药物动力学、安全性和耐受性的提升单剂量静脉oritavancin管理健康的人体试验。

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Bhavnani SM,欧文JS Loutit JS,波特某人,安布罗斯PG

药物动力学、安全性和耐受性的提升单剂量静脉oritavancin管理健康的人体试验。

成岩作用Microbiol感染说。2004年10月;(2):95 - 102。

PubMed ID

15474317 (在PubMed

]

文摘

Oritavancin (LY333328二磷酸)是一种新型的糖肽抗菌剂与有效的微生物活动在体外对革兰氏阳性细菌。单剂,非盲、无控,剂量递增研究11健康人体进行评估的安全性和药物动力学oritavancin。一个主题在每个剂量水平收到一个静脉注射剂量的0.02,0.03,0.05,0.08,0.125,0.20,和0.325毫克/公斤注入超过1小时和四个科目每个接受单剂量为0.5毫克/公斤。安全性和耐受性进行评估通过监测不良事件和实验室参数。Oritavancin药物动力学评估通过血液、尿液和粪便样本。血浆浓度oritavancin输液结束后跟随multiexponential下降超过两周。中位数(范围)C (max)为0.5毫克/公斤剂量组为6.5 (4.7 - -7.6)microg /毫升。在每一个主题,等离子体浓度拒绝<或= 10%的C (max)在24小时内。短后,恒速输注,oritavancin的药物动力学线性在总剂量范围从3.66 - -44.6毫克。肾清除率是大约0.457毫升/分钟。 The mean (range) plasma terminal half-life of oritavancin was 195.4 (135.8-273.8) hours across all dose levels from 0.05-0.5 mg/kg. Less than 5% and 1% of administered drug were recovered in the urine and feces, respectively, after 7 days. This first time in man evaluation of oritavancin revealed that single doses of oritavancin of up to and including 0.5 mg/kg were safe and well tolerated. Although no clinically relevant changes in renal, hepatic and hematologic indices from baseline were observed, five subjects did manifest asymptomatic and transient elevations of hepatic transaminase concentrations. Because this study was not placebo-controlled and enrolled a small number of subjects, the safety and pharmacokinetic profiles of oritavancin need to be confirmed in additional studies.

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药物

Oritavancin