Raltegravir + Omeprazole = Unknown or no reaction

Effect on Concentration

Raltegravir
Increase
Applies within class?
No
Omeprazole
No change
Applies within class?
No

Pharmacologic Effects

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

Interaction History

N/A

Last Updated 26-Jun-2018

Summary

Sources

Effects of omeprazole on plasma levels of raltegravir. ^

Study Design

A single-blind, randomized, 2-period crossover trial evaluated the effect of omeprazole on raltegravir (RAL) concentrations. Treatment A consisted of placebo or RAL 400mg once daily for 4 days, then RAL 400mg on day 5; Treatment B consisted of placebo or RAL 400mg plus omeprazole 20mg once daily for 4 days, then a dose of omeprazole 20mg plus RAL 400mg on day 5.

Study Results

Coadministration increased raltegravir AUC by 3.12-fold, Cmax by 4.15-fold and Cmin by 1.46-fold.

Study Conclusions

Although omeprazole increased raltegravir exposure by 3-4-fold in healthy subjects, exploratory pharmacokinetic data in HIV+ subjects demonstrated a reduced effect. Evaluation of the safety profile in HIV+ patients receiving acid reducing agents has not identified any areas of concern and therefore the authors indicate that the data support the use of raltegravir in patients receiving acid reducing agents with no dosage adjustment.

References

Iwamoto M, Wenning LA, Nguyen BY, Teppler H, Moreau AR, Rhodes RR, Azrolan N. Effects of omeprazole on plasma levels of raltegravir. Clinical Infectious Diseases. 2009; 4: 489-492.