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单次24小时剂量给药后慢性支气管炎患者血清和支气管分泌物中头孢噻肟及去乙酰头孢噻肟的药代动力学

[Pharmacokinetics of cefotaxime and desacetylcefotaxime in the blood serum and bronchial secretion in patients with chronic bronchitis after administration of a single 24-hour dose].

作者信息

Kamnev Iu V, Manuĭlov K K, Orlov V A, Sokolova V I

出版信息

Antibiot Khimioter. 1991 Oct;36(10):42-4.

PMID:1805696
Abstract

Concentrations of cefotaxime and its major active metabolite, desacetylcefotaxime, were determined in the serum and bronchial secretion of patients with chronic bronchitis aggravated after intramuscular injection of cefotaxime in a dose of 4 g once a day. Characteristic patterns of cefotaxime metabolism and high peak concentrations of desacetylcefotaxime in the serum (67.6 +/- 17.2 micrograms/ml) defined the prolonged retention of the metabolite both in the blood and bronchial secretion. The metabolite concentrations in more than half of the patients maintained within 2 micrograms/ml in the bronchial secretion by the 12th hour after the injection and in the blood serum by the 24th hour. Therefore, 4 g cefotaxime administered intramuscularly once a day provided the blood concentrations of the metabolite comparable with the MIC for the majority of the pathogens causing nosocomial infections of the respiratory tract practically within the whole period of the daily dosage. In the bronchial secretion such concentrations were attained within half of the period of the daily dosage.

摘要

对慢性支气管炎急性加重患者每日一次肌内注射4g头孢噻肟后,测定其血清及支气管分泌物中头孢噻肟及其主要活性代谢产物去乙酰头孢噻肟的浓度。头孢噻肟代谢的特征模式以及血清中去乙酰头孢噻肟的高峰浓度(67.6±17.2μg/ml)表明该代谢产物在血液和支气管分泌物中均有较长时间的留存。超过半数患者的代谢产物浓度在注射后12小时支气管分泌物中和24小时血清中维持在2μg/ml以下。因此,每日一次肌内注射4g头孢噻肟,在每日剂量的几乎整个时间段内,均可使代谢产物的血药浓度与引起呼吸道医院感染的大多数病原体的最低抑菌浓度相当。在支气管分泌物中,该浓度在每日剂量时间段的一半时间内即可达到。

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