泊沙康唑:extended-spectrum三唑抗真菌剂。

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席勒DS, Fung HB

泊沙康唑:extended-spectrum三唑抗真菌剂。

其他。2007年9月,29 (9):1862 - 86。

PubMed ID

18035188 (在PubMed

]

文摘

背景:侵袭性真菌感染的发病率(金融机构)引起的投机取巧的丝状模具越来越多,随着新兴的真菌耐药性。泊沙康唑、伊曲康唑的结构类似物被批准用于市场营销在美国,2006年似乎是一个有前途的抗真菌剂。目的:本文概述药理学,泊沙康唑疗效和耐受性,用于预防和治疗各种常见和罕见的真菌感染。方法:通过搜索相关信息被确认的MEDLINE(1966 - 2007年4月),国际制药抽象(1970 - 2007年4月),和抽象的抗菌药物和化疗使用跨学科会议上公布56592年泊沙康唑和原理图。额外的资源被发现通过搜索发现文章的引用列表和美国食品和药物管理局网站。结果:泊沙康唑可作为口腔悬挂。是高度分布的各种网站,包括骨,中枢神经系统,和眼睛组织。其Vd 2447 L在多个管理每日剂量(800毫克/天)在存在高脂肪餐。因为它主要改变药物的排泄粪便(77%),泊沙康唑可以为贫困患者肾功能没有任何剂量调整。泊沙康唑在体外和体内活动对多种真菌,包括那些是罕见的和相对耐药。 Two clinical trials have compared posaconazole with fluconazole or itraconazole for the prophylaxis of IFIs in immunocompromised patients. The first, a randomized, double-blind trial in 600 recipients of hematopoietic stem cell transplants, found that overall rates of IFI did not differ significantly between posaconazole and fluconazole (5% vs 9%, respectively). The other, a randomized, open-label trial in 602 neutropenic patients, reported significantly fewer IFIs in patients receiving posaconazole compared with those receiving fluconazole or itraconazole (>2% vs >8%, respectively; P = 0.001). An additional 2 trials have investigated posaconazole for the treatment of oropharyngeal candidiasis (OPC) in patients with HIV infection. A randomized, controlled, evaluator-blinded study in 350 HIV-infected patients with OPC found similar 14-day clinical success rates with posaconazole and fluconazole (91.7% and 92.5%, respectively; 95% CI, -6.6l to 5.04), whereas an open-label study in 176 HIV-infected patients with a history of refractory OPC reported a 28-day clinical success rate of 75%. Numerous small studies and case reports have described successful posaconazole treatment of zygomycosis, aspergillosis, fusariosis, endemic dimorphic fungal infection, and superficial and subcutaneous fungal infections that were refractory to conventional antifungal agents or in patients who were unable to tolerate these agents. Posaconazole has been well tolerated. The most common complaints have been gastrointestinal in nature, including nausea (7%-8%) and diarrhea (3%-11%), although these have rarely led to permanent discontinuation of therapy. Other common adverse effects have included vomiting (4%-7%), headache (2%-8%), and liver enzyme elevations (2%-3%). CONCLUSIONS: Posaconazole suspension administered at up to 800 mg/d is a reasonable alternative to conventional antifungal agents for the prevention and treatment of IFIs in high-risk populations. It may also be suitable in patients with infections caused by rare or relatively resistant fungi, and those who are unable to tolerate long-term therapy with other antifungal agents.

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药物

泊沙康唑

药物靶点

药物	目标	类	生物	药理作用	行动
泊沙康唑	细胞色素P450 51	蛋白质	酵母	是的	拮抗剂	细节