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Itraconazole是一种新的三唑类抗真菌药,有广谱作用。其作用机制与其他唑类抗真菌剂相似,对真菌细胞色素P450有选择性抑制作用而导致损害真菌细胞膜中的类固醇合成。在研究中,用相似的化合物酮康唑治疗病人,已报道对肝脏有毒性作用。为了解Itraconazole对细胞色素P450的影响,作者通过动物试验观察:1.对苯妥因抗戊四氮作用的影响:已知苯妥因可明显地(P<0.001)减低戊四氮在鼠身上的致惊厥作用。给予单剂量5或10mg/kg的Itraconazole不改变苯妥因的抗惊厥作用,Itraconazole本身亦无任何抗惊厥作用。而氨基导眠能-苯巴比妥样肝混合功能氧化酶诱导剂能明显降低苯妥
Itraconazole is a new triazole antifungal agent with broad spectrum effects. Its mechanism of action and other azole antifungal agents similar to the fungal cytochrome P450 selective inhibition caused damage to fungal cell membrane steroid synthesis. In the study, a similar compound, ketoconazole, was used to treat patients and toxic effects on the liver have been reported. To understand the effect of Itraconazole on cytochrome P450, the authors observed by animal experiments: 1. Effect of phenytoin on pentylenetetrazole: Phenytoin is known to significantly (P <0.001) reduce pentylenetetrazol in mice Convulsive effect. Itraconazole given a single dose of 5 or 10 mg / kg did not alter the anticonvulsant effect of phenytoin and itraconazole itself had no anticonvulsant effect. However, amylamine-phenobarbital-like hepatic mixed-function oxidase inducer can significantly reduce phenytoin