2.4 Beta-adrenoceptor blocking drugs
Atenolol (tablets, syrup, injection) is a relatively cardioselective drug which is usually taken as a once daily dose. It is water-soluble and is excreted by the kidneys. It accumulates in patients with renal impairment.
SPECIAL INDICATIONS
Metoprolol (tablets, IV injection) is a selective, lipophilic beta-blocker with a short half-life. This makes it an attractive drug for those patients in whom it is not certain that a beta-blocker will be well tolerated. It is not recommended for general use in view of its short half-life.
Propranolol (tablets, m/r tablets, oral solution, IV injection) is a non-cardioselective beta-blocker which can be used for the treatment of anxiety, essential tremors, and the prophylaxis of migraine. Modified-release preparations permit once daily dosing but are expensive.
Labetalol (tablets, IV injection) may be used for the treatment of hypertension in pregnancy.
Pindolol (tablets) has prominent partial agonist activity, which may occasionally be used in combination with digoxin to control heart rate in atrial fibrillation.
Sotalol (tablets, injection) is a non-selective beta-blocker with additional Class III anti-arrhythmic activity, which may be used for treating supraventricular arrhythmias. It is given twice a day. It should be avoided following myocardial infarction.
Timolol (tablets) is a non-selective lipophilic beta-blocker. It is used post-myocardial infarction for secondary prevention.
Esmolol (IV injection) is used intravenously for the short-term treatment of supraventricular arrhythmias and hypertension in the peri-operative period.
Co-tenidone (atenolol 50mg/chlortalidone 12.5mg tablets, atenolol 100mg/chlortalidone 25mg tablets) is a combination of atenolol and a thiazide-related diuretic. Its use may be considered when compliance is a major problem, in patients who require both a diuretic and a beta-blocker to control hypertension. Prescribers should state the strength required. The higher strength is very prone to cause electrolyte and biochemical disturbances.
Carvedilol (tablets) is available for restricted off-label use for prophylaxis against variceal bleeding in patients with portal hypertension. Use is restricted to initiation by Gastroenterologists.
PRESCRIBING POINTS FOR BETA-ADRENOCEPTOR BLOCKING DRUGS
- Beta-blockers are used for the treatment of hypertension, angina, myocardial infarction and supraventricular arrhythmias.
- All beta-blockers are generally equally effective. The choice of product is usually made following consideration of side-effect profiles.
- Several studies have shown that beta-blockers reduce mortality and recurrence rate after myocardial infarction.
- Beta-blockers, even those with apparent cardioselectivity, should not be used in patients with asthma, and should be used with due caution in patients with obstructive airways disease.
- Beta-blockers are contra-indicated in those with second or third degree heart block.
- Non-selective beta-blockers such as propranolol or labetalol are contra-indicated in diabetics on insulin or sulphonylureas since they can mask the symptoms of hypoglycaemia. Selective beta-blockers such as atenolol or metoprolol may be used in diabetics.
- Beta-blockers are frequently given with thiazide diuretics to patients whose hypertension is not controlled by diuretics alone. The use of combination products reduces the choice of drugs and dosages and should only be considered where compliance is a genuine problem.
BETA-ADRENOCEPTOR BLOCKING DRUGS FOR HEART FAILURE
The beta-blockers carvedilol and bisoprolol reduce mortality in patients with stable heart failure and left ventricular systolic dysfunction.
Bisoprolol (tablets): - selective beta1-adrenoceptor blocker.
Carvedilol (tablets): - non-selective beta-adrenoceptor blocker, blocks alpha-receptors and has anti-oxidant activity.
PRESCRIBING POINTS FOR BETA-ADRENOCEPTOR BLOCKING DRUGS FOR HEART FAILURE
- Beta-blocker treatment should be started under specialist supervision at a very low dose and titrated very slowly over a period of weeks or months. Symptoms may deteriorate initially, calling for adjustment of concomitant therapy.
- Patients should be monitored for heart rate, oedema, breathlessness, and blood pressure after each dose increment.
- Bisoprolol is less expensive than carvedilol when optimum maximum dosages are compared.
- Bisoprolol is given once daily while carvedilol is given twice daily. Bisoprolol may offer better compliance.
- Beta-blocker treatment should be started under specialist supervision at a very low dose and titrated very slowly over a period of weeks or months. Symptoms may deteriorate initially, calling for adjustment of concomitant therapy.
PAEDIATRIC NOTES - BETA-ADRENOCEPTOR BLOCKING DRUGS
Atenolol (tablets, syrup) and metoprolol (tablets) are not licensed for use in children but are used to treat hypertension and some children with Marfan's syndrome.
Propranolol (tablets, oral solution, injection) is used for hypertension and migraine prophylaxis. The 5mg/5mL syrup formulation of propranolol is available as a "special". ECG monitoring should always be carried out if propranolol is used intravenously. It is also used to treat SVT.
Labetalol injection is not licensed for use in children but has been used to treat hypertensive crisis.
GERIATRIC NOTES - BETA-ADRENOCEPTOR BLOCKING DRUGS
Elderly patients are particularly susceptible to the side-effects of beta-blockers which include cold extremities, bradycardia, conduction disorders, heart failure and fatigue. Reduced doses may be required in the elderly.

