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腹水对阿米卡星药代动力学的影响。

The influence of ascites on the pharmacokinetics of amikacin.

作者信息

Lanao J M, Dominguez-Gil A, Macias J G, Diez J L, Nieto M J

出版信息

Int J Clin Pharmacol Ther Toxicol. 1980;18(2):57-61.

PMID:7372376
Abstract

The pharmacokinetics of Amikacin are studied after the administration of 7.5 mg/kg body weight to 10 ascitic patients diagnosed with various hepatic disorders. The antibiotic was determined microbiologically in plasma and in the ascitic fluid. The antibiotic follows a two-compartment kinetic model, and it may be seen that once the rapid disposition phase has ended, an inflexion in the plasma-time levels curve takes place, with a passing increase in the plasma concentrations. From the pharmacokinetic study of Amikacin in these patients, it may be deduced that the ascitic liquid forms part of the central compartment for the effects of distribution, though not for the effects of elimination. The plasma half-life of the slow disposition phase is analogous to that obtained from non-ascitic patients with normal renal function. In one of the patients, the antibiotic was administered intraperitoneally; following this, the plasma concentrations of Amikacin were detected. In the last of the 10 patients included in the survey, the evolution of the plasma concentrations of the antibiotic were studied while the patient was undergoing a multiple dosage regimen with the aim of determining the accumulation of Amikacin in the ascitic fluid. A dosage regimen of multiple doses is programmed which should guarantee the efficiency and safety of the antibiotic.

摘要

对10名被诊断患有各种肝脏疾病的腹水患者给予7.5毫克/千克体重的阿米卡星后,研究了其药代动力学。通过微生物学方法测定血浆和腹水中的抗生素含量。该抗生素遵循二室动力学模型,可以看出,一旦快速消除相结束,血浆-时间水平曲线就会出现拐点,血浆浓度会短暂升高。从这些患者中阿米卡星的药代动力学研究可以推断,腹水构成了分布效应的中央室的一部分,但不构成消除效应的中央室的一部分。缓慢消除相的血浆半衰期与肾功能正常的非腹水患者相似。在其中一名患者中,抗生素通过腹腔内给药;随后,检测到了阿米卡星的血浆浓度。在纳入调查的10名患者中的最后一名患者中,在患者接受多剂量方案治疗时研究了抗生素血浆浓度的变化情况,目的是确定阿米卡星在腹水中的蓄积情况。制定了多剂量给药方案,该方案应保证抗生素的有效性和安全性。

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