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米卡芬净在成人、儿童及新生儿中的药效学与药代动力学

[Pharmacodynamics and pharmacokinetics of micafungin in adults, children and neonate].

作者信息

Catalán-González Mercedes, Carlos Montejo-González Juan

机构信息

Servicio de Medicina Intensiva, UCI-Polivalente, Hospital Universitario 12 de Octubre, Madrid, España.

出版信息

Rev Iberoam Micol. 2009 Mar 31;26(1):23-34. doi: 10.1016/S1130-1406(09)70005-1. Epub 2009 May 7.

DOI:10.1016/S1130-1406(09)70005-1
PMID:19463274
Abstract

BACKGROUND

Invasive fungal infections are a significant cause of morbidity and mortality among immunocompromised patients. Although several new antifungal agents have been developed in the past few years, the management of serious fungal infections continues to be problematic.

AIMS

To review the pharmacodynamics and pharmacokinetics of a new antifungal agent: micafungin.

METHODS

A systematic review of biomedic databases (EBSCO Open Journals, Ovid Online, Proquest Medical Library, PubMed/Medline, Science Direct, Springer Links and Wiley Interscience) has been performed. Search was conducted from 2000 to 2008. Supplementary sources included abstracts from the Interscience Conference on Antimicrobial Agents (ICAAC) and Chemotherapy and the Infectious Diseases Society of America (IDSA) from 1998 to 2008.

RESULTS

Micafungin has a potent mechanism of action: inhibits beta-1,3-D-glucan synthase interfering with fungal cell wall synthesis. This agent shares with caspofungin an identical spectrum of in vitro activity against Candida albicans, non-albicans Candida species, and Aspergillus. Due to the limited oral availability, micafungin is available for parenteral administration only. Micafungin is characterized by a linear pharmacokinetic profile and substantially fewer toxic effects. Micafungin is a poor substrate for the cytochrome P450 enzymes, and compared to azoles, fewer drug interactions have been described. No dose reduction is required in renal impairment or in mild to moderate liver failure.

CONCLUSIONS

The pharmacodynamic and pharmacokinetic profiles of micafungin imply that this drug is a safe alternative for the treatment of fungal infections. Micafungin can be safely co-administered with most drugs without the need for dosage adaptation even in patients with renal o liver function impairment.

摘要

背景

侵袭性真菌感染是免疫功能低下患者发病和死亡的重要原因。尽管在过去几年中已研发出几种新型抗真菌药物,但严重真菌感染的治疗仍然存在问题。

目的

综述新型抗真菌药物米卡芬净的药效学和药代动力学。

方法

对生物医学数据库(EBSCO开放期刊、Ovid在线、Proquest医学图书馆、PubMed/Medline、科学Direct、Springer Links和Wiley Interscience)进行了系统综述。检索时间为2000年至2008年。补充资料包括1998年至2008年抗菌药物跨学科会议(ICAAC)、化疗会议及美国传染病学会(IDSA)的摘要。

结果

米卡芬净具有强大的作用机制:抑制β-1,3-D-葡聚糖合酶,干扰真菌细胞壁合成。该药物与卡泊芬净对白色念珠菌、非白色念珠菌及曲霉菌具有相同的体外活性谱。由于口服生物利用度有限,米卡芬净仅可用于胃肠外给药。米卡芬净具有线性药代动力学特征,毒性作用明显较少。米卡芬净是细胞色素P450酶的不良底物,与唑类药物相比,药物相互作用较少。肾功能损害或轻度至中度肝功能衰竭患者无需减量。

结论

米卡芬净的药效学和药代动力学特征表明,该药物是治疗真菌感染的安全选择。即使在肾功能或肝功能损害患者中,米卡芬净也可与大多数药物安全联用,无需调整剂量。

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