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健康受试者中头孢噻肟的动力学(作者译)

[Kinetics of cefotaxime in healthy subjects (author's transl)].

作者信息

Acar J F, Guibert J, Kitzis M D

出版信息

Nouv Presse Med. 1981 Feb 26;10(8):559-63.

PMID:6259593
Abstract

Serum and urinary levels of cefotaxime after either intramuscular (i.m.) or intravenous (i.v.) administration were determined in 6 normal human subjects. By the i.m. route the serum half-life was 80 minutes. The peak serum concentration, at 30 minutes, reached 12 and 24 mcg/ml after injection of 500 mg and 1 g. Concentrations in the urine were 500 mcg/ml within 6 hours after an injection of 500 mg; they reached 1000 mcg/ml after an injection of 1 g. Urinary elimination amounted to 50% during the first 6 hours; it reached 60% during 24 hours. By the i.v. route, the serum half-life was 40 minutes. The concentration in the serum was more than 100 mcg/ml at the fifth minute after an injection of 1 g. Concentrations in the urine were 1300 mcg/ml within 4 hours after injection of cefotaxime. The urinary elimination amounted to 60--64% during 12 hours. Intravenous infusion of 1 g during 4 hours gave a serum level, from the second hour, approaching 15 mcg/ml. The concentration in the urine was 600 mcg/ml within 4 hours. The urinary elimination amounted to 50% in 12 hours. Protein binding of cefotaxime ranged from 36 to 38%.

摘要

在6名正常人体受试者中测定了肌内注射(i.m.)或静脉注射(i.v.)后头孢噻肟的血清和尿液水平。通过肌内注射途径,血清半衰期为80分钟。注射500mg和1g后,30分钟时血清峰值浓度分别达到12和24mcg/ml。注射500mg后6小时内尿液浓度为500mcg/ml;注射1g后达到1000mcg/ml。在前6小时内尿液消除量为50%;24小时内达到60%。通过静脉注射途径,血清半衰期为40分钟。注射1g后第5分钟血清浓度超过100mcg/ml。注射头孢噻肟后4小时内尿液浓度为1300mcg/ml。12小时内尿液消除量为60%-64%。4小时内静脉输注1g,从第2小时起血清水平接近15mcg/ml。4小时内尿液浓度为600mcg/ml。12小时内尿液消除量为50%。头孢噻肟的蛋白结合率在36%至38%之间。

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