What it is
Bisoprolol is a long-acting (24-hour) β1-selective beta-blocker that reduces heart rate and the force of contraction. It is especially useful in hypertension with comorbidities (ischaemic heart disease, heart failure with reduced ejection fraction) and after a heart attack.
It has advantages over older beta-blockers: β1 selectivity (less bronchoconstriction), a long half-life (one dose a day) and a better metabolic profile. It has a proven mortality benefit in heart failure.
Mechanism of action
It blocks:
- Cardiac β1 adrenergic receptors, with high selectivity over β2
- It reduces heart rate and contractility
- It lowers the heart muscle's oxygen consumption
At the counter
When to recommend it
- Hypertension with ischaemic heart disease
- Heart failure with reduced ejection fraction (it reduces mortality)
- After a heart attack
- Stable angina
When not to
- Severe asthma; in COPD, only with caution and on medical advice
- Severe bradycardia (heart rate below 50)
- Advanced AV block
- Cardiogenic shock
Warnings
- Important Stopping suddenly: risk of rebound hypertension, tachycardia and angina. Gradual tapering is essential.
- Important Excessive bradycardia: a heart rate below 50 needs assessment and possibly a dose adjustment.
- Caution Tiredness and cold hands and feet: common at the start; they usually improve over time.
- Caution Erectile dysfunction: it can occur. It is a frequent reason for quietly stopping treatment: ask about it naturally.
Pharmacokinetics
- Absorption
- Rapid and almost complete oral absorption. Bioavailability of 90%. Peak at 2–3 hours.
- Distribution
- Wide distribution. Moderate penetration into the CNS. Protein binding of 26–35%.
- Metabolism
- About half is metabolised in the liver into inactive metabolites; the other half is eliminated unchanged by the kidney.
- Elimination
- Renal and hepatic elimination in roughly equal parts. Half-life of 10–12 hours, allowing one dose a day.
Bisoprolol vs amlodipine
| Aspect | Bisoprolol | Amlodipine |
|---|---|---|
| Mechanism | Cardiac β1 blockade | Calcium channel blocker |
| Heart rate | Reduces it | No effect / reflex increase |
| Benefit in heart failure | High (reduces mortality) | Low |
| Peripheral oedema | No | Common |
| Asthma | Avoid | Safe |
Bisoprolol in heart failure with reduced ejection fraction or after a heart attack. Amlodipine in uncomplicated hypertension or angina without heart failure.
Self-assessment
Three questions. When you check your answers you will see the explanation for each one.
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β1 selectivity means bisoprolol has little effect on the β2 receptors in the bronchi: less bronchoconstriction than non-selective beta-blockers.
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Stopping a beta-blocker suddenly causes a cardiac rebound. It is always tapered gradually (1–2 weeks).
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Beta-blockers in heart failure might seem a bad idea (less force), but paradoxically they reduce mortality. The benefit is proven.
Training content. It does not replace the summary of product characteristics or clinical judgement.