Drug reference

nebivolol

Beta-1 selective adrenergic receptor antagonist (cardioselective) with nitric oxide-mediated vasodilation · Antihypertensive

START

HTN: 5 mg OD. HFrEF: 1.25 mg OD (very low start); check baseline HR, BP, eGFR, LFTs, asthma/COPD history, signs of decompensated HF; do NOT start if acute decompensated HF

TYPICAL MAX

10 mg/day (HFrEF target); 20 mg/day HTN

STOP IF

HR <50 bpm, symptomatic hypotension (SBP <90), acute decompensated HF, severe bronchospasm, 2nd/3rd degree heart block

WATCH

HR and BP at each visit (especially during titration), weight (HF fluid status), signs of worsening HF, glucose (masking of hypoglycemia), peripheral perfusion

CDSCO approvedSchedule HATC C07AB12

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 41min · absorption onset
PEAK: 2.8h · 1.5-4 hours
t½: 15.5h · 12-19 hours (parent)
DURATION: 1d · 24-hour coverage with OD dosing

EXCRETION

Fecal (44%); renal (38%, metabolites)

route + CYP

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Use only if clearly needed; beta-blockers may cause fetal bradycardia, hypoglycemia, and growth restriction; third trimester risk of neonatal bradycardia and hypotension

FDA category + note

Top interactionssee all 12 →

AdrenalineSevereTextbookKDT 7e · p133
AmilorideSevereTextbookKDT 7e
MethacholineSevereTextbookG&G 14e · p212
SofosbuvirSevereTextbookHarrison 22e · unknown

Available in India

140 branded formulations and 23 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Mechanism

Highly selective beta-1 adrenergic receptor antagonist (much greater affinity for beta-1 vs beta-2 receptors, especially at doses </=10 mg). Unique among beta-blockers for its additional nitric oxide (NO)-mediated vasodilatory effect via stimulation of endothelial NO synthase (eNOS), leading to arterial and venous dilation. The d-nebivolol isomer provides beta-blockade; the l-nebivolol isomer stimulates eNOS.

Indications

HypertensionChronic heart failure with reduced ejection fraction (HFrEF) - NYHA class II-IVAngina (off-label)Left ventricular dysfunction post-MI (off-label)

Dosing

Adult: Hypertension: 5 mg OD; may increase to 10 mg OD after 2 weeks if needed. HFrEF: start 1.25 mg OD, titrate every 1-2 weeks to 2.5 mg, 5 mg, then 10 mg OD (target)
Pediatric: >18 years only; no established pediatric dosing
Renal adjustment: eGFR <30: start 2.5 mg OD; max 5 mg OD (hypertension)
Hepatic adjustment: Mild: no adjustment; Moderate-severe: contraindicated (extensive hepatic metabolism)
Geriatric: Start 2.5 mg OD; increased sensitivity to bradycardia and hypotension
Max dose: 10 mg/day (HFrEF target); 20 mg/day (hypertension, not commonly used)

Pharmacokinetics

Onset

Hours to days (BP reduction); Weeks to months (HF mortality benefit)

Peak effect

1.5-4 hours (Tmax); BP effect builds over 1-2 weeks

Duration

24 hours

Half-life

12-19 hours (parent); active hydroxyl metabolites: 24 hours

Bioavailability

12-96% (high first-pass metabolism; varies with genotype - CYP2D6 poor metabolizers have higher levels)

Protein binding

98%

Metabolism

Hepatic CYP2D6 (major pathway - extensive metabolism to active hydroxyl metabolites); also CYP2C19

Excretion

Fecal (44%); renal (38%, primarily as metabolites); urine (16%)

Contraindications

Severe bradycardia (<60 bpm) or heart block (>1st degree without pacemaker)
Cardiogenic shock
Sick sinus syndrome
Severe peripheral arterial disease
Severe asthma or COPD (relative - cardioselectivity reduces but does not eliminate risk)
Untreated pheochromocytoma
Metabolic acidosis
Hypersensitivity to nebivolol

Side effects

Common

FatigueDizzinessHeadacheBradycardiaNauseaDiarrheaInsomniaDyspneaPeripheral edema

Serious

Severe bradycardia / heart block
Bronchospasm (less likely than non-selective beta-blockers, but possible)
Worsening heart failure (during initiation/titration)
Severe hypotension
Masking of hypoglycemia symptoms
Peripheral ischemia
Depression
Impotence

Pregnancy & lactation

Pregnancy

Use only if clearly needed; beta-blockers may cause fetal bradycardia, hypoglycemia, and growth restriction; third trimester risk of neonatal bradycardia and hypotension

Lactation

Excretion in breast milk unknown; likely compatible but monitor infant for bradycardia and hypoglycemia

Drug interactions

Adrenaline

Severe

Textbook

Marked rise in BP.

Adrenaline should not be given to patients receiving β blockers.

Source: KDT 7e · p133

Amiloride

Severe

Textbook

Hyperkalaemia more likely.

Source: KDT 7e

Methacholine

Severe

Textbook

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: G&G 14e · p212

Sofosbuvir

Severe

Textbook

Severe bradycardia.

Extreme caution advised if amiodarone is co-administered with sofosbuvir and a beta blocker.

Source: Harrison 22e · unknown

Aminophylline

Severe

Database

Drug interaction classified as: antagonism

Source: DDInter