Generic
Nebivolol
37 brands available in the market
At a glance
Nebivolol is a beta-blocker used for hypertension and heart failure. It lowers blood pressure by reducing heart rate and dilating blood vessels, helping prevent future heart attack and stroke.
Description
Nebivolol exhibits high selectivity for beta1-adrenergic receptors and has vasodilating activity due to a direct action on the endothelium, involving nitric oxide release. It lacks intrinsic sympathomimetic and membrane-stabilising activity.
Indications
- Essential hypertension
- Stable mild and moderate chronic heart failure (in elderly patients)
Therapeutic class
Beta-adrenoceptor Blocking Drugs
Pharmacological class
Selective β1-Blocker
Pharmacology
Nebivolol blocks β1-adrenergic receptors to reduce heart rate and myocardial contractility. It causes vasodilation through nitric oxide release and reduces peripheral vascular resistance.
Mechanism of action
Lowers blood pressure by reducing heart rate and dilating blood vessels.
Dosage
Adult Dose (Oral):
- Hypertension: 5 mg once daily (initial); may increase to 40 mg/day at 2-week intervals
- Heart failure: 1.25 mg once daily (initial); double every 1-2 weeks if tolerated; max 10 mg/day
- Elderly (>65 years): 2.5 mg/day (initial), increase to 5 mg/day if needed
- Hepatic impairment: 2.5 mg/day (initial); increase cautiously
Administration
- Swallow tablet whole; do not chew, crush or break
- May be taken with or without food
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Headache
- Fatigue
- Dizziness
- Nausea
- Constipation
- Diarrhea
- Cold extremities
- Bradycardia
Precautions & warnings
- Do not abruptly discontinue (risk of angina and heart attack)
- Monitor blood glucose regularly in diabetic patients
- Caution in slow heart rate or low blood pressure
- Caution while driving (may cause dizziness)
- Avoid alcohol
Contraindications
- Hepatic impairment
- Sick sinus syndrome
- 2nd and 3rd degree heart block (without pacemaker)
- History of asthma
- Metabolic acidosis
- Severe peripheral arterial disease
- Severe bradycardia
- Cardiogenic shock or decompensated heart failure
- Untreated phaeochromocytoma
- Pregnancy and lactation
Drug interactions
- Increased plasma concentrations with CYP2D6 inhibitors (paroxetine, fluoxetine, propafenone, thioridazine, quinidine)
- Conduction disturbance with antiarrhythmics or non-dihydropyridine Ca channel blockers
- Additive negative effects on AV conduction and heart rate with other beta-blockers or digoxin
- Additive hypotension or bradycardia with catecholamine-depleting agents
Food interactions
Caution with alcohol; consult doctor.
Use in pregnancy
Use in Pregnancy: Nebivolol may be unsafe during pregnancy; animal studies show evidence of fetal harm.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Nebivolol is probably unsafe during breastfeeding; may pass into breast milk and harm the baby.
Pediatric use
Safety and efficacy not established in children.
Geriatric use
Elderly starting dose: 2.5 mg/day.
Renal / hepatic impairment
Renal Impairment: CrCl <30 mL/min: 2.5 mg/day (initial); increase to 5 mg/day if needed; caution in severe kidney disease.
Hepatic Impairment: Contraindicated in severe liver disease; caution in moderate hepatic impairment.
Overdose effects
Overdose: Bradycardia, hypotension, heart block, heart failure, bronchospasm; treat with atropine, IV fluids, vasopressors, glucagon, isoproterenol, digitalis, bronchodilators.
Storage conditions
Store below 30°C; protect from light & moisture; keep out of reach of children.
Chemical structure
Nebivolol