Telavancin对细胞色素P450的药物代谢动力学的影响3探测衬底咪达唑仑:一项随机、双盲、交叉研究在健康受试者。

文章的细节

引用

复制到剪贴板

黄SL,戈德堡先生,深水区CH,小猫MM, Barriere SL

Telavancin对细胞色素P450的药物代谢动力学的影响3探测衬底咪达唑仑:一项随机、双盲、交叉研究在健康受试者。

药物治疗。2010年2月,30 (2):136 - 43。doi: 10.1592 / phco.30.2.136。

PubMed ID

20099988 (在PubMed

]

文摘

研究目的:研究telavancin的影响,lipoglycopeptide抗生素与强有力的革兰氏阳性活动,咪达唑仑的药物动力学,细胞色素P450 (CYP) 3探针底物。设计。第一阶段,随机,双盲,安慰剂对照,交叉研究。设置。临床研究中心。必威国际app参与者:16名健康成人志愿者。干预。受试者被随机分配接受静脉输液telavancin 10毫克/公斤/天或安慰剂一次7天。7天,单剂静脉咪达唑仑1毫克的最后注入完成后立即被telavancin或安慰剂。病人进入了替代治疗方案在冲刷时间的至少7天。 MEASUREMENTS AND MAIN RESULTS: Pharmacokinetic sampling was performed on study days 7 and 21. Blood was collected before telavancin or placebo dosing and at 0.25, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours after midazolam administration. Formal equivalence analysis using the two one-sided t test method showed that the geometric mean ratios for maximum plasma concentration (C(max)) and areas under the plasma concentration-time curve (AUC) for midazolam coadministered with telavancin versus midazolam coadministered with placebo were close to unity. The 90% confidence intervals (CIs) around the ratios fell within the 0.8-1.25 bioequivalence bounds (geometric mean ratio for AUC from time zero to the last measured plasma concentration 0.95, 90% CI 0.910-0.984; C(max) geometric mean ratio 1.03, 90% CI 0.956-1.11). The multiple-dose pharmacokinetic profile of telavancin with concomitant administration of midazolam (C(max) 97 microg/ml, concentration 24 hrs after completion of telavancin infusion 9 microg/ml, terminal-phase elimination half-life 8.9 hrs, clearance 13.3 ml/hr/kg) was consistent with data from earlier studies. CONCLUSION: These pharmacokinetic data show that intravenous telavancin administered at the intended therapeutic dose does not affect the pharmacokinetics of intravenous midazolam. The results indicate that telavancin is unlikely to inhibit hepatic CYP3A activity to a clinically meaningful extent.

DrugBank数据引用了这篇文章

药物

Telavancin