Bisoprolol is a cardio-selective beta-1 adrenergic receptor blocker used for hypertension, angina, heart failure with reduced ejection fraction (HFrEF), and rate control of supraventricular tachyarrhythmias. By antagonising beta-1 receptors in the SA/AV nodes and ventricular myocardium, it lowers heart rate, decreases contractility, and slows AV conduction, reducing myocardial oxygen demand and stabilising rhythm. Selectivity for beta-1 over beta-2 receptors (lungs, peripheral vasculature) is high at therapeutic doses but diminishes with higher exposure.
Oral bioavailability is ≈80–90%, peak concentrations at 2–4 hours, and a terminal half-life of 10–12 hours support once-daily dosing. Elimination is ~50% renal (unchanged) and ~50% hepatic (inactive metabolites), so moderate impairment of one pathway is usually manageable; severe renal or hepatic dysfunction warrants conservative dosing and closer monitoring. Bisoprolol shows predictable kinetics (less CYP polymorphism impact than metoprolol), assisting dose titration.
Outcome data are strong. The CIBIS-II trial demonstrated significant reductions in all-cause mortality and hospitalisation in HFrEF, establishing bisoprolol—along with metoprolol succinate and carvedilol—as a beta-blocker with survival benefit. In hypertension, current guidelines prioritise ACEi/ARB, CCB, and thiazide-like diuretics for uncomplicated cases; however, bisoprolol remains first-line when there is a compelling indication (post-MI, angina, arrhythmia, HFrEF) or tachycardic hypertension. In rate control (e.g., AF), it is widely used alone or with other AV-nodal agents in selected patients.
Practical points: start low and titrate slowly, especially in HFrEF; avoid abrupt withdrawal (rebound sympathetic activation may trigger angina, severe hypertension, or arrhythmia); teach home pulse/BP checks and red flags (syncope, wheeze, rapid weight gain/oedema). Symptom relief may be early, but event reduction depends on sustained, guideline-directed therapy with lifestyle measures.
Common licensed and guideline-supported uses:
Administration: Once daily, same time each morning, with or without food. If therapy is interrupted, re-titration may be required.
Adverse effects are usually dose-related and often settle with slower titration. Counselling improves adherence and reduces premature discontinuation.
Management: If fatigue/bradycardia limits progress, hold dose longer before up-titration, review AV-nodal co-meds (verapamil, diltiazem, digoxin, amiodarone), and optimise diuretics in HF. Do not stop abruptly—taper over ≥1–2 weeks.
Sick-day rules: With vomiting/diarrhoea or poor intake causing hypotension, seek advice about temporarily holding/reducing dose; restart when recovered.
Key drug and OTC/herbal interactions—mostly pharmacodynamic (HR/AV node/BP) with a few pharmacokinetic considerations:
Keep a current medicines list (including decongestants and herbals) and share it at every prescribing encounter to prevent conflicts.
Overdose—what to expect: Severe bradycardia, hypotension, high-grade AV block, cardiogenic shock, acute HF, bronchospasm (especially in reactive airway disease), hypoglycaemia (notably in children), and CNS effects (confusion, seizures). Onset can be rapid.
Immediate steps: Call emergency services. Secure airway/breathing/circulation; start continuous ECG and BP monitoring; check glucose and correct if low. If within ~1 hour of ingestion and airway protected, consider activated charcoal.
Targeted therapy: For bradycardia/hypotension give IV atropine. If inadequate, use IV glucagon (bolus → infusion) to raise cAMP independent of beta-receptors. Persistent shock may require high-dose insulin euglycaemia therapy (insulin + dextrose with close K⁺/glucose monitoring) and vasopressors (e.g., norepinephrine). Temporary transvenous pacing can be life-saving in refractory high-grade block. Treat bronchospasm with inhaled beta-agonists and nebulised anticholinergics; consider IV aminophylline if severe and unresponsive.
Disposition: Significant symptoms/ECG changes warrant admission to a monitored unit. Dialysis is not useful; bisoprolol is not effectively removed extracorporeally.
Everyday dosing errors: If a dose is missed, take it when remembered unless close to the next scheduled dose—never double up. If an extra dose was taken, skip the next one and monitor for dizziness, fatigue, slow pulse, or breathlessness; seek advice if symptoms occur.
Verify tablet strength before each dose—especially if tablet appearance changes after a manufacturer switch. When in doubt, confirm with a pharmacist to prevent dosing errors.
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