bisoprolol
Beta-adrenergic blockers· Brands: Cardicor, Zebeta, Concor, EmconcorPO
Mechanism of action
Bisoprolol is a selective beta-1 adrenergic receptor antagonist. It blocks the actions of endogenous catecholamines at beta-1 receptors in the heart, reducing heart rate, myocardial contractility, and cardiac output. This lowers myocardial oxygen demand and blood pressure. It also decreases renin release from the kidneys, contributing to its antihypertensive effect. At therapeutic doses it has minimal effect on beta-2 receptors in the bronchi and vasculature.
Pharmacokinetics
About 50% of the dose is metabolised hepatically, via CYP3A4 to inactive metabolites. Elimination is biphasic: the beta half-life is about 10 to 12 hours. Approximately 50% of the dose is excreted unchanged in urine, with the remainder as metabolites.
Indications & dosing
Heart failure with reduced ejection fraction
- adult · PO: 1.25–10 mg OD · Start 1.25 mg and up-titrate slowly
Rate control in atrial fibrillation
- adult · PO: 1.25–10 mg OD
Contraindications & precautions
- Severe bradycardia / second- or third-degree heart block
- Acute decompensated heart failure
- Severe asthma · Cardioselectivity is dose-dependent
- Do not stop abruptly; withdraw gradually over 1-2 weeks to avoid rebound hypertension or ischaemia.
- Monitor heart rate and blood pressure regularly, especially in patients with heart failure.
- Use caution in diabetes; beta-blockers may mask symptoms of hypoglycaemia.
- Use caution in thyrotoxicosis; beta-blockers may mask signs of hyperthyroidism.
- Use caution in peripheral vascular disease; may worsen symptoms of claudication.
- Use caution in COPD; consider cardioselective beta-blocker but monitor for respiratory symptoms.
Adverse effects
- Bradycardia
- Fatigue
- Cold extremities
Interactions
- diltiazemmajorIf possible, avoid the combination, especially in patients with heart failure, bradycardia, AV conduction disease, or hypotension. If co-prescription is necessary, start with low doses, monitor heart rate, blood pressure, and ECG regularly, and adjust doses cautiously. Consider alternatives such as a dihydropyridine calcium channel blocker or an alpha/beta blocker if appropriate. Patients should be advised to report symptoms of bradycardia, dizziness, or syncope.
- verapamilmajorAvoid co-prescription where possible. If combination is necessary, use cautiously with lower doses of both agents. Monitor heart rate, blood pressure and ECG at baseline and after any dose change. Consider switching to a dihydropyridine calcium channel blocker if rate control is not the primary goal. Intravenous verapamil should be avoided in patients taking bisoprolol.
- salbutamolmoderateBeta-blockers blunt bronchodilation; prefer cardioselective agents at low dose in reactive airways.
- amiodaronemajorMonitor heart rate and blood pressure closely, especially after starting amiodarone. Consider reducing the bisoprolol dose or avoiding the combination in patients with bradycardia, heart block, or heart failure. Adjust doses based on clinical response and ECG findings.
- digoxinmoderateCo-prescription is often intentional in heart failure and atrial fibrillation, but requires caution. Monitor heart rate and blood pressure before and after initiating therapy or dose changes. Consider ECG monitoring for patients with underlying conduction disease or at risk of hypokalaemia. Adjust doses as needed; avoid in patients with marked bradycardia or high-degree AV block without a pacemaker. Monitor digoxin levels if renal function changes or signs of toxicity appear.
Renal & hepatic adjustment
- eGFR 0–20: Maximum dose 10 mg daily
- Hepatic impairment (mild): No dose adjustment required
- Hepatic impairment (moderate): No dose adjustment required
- Hepatic impairment (severe): Reduce initial dose, monitor closely
Monitoring, pregnancy & toxicity
- Heart rate · Before each dose increase and at regular intervals during treatment
- Blood pressure · Before each dose increase and at regular intervals during treatment
- Signs of worsening heart failure (e.g., weight gain, oedema, dyspnoea) · During dose titration and regularly in patients with heart failure
- Pregnancy: Bisoprolol is not recommended in pregnancy unless considered essential. Beta-blockers may cause fetal growth retardation, bradycardia, and neonatal hypoglycaemia. Use only if the benefit to the mother outweighs the risk, and consider alternative agents such as labetalol where appropriate.
- Toxicity: Bradycardia and hypotension · Withdraw the drug. Atropine IV may be given for bradycardia. Glucagon is effective in severe beta-blocker toxicity; if unavailable, consider isoprenaline or adrenaline.
- Toxicity: Bronchospasm · Administer a beta2-agonist (e.g., salbutamol) by nebulisation. In severe cases, consider IV aminophylline or glucagon.
- Toxicity: Heart failure or cardiogenic shock · Intensive supportive care. Consider inotropic support (e.g., dobutamine or noradrenaline). Glucagon may be used as a cardiac stimulant.
Antidotes & reversal
- Glucagon · 1-5 mg IV then infusion; high-dose insulin-euglycaemia for refractory cardiogenic shock.
Clinical notes
Bisoprolol is indicated for hypertension, stable angina, and chronic heart failure. In heart failure, it is initiated at a low dose and titrated gradually. Common adverse effects include bradycardia, fatigue, dizziness, and gastrointestinal disturbances. It should be avoided in patients with second or third degree atrioventricular block, severe bradycardia, or acute decompensated heart failure. Caution is needed in asthma, chronic obstructive pulmonary disease, and diabetes as it may mask hypoglycaemia. Abrupt withdrawal can precipitate angina, hypertension, or arrhythmias, so taper over at least a week.
Log in to read the full bisoprolol monograph
A free account unlocks the complete drug reference, the interaction checker, prescription practice and every other learning tool.
BNF; local formulary