Efavirenz + Pitavastatin = Precautionary

Effect on Concentration

Efavirenz
Unknown
Applies within class?
No
Pitavastatin
No change
Applies within class?
No

Pharmacologic Effects

Efavirenz
Effect
N/A
Applies within class?
No
Pitavastatin
Effect
N/A
Applies within class?
No

Interaction History

N/A

Last Updated 22-Nov-2022

Summary

Sources

Pitavastatin vs efavirenz ^

Study Design

The drug-drug interactions between pitavastatin and efavirenz (EFV) were examined in an open-label, parallel-arm, pharmacokinetic (PK) study in HIV-uninfected healthy volunteers. Subjects received a pitavastatin dose of 2 mg for 4 days, followed by either EFV 600 mg (n = 14) or DRV/r 800/100 mg (n = 14) daily for 10 days, and pitavastatin 2 mg coadministered with EFV 600 mg or DRV/r 800/100 mg for 4 days. Full PK profiles were determined for pitavastatin and its lactone metabolite on days 4 and 18 and for EFV or DRV on days 14 and 18.

Study Results

AUC 0-tCmax Geometric Mean Ratio (90% CI)0.89 (0.73-1.09)1.20 (0.79-1.83)Based on the results shown, there were no significant PK interactions between pitavastatin and EFV, however, the upper bounds of the 90% CI for the change in Cmax, warrents caution and monitoring for "statin" adverse events. There were no significant saftey issues or lipid changes noted in the study.The effect on EFV was not noted.

Study Conclusions

References

Carlos D Malvestutto, Qing Ma, Gene D Morse, James A Underberg, Judith A Aberg. Lack of pharmacokinetic interactions between pitavastatin and efavirenz or darunavir/ritonavir. Journal Of Acquired Immune Deficiency Syndromes. 1999; 4: 390.