Rilpivirine

Famotidine

Administration time adjustment is recommended.

No pharmaceutical opinion available for this interaction.

Mechanism

Famotidine by increasing gastric pH may decrease the solubility, absorption, and plasma concentration of Rilpivirine.

Rilpivirine

Pharmacodynamic effects

Possible decrease of clinical efficacy.

Risk of possible development of resistance to rilpivirine and other NNRTIs.

Recommendations

Spacing of doses is required.

Rilpivirine 4 hours before or 12 hours after the anti-H2.

Or choose an alternative.

See comments.

Alternative solution(s)

Famotidine

Pharmacodynamic effects

Recommendations

Alternative solution(s)

Monitor

Tests

Pharmacokinetic parameters
Parameters
Reference number
# patients
HIV
Dose
Frequency
AUC
Cmax
Famotidine
2604 2604 2604
24 23 24
- - -
40 mg* 40 mg** 40 mg***
x1 x1 x1
     
     
Rilpivirine
2604 2604 2604
23 24 24
- - -
150 mg 150 mg 150 mg
x1 x1 x1
- 9% - 76% + 13%
- 1% - 85% + 21%
Comment

Ref #2604:
* 12 hours before Rilpivirine,
** 2 hours before Rilpivirine,
*** 4 hours after Rilpivirine.

The combination of Rilpivirine and H2-receptor antagonists should be used with caution as coadministration may cause significant decreases in rilpivirine plasma concentrations. H2-receptor antagonists should be administered 12 hours before or 4 hours after rilpivirine.

Note, the recommended anti-H2 dosage frequency is QD:
Take rilpivirine 12 hours after the H2 antagonist.
Eg: Rilpivirine (with food) at 9 am and the H2 antagonist at 9 pm.
If it is necessary to take the dosage BID:
Take the first dosage of the H2 antagonist 3 hours after the rilpivirine intake, and the second dosage of the H2 antagonist 12 hours before the next dosage of rilpivine.
Eg: Rilpivirine (with food) at 9 am and the H2 antagonist at 1 pm and 9 pm.

Reference
  • 2587
    Emtricitabine/Rilpivirine/Ténofovir DF (Complera), Gilead, Ontario, Canada, 17 octobre 2019.
  • 2598
    Rilpivirine (Edurant), Janssen, Ontario, Canada, 4 mars 2019.
  • 2604
    Van Heeswijk RP, Hoetelmans RM, Kestens D, et al. The pharmacokinetic (PK) interaction between famotidine and TMC278, a next generation non-nucleoside reverse transcriptase inhibitor (NNRTI), in HIV-negative volunteers. 4th IAS Conference on HIV Pathogenesis, Treatment and Prevention, July 22-25 2007, Sydney, Australia, abstract TUPDB01.
  • 2599
    Ford N, Lee J, Andrieux-Meyer I and Calmy A. Safety, efficacy, and pharmacokinetics of rilpivirine : systematic review with emphasis on resource-limited setting. HIV/AIDS – Reseach and Paliative Care 2011; 3: 34-55.
  • 3441
    Dolutegravir/Rilpivirine (Juluca), ViiV Healthcare ULC, Quebec, Canada, 19 août 2021.
  • 3460
    Rilpivirine/Emtricitabine/Tenofovir alafenamide (Odefsey), Gilead Sciences, Ontario, Canada, 13 novembre 2019.