Coadministration with pantoprazole has not been studied. Significant decreases in rilpivirine plasma concentrations are expected 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 famotidine (40 mg single dose taken 12 hours before rilpivirine) and a higher than the recommended dose of rilpivirine decreased rilpivirine AUC by 9% but had no effect on Cmax. Coadministration of famotidine (40 mg single dose taken 2 hours before rilpivirine) and a higher than the recommended dose of rilpivirine decreased rilpivirine AUC and Cmax by 76% and 85%, respectively, due to reduced absorption due to gastric pH increase. Coadministration of famotidine (40 mg single dose taken 4 hours after rilpivirine) and a higher than the recommended dose of rilpivirine increased rilpivirine AU and Cmax by 13% and 21%, respectively. The combination of rilpivirine and H2-receptor antagonists should be used with particular caution. Only H2-receptor antagonists that can be dosed once daily should be used. A strict dosing schedule, with intake of H2-receptor antagonists at least 12 hours before or at least 4 hours after rilpivirine should be used. 

 

The combination of rilpivirine and H2-receptor antagonists should be used with caution as co-administration may cause significant decreases in rilpivirine plasma concentrations (increase in gastric pH). H2-receptor antagonists should only be administered at least 12 hours before or at least 4 hours after rilpivirine.  Coadministration of rilpivirine (150 mg single dose) and famotidine (40 mg single dose) was studied in 24 subjects. When famotidine was administered 2 hours before rilpivirine, the Cmax and AUC of rilpivirine decreased by 85% and 76%, respectively (data from 23 subjects).  Coadministration of famotidine 12 hours before rilpivirine decreased rilpivirine Cmax and AUC by 1% and 9% respectively. Coadministration of famotidine 4 hours after rilpivirine increased rilpivirine Cmax and AUC by 21% and 13%, respectively.

Edurant US Prescribing Information, Janssen Therapeutics, May 2019.

Coadministration of rilpivirine (150 mg single dose) and famotidine (40 mg single dose) was studied in 24 HIV-negative subjects. When famotidine was administered 2 hours before rilpivirine, the Cmax and AUC of rilpivirine decreased by 85% and 76%, respectively (data from 23 subjects).  Coadministration of famotidine 12 hours before rilpivirine decreased rilpivirine Cmax and AUC by 1% and 9% respectively. Coadministration of famotidine 4 hours after rilpivirine increased rilpivirine Cmax and AUC by 21% and 13%, respectively.
van Heeswijk R, et al. The pharmacokinetic interaction between famotidine and TMC278, a next generation non-nucleoside reverse transcriptase inhibitor, in HIV-negative volunteers. 4th IAS Conference on HIV Pathogenesis, Treatment and Prevention, Sydney, July 2007, abstract TUPDB01.