Efavirenz + Rosiglitazone = Precautionary

Effect on Concentration

Efavirenz
No change
Applies within class?
No
Rosiglitazone
No change
Applies within class?
No

Pharmacologic Effects

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

Interaction History

N/A

Last Updated 25-Jun-2018

Summary

Due to limited sample size, caution is required when interpreting the results

Sources

Efavirenz vs Rosiglitazone ^

Study Design

Eighteen HIV-infected patients receiving ARV were treated with 4 mg of Rosiglitazone for lipodystrophy syndrome.

Study Results

TDM of the NNRTI’s and PI’s revealed no significant decreases in the Cmax, Cmin, and AUC of efavirenz (n=10) and lopinavir (n=4). The mean Cmax of nevirapine (n=4) was reduced significantly and there was a trend towards a lower AUC and Cmin which not did not reach significance. The Cmin of nevirapine was found to be < 3400 ng/mL on day 1 in two cases and in all cases on day 28.

Study Conclusions

Delavirdine is an inhibitor of CYP3A, and as such it is not expected that rosiglitazone and delavirdine will have clinically significant drug interactions. Rosiglitazone is predominately metabolized by CYP 2C8 and to a lesser extent 2C9; in vitro studies have found that Rosiglitazone does not inhibit the CYP450 enzymes at any significant concentrations. Due to the limited size of the studied population, this data must be viewed with caution and requires confirmation by larger trials before being incorporated into clinical practice.

References

Oette M. Impact of rosiglitazone treatment on the bioavailability of antiretroviral compounds in hiv-positive patients. Journal Of Antimicrobials And Chemotherapy. 2005; : 416-419.