Rilpivirine should not be co-administered with omeprazole as significant decreases in rilpivirine plasma concentrations may occur (due to gastric pH increase), which may result in loss of therapeutic effect of rilpivirine. Coadministration of omeprazole (20 mg once daily) and a higher than the recommended dose of rilpivirine decreased omeprazole AUC and Cmax by 14%. Rilpivirine AUC, Cmin and Cmax decreased by 40%, 33% and 40%, respectively, due to reduced absorption due to gastric pH increase.  Rilpivirine must not be used in combination with proton pump inhibitors as co-administration is likely to result in loss of therapeutic effect of rilpivirine.

 

Coadministration is contraindicated due to the potential for significant decreases in rilpivirine plasma concentrations due to gastric pH increase, which may result in loss of virologic response. Coadministration of rilpivirine (150 mg once daily) and omeprazole (20 mg once daily) was studied in 16 subjects. Rilpivirine Cmax, AUC and Cmin decreased by 40%, 40% and 37%, respectively.  Omeprazole Cmax and AUC both decreased by 14%.

Edurant US Prescribing Information, Janssen Therapeutics, May 2019.

Coadministration of rilpivirine (150 mg once daily) and omeprazole (20 mg once daily) was studied in 16 HIV-negative subjects. Rilpivirine Cmax, AUC and Cmin decreased by 40%, 40% and 37%, respectively.  Omeprazole Cmax and AUC both decreased by 14%.
Crauwels HM, et al. The pharmacokinetic interaction between omeprazole and TMC278, a next generation non-nucleoside reverse transcriptase inhibitor. 9th International Congress on Drug Therapy in HIV Infection, Glasgow, November 2008, abstract P239.