Drug reference

Rilpivirine

Antiretroviral

Also known as Rilpivirine hydrochloride

Antiretroviral

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

FDA category + note

Top interactionssee all 12 →

LansoprazoleContraindicatedDatabaseDDInter
RabeprazoleContraindicatedDatabaseKimi deep-research + Cla
Domperidone + OmeprazoleSevereTextbookG&G 14e · p1245-1266
Pantoprazole + DomperidoneSevereTextbookG&G 14e · p1245-1266

Mechanism

Rilpivirine is a nonnucleoside reverse transcriptase inhibitor (NNRTI). It works by blocking the activity of reverse transcriptase, an enzyme necessary for HIV-1 replication. Rilpivirine also has activity against human immunodeficiency virus type 1 strains resistant to previous nonnucleoside agents.

Indications

Treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults who are virologically suppressed (HIV-1 RNA < 50 copies/ml) on a stable antiretroviral regimen for at least six months with no history of virological failure and no known or suspected resistance to any nonnucleoside reverse transcriptase inhibitor or integrase inhibitor (as part of combination therapy with dolutegravir)Activity against human immunodeficiency virus type 1 strains resistant to previous nonnucleoside agentsHIV-1 infection in children >12 years of age and adults (oral formulation)HIV-1 infection in adults with chronically suppressed plasma HIV RNA (injectable LA formulation)

Dosing

Adult: 25 mg orally once daily (as part of combination therapy with dolutegravir or cabotegravir); 600 mg intramuscularly once monthly (as part of combination therapy with cabotegravir)

Pharmacokinetics

Half-life

50 (oral); 13 to 28 weeks (injectable nanoformulation)

Bioavailability

40–50% (oral, with food)

Protein binding

99.7%

Metabolism

CYP3A4, 3A5

Excretion

6% (renal, unchanged)

Contraindications

Known or suspected resistance to any nonnucleoside reverse transcriptase inhibitor or integrase inhibitor (when used in combination with dolutegravir)

Side effects

Common

rashdepressive symptomselevated hepatic transaminases

Serious

prolongation of the QTc interval
drug reaction with eosinophilia and systemic symptoms (DRESS)
postinjection reactions (dyspnea, agitation, abdominal cramping, flushing, sweating, oral numbness, changes in blood pressure)
hepatotoxicity

Pregnancy & lactation

Pregnancy

Lactation

The drug readily crosses the placenta and has been found in breast milk (context of nevirapine, likely shared class property).

Drug interactions

Lansoprazole

Contraindicated

Database

Reduced absorption and plasma concentrations of rilpivirine, potentially leading to loss of efficacy.

Should not be given with proton pump inhibitors.

Source: DDInter

Rabeprazole

Contraindicated

Database

Rabeprazole increases gastric pH, which significantly reduces the solubility and absorption of rilpivirine (an HIV NNRTI that requires acidic pH for dissolution). Coadministration results in subtherapeutic rilpivirine plasma concentrations and risk of virologic failure and resistance.

CONTRAINDICATED. Do not coadminister. If PPI therapy is essential, consider alternative antiretroviral regimen (e.g., efavirenz- or dolutegravir-based).

Source: Kimi deep-research + Cla

Domperidone + Omeprazole

Severe

Textbook

Reduced absorption and plasma concentrations of rilpivirine, potentially leading to loss of efficacy.

Should not be given with proton pump inhibitors.

Source: G&G 14e · p1245-1266

Pantoprazole + Domperidone

Severe

Textbook

Reduced absorption and plasma concentrations of rilpivirine, potentially leading to loss of efficacy.

Should not be given with proton pump inhibitors.