Etravirine + Fluconazole = Unknown or no reaction

Effect on Concentration

Etravirine
No change
Applies within class?
No
Fluconazole
No change
Applies within class?
No

Pharmacologic Effects

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

Interaction History

N/A

Last Updated 30-Jul-2018

Summary

Sources

Etravirine versus Fluconazole or Voriconazole ^

Study Design

Pharmacokinetic interactions and safety of etravirine 200 mg twice daily coadministered with fluconazole 200 mg daily or voriconazole 200 mg twice daily, both inhibitors of CYP3A4, CYP2C9, and CYP2C19, were evaluated in an open‐label, randomized, 3‐period crossover trial in 18 HIV‐negative volunteers.

Study Results

Based on least squares means (LSM) ratios, coadministration of etravirine with fluconazole or voriconazole resulted in higher etravirine exposures (area under plasma concentration‐time curve from 0‐12 hours [AUC12 h] 1.86‐ and 1.36‐fold, respectively). Fluconazole pharmacokinetics were unchanged with etravirine coadministration (AUC12 h LSM ratio: 0.94), and voriconazole plasma concentrations were slightly raised (AUC12 h LSM ratio: 1.14). All treatments and combinations were well tolerated, with no grade 3 or 4 adverse events observed during treatment.

Study Conclusions

Pharmacokinetic interactions between etravirine and fluconazole or voriconazole are not expected to be clinically relevant; no dose adjustments are required during coadministration.

References

Kakuda TN, Solingen-Ristea V, Aharchi F, Smedt GD, Witek J, Nijs S, Hoetelmans RM. Pharmacokinetics and short‐term safety of etravirine in combination with fluconazole or voriconazole in hiv‐negative volunteers. The Journal Of Clinical Pharmacology. 2013; 1: 41-50.