-2%
Nebicard is prescribed for:
- Essential hypertension
- Chronic heart failure (CHF) – for the treatment of stable, mild to moderate chronic heart failure in elderly patients, used alongside standard heart failure therapies
Nebivolol is a beta-adrenergic receptor blocker with high selectivity for β₁-adrenergic receptors. It does not possess intrinsic sympathomimetic or membrane-stabilizing activity at therapeutic doses. Its beta-blocking effects are supported by active metabolites, including glucuronide conjugates.
At clinically relevant doses, nebivolol reduces cardiovascular workload without significant non-selective beta-blockade.
Pharmacokinetics
Absorption & Distribution
- Rapidly absorbed following oral administration
- Peak plasma levels occur within 1.5–4 hours
- Food does not affect absorption; can be taken with or without meals
- Approximately 98% protein-bound, mainly to albumin
Metabolism
- Extensively metabolized via glucuronidation and CYP2D6-mediated hydroxylation
- Active isomer half-life:
- ~12 hours in extensive metabolizers
- ~19 hours in poor metabolizers
Excretion
- Eliminated through urine and feces
- Metabolites significantly contribute to beta-blocking activity
