Interactions between antifungal medications and antiretroviral therapy

Authors: Koks CH, Crommentuyn KM, Hoetelmans RM, et al.

Title: The effect of fluconazole on ritonavir and saquinavir pharmacokinetics in HIV-1-infected individuals.

Source: British Journal of Clinical Pharmacology. 51(6):631-5, 2001 Jun.

Summary of Abstract Info: Five subjects treated with saquinavir (1200 mg TID) and three with ritonavir (600 mg BID), were first given the protease inhibitor alone on day one, then in combination with fluconazole on days 2 thru 8 (400 mg on day 2, 200 mg on days 3 thru 8). Pharmacokinetic parameters were evaluated on days 1 thru 8 for both drugs. No detectable PK changes were found in the ritonavir group upon addition of fluconazole. The saquinavir group demonstrated a median increase of 50% in area under the plasma concentration vs. time curve and 56% increase in peak plasma concentration. It was concluded that dose adjustments are probably not necessary with either protease inhibitor when fluconazole is added due to the favorable safety profile of saquinavir and the lack of effect on ritonavir. However, ritonavir induces its own metabolism so a longer trial with more than 3 subjects is needed to draw a more definitive conclusion concerning the combination of fluconazole and ritonavir.

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