Pitavastatin and Darunavir/Ritonavir

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.

References

  • 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.
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