[抗生素治疗支气管-肺部细菌感染的药代动力学基础[作者简介]。

J Grosset, R Bismuth, J Nguyen
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引用次数: 0

摘要

药代动力学是研究药物在体内的吸收、分布和消除。应用于抗生素治疗时,它提供了在给定的剂量和给药途径下,在给定时间到达细菌增殖部位的抗生素浓度的信息。抗生素在体内的未来很大程度上与被动转移有关。这可以与分子在半透膜上的透析进行比较,从一侧到另一侧的通道是“上游”一侧分子浓度、分子大小和它们自身特定传递速度的函数。最终结果受到以下因素的影响:1)与分子的水溶性和脂溶性程度相关的分配系数本身;2)分子的电离程度,非电离分子是唯一被转移的分子;3)蛋白质结合,因为只有未结合的部分具有生物活性并能够在膜上扩散;4)吸收、分布和消除等综合现象的相互作用。青霉素类和大环内酯类抗生素是支气管肺部感染的首选抗生素。四环素类药物和磺胺甲恶唑-甲氧苄啶联合用药位居第二。β -内酰胺、氨基糖苷和/或甲硝唑的联合治疗用于最严重的感染。肺是一个血管特别发达的器官,肺中抗生素的浓度可能等于血清水平。但克林霉素在支气管分泌物中的浓度仅达到血清水平的55%,氨基糖苷类、米诺环素和巴氨苄西林的浓度为25 - 30%,头孢菌素和多西环素的浓度为20%,氨苄西林和红霉素的浓度不到10%。只有夹竹桃霉素、螺旋霉素和甲氧苄啶的浓度与血清中的浓度相等。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[Pharmacokinetic basis for antibiotic therapy in broncho-pulmonary bacterial infections (author's transl)].

Pharmacokinetics is the study of the absorption, distribution and elimination of a drug in the body. Applied to antibiotic therapy it gives information on the concentrations of antibiotic that reach the bacteria at a given time at their site of multiplication for a given dose and route of administration. The future of an antibiotic within a body is largely related to passive transfer. This can be compared to the dialysis of molecules across a semi-permeable membrane, the passage from one side to the other being a function of the concentration of molecules in the "upstream" side, the size of the molecules and their own particular transfer speed. The final result is affected by 1) the partition coefficient itself related to the degree of aqueous and lipid solubility of the molecules, 2) the degree of ionisation of the molecules, non-ionised molecules being the only ones to be transferred, 3) protein binding as only the unbound fraction is biologically active and capable of diffusing across the membranes, 4) by the interplay of the combined phenomena of resorption, distribution and elimination. Penicillins and macrolides are the antibiotics of choice in broncho-pulmonary infections. The tetracyclines and the sulfamethoxazole-trimethoprim combination come second. The combination of a beta-lactam, an aminoglycoside and/or metronidazole are reserved for the most severe infections. The lung is a particularly well vascularised organ, the pulmonary concentrations of the antibiotic may equal the serum levels. But the concentration in the bronchial secretions only reaches 55% of the serum levels for clindamycin, 25 to 30% for aminoglycosides, minocycline and bacampicillin, 20% for cephalosporins and doxycycline and less than 10% for ampicillin and erythromycin. Only oleandomycine, spiramycin and trimethoprim are present in concentrations equal to those in the serum.

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