Veverka Angie, Salinas Jennifer L
Wingate University School of Pharmacy, 316 North Main Street, Wingate, NC 28174-0157, USA.
Vasc Health Risk Manag. 2007;3(5):647-54.
Nebivolol is a highly selective beta1-adrenergic blocker that also enhances nitric oxide bioavailability via the L-arginine-nitric oxide pathway, leading to vasodilation and decreased peripheral vascular resistance. It is marketed in Europe for the treatment of hypertension and heart failure and is currently being reviewed for use in the US by the Food and Drug Administration. Nebivolol appears to be well tolerated with an adverse event profile that is at least similar, if not better, than that of other beta-adrenergic blockers. Studies suggest that long-term therapy with nebivolol improves left ventricular function, exercise capacity, and clinical endpoints of death and cardiovascular hospital admissions in patients with stable heart failure. To date, it is one of the only beta-adrenergic blockers that have been exclusively studied in elderly patients. Additionally, the unique mechanism of action of nebivolol makes it a promising agent for treatment of chronic heart failure in high-risk patient populations, such as African Americans. This article will review the pharmacologic and pharmacokinetic properties of nebivolol as well as clinical studies assessing its efficacy for the treatment of heart failure.
奈必洛尔是一种高度选择性的β1肾上腺素能阻滞剂,它还通过L-精氨酸-一氧化氮途径提高一氧化氮的生物利用度,从而导致血管舒张并降低外周血管阻力。它在欧洲上市用于治疗高血压和心力衰竭,目前美国食品药品监督管理局正在对其在美国的使用进行审查。奈必洛尔似乎耐受性良好,其不良事件谱至少与其他β肾上腺素能阻滞剂相似,甚至可能更好。研究表明,奈必洛尔长期治疗可改善稳定型心力衰竭患者的左心室功能、运动能力以及死亡和心血管住院等临床终点。迄今为止,它是仅在老年患者中进行过专门研究的少数β肾上腺素能阻滞剂之一。此外,奈必洛尔独特的作用机制使其成为治疗高危患者群体(如非裔美国人)慢性心力衰竭的有前景药物。本文将综述奈必洛尔的药理和药代动力学特性以及评估其治疗心力衰竭疗效的临床研究。