Voriconazole: A new triazole antifungal agent
Voriconazole: A new triazole antifungal agent
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DOI：
10.1345/aph.1c261
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发表时间：
2003-03-01
影响因子：
2.9
通讯作者：
Chapman, SW
中科院分区：
文献类型：
--
作者：
Pearson, MM;Rogers, D;Chapman, SW
目的：综述三唑类抗真菌药物伏立康唑的药理学、体外药敏、药动学、临床疗效及不良反应。资料来源：从1990年到2002年6月进行MEDLINE检索，仅限于英语语言。补充资料来源包括1996年至2001年抗菌剂和化疗科学会议和美国传染病学会的项目摘要，以及食品和药物管理局网站上提供的制造商信息。资料提取：选取所有引用伏立康唑的已发表和未发表的试验和摘要。资料综合：伏立康唑已显示出对许多酵母菌和多种霉菌和皮肤真菌分离物的体外活性。伏立康唑可口服或静脉注射。它具有良好的口服生物利用度，广泛的组织分布，包括分布到中枢神经系统和肝脏代谢。药物相互作用通过抑制CYP2C9、CYP2C19和CYP3A4同工酶发生，导致伏立康唑或相互作用剂的动力学参数改变。在免疫功能低下患者的曲霉病的公开、非比较性研究中，疗效已得到证实。人类病例报告描述了罕见真菌病原体的成功治疗。最常见的不良事件包括视力障碍和肝功能检查升高。结论：伏立康唑治疗免疫功能低下患者急性侵袭性曲霉病的疗效至少与两性霉素B相同。与氟康唑治疗食道念珠菌病疗效相近。伏立康唑在中性粒细胞减少症和持续性发热患者的经经性治疗中没有达到与两性霉素B脂体的统计非劣性，在进一步的试验完成之前，这降低了对该适应症的使用热情。根据病例报告和体外疗效，伏立康唑可能被证明是治疗其他真菌疾病的临床有用药物。
OBJECTIVE: To review the pharmacology, in vitro susceptibility, pharmacokinetics, clinical efficacy, and adverse effects of voriconazole, a triazole antifungal agent.DATA SOURCES: A MEDLINE search, restricted to English language, was conducted from 1990 to June 2002. Supplementary sources included program abstracts from the Interscience Conference on Antimicrobial Agents and Chemotherapy and the Infectious Diseases Society of America from 1996 to 2001 and manufacturer information available through the Food and Drug Administration's Web site.DATA EXTRACTION: All published and unpublished trials and abstracts citing voriconazole were selected.DATA SYNTHESIS: Voriconazole has shown in vitro activity against many yeasts and a variety of mold and dermatophyte isolates. Voriconazole can be administered either orally or parenterally. It exhibits good oral bioavailability, wide tissue distribution including distribution into the central nervous system, and hepatic metabolism. Drug interactions occur through inhibition of the CYP2C9, CYP2C19, and CYP3A4 isoenzymes, resulting in alterations in kinetic parameters of either voriconazole or the interacting agent. Efficacy has been illustrated in open, noncomparative studies of aspergillosis in immunocompromised patients. Human case reports describe successful treatment of rare fungal pathogens. The most commonly reported adverse events include visual disturbances and elevations in liver function tests.CONCLUSIONS: Voriconazole is at least as effective as amphotericin B in the treatment of acute invasive aspergillosis in immunocompromised patients. It has similar efficacy as fluconazole in treatment of esophageal candidiasis. Voriconazole did not achieve statistical non-inferiority to liposomal amphotericin B for empirical therapy in patients with neutropenia and persistent fever, diminishing enthusiasm for use in this indication until additional trials are completed. Based on case reports and in vitro efficacy, voriconazole may prove to be a clinically useful agent in the treatment of other fungal disease.