Bisoprolol
Emconcor · Emconcor CHF · Bisoprolol Krka · Bisoprolol Teva
The most β₁-selective of the routinely used beta-blockers, with documented mortality benefit in heart failure from CIBIS-II. Bioavailability is close to 90 % and elimination is equally shared between liver and kidney, giving a predictable dose–effect relationship without the CYP2D6-dependent variability that makes metoprolol response unpredictable. The half-life of 10–12 hours is sufficient for once-daily dosing.
Never initiate or increase the dose during decompensation — negative inotropy can precipitate pulmonary oedema. Abrupt discontinuation causes rebound tachycardia and ischaemia; taper over at least two weeks.
Dosing in adults
| Indication | Regimen | Comment |
|---|---|---|
| Heart failure (HFrEF), uptitration | 1,25 mg × 1 week 1 → 2,5 mg week 2 → 3,75 mg week 3 → 5 mg weeks 4–7 → 7,5 mg weeks 8–11 → 10 mg from week 12 | in clinical practice do not double faster than every other week |
| Heart failure, maintenance | 10 mg × 1 (target dose, maximum daily dose) | target dose, not symptom dose — keep even if symptoms have resolved |
| Hypertension | 5 mg × 1, if needed 10 mg × 1 | maximum 20 mg daily, rarely meaningful above 10 mg |
| Angina pectoris | 5–10 mg × 1 | titrate to resting heart rate 55–60 |
| Rate control in atrial fibrillation | 2,5–10 mg × 1 | responds less well at high catecholamine levels than in stable sinus rhythm |
No adjustment in mild to moderate impairment. At eGFR below 20 ml/min the maximum daily dose is 10 mg — half the dose is eliminated unchanged renally. Titrate more slowly in heart failure with concurrent renal impairment.
No adjustment in mild to moderate hepatic impairment. In severe hepatic impairment the maximum daily dose is 10 mg.
Insufficient evidence in patients under 18 years. Oral dosing for paediatric cardiology indications is managed by a specialist.
Do not freely interchange bisoprolol and metoprolol succinate — 10 mg bisoprolol corresponds to approximately 200 mg metoprolol succinate, and both target doses are the ones studied. Avoid stopping at a low dose because the patient feels well: the mortality benefit in CIBIS-II lies in the fully uptitrated dose, not in having the drug on the list.
Pharmacokinetics
- BIOAVAIL.
- approximately 90 %
- t½
- 10–12 h (17 ± 5 h in heart failure)
- PROTEIN BINDING
- approximately 30 %
- METABOLISM
- 50 % hepatic, inactive metabolites
- EXCRETION
- 50 % renal unchanged
- β₁-SELECTIVITY
- high — but not absolute at 10 mg
- ISA / MEMBRANE EFFECT
- absent
- ONSET
- 1–3 h · full effect after 2 weeks