Nevirapine + Amodiaquine = Precautionary

Effect on Concentration

Nevirapine
No change
Applies within class?
No
Amodiaquine
Decrease
Applies within class?
No

Pharmacologic Effects

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

Interaction History

N/A

Last Updated 17-Jul-2018

Summary

Sources

Nevirapine versus Amodiaquine ^

Study Design

In an open-label, parallel-group study, 10 HIV-infected patients on steady-state antiretroviral (ARV) therapy with nevirapine (NVP) 200 mg twice daily (BID) (ART group) and 11 HIV-infected ART-naïve patients (control group) received artesunate/amodiaquine (AS/AQ) 200/600 mg for 3 days (Days 1-3). Blood samples for amodiaquine (AQ) and desethylamodiaquine (DEAQ; active metabolite of AQ) were obtained pre-dose on Day 3 and up to 96 hours post-dose.

Study Results

Exposures to both amodiaquine and DEAQ were significantly lower in the nevirapine-based ART group compared with the control group (amodiaquine AUC0–24 145 versus 204 ng·h/mL, P = 0.02; DEAQ AUC0–96 14 571 versus 21 648 ng·h/mL, P < 0.01). The AUCDEAQ/AUCamodiaquine ratio was not different between groups (ART group 116 versus control group 102, P = 0.67).

Study Conclusions

Subjects on nevirapine-based ART had lower exposure to both amodiaquine and DEAQ (28.9% and 32.7%, respectively). Consequently, this may negatively impact the effectiveness of artesunate/amodiaquine in HIV-infected individuals on this ART combination.

References

Scarsi KK, Fehintola FA, Ma Q, Aweeka FT, Darin KM, Morse GD, Ojengbede O. Disposition of amodiaquine and desethylamodiaquine in hiv-infected nigerian subjects on nevirapine-containing antiretroviral therapy. Antimicrobial Agents And Chemotherapy . 2014; 5: 1370-1376.