在onychomycoses抗真菌药物药物动力学。

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Debruyne D, Coquerel

在onychomycoses抗真菌药物药物动力学。

40 Pharmacokinet。2001; (6): 441 - 72。

PubMed ID

11475469 (在PubMed

]

文摘

甲真菌病是由真菌引起的感染,主要是真菌和nondermatophyte酵母或模具;更频繁,影响指甲和脚趾甲。真菌负责约90真菌感染的95%。毛癣菌属石是最常见的皮肤真菌;白色念珠菌是主要nondermatophyte酵母。虽然onchomycosis局部治疗不会导致系统性不良反应或相互作用与此同时采取药物,它不提供高治愈率和要求完全合规的病人。目前有3口服抗真菌药物,通常用于短期治疗甲真菌病:伊曲康唑,terbinafine和氟康唑。这些活性药物的持久性指甲允许每周管理,减少治疗或脉冲疗法。良好的临床和真菌学的功效得到了伊曲康唑100到200毫克每日,terbinafine 250毫克每日3个月,或氟康唑150毫克每周至少6个月。伊曲康唑是合成三唑与广泛的行动。 It is well absorbed when administered orally and can be detected in nails 1 to 2 weeks after the start of therapy. The nail : plasma ratio stabilises at around 1 by week 18 of treatment. Itraconazole is still detectable in nails 27 weeks after stopping administration. Nail concentrations are higher than the minimum inhibitory concentration (MIC) for most dermatophytes and Candida species from the first month of treatment. The elimination half-life of itraconazole from nails is long, ranging from 32 to 147 days. Terbinafine is a synthetic allylamine that is effective against dermatophytes. Terbinafine is well absorbed from the gastrointestinal tract, and the time to reach effective concentrations in nail is 1 to 2 weeks. The half-life is from 24 to 156 days, explaining the observed persistence of terbinafine in nails for longer than 252 days. Fluconazole is a bis-triazole broad spectrum antifungal with high oral bioavailability. The uptake of fluconazole by nail increases with the length of treatment, and nail : plasma ratios are generally 1.5 to 2 at steady state. Fluconazole concentrations exceed the MIC for Candida species soon after the start of treatment. Fluconazole concentrations fall slowly after the drug is stopped, with a half-life of 50 to 87 days, and fluconazole is still detectable in nails 5 months after the end of treatment. All these drugs are potent inhibitors of cytochrome P450 (CYP) enzymes and may increase the plasma concentrations of concomitantly used drugs. Itraconazole inhibits CYP3A4. Fluconazole inhibits CYP3A4, but to a lesser degree than itraconazole, CYP2C9 and CYP2C19. Terbinafine inhibits CYP2D6.

DrugBank数据引用了这篇文章

药物酶

药物	酶	类	生物	药理作用	行动
氟康唑	细胞色素P450 2 c9	蛋白质	人类	未知的	抑制剂	细节
Terbinafine	细胞色素P450 2 d6	蛋白质	人类	未知的	抑制剂	细节