Background

Amoxicillin has been in use since the 1970s; it is the most widely used penicillin both alone and in combination with the β-lactamase clavulanic acid.

Objectives

In this narrative review, we re-examine the properties of oral amoxicillin and clavulanic acid and provide guidance on their use, with emphasis on the preferred use of amoxicillin alone.

Sources

Published medical literature (MEDLINE database via Pubmed).

Content

While amoxicillin and clavulanic acid have similar half-lives, clavulanic acid is more protein bound and even less heat stable than amoxicillin, with primarily hepatic metabolism. It is also more strongly associated with gastrointestinal side effects, including Clostridium difficile infection, and, thus, in oral combination formulations, limits the maximum daily dose of amoxicillin that can be given. The first ratio for an amoxicillin–clavulanic acid combination was set at 4:1 due to clavulanic acid's high affinity for β-lactamases; ratios of 2:1, 7:1, 14:1 and 16:1 are currently available in various regions. Comparative effectiveness data for the different ratios are scarce. Amoxicillin–clavulanic acid is often used as empiric therapy for many of the World Health Organization's Priority Infectious Syndromes in adults and children, leading to extensive consumption, when some of these syndromes could be handled with a delayed antibiotic prescription approach or amoxicillin alone.

Implications

Using available epidemiological and pharmacokinetic data, we provide guidance on indications for amoxicillin versus amoxicillin–clavulanic acid and on optimal oral administration, including choice of combination ratio. More data are needed, particularly on heat stability, pharmacodynamic effects and emergence of resistance in ‘real-world’ clinical settings.

中文翻译：

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口服阿莫西林和阿莫西林-克拉维酸：性质，适应症和用法。

背景

阿莫西林自1970年代开始使用。它是单独使用或与β-内酰胺酶棒酸结合使用的最广泛的青霉素。

目标

在本篇叙述性综述中，我们重新检查了口服阿莫西林和克拉维酸的性质，并为它们的使用提供了指导，重点放在了阿莫西林单独的优选用法上。

资料来源

已出版的医学文献（通过Pubmed获得MEDLINE数据库）。

内容

尽管阿莫西林和克拉维酸的半衰期相似，但与阿莫西林相比，克拉维酸具有更多的蛋白质结合能力，甚至热稳定性更低，主要是通过肝脏代谢。它也与胃肠道副作用（包括艰难梭菌）密切相关。感染，因此，在口服联合制剂中，限制了可给予的阿莫西林的最大每日剂量。由于阿魏酸对β-内酰胺酶的高亲和力，阿莫西林-克拉维酸组合的第一个比例设定为4：1。目前在各个地区都可以使用2：1、7：1、14：1和16：1的比率。不同比率的比较有效性数据很少。阿莫西林-克拉维酸经常被成人和儿童使用作为世界卫生组织许多优先感染综合症的经验疗法，导致大量食用，而其中某些综合症可以通过延迟抗生素处方方法或单独使用阿莫西林治疗。

含意

利用现有的流行病学和药代动力学数据，我们为阿莫西林与阿莫西林-克拉维酸的适应症以及最佳口服给药（包括组合比例的选择）提供了指导。需要更多的数据，尤其是在“现实”临床环境中的热稳定性，药效学效应和耐药性的出现。