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Rilpivirine

Class
Antiretroviral agents
Subclass
Non-nucleoside reverse-transcriptase inhibitors
Substance name
Rilpivirine hydrochloride
Brand names
Edurant®
Common formulations
Film-coated tablet
Contained in
Dolutegravir / rilpivirine (Juluca®)
Emtricitabine / rilpivirine / tenofovir alafenamide (Odefsey®)
Dosage and administration
Adults patients
HIV-1 infection • Treatment-naïve, HIV-1 RNA ≤ 100,000 copies/mL
•
25 mg PO daily
Taken with a meal
HIV-1 infection • Treatment-experienced, HIV-1 RNA < 50 copies/mL
•
25 mg PO daily for 28 days, followed by cabotegravir/rilpivirine extended-release injections
Administered in combination with cabotegravir. Administer the final oral dose on the same day of initiation of injections. Administer daily oral therapy for up to 2 months in patients planning to miss a scheduled monthly injection by > 7 days. Taken with a meal
Indications for use
Labeled indications
Adults
•
Treatment of HIV-1 infection (treatment-experienced, HIV-1 RNA < 50 copies/mL)
•
Treatment of HIV-1 infection (treatment-naïve, HIV-1 RNA ≤ 100,000 copies/mL)
Safety risks
Contraindications
Hypersensitivity to rilpivirine or its components
Concomitant use of CYP3A inducers
•
Do not use rilpivirine with CYP3A inducers, such as certain anticonvulsants (carbamazepine, oxcarbazepine, phenobarbital, phenytoin), antimycobacterials (rifampin, rifapentine), dexamethasone (more than a single-dose treatment), St. John's wort, or drugs increasing gastric pH, such as PPIs (esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole).
Warnings and precautions
Immune reconstitution inflammatory syndrome
•
Use caution in patients with asymptomatic or residual opportunistic infections (such as Mycobacterium avium infection, CMV, P. jirovecii pneumonia, or tuberculosis) being treated with combined antiretroviral therapy. Graves' disease, polymyositis, Guillain-Barré syndrome, and AIH have also been reported in the setting of immune reconstitution.
Increased liver enzymes
•
Use caution in patients with a history of HBV or HCV infection or marked elevations in transaminase levels. Consider monitoring liver enzyme levels.
Prolonged QT interval, depression, DRESS syndrome
•
Maintain a high level of suspicion, as rilpivirine has been associated with an increased risk for these adverse events.
Specific populations
Renal impairment
eGFR ≥ 30 mL/min/1.73 m²
•
Use acceptable. No dose adjustment required.
eGFR < 30 mL/min/1.73 m²
•
Use with caution.
Renal replacement therapy
Any modality
•
No guidance available.
Hepatic impairment
Child-Pugh A (mild)
•
Use acceptable. No dose adjustment required.
Child-Pugh B (moderate)
•
Use acceptable. No dose adjustment required.
Child-Pugh C (severe)
•
No guidance available.
Unexplained abnormality in LFTs
•
Use with caution. Monitor serum aminotransferases.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: B1
•
Generally acceptable for use. Enroll patients in a dedicated pregnancy outcome monitoring registry. Initiate antiretroviral therapy in all patients during pregnancy, regardless of HIV RNA concentrations or CD4 cell count.
Breastfeeding
Strongly consider avoiding breastfeeding in HIV-positive mothers who have access to formula feeding.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
Adverse reactions
Very common > 10%
•
↑ serum cholesterol, depression, headache, somnolence
Common 1-10%
•
Acute cholecystitis, cholelithiasis, ↑ liver enzymes, ↑ serum TBIL, ↑ serum triglycerides, membranous glomerulonephritis, mesangial proliferative glomerulonephritis, nephrolithiasis, abdominal pain, anxiety, diarrhea, dizziness, fatigue, insomnia, nausea, nightmares, skin rash, suicidal ideation, vomiting
Unknown frequency
•
Adrenocortical insufficiency, DRESS syndrome, immune reconstitution inflammatory syndrome, ↑ serum cortisol, nephrotic syndrome
Interactions
Drug(s)
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