摘要
目的：探讨合理的比伐卢定临床序贯给药方案。方法：筛选健康受试者12名，给予比伐卢定0．75mg／kg静脉推注后，1．75mg·kg^-1·h^-1的速度匀速静滴4h，不同时间点采集血样，测定血药浓度、活性凝血时间（ACT）及凝血功能，计算药代动力学、药效学参数，同时观察试验期间的不良事件。结果：序贯给药期间药-时曲线与时-效曲线吻合良好，ACT稳定在220～240S，药效动力学符合M—Mequation模型。试验期间未出现严重不良事件，凝血功能于停药后24h恢复至正常水平。结论：比伐卢定序贯给药（0．75mg／kg静脉推注后，1．75mg·kg^-1·h^-1静滴）的药效及安全性能够满足临床要求。
ABSTRACT AIM： To investigate the reasona- ble sequential regimen of bivalirudin in clinic. METHODS： 12 Chinese healthy volunteers were selected. During bivalirudin administration （0.75 mg/kg bolus followed by a 1.75 mg · kg^1- · h ^-1 infusion for 4 h）, blood samples were collected in regular time, and blood concentra- tion of bivalirudin, active coagulation time （ACT） and function were measured. Then the primary pharmacokinetic parameters were cacu- lated using WinNonlin 5. 2. 1. The adverse e- vents were observed during the clinical trial. RE- SULTS： The time-effect curves and time-concen-tration curve of bivalirudin in this clinical trial were paralleled. The ACT was 220- 240 s steadily respectively. During the clinical trial, there were no serve adverse events, and the co- agulation function recovered to normal after 24 h. CONCLUSION. Bivalirudin sequential regi- men （0.75 mg/kg bolus followed by a 1.75 mg · kg ^-1 · h^-1 infusion for 4 h） is effective and safe for clinic.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2014年第7期785-788,共4页
Chinese Journal of Clinical Pharmacology and Therapeutics
关键词
比伐卢定
序贯给药
活性凝血时间
bivalirudin
sequential regimen
active coagulation time （ACT）
