Nebivolol
BYSTOLIC
What it isBeta-1 antagonist with beta-3 agonism and nitric-oxide vasodilation; hypertension.
Why this oneIt uniquely couples beta-1 blockade to beta-3-mediated vasodilation, separating it from conventional beta blockers.
What limits itBradycardia still limits use; beta-1 selectivity fades as exposure rises, and CYP2D6 inhibition can markedly raise levels.
FDA-approved for
- hypertension (2007)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Hypertension | Adults | 5 mg QD | individualized | 40 mg QD |
Titration Increase at 2-week intervals
Renal Severe (CLcr <30 mL/min): start 2.5 mg QD, titrate slowly; not studied in dialysis
Hepatic Moderate impairment: start 2.5 mg QD, titrate slowly; contraindicated/not recommended in severe (Child-Pugh >B)
Instructions
- Take with or without food
- Do not discontinue abruptly — taper over 1 to 2 weeks (esp. in CAD)
Contraindications
- Severe bradycardia
- Heart block greater than first degree
- Cardiogenic shock
- Decompensated cardiac failure
- Sick sinus syndrome (unless permanent pacemaker in place)
- Severe hepatic impairment (Child-Pugh >B)
Cautions
- Do not abruptly discontinue in CAD (angina exacerbation, MI, ventricular arrhythmia)
- May mask hypoglycemia symptoms and alter glucose
- Avoid in bronchospastic disease
- Anesthesia/major surgery — monitor
- May mask hyperthyroidism; abrupt withdrawal may precipitate thyroid storm
- Peripheral vascular disease
- Caution with non-dihydropyridine CCBs (verapamil/diltiazem)
- Enhanced anaphylaxis reactivity
- Pheochromocytoma — start alpha-blocker first
Adverse reactions
- Headache
- Fatigue
- Dizziness
- Diarrhea
- Nausea
Pregnancy Data insufficient; third-trimester beta-blocker risk of neonatal hypotension, bradycardia, hypoglycemia, respiratory depression
Lactation Not recommended during nursing (beta-blocker risk, esp. bradycardia)
NO BOXED WARNINGS
Principal riskBradycardia; the most beta-1 selective
Cost, est. cash$5–$150/month
Generic entry2015
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityBradycardia, hypotension and bronchospasm; overdose may cause conduction block or cardiogenic shock.
Mechanism of action: Nebivolol ballicule
Open Nebivolol in the interactive console ↗
Memory aids: mascots and interaction avatars
LOL hat → beta blocker
