Bisoprolol !
A highly β1-selective beta blocker. Used for high blood pressure and, started low and raised slowly, for heart failure with reduced ejection fraction.
Updated 2026-11-01
The figure shows the turkey β1 receptor with cyanopindolol, another beta blocker in the same binding site where bisoprolol acts; no structure with bisoprolol bound is available.
Mechanism of action
Bisoprolol blocks β1 receptors with high selectivity. Heart rate, contractility and renin release fall, lowering blood pressure and oxygen demand. In heart failure, long-term blockade protects the heart from chronic sympathetic overdrive, which reduces deaths and hospital stays. At higher exposure it also blocks β2 receptors.
- Bisoprolol selectively blocks β1 receptors
- Heart rate, contractility and renin release fall
- Long-term, the heart is shielded from sympathetic overdrive
Pharmacokinetics
- Absorption
- Well absorbed by mouth, with high bioavailability
- Elimination
- Half by the kidneys unchanged and half as liver metabolites
- Half-life
- About 9 to 12 hours, longer in kidney failure and in the elderly
Indications
- High blood pressure Arterial hypertension →
- Heart failure with reduced ejection fraction (WHO list) Heart failure →
- Angina and rate control in atrial fibrillation (WHO list) Atrial fibrillation →
Adverse effects
Common
- Fatigue
- Bradycardia
- Dizziness
- Cold extremities
Contraindications
- Cardiogenic shock
- Overt (decompensated) heart failure
- Second- or third-degree AV block
- Marked sinus bradycardia
Key interactions
- Verapamil, diltiazem or disopyramide
- Added depression of the AV node and of contractility
- Clonidine
- Rebound hypertension if clonidine is stopped first
- Rifampicin
- Faster clearance and shorter half-life of bisoprolol
What is monitored
- Heart rate and blood pressure
- Weight, oedema and breathlessness in heart failure
- ECG if bradycardia appears
Administration and safety
- Given by mouth once a day; in heart failure it is started low and raised step by step over weeks
- Tapered, never stopped suddenly
- Check the name: several «-olol» drugs look alike
Nursing care
- Check pulse and blood pressure before each dose
- In heart failure, weigh the patient daily during titration and report rapid weight gain or more breathlessness
- Explain that tiredness in the first weeks is common and usually improves
Pregnancy and breastfeeding
Human data are limited; beta blockers can slow fetal growth and cause bradycardia and hypoglycaemia in the newborn, so it is used only when needed.
Test yourself
Think of the answer, then tap the question to see it.
Why is bisoprolol started low and raised slowly in heart failure?
Its first effect is to reduce contractility, which can worsen congestion; the long-term benefit appears as the heart adapts.
Which beta blockers have shown a survival benefit in heart failure with reduced ejection fraction?
Bisoprolol, carvedilol and extended-release metoprolol succinate.
Is bisoprolol started in decompensated heart failure?
No. Overt, decompensated failure is a contraindication; it is started once the patient is stable.
Related drugs
Related conditions
← Back to the class: Beta blockers
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - BISOPROLOL FUMARATE tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); eEML - Electronic Essential Medicines List (World Health Organization, 2025).
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Representative model, for educational purposes only.