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单次静脉给药后头孢吡肟的安全性、耐受性及药代动力学评估。

Safety, tolerance, and pharmacokinetic evaluation of cefepime after administration of single intravenous doses.

作者信息

Barbhaiya R H, Forgue S T, Gleason C R, Knupp C A, Pittman K A, Weidler D J, Martin R R

机构信息

Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb Company, Syracuse, New York 13221-4755.

出版信息

Antimicrob Agents Chemother. 1990 Jun;34(6):1118-22. doi: 10.1128/AAC.34.6.1118.

DOI:10.1128/AAC.34.6.1118
PMID:2203303
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC171768/
Abstract

In this double-blind, single-dose phase I study, the safety and tolerance of cefepime were assessed in 24 healthy male subjects, with ceftazidime as the control drug. Four subjects in each of the six dose groups (62.5, 125, 250, 500, 1,000, or 2,000 mg as a 30-min intravenous infusion) received each antibiotic, according to a crossover design, with a 2-day washout period between treatments. Blood and urine samples were obtained to characterize the pharmacokinetics of cefepime. Plasma and urine samples were assayed for intact cefepime. Samples containing ceftazidime were discarded. The adverse effects observed in the study were mild and infrequent, with prompt recovery from adverse experiences and abnormal laboratory values. The cefepime pharmacokinetic parameters for the therapeutically significant doses of 250 to 2,000 mg appeared to be proportional to dose and similar to literature values for ceftazidime. The elimination half-life of about 2 h was independent of the dose. Urinary recovery of intact cefepime was invariant with respect to dose; an overall mean value of 82% of dose was obtained for the four highest levels. Mean renal clearance was 105 ml/min and suggestive of glomerular filtration as the primary excretion mechanism. In normal humans, the safety and pharmacokinetic profiles of cefepime are very similar to those of ceftazidime.

摘要

在这项双盲、单剂量I期研究中,以头孢他啶作为对照药物,对24名健康男性受试者评估了头孢吡肟的安全性和耐受性。六个剂量组(分别为62.5、125、250、500、1000或2000mg,静脉输注30分钟)每组有4名受试者,按照交叉设计接受每种抗生素治疗,治疗之间有2天的洗脱期。采集血液和尿液样本以表征头孢吡肟的药代动力学。检测血浆和尿液样本中的完整头孢吡肟。含有头孢他啶的样本被丢弃。研究中观察到的不良反应轻微且不常见,不良经历和实验室异常值均迅速恢复。250至2000mg治疗有效剂量的头孢吡肟药代动力学参数似乎与剂量成正比,且与头孢他啶的文献值相似。约2小时的消除半衰期与剂量无关。完整头孢吡肟的尿回收率与剂量无关;四个最高剂量水平的总体平均值为剂量的82%。平均肾清除率为105ml/min,提示肾小球滤过是主要排泄机制。在正常人体内,头孢吡肟的安全性和药代动力学特征与头孢他啶非常相似。

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本文引用的文献

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Pharmacokinetics of beta-lactam antibiotics.β-内酰胺类抗生素的药代动力学
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