Interaction Checker
Potential Interaction
Lopinavir/ritonavir (LPV/r)
Albendazole
Quality of Evidence: Very Low
Summary:
Coadministration has not been studied. In vitro studies have demonstrated that CYP3A4 and the flavine-containing monooxygenase system are involved in formation of the active metabolite albendazole sulfoxide. Short term (2 doses) coadministration with ritonavir (200 mg) did not impact albendazole pharmacokinetics whereas long-term coadministration (8 days) decreased albendazole exposure likely due to ritonavir inducing effect. Lopinavir/ritonavir is unlikely to significantly affect albendazole exposure when used for a short duration treatment but may reduce the clinical effect of albendazole when used for a long duration treatment.
Description:
In a sequential pharmacokinetic study, healthy male volunteers (n=8) were administered a single oral dose of 400 mg albendazole, in absence and after short-term (2 doses) and long-term (8 days) treatment with ritonavir 200 mg twice daily. Pharmacokinetic parameters of albendazole and its metabolite albendazole sulfoxide, were not changed by short-term administration of ritonavir. However long-term administration resulted in significant changes in albendazole disposition, with a significant decrease in albendazole and albendazole sulfoxide AUC0-24 (73% and 59% respectively) and Cmax (74% and 48% respectively). Tmax and the terminal half-life were not significantly changed. The observation is most likely due to a ritonavir-mediated induction of metabolising enzymes (CYP2C9, CYP1A2, UGTs) or transporters, although changes in absorption are also possible. These findings need to be replicated with a key boosted PI such as lopinavir/ritonavir.
Effect of ritonavir on the pharmacokinetics of the benzimidazoles albendazole and mebendazole: an interaction study in healthy volunteers. Corti N, Heck A, Rentsch K, et al.Eur J Clin Pharmacol. 2009;65:999-1006.
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