BLACK BOX WARNING
- abrupt withdrawal
bisoprolol
Brand: Zebeta, Concor
⚠ BBW Prototype: metoprolol-succinate
Drug Class: beta-blocker
Drug Family: antihypertensive
Subclass: highly selective beta-1 blocker
Organ Systems: cardiovascular
Mechanism of Action
Most cardioselective beta-1 blocker available; reduces HR and myocardial oxygen demand.
beta-1 adrenergic receptor
Indications
- hypertension
- heart failure (HFrEF, CIBIS-II)
- angina
Contraindications
- cardiogenic shock
- decompensated HF
- severe bradycardia
- high-degree AV block
Adverse Effects
Common
- bradycardia
- fatigue
- dizziness
Serious
- bronchospasm (rare at low doses)
- heart block
Pharmacokinetics (ADME)
| Absorption | 90% oral bioavailability |
| Distribution | moderate lipophilicity; partial CNS penetration |
| Metabolism | 50% hepatic CYP3A4; 50% renal |
| Excretion | 50% renal, 50% fecal |
| Half-life | 10-12 hours |
| Onset | 1-2 hours |
| Peak | 2-4 hours |
| Duration | 24 hours |
| Protein Binding | 30% |
| Vd | 3.5 L/kg |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| CYP3A4 inhibitors | increased bisoprolol levels | moderate |
| verapamil/diltiazem | additive AV block | major |
Nursing Considerations
- Highest beta-1 selectivity of available agents
- CIBIS-II: reduced mortality in HFrEF
- Once-daily dosing; 90% bioavailability (minimal first-pass)
- Safe in mild-to-moderate COPD due to high selectivity
Clinical Pearls
- CIBIS-II: 34% relative risk reduction in all-cause mortality in HFrEF
- Highest beta-1 selectivity makes it safest option in COPD
- 90% bioavailability — minimal variability unlike metoprolol
Safety Profile
Pregnancy use-with-caution
Lactation avoid
Renal Adjustment Required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.