13 oct 2009-- Nebivolol, a third generation β-blocker that has recently become available in the United States, offers a treatment alternative for hypertension, coronary artery disease and heart failure that goes beyond simple adrenergic blocking with direct vasodilation and stimulatory effects to improve arterial endothelial function, according to a paper in the Oct. 13 Journal of the American College of Cardiology.
Thomas Münzel, M.D., of II Medizinische Klinik für Kardiologie/Angiologie in Mainz, Germany, and a colleague reviewed the medication's properties, focusing on the mechanisms by which nebivolol may help improve endothelial function, reduce risk of platelet aggregation and thrombus formation, and reduce inflammation. Unlike other β-blockers, nebivolol has been shown to stimulate activity of the endothelial nitric oxide synthase to increase beneficial nitric oxide levels, while its antioxidative properties reduce oxidative stress, the researchers note. Nebivolol also has been shown to inhibit platelet aggregation and down-regulate multiple genes involved in inflammatory processes, oxidative stress, and smooth muscle cell proliferation, offering a possible benefit in the treatment of atherosclerosis. Also, because nebivolol has a greater selectivity for β1-receptors, it offers improved tolerability for patients with asthma or chronic obstructive pulmonary disease. Nebivolol contraindications include severe bradycardia, cardiogenic shock, atroventricular nodal block, decompensated heart failure, and severe hepatic disease. "Although a decade of clinical experience with this drug in Europe provides support to its blood pressure-lowering and anti-ischemic effects, further clinical trial data are necessary. Particularly, comparative trials on the efficacy of nebivolol versus other β-blockers and/or other antihypertensive drugs are awaited," Münzel and colleagues conclude. The lead author has received honoraria and research grants from Berlin Chemie and Forrest Hill.
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