Classes
DEA Class; Rx
Common Brand Names; Edurant
- HIV, NNRTIs
Description
Oral, non-nucleoside reverse transcriptase inhibitor (NNRTI)
Used with other antiretrovirals to treat HIV-1 infection in treatment-naive patients 12 years and older weighing at least 35 kg with HIV-1 RNA of 100,000 copies/mL or less at initiation of therapy; also used with cabotegravir for patients 12 years and older weighing at least 35 kg who are virologically suppressed on a stable regimen with no history of treatment failure and no known or suspected resistance to rilpivirine or cabotegravir
Virologic failures more common if baseline HIV-1 RNA concentrations are more than 100,000 copies/mL
Indications
Indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in treatment-naïve adult patients with HIV-1 RNA <100,000 copies/mL
Indicated in combination with cabotegravir PO as a complete regimen for short-term 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 therapy (ART) regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine
Contraindications
Hypersensitivity
Coadministration with drugs (eg, CYP inducers like phenobarbital, dexamethasone, oxcarbazepine, phenytoin, or carbamazepine) where significant decreases in rilpivirine plasma concentrations may occur, which may result in loss of virologic response and possible resistance and cross-resistance to other NNRTIs
Contraindicated with drugs that increase gastric pH (eg, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole) that may decrease rilpivirine absorption and result in decreased rilpivirine plasma concentrations
Adverse Effects
- Depressive disorders (4%)
- Insomnia (3%)
- Headache (3%)
- Rash (3%)
- Increased AST (2%; grade 3 or higher)
- ALT increased (19%)
- Abnormal dreams (1%)
- Nausea (1%)
- Suicidal ideation (4-8%)
- Abdominal pain (1%)
- Vomiting (1%)
- Fatigue (1%)
- Dizziness (1%)
Warnings
Coadministration with other NNRTIs may either increase or decrease rilpivirine; avoid use with other NNRTIs
May increase risk for depressive disorders
Hepatic adverse effects reported; patients with underlying hepatitis B or C, or marked increased transaminases prior to treatment may be at increased risk; monitor for hepatotoxicity before initiating and during treatment
Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance” have been observed in patients receiving antiretroviral therapy
Immune reconstitution syndrome: During initial phase of combination ART treatment, patients whose immune system responds may develop an inflammatory response to indolent or residual opportunistic infections (eg, Mycobacterium avium complex, CMV, Pneumocystis pneumonia, TB)
Severe skin and hypersensitivity reactions reported, including cases of drug reaction with eosinophilia and systemic symptoms (DRESS), with rilpivirine-containing regimens; immediately discontinue treatment if hypersensitivity or rash with systemic symptoms or elevations in hepatic serum biochemistries develop and closely monitor clinical status, including hepatic serum biochemistries
Pregnancy and Lactation
Available data from the APR show no difference in the overall risk of birth defects for rilpivirine compared with the background rate for major birth defects of 2.7% in the Metropolitan Atlanta Congenital Defects Program (MACDP) reference population
Unknown whether distributed in human breast milk; there are no data on presence of drug in human milk, effects on breastfed infant, or on milk production; drug is present in rat milk
The CDC recommends that women in the United States should not breastfeed their infants because of risk of the following
- Postnatal HIV transmission (in HIV-negative infants)
- Developing viral resistance (in HIV-positive infants)
- Adverse reactions in nursing infants
Maximum Dosage
25 mg/day PO.
25 mg/day PO.
weight 35 kg or more: 25 mg/day PO.
weight less than 35 kg: Safety and efficacy have not been established.
12 years and weight 35 kg or more: 25 mg/day PO.
1 to 11 years or weight less than 35 kg: Safety and efficacy have not been established.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
How supplied
Rilpivirine
tablet
- 25mg
