Highly selective β1-blocker with endothelial nitric oxide release
ATC code: C07AB12 (Nebivolol)
The d-enantiomer is a highly selective β1-antagonist (β1/β2 selectivity ~290:1 in Caucasians). The l-enantiomer stimulates endothelial NO synthase, producing peripheral vasodilation and reduced vascular resistance. Less likely than classical β-blockers to cause bronchospasm, cold extremities, and sexual dysfunction. CYP2D6-metabolized – exposure rises 5–10-fold in poor metabolizers.
First line
In heart failure in patients over 70, nebivolol cuts the composite of death and cardiovascular hospitalization by 14% (SENIORS). Start at 1.25 mg with weekly–biweekly titration up to the target 10 mg under BP and HR monitoring.
Approved for HF in patients over 70 (SENIORS trial).
Sources
First line
In hypertension, β-blockers are no longer universal first-line per 2024 – they are preferred when comorbid indications exist (CAD, HF, tachyarrhythmia). Among β-blockers, nebivolol has the most favorable metabolic profile, with less weight gain and glucose intolerance. Standard dose 5 mg once daily; start at 2.5 mg in older adults.
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Nebivolol is a selective β1-adrenergic blocker with additional NO-mediated vasodilating activity. It is prescribed for hypertension and heart failure in older adults ( 2023, SEH-LELHA). In anti-aging regimens, nebivolol is promoted as a modern selective β1-blocker with NO effects for healthy normotensives. In people with normal blood pressure, no clinical studies of prophylactic use exist. The drug causes bradycardia, hypotension, fatigue, and headache. If nebivolol was prescribed to a healthy person, consider seeking a second opinion.
Opens the checker prefilled with this drug. Pick the second one from your regimen.
Direct links to regulator labels. Open in a new tab.
β-blockers in T3 are linked to fetal growth restriction and neonatal hypoglycemia and bradycardia. For pregnancy hypertension, labetalol or methyldopa with more data are preferred.
Limited data. When a β-blocker is needed during lactation, metoprolol with better lactation data is preferred.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Nebivolol is evaluated for the following indications with varying evidence strength: Hypertension (evidence tier A), Heart failure (evidence tier A), Anti-aging and longevity (evidence tier F). See the full indication matrix with dosing and citations above on this page.
Common side effects of Nebivolol (≥ 1 in 100): Headache, Fatigue, Bradycardia, Dizziness, GI complaints. See the Safety section for uncommon and serious reactions.
FDA category C. β-blockers in T3 are linked to fetal growth restriction and neonatal hypoglycemia and bradycardia. For pregnancy hypertension, labetalol or methyldopa with more data are preferred.
Limited data. When a β-blocker is needed during lactation, metoprolol with better lactation data is preferred.
Nebivolol is contraindicated in: Acute heart failure, cardiogenic shock; Second- or third-degree AV block without pacemaker; Sick sinus syndrome; Severe bradycardia (HR under 50/min); Severe asthma (for doses over 5 mg). Full list in the Safety section.