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Effects of voriconazole on tacrolimus metabolism in a kidney transplant recipient
肾移植患者应用伏立康唑对他克莫司代谢的影响

出处: Journal of Clinical Pharmacy and Therapeutics   2010      35 (1) :121-124

作者:D. CaponeG. TarantinoA. GentileM. SabbatiniG. PolichettiM. SantangeloR. NappiA. CiotolaV. D'AlessandroA. RendaV. BasileS. Federico

Infection occurs frequently in the organ transplant recipients during the post-transplant period because of immunosuppression. Therefore, prophylactic antimicrobial agents are often used. The azole antifungals, widely prescribed prophylactically, are known to have many drug2013drug interactions. This report presents a case of drug2013drug interaction between voriconazole and tacrolimus in a kidney transplant recipient. Voriconazole treatment led to a dramatic increase in tacrolimus concentration that required its discontinuation in spite of the manufacturer's guidelines that recommend a reduction of tacrolimus dosage by one-third. The present drug2013drug interaction can be attributed to a strong inhibitory effect on cytochrome P450-3A4 activity by voriconazole. When voriconazole and tacrolimus are coadministered, close monitoring of tacrolimus blood levels is recommended as the rule-of-thumb reduction of tacrolimus dose by one-third may not be satisfactory.

由于免疫抑制剂的应用,接受器官移植的患者常在移植后期出现感染。因此,常常会预防性使用抗菌制剂。处方中经常使用的三唑类抗真菌制剂已知有许多药物相互作用。本病例报告了一例肾移植患者伏立康唑与他克莫司之间的相互作用。伏立康唑的使用导致了他克莫司浓度的显著增加,尽管药物说明中推荐将他克莫司的浓度减少1/3即可,但该病例最终还是需要停止使用他克莫司。究其原因,是因为伏立康唑对细胞色素P450-3A4活性有强大的抑制作用。因此,当同时服用伏立康唑和他克莫司时,应对他克莫司的血药浓度进行密切监测,因为根据经验将他克莫司的浓度减少1/3也不一定令人满意。