Interaction Checker
Potential Interaction
Lopinavir/ritonavir (LPV/r)
Itraconazole
Quality of Evidence: Very Low
Summary:
Coadministration has not been studied. Itraconazole is metabolized by CYP3A4 and is a strong inhibitor of CYP3A4. Coadministration may increase concentrations of itraconazole and lopinavir/ritonavir. High doses of itraconazole (greater than 200 mg/day) are not recommended. Note, both drugs have risks of QT prolongation and/or TdP on the CredibleMeds.org website (possible risk for lopinavir; conditional risk for itraconazole).
Description:
Ketoconazole and itraconazole may have serum concentrations increased due to CYP3A inhibition by Kaletra. High doses of ketoconazole and itraconazole (greater than 200 mg/day) are not recommended.
Kaletra Summary of Product Characteristics, AbbVie Ltd, January 2021.
Coadministration of Kaletra and itraconazole may result in increased concentrations of itraconazole. High doses of itraconazole (greater than 200 mg/day) are not recommended.
Kaletra Prescribing Information, AbbVie Ltd, October 2020.
The interaction between itraconazole and Kaletra was described in an HIV+ patient treated for disseminated histoplasmosis. Itraconazole (200 mg twice daily) was administered for 10 days prior to the addition of Kaletra (400/100 mg twice daily); the dose of itraconazole was reduced to 200 mg once daily when Kaletra was commenced. Coadministration of itraconazole and Kaletra resulted in a strong increase in itraconazole concentrations and a decrease in hydroxyitraconazole (an equally pharmacologically active metabolite). Immediately after starting Kaletra, itraconazole concentrations remained similar to pre-Kaletra levels (Cmax ~750 ng/ml), despite the dose reduction. After 5 weeks of treatment, itraconazole Cmax was >2000 ng/ml and half life had increased from 16 h to >160 h. Lopinavir Cmin and Cmax values were 3.4 and 8.5 mg/L respectively, and were comparable to those obtained in HIV+ adults not receiving itraconazole. If long term maintenance treatment of disseminated histoplasmosis with itraconazole (200 mg once daily) and Kaletra (400/100 mg twice daily) is required, close monitoring of the treatment and plasma concentration is important, especially if dosages or concomitant drugs are altered.
Drug-drug interaction between itraconazole and the antiretroviral drug lopinavir/ritonavir in an HIV-1-infected patient with disseminated histoplasmosis. Crommentuyn KML, Mulder JW, Sparidans RW, et al. Clin Infect Dis, 2004, 38: e73-e75.
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