Pitavastatin and Darunavir/Ritonavir
October 5, 2012
Coauthor: Susa Coffey, MD; Medical Editor, AETC National Resource Center
Treatment of dyslipidemia is often complicated by drug interactions between statins and antiretrovirals. Pitavastatin is one of the newer statins approved and is one of the few that is not metabolized primarily by the CYP450 3A4 pathway. It is predominantly metabolized via glucuronidation and so, theoretically, is less likely to interact with NNRTIs or PIs.
A recent pharmacokinetic study examined interactions between pitavastatin and ritonavir-boosted darunavir. Twenty-eight HIV-uninfected subjects were given pitavastatin (4 mg daily) for 5 days, then darunavir/ritonavir (800 mg/100 mg daily) alone for 5 days, then both the statin and the PI for 5 days. Intensive pharmacokinetic sampling was conducted on day 5, day 11, and day 16.
When the medications were given together, the darunavir and ritonavir geometric mean AUC and Cmax did not change, but the pitavastatin mean AUC decreased 26%.
Clinical Bottom Line
These study findings are reassuring in that there is no increase in pitavastatin levels, nor are there adverse changes in darunavir or ritonavir concentrations. In fact, pitavastatin exposure appears to be decreased by darunavir/ritonavir; this can be clinically managed by titrating the pitavastatin dosage to the patient's LDL goal.
- Yu CY, Campbell SE, Sponseller CA, et al. Steady-state pharmacokinetic interactions of darunavir/ritonavir with pitavastatin in healthy adult volunteers. In: Program and abstracts of the XIX International AIDS Conference; July 22-27, 2012; Washington, DC. Abstract TUPE053.
Dr. McNicholl's primary focus is maintaining a clinical practice at the UCSF Positive Health Practice at San Francisco General Hospital where the clinic provides comprehensive healthcare for approximately 3,000 HIV positive patients. Other major responsibilities include managing a pharmacist staffed Adherence Support Program and serving as Editor, UCSF Center for HIV Information, Database of Antiretroviral Drug Interactions. He has published and presented on lectures, Continuing Education programs and research findings on Infectious Diseases and Primary Care issues from the local level on up.