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氨基糖苷类药物——问世50年

Aminoglycosides--50 years on.

作者信息

Begg E J, Barclay M L

机构信息

Department of Clinical Pharmacology, Christchurch School of Medicine, New Zealand.

出版信息

Br J Clin Pharmacol. 1995 Jun;39(6):597-603.

Abstract
  1. The aminoglycoside antibiotics are 50 years old. Their success and continuing use can be attributed to various factors including rapid concentration-dependent bactericidal effect, synergism with beta-lactam antibiotics, clinical effectiveness, a low rate of true resistance and low cost. 2. The aminoglycosides remain drugs of choice in many circumstances including septicaemia, other serious infections due to Gram negative bacilli, and bacterial endocarditis. 3. Nephrotoxicity and ototoxicity have been the main drawbacks clinically for the aminoglycosides. 4. There has been an evolution in dosing strategies largely aimed at reducing toxicity. Therapeutic drug monitoring has been used extensively to assist dosing, and target concentrations have been advocated, such as peak concentrations of between 6 and 10 mg l-1 and through concentrations of < 2 mg l-1 for gentamicin, tobramycin and netilmicin. 5. Recently there has been a minor revolution in the approach to aminoglycoside dosing, with a change to larger doses, given less frequently. In its most convenient form this is 'Once-daily aminoglycoside dosing'. It offers the hope of better efficacy, less toxicity, and easier administration and monitoring. 6. This article summarises the background of aminoglycoside usage, leading up to the recent changes in dosing strategy.
摘要
  1. 氨基糖苷类抗生素已有50年历史。它们的成功及持续应用可归因于多种因素,包括快速的浓度依赖性杀菌作用、与β-内酰胺类抗生素的协同作用、临床有效性、真正耐药率低以及成本低廉。2. 在许多情况下,氨基糖苷类药物仍是首选药物,包括败血症、革兰氏阴性杆菌引起的其他严重感染以及细菌性心内膜炎。3. 肾毒性和耳毒性一直是氨基糖苷类药物临床上的主要缺点。4. 给药策略不断演变,主要目的是降低毒性。治疗药物监测已被广泛用于辅助给药,并提倡使用目标浓度,例如庆大霉素、妥布霉素和奈替米星的峰值浓度在6至10 mg l-1之间,谷浓度<2 mg l-1。5. 最近,氨基糖苷类药物的给药方法发生了一场小变革,改为更大剂量、给药频率更低。最便捷的形式是“每日一次氨基糖苷类给药”。它带来了疗效更好、毒性更小、给药及监测更简便的希望。6. 本文总结了氨基糖苷类药物的使用背景,直至近期给药策略的变化。

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