Dihydroartemisinin + Efavirenz = Precautionary

Effect on Concentration

Applies within class?
No
Efavirenz
Unknown
Applies within class?
No

Pharmacologic Effects

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

Interaction History

N/A

Last Updated 22-Nov-2022

Summary

The authors state that PQ is expected to be the more important component of the two when used for prevention of malaria. Therefore, the clinical impact of these PK changes in the context of EFV-based ART (and pregnancy) needs to be determined before dosing recommendations can be made.Consider alternative agents for malaria chemoprevention. If co-administration of these agents is necessary, dose modification of dihydroartemisinin and/or PQ may be warranted; use caution and monitor patients closely.

Sources

Study Design

This was a randomized, double-blind, placebo-controlled study to evaluate the impact of efavirenz (EFV)-based antiretroviral therapy (ART) on the pharmacokinetics (PK) of piperaquine (PQ) in HIV-infected pregnant women (n=52), compared to HIV-negative pregnant women (n=40) not on ART. PQ was adminstered as 3 standard doses, monthly or bi-monthly, in addition to dihydroartemisinin.

Study Results

A reduction in dihydroartemisinin exposures was observed among women on EFV-based ART.Using geometric mean ratios and 95% confidence intervals, PK parameters fordihydroartemisininresulted in a 27% and 34% decrease in AUC and Cmax, respectively, in those treated with EFV versus those who were not.In addition, modest reductions were observed in the PK parameters of PQ; AUC and Cmax were 40% and 12% lower, respectively, in those treated with EFV versus those who were not.The effect of dihydroartemisinin and PQ on the PK of EFV, as well as the impact of pregnancy on the PK of all agents was not reported.

Study Conclusions

References

R Kajubi, L Huang, N Mwebaza, et al. Efv reduced pk of piperaquine for malaria prevention in hiv ugandan pregnant women. Conference On Retroviruses And Opportunistic Infections. Boston, MA. ; 2016.