Nebivolol (Nebicard) for Hypertension
Nebivolol is an effective first-line antihypertensive agent for most patients with hypertension, with a recommended starting dose of 5 mg once daily, which can be titrated up to 40 mg daily if needed for blood pressure control. 1
Starting Dose and Titration
- The standard initial dose is 5 mg once daily, taken with or without food, as monotherapy or in combination with other agents. 1
- For patients requiring further blood pressure reduction, increase the dose at 2-week intervals up to a maximum of 40 mg daily. 1
- The 5 mg dose of nebivolol is therapeutically equivalent to metoprolol 50 mg once daily. 2
Special Populations Requiring Dose Adjustment
Severe renal impairment (creatinine clearance <30 mL/min):
- Start with 2.5 mg once daily and titrate slowly as needed. 1
- Nebivolol has not been studied in dialysis patients. 1
Moderate hepatic impairment:
- Start with 2.5 mg once daily and titrate slowly as needed. 1
- Do not use in severe hepatic impairment (not studied). 1
Elderly patients:
- No dose adjustment necessary. 1
CYP2D6 poor metabolizers:
- No dose adjustment required; clinical effects are similar to extensive metabolizers. 1
Position as First-Line Therapy
Nebivolol is recommended as one of the preferred vasodilating beta-blockers when beta-blockers are chosen for hypertension management. 3, 2 The drug has several advantages over traditional beta-blockers:
- It is a highly selective β1-blocker with vasodilating properties mediated through nitric oxide release. 4, 5
- Unlike older beta-blockers (atenolol, metoprolol), nebivolol does not adversely affect glucose metabolism or lipid profiles. 3, 4
- It reduces central pulse pressure and aortic stiffness better than atenolol or metoprolol. 3
- It does not increase the risk of new-onset diabetes when combined with diuretics, unlike traditional beta-blockers. 3
Efficacy Compared to Other Antihypertensives
Nebivolol achieves similar or superior blood pressure control compared to other first-line agents:
- Response rates (achieving target BP or ≥10 mmHg reduction in diastolic BP) range from 58-81% after 4-52 weeks of treatment. 4
- A meta-analysis showed higher response rates with nebivolol than ACE inhibitors (OR 1.92, p=0.001) and similar rates to other beta-blockers, calcium channel blockers, and ARBs. 6
- Nebivolol 5 mg once daily reduces blood pressure as effectively as atenolol, metoprolol, lisinopril, and nifedipine at standard doses. 4
- It has additive effects when combined with hydrochlorothiazide. 4
Tolerability Profile
Nebivolol demonstrates superior tolerability compared to most other antihypertensive classes:
- Adverse event rates are similar to placebo and significantly lower than losartan (OR 0.52, p=0.016), other beta-blockers (OR 0.56, p=0.007), and nifedipine (OR 0.49, p<0.001). 6
- Most common adverse events are mild and transient: headache, fatigue, paresthesias, and dizziness. 4
- Unlike atenolol or enalapril, nebivolol does not cause impotence or decreased libido. 4
- No orthostatic hypotension has been reported in multiple studies. 4, 7
Clinical Context Within Guidelines
While current major guidelines (ACC/AHA, ESC) recommend ACE inhibitors, ARBs, thiazide-like diuretics, or dihydropyridine calcium channel blockers as first-line therapy for most patients with hypertension 3, 8, beta-blockers including nebivolol are specifically recommended when there are compelling indications:
- Post-myocardial infarction 3
- Active angina 3
- Heart failure with reduced ejection fraction (nebivolol specifically proven in SENIORS trial for patients ≥70 years) 3
- Heart rate control in atrial fibrillation 3
However, nebivolol's unique vasodilating properties and superior metabolic profile position it as a reasonable first-line option even without these specific indications, particularly in patients where traditional beta-blockers would be avoided due to metabolic concerns. 3, 9
Practical Prescribing Algorithm
- Start with 5 mg once daily for most patients with hypertension (BP ≥140/90 mmHg). 1
- Assess blood pressure response after 2 weeks. 1
- If BP target not achieved (<130/80 mmHg for most adults), increase to 10 mg once daily. 1
- Continue titrating at 2-week intervals (20 mg, then 40 mg maximum) until target BP reached. 1
- Consider combination therapy with a dihydropyridine calcium channel blocker or thiazide-like diuretic if monotherapy at maximum dose is insufficient. 3, 4
Key Advantages Over Traditional Beta-Blockers
- Maintains exercise tolerance better than traditional beta-blockers. 5
- Improves endothelial function through nitric oxide-mediated vasodilation. 5, 7
- Neutral effects on glucose and lipid metabolism. 3, 4, 7
- Better tolerability and adherence profile. 5, 6
- Trough-to-peak antihypertensive effect ratio of 90%, ensuring 24-hour blood pressure control. 7