伊曲康唑影响的药代动力学相互作用研究进展

Progress and research in the effect of itraconazole on pharmacokinetic drug-drug interactions

伊曲康唑为三唑类广谱抗真菌药,临床应用广泛,具有CYP3A4和P-糖蛋白抑制作用。由于临床CYP3A4和P-糖蛋白底物广泛,它们在口服药物吸收的主要部位胃肠道均有高表达,同时两者的底物具有显著的重叠性,由此导致的受伊曲康唑影响的药代动力学相互作用广泛产生,甚至引起显著的临床意义。本文综述并讨论了受其影响的药代动力学相互作用研究,以促进临床的安全用药。

Itraconazole,as one of the broad-spectrum antifungal drugs,is an inhibitor of CYP3A4 and P-glycoprotein and was widely used in clinic.CYP3A4 and P-glycoprotein with extensive substrate have present at high levels in gastrointestinal tract,the primary site of absorption for orally administrated drugs,and share a significant overlap in substrate specificity,thus resulting in widely pharmacokinetic interaction by itraconazole,part of which has clinical importance.In this article,the effect of itraconazole on pharmacokinetic drug-drug interactions is reviewed and discussed in order to promote its safe usage.