Department of Pharmacy Practice, Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan.
Department of Pharmacology, Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan.
Drug Metab Rev. 2023 Nov;55(4):428-440. doi: 10.1080/03602532.2023.2271195. Epub 2023 Oct 28.
Nebivolol is a beta-1 receptor blocker used to treat hypertension, heart failure, erectile dysfunction, vascular disease, and diabetes mellitus. This review investigated the data regarding pharmacokinetic (PK) parameters, drug-drug interactions, dextrorotatory (D), and levorotatory (L) stereoisomers of nebivolol. The articles related to the PK of nebivolol were retrieved by searching the five databases; Google Scholar, PubMed, Cochrane Library, ScienceDirect, and EBSCO. A total of 20 studies comprising plasma concentration-time profile data following the nebivolol's oral and intravenous (IV) administration were included. The area under the concentration-time curve from zero to infinity (AUC) was 15 times greater in poor metabolizers (PMs) than in extensive metabolizers (EMs). In hypertensive patients, L-nebivolol expressed a higher maximum plasma concentration (C) than D-nebivolol, i.e. 2.5 ng/ml vs 1.2 ng/ml. The AUC of nebivolol was 3-fold greater in chronic kidney disease (CKD). The clearance (CL) was increased in obese than in controls from 51.6 ± 11.6 L/h to 71.6 ± 17.4 L/h when 0.5 mg/ml IV solution was infused. Nebivolol showed higher C, AUC and half-life (t) when co-administered with bupropion, duloxetine, fluvoxamine, paroxetine, lansoprazole, and fluoxetine. This concise review of nebivolol would be advantageous in assessing all PK parameters, which may be crucial for clinicians to avoid drug-drug interactions, prevent adverse drug events and optimize the dosage regimen in diseased patients diagnosed with hypertension and cardiovascular disorders.
比索洛尔是一种用于治疗高血压、心力衰竭、勃起功能障碍、血管疾病和糖尿病的β-1 受体阻滞剂。本综述调查了比索洛尔的药代动力学（PK）参数、药物相互作用、右旋（D）和左旋（L）立体异构体的数据。通过搜索五个数据库：谷歌学术、PubMed、Cochrane Library、ScienceDirect 和 EBSCO，检索到与比索洛尔 PK 相关的文章。共有 20 项研究纳入了比索洛尔口服和静脉（IV）给药后的血浆浓度-时间曲线数据。与广泛代谢者（EMs）相比，代谢不良者（PMs）的比索洛尔零到无穷大（AUC）面积增加了 15 倍。在高血压患者中，L-比索洛尔的最大血浆浓度（C）高于 D-比索洛尔，即 2.5 ng/ml 对 1.2 ng/ml。在慢性肾脏病（CKD）患者中，比索洛尔的 AUC 增加了 3 倍。与对照组相比，肥胖者的清除率（CL）从 51.6±11.6 L/h 增加到 71.6±17.4 L/h，当 0.5 mg/ml IV 溶液输注时。比索洛尔与安非他酮、度洛西汀、氟伏沙明、帕罗西汀、兰索拉唑和氟西汀合用时，C、AUC 和半衰期（t）更高。这篇简明的比索洛尔综述将有助于评估所有 PK 参数，这对于临床医生避免药物相互作用、预防不良药物事件以及优化诊断为高血压和心血管疾病的患者的剂量方案可能至关重要。
