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抗生素在妊娠及分娩期的药代动力学

Pharmacokinetics of antibiotics in pregnancy and labour.

作者信息

Philipson A

出版信息

Clin Pharmacokinet. 1979 Jul-Aug;4(4):297-309. doi: 10.2165/00003088-197904040-00003.

Abstract

Few of the articles published on antibiotics and pregnancy are concerned with pharmacokinetics. It is particularly difficult to evaluate possible alterations in pharmacokinetic parameters that may be due to pregnancy. Most data available have been obtained in connection with abortion or delivery. Such data may not be representative for pregnancy as such. Marked changes in most organ systems, particularly in renal function, but in composition and amounts of body fluids as well, make it likely that several pharmacokinetic parameters change, possibly gradually as pregnancy progresses. Accumulated data for several beta-lactam antibiotics, and also for aminoglycosides indicate that antibiotics eliminated mainly by renal excretion will produce lower levels in serum or plasma in pregnant women than in other individuals. Also, the half-life of certain antibiotics in serum is shorter during pregnancy. Transplacental passage occurs for all antibiotics according to the physicochemical properties of the drug. Bolus injections to a pregnant woman are more efficient than continuous infusion in producing high levels of antibiotic in fetal serum and amniotic fluid. Fetal tissue levels are higher following multiple doses than after a single dose. Lower serum levels of antibiotics in pregnant women than in other individuals following the same dosage will be unsatisfactory as micr-organisms are less likely to be affected.

摘要

已发表的关于抗生素与妊娠的文章中,涉及药代动力学的很少。评估可能因妊娠导致的药代动力学参数改变尤其困难。现有的大多数数据是在人工流产或分娩相关情况下获得的。此类数据可能并不足以代表妊娠本身的情况。大多数器官系统都会发生显著变化,特别是肾功能,还有体液的成分和数量也会改变,这使得几个药代动力学参数很可能发生变化,而且可能随着妊娠进展而逐渐变化。几种β-内酰胺类抗生素以及氨基糖苷类抗生素的累积数据表明,主要经肾脏排泄的抗生素在孕妇血清或血浆中的水平会低于其他个体。此外,某些抗生素在孕期血清中的半衰期较短。根据药物的理化性质,所有抗生素都会发生经胎盘转运。对孕妇进行大剂量注射比持续输注更能有效地在胎儿血清和羊水中产生高浓度的抗生素。多次给药后胎儿组织中的抗生素水平高于单次给药后。相同剂量下孕妇血清中的抗生素水平低于其他个体,这是不理想的,因为微生物不太可能受到影响。

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