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

  1. Third-generation beta-blocker with vasodilatory properties
  2. Highly sensitive to CYP2D6 polymorphism — poor metabolizers have significantly higher exposure
  3. Once-daily dosing
  4. 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.