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Drug-drug interaction of antifungal drugs.

机译：抗真菌药物的药物相互作用。

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This article reviews the in vitro metabolic and the in vivo pharmacokinetic drug-drug interactions with antifungal drugs, including fluconazole, itraconazole, micafungin, miconazole, and voriconazole. In the in vitro interaction studies, the effects of antifungal drugs on specific activities of cytochrome P450s (CYPs), including CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4, in human liver microsomes are compared to predict the possibility of drug interactions in vivo. Fluconazole, micafungin, and voriconazole have lower inhibitory effects on CYP3A4 activities than itraconazole and miconazole, and IC(50) and/or K(i) values against CYP2C9 and CYP2C19 activities are the lowest for miconazole, followed by voriconazole and fluconazole. In in vivo pharmacokinetic studies, it is well known that itraconazole is a potent clinically important inhibitor of the clearance of CYP3A4 substrates, and fluconazole and voriconazole are reported to increase the blood or plasma concentrations of not only midazolam and cyclosporine (CYP3A4 substrates) but also of phenytoin (CYP2C9 substrate) and/or omeprazole (CYP2C19/CYP3A4 substrate). On the other hand, no inhibition of CYP activities except for CYP3A4 activity by micafungin is observed in vitro, and the blood concentrations of cyclosporine and tacrolimus are not affected by coadministration of micafungin in vivo, suggesting that micafungin would not cause clinically significant interactions with drugs that are metabolized by CYPs via the inhibition of metabolism. Miconazole is a potent inhibitor of all CYPs investigated in vitro, although there are few detailed studies on the clinical significance of this except for CYP2C9. Therefore the differential effects of these antifungal drugs on CYP activities must be considered in the choice of antifungal drugs in patients receiving other drugs.
机译：本文回顾了与抗真菌药（包括氟康唑，伊曲康唑，米卡芬净，咪康唑和伏立康唑）的体外代谢和体内药代动力学药物相互作用。在体外相互作用研究中，比较了抗真菌药对人肝微粒体中细胞色素P450（CYPs）包括CYP1A2，CYP2C9，CYP2C19，CYP2D6，CYP2E1和CYP3A4特定活性的影响，以预测药物相互作用的可能性。体内。与伊曲康唑和咪康唑相比，氟康唑，米卡芬净和伏立康唑对CYP3A4活性的抑制作用更低，并且对CYP2C9和CYP2C19活性的IC（50）和/或K（i）值对米康唑最低，其次是伏立康唑和氟康唑。在体内药代动力学研究中，众所周知伊曲康唑是一种有效的临床上重要的CYP3A4底物清除抑制剂，据报道氟康唑和伏立康唑不仅会增加咪达唑仑和环孢霉素（CYP3A4底物）的血药浓度，而且还会增加血浆或血浆中的血浆浓度。苯妥英钠（CYP2C9底物）和/或奥美拉唑（CYP2C19 / CYP3A4底物）。另一方面，在体外未观察到米卡芬净对CYP活性有抑制作用（除CYP3A4活性外），并且在体内并用米卡芬净对环孢霉素和他克莫司的血药浓度没有影响，这表明米卡芬净不会与药物产生临床上显着的相互作用通过CYPs通过代谢的抑制而代谢。咪康唑是体外研究的所有CYP的有效抑制剂，尽管除CYP2C9外，很少有关于其临床意义的详细研究。因此，在接受其他药物的患者选择抗真菌药物时，必须考虑这些抗真菌药物对CYP活性的不同作用。

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