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.