Recommended Dose and Frequency of Nebivolol for Hypertension
The recommended starting dose of nebivolol for hypertension is 5 mg once daily, with or without food, as monotherapy or in combination with other agents. 1
Dosing Guidelines
- Initial dose: 5 mg once daily 1, 2
- Titration: Dose can be increased at 2-week intervals if needed 1
- Maximum dose: Up to 40 mg daily, though doses beyond 10 mg provide limited additional benefit 1, 3
- Administration: Can be taken with or without food 1
Special Population Considerations
Renal Impairment
- Severe renal impairment (CrCl <30 mL/min): Start with 2.5 mg once daily and titrate slowly if needed 1
- Not studied in dialysis patients - use with caution 1
Hepatic Impairment
- Moderate hepatic impairment: Start with 2.5 mg once daily and titrate slowly if needed 1
- Not recommended in severe hepatic impairment 1
Elderly Patients
- No dose adjustment necessary for elderly patients 1
CYP2D6 Poor Metabolizers
- No dose adjustments necessary as clinical effect and safety profile are similar to extensive metabolizers 1
Clinical Efficacy
- Nebivolol 5 mg once daily reduces resting diastolic blood pressure as effectively as standard therapeutic dosages of atenolol, metoprolol, lisinopril, and nifedipine 2
- Response rates range from 58% to 81% after 4 to 52 weeks of treatment 2
- Nebivolol has an additive effect when combined with hydrochlorothiazide 2, 4
- The 5 mg dose is therapeutically equivalent to metoprolol 50 mg once daily 5
Mechanism and Benefits
- Nebivolol is a highly selective β1-receptor blocker with nitric oxide-mediated vasodilatory effects 2, 4
- The vasodilatory properties may contribute to its favorable hemodynamic profile compared to traditional beta-blockers 4, 6
- Produces less impact on augmentation index (a measure of arterial stiffness) than atenolol 6
- Does not significantly influence glucose or plasma lipid metabolism 2
Adverse Effects
- Most common adverse events are transient headache, dizziness, fatigue, and paresthesias 2, 3
- Generally well-tolerated with infrequent, mild to moderate side effects 2
- No significant reports of orthostatic hypotension 2
- Lower incidence of sexual dysfunction compared to some other beta-blockers 2
Clinical Pearls
- For patients with hypertension and heart failure, nebivolol can be titrated up to 10 mg daily 5
- When switching from metoprolol 50 mg, start with nebivolol 5 mg once daily 5
- Nebivolol is administered as a racemic mixture of equal proportions of d- and l-enantiomers 2, 4
- Metabolized primarily through CYP2D6 in the liver 4
Place in Therapy
- Recommended as a useful first-line treatment option for mild to moderate uncomplicated essential hypertension 2, 4
- May be particularly beneficial in patients who experience side effects with traditional beta-blockers 2
- According to the 2024 ESC guidelines, nebivolol is one of the preferred vasodilating beta-blockers when beta-blockers are chosen for hypertension management 7