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常用药物和遗传因素对奈必洛尔药代动力学的影响:药物相互作用研究。

Effects of commonly administered agents and genetics on nebivolol pharmacokinetics: drug-drug interaction studies.

机构信息

Toxicology and Clinical Pharmacology, Forest Research Institute, Harborside Financial Center; Plaza V, Jersey City, NJ 0731, USA.

出版信息

J Clin Pharmacol. 2011 Apr;51(4):575-85. doi: 10.1177/0091270010370846. Epub 2010 May 20.

Abstract

Drug interactions are a significant clinical concern, particularly in patients with conditions such as heart disease and hypertension, in whom coadministration of multiple drugs is common. Nebivolol is a selective β(1)-blocker with vasodilatory properties approved for the treatment of hypertension. Drug-drug interactions were investigated when nebivolol was coadministered to subjects classified as poor CYP2D6 metabolizers and extensive CYP2D6 metabolizers who were receiving other drugs commonly administered to patients with hypertension or compounds metabolized by cytochrome P450 (CYP) 2D6. There were no drug-drug interactions when nebivolol was coadministered with hydrochlorothiazide, furosemide, ramipril, losartan, digoxin, or warfarin. Coadministration with fluoxetine (also metabolized by CYP2D6) in extensive CYP2D6 metabolizers impeded the apparent clearance of nebivolol. The authors conclude that nebivolol is safe and well tolerated regardless of genotype and type of medication coadministered.

摘要

药物相互作用是一个重要的临床关注点,特别是在心脏病和高血压等疾病患者中,这些患者通常同时服用多种药物。比索洛尔是一种具有血管扩张作用的选择性β(1)-受体阻滞剂,已被批准用于治疗高血压。当比索洛尔与被归类为 CYP2D6 弱代谢者和 CYP2D6 广泛代谢者的受试者同时使用时,研究了与其他通常用于高血压患者或细胞色素 P450(CYP)2D6 代谢的化合物一起给药的药物的药物相互作用。当比索洛尔与氢氯噻嗪、呋塞米、雷米普利、氯沙坦、地高辛或华法林同时使用时,没有药物相互作用。在 CYP2D6 广泛代谢者中与氟西汀(也由 CYP2D6 代谢)同时使用会阻碍比索洛尔的表观清除率。作者得出结论,无论基因型和同时使用的药物类型如何,比索洛尔都是安全且耐受良好的。

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