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CHARNELDA L. GRAY, PHARM.D., BCPS, is Interim Clinical Pharmacy Manager, Kaiser Permanente of Georgia, Atlanta. UCHE A. NDEFO, PHARM.D., BCPS, is Assistant Professor, College of Pharmacy & Health Science, Texas Southern University, Houston.

Address correspondence to Dr. Gray at Kaiser Permanente of Georgia, 3495 Piedmont Road NE, Building 9, Atlanta, GA 30305 (charnelda.l.gray{at}kp.org).

Purpose. The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, safety, economic issues, dosage, and place in therapy of nebivolol are reviewed. Summary. Nebivolol is a novel, highly selective β1-receptor blocker that causes peripheral vasodilation by increasing the production and release of nitric oxide and decreasing nitric oxide degradation. The nitric oxide-mediated effects of nebivolol lead to decreases in systemic vascular resistance and large artery stiffness and possible reversal of endothelial dysfunction. Clinical studies have shown nebivolol to be at least as effective at lowering blood pressure as other antihypertensive drugs, including other β-blockers. The most frequent adverse events reported in nebivolol clinical trials were transient headache, dizziness, and tired-ness. In a large trial in patients with heart failure, nebivolol was shown to reduce the composite endpoint of mortality and hospitalizations. Nebivolol is highly lipophilic and is rapidly absorbed after oral administration. The nebivolol dose most commonly used in clinical trials for hypertension was 5 mg daily; no significant further decreases in blood pressure were shown with higher doses. The average dose in clinical trials for patients with heart failure was 5–10 mg daily. Dosage adjustments are recommended in elderly patients and patients with severe renal impairment. Conclusion. Nebivolol is a unique, highly selective β-blocker with vasodilatory properties mediated through the nitric oxide pathway; it may be useful in the treatment of uncomplicated mild-to-moderate essential hypertension and in patients with heart failure. Index terms: Costs; Dosage; Geriatrics; Hypertension; Hypotensive agents; Mechanism of action; Nebivolol; Pharmacokinetics; Toxicity

 

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