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首页> 外文期刊>Infection and Drug Resistance >In vitro activity and pharmacodynamic/pharmacokinetic parameters of clarithromycin and azithromycin: why they matter in the treatment of respiratory tract infections
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In vitro activity and pharmacodynamic/pharmacokinetic parameters of clarithromycin and azithromycin: why they matter in the treatment of respiratory tract infections

机译：克拉霉素和阿奇霉素的体外活性和药代动力学/药代动力学参数：为什么它们对呼吸道感染的治疗很重要

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Clarithromycin and azithromycin are second-generation macrolides established and widely used for treating a range of upper and lower respiratory tract infections. Extensive clinical trials data indicate that these drugs are highly effective in these applications and broadly comparable in their clinical and microbiological effectiveness. However, consideration of pharmacokinetic, metabolic, and tissue-penetration data, including the significant antibacterial activity of the metabolite 14-hydroxy-clarithromycin, plus the findings of pharmacodynamic modeling, provide evidence that the long half-life and lower potency of azithromycin predispose this agent to select for resistant isolates. Comparison of the “mutant-prevention concentrations” of clarithromycin and azithromycin, and examination of large-scale epidemiological data from Canada, also support the view that these drugs differ materially in their propensity to promote resistance among bacterial strains implicated in common respiratory infections, and that clarithromycin may offer important advantages over azithromycin that should be considered when choosing a macrolide to treat these conditions.
机译：克拉霉素和阿奇霉素是第二代大环内酯类药物，已建立并广泛用于治疗各种上，下呼吸道感染。大量的临床试验数据表明，这些药物在这些应用中非常有效，并且在临床和微生物功效方面具有可比性。但是，考虑到药代动力学，代谢和组织渗透性数据，包括代谢物14-羟基-克拉霉素的显着抗菌活性，以及​​药效学模型的发现，提供了证据表明阿奇霉素的半衰期长和药效低是这种情况的前兆剂以选择抗性菌株。比较克拉霉素和阿奇霉素的“预防突变浓度”，以及检查来自加拿大的大规模流行病学数据，也支持以下观点：这些药物在促进与常见呼吸道感染有关的细菌菌株之间产生耐药性的倾向存在实质性差异。克拉霉素可能比阿奇霉素具有重要的优势，在选择大环内酯类药物治疗这些疾病时应考虑阿奇霉素。

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