half-lives. They penetrate the blood-brain barrier poorly.

 

For link to BNF section: 2.4 Beta-adrenoceptor blocking drugs