摘要
目的:探索新型α-受体阻滞剂萘哌地尔在中国高血压病患者体内的药动学及降压效果。方法:10例高血压病患者单次口服萘哌地尔50 mg,用反相HPLC荧光检测方法测定患者血浆中萘哌地尔的浓度。用3P87程序软件处理数据;抽血测血药浓度的同时,亦进行动态血压监测,分析患者体内血药浓度与降压效应之间的关系。结果:单次口服萘哌地尔50 mg在中国高血压病患者体内符合一室模型、一级吸收过程;平均药动学参数分别为t_(1/2) 6.03 h,T_(max) 2.59 h,C_(max) 71.86 ng·mL^(-1),AUC 321.07 ng·h·mL^(-1),CL 195.5 L·h^(-1)。随着患者体内血药浓度的上升,血压有逐渐下降的趋势,同时伴心率增快,无心动过速和体位性低血压的现象发生。结论:萘哌地尔在中国高血压病患者体内的药动学特点与健康志愿者基本一致,适用于中国高血压患者的降压治疗。
Objective: To explore the pharmacokinetics and antihypertensive effect of nafiopidil, a novel selective α1-adrenoceptor antagonist .Methods: 10 essential hypertensive patients were administered a single oral dose of naftopidil 50 mg. The blood samples from the patients were collected to determine the plasma levels of naftopidil by RP-HPLC with fluorescence detection. A 24-hour ambulatory blood pressure monitoring was simultaneously performed. Results: The pharmacokinetic profile of naftopidil obeyed one-compartment model and first-order absorption with t1/2 6.03 h, T 2.59 h, C 71.86 ng· mL^-1 and AUC 321.07 ng·h·mL^-1. The blood pressure was gradually reduced in a positive plasma naftopidil-dependent manner. The patients experienced faster heartbeats and no tachycardia and orthostatic hypotension. Conclusion:Naftopidil offered a therapeutic option in Chinese patients with hypertension.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2006年第16期1397-1400,共4页
Chinese Journal of New Drugs
关键词
萘哌地尔
Α-受体阻滞剂
药动学
高血压
动态血压监测
naftopidil
α1-adrenoceptor antagonist
pharmacokinetics
hypertension
24-hour ambulatory blood pressure monitoring