Faculty of Medicine, Imperial College London, London, UK.
Expert Opin Drug Metab Toxicol. 2013 Jul;9(7):911-26. doi: 10.1517/17425255.2013.794785. Epub 2013 May 6.
Fungal infections are a major source of global morbidity and mortality. Itraconazole is a triazole antifungal agent that is widely used for the prevention and treatment of fungal infection. While newer antifungal agents are now available, itraconazole is an orally bioavailable agent with broad-spectrum antifungal activity. Itraconazole remains a useful drug for the management of allergic and invasive mycoses worldwide.
This article provides a summary of the pharmacokinetics, pharmacodynamics and clinical uses of itraconazole. Additionally, the authors summarise the safety and recently described toxicodynamics and discuss the value of therapeutic drug monitoring (TDM) with itraconazole. The following search criteria were constructed in order to identify relevant literature using PubMed and Ovid-MEDLINE: itraconazole, triazole, pharmacokinetics, pharmacodynamics, toxicodynamics and TDM. Relevant abstracts and articles identified from reviewing secondary citations were additionally retrieved and included if relevant.
Itraconazole remains an important agent in the prevention and treatment of fungal infection. Itraconazole has a broad-spectrum of activity and is available in both an intravenous and oral form making long-term use in chronic mycoses practical. Itraconazole is widely used for the treatment of endemic fungal infections. Pharmacokinetic variability and clinically important drug interactions make TDM of itraconazole an important consideration.
真菌感染是全球发病率和死亡率的主要原因。伊曲康唑是一种三唑类抗真菌药物,广泛用于预防和治疗真菌感染。虽然现在有更新的抗真菌药物,但伊曲康唑是一种口服生物利用度广泛的抗真菌药物,具有广谱抗真菌活性。伊曲康唑仍然是全球管理过敏和侵袭性真菌感染的有用药物。
本文总结了伊曲康唑的药代动力学、药效学和临床用途。此外,作者总结了其安全性和最近描述的毒代动力学,并讨论了伊曲康唑治疗药物监测(TDM)的价值。为了使用 PubMed 和 Ovid-MEDLINE 识别相关文献,构建了以下搜索标准:伊曲康唑、三唑、药代动力学、药效学、毒代动力学和 TDM。从审查二次引用中识别出的相关摘要和文章也被检索并收录在内。
伊曲康唑仍然是预防和治疗真菌感染的重要药物。伊曲康唑具有广谱活性,有静脉内和口服两种剂型,可用于长期慢性真菌感染。伊曲康唑广泛用于治疗地方性真菌感染。药代动力学变异性和临床上重要的药物相互作用使伊曲康唑的 TDM 成为一个重要的考虑因素。