Overview
Nebivolol is a beta-1 selective adrenergic receptor blocker with vasodilatory properties used primarily for hypertension and heart failure. It reduces blood pressure through beta-blockade and nitric oxide-mediated vasodilation. The drug requires careful monitoring in patients with certain cardiovascular conditions.
Mechanism of Action
Nebivolol is a third-generation beta-blocker that selectively antagonizes beta-1 adrenergic receptors, reducing heart rate and myocardial contractility. It also induces vasodilation through endothelial nitric oxide release via beta-3 agonism, providing additional antihypertensive effects.
Indications
- Treatment of hypertension
- Management of chronic heart failure (NYHA Class II or III) to reduce cardiovascular mortality and hospitalizations
Common Doses
- 1.25 mg
- 2.5 mg
- 5 mg
- 10 mg
Dosage
For hypertension: Initial dose 5 mg once daily, may be increased to 10 mg once daily after 2 weeks. For heart failure: Start at 1.25 mg once daily, titrate gradually to target dose of 10 mg once daily. Dose adjustments required in renal impairment and elderly patients.
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)
- Hypersensitivity to any component
Side Effects
- Bradycardia
- Headache
- Dizziness
- Fatigue
- Nausea
- Diarrhea
- Peripheral edema
- Bronchospasm
- Hypotension
- Heart block
- Depression
- Impotence
Interactions
- CYP2D6 inhibitors (fluoxetine, paroxetine) increase nebivolol levels
- Other antihypertensives potentiate blood pressure lowering
- Calcium channel blockers (especially verapamil, diltiazem) increase risk of bradycardia
- Digoxin increases risk of bradycardia
- Insulin and oral hypoglycemics may mask hypoglycemia symptoms
Counseling Points
- Take at same time daily, with or without food
- Do not stop abruptly - taper under medical supervision
- Monitor blood pressure regularly
- Report dizziness, excessive fatigue, or shortness of breath
- May cause initial dizziness - use caution when rising from sitting/lying
- Inform healthcare providers about all medications including OTC drugs