BLACK BOX WARNING
- abrupt withdrawal
nebivolol
Brand: Bystolic
⚠ BBW Prototype: metoprolol-succinate
Drug Class: beta-blocker
Drug Family: antihypertensive
Subclass: highly selective beta-1 blocker + NO-mediated vasodilation
Organ Systems: cardiovascular
Mechanism of Action
Third-generation cardioselective beta-1 blocker; enhances eNOS-mediated nitric oxide production causing vasodilation; reduces peripheral vascular resistance.
beta-1 adrenergic receptorendothelial nitric oxide synthase (eNOS)
Indications
- hypertension
Contraindications
- severe bradycardia
- heart block > 1st degree
- decompensated HF
- cardiogenic shock
- severe hepatic impairment
Adverse Effects
Common
- headache
- fatigue
- dizziness
- bradycardia
Serious
- bronchospasm (rare)
- heart block
Pharmacokinetics (ADME)
| Absorption | 26-96% (extensive CYP2D6 polymorphism) |
| Distribution | moderate |
| Metabolism | extensive hepatic CYP2D6 |
| Excretion | renal 38%, fecal 44% |
| Half-life | 12-19 hours (extensive metabolizers), 19-32h (poor) |
| Onset | 1-4 hours |
| Peak | 1.5-4 hours |
| Duration | 24 hours |
| Protein Binding | 98% |
| Vd | 12 L/kg |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| CYP2D6 inhibitors | markedly increased nebivolol exposure | major |
| verapamil/diltiazem | additive AV block | major |
Nursing Considerations
- Third-generation beta-blocker with vasodilatory properties
- Highly sensitive to CYP2D6 polymorphism — poor metabolizers have significantly higher exposure
- Once-daily dosing
- Monitor for bradycardia and hypotension
Clinical Pearls
- Unique NO-mediated vasodilation differentiates from older beta-blockers
- Metabolic neutrality: does not worsen insulin resistance or lipid profile
- CYP2D6 poor metabolizers (7-10% of Caucasians) may require lower doses
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.