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(ril-pi-vir-een ) ,


(trade name)


Therapeutic: antiretrovirals
Pharmacologic: non nucleoside reverse transcriptase inhibitors
Pregnancy Category: B


Treatment-naïve adult patients with HIV infection with HIV-1 RNA ≤100,000 copies/mL at start of therapy.


Inhibits HIV-replication by non-competitively inhibiting HIV reverse transcriptase.

Therapeutic effects

Slowed progression of HIV infection and decreased occurrence of sequelae. Increases CD4 cell counts and decreases viral load.


Absorption: Well absorbed following oral administration.
Distribution: Unknown.
Protein Binding: 99.7%.
Metabolism and Excretion: Mostly metabolized by the liver (CYP3A enzyme system); 25% excreted in feces unchanged, <1% excreted unchanged in urine.
Half-life: 50 hr.

Time/action profile (blood levels)

POunknown4–5 hr24 hr


Contraindicated in: Concurrent use of drugs that inhibit the CYP3A enzyme system or ↑ gastric pH (↓ blood levels and effectiveness, ↑ resistance); Lactation: Breast feeding should be avoided due to possible transmission of virus in breast milk.
Use Cautiously in: Concurrent use of drugs that ↑ risk of torsades de pointes (may ↑ risk of arrhythmias);History of depression or suicide attempt;Hepatitis B or CConcurrent use of antacids or H2 antagonists (↓ blood levels and effectiveness); Geriatric: Consider ↓ hepatic/renal/cardiac function, concurrent diseases, and drug therapy; Obstetric: Use only if potential maternal benefit justifies potential risk to fetus; Pediatric: Safety and effectiveness not established.

Adverse Reactions/Side Effects

Central nervous system

  • depression
  • dizziness
  • headache
  • insomnia


  • rash


  • hepatotoxicity


  • fat redistribution
  • immune reconstitution syndrome


Drug-Drug interaction

Drugs that inhibit the CYP3A enzyme system including carbamazepine, dexamethasone (more than a single dose), oxcarbazepine, phenobarbital, phenytoin, rifabutin, rifampin, or, rifapentine ↓ blood levels and effectiveness and promote of virologic resistance; concurrent use contraindicated.Proton pump inhibitors including esomeprazole, lansoprazole, omeprazole, pantoprazole, and rabeprazole ↓ blood levels and effectiveness and may ↑ resistance; concurrent use contraindicated.Concurrent use with antacids may ↓ blood levels and effectiveness; use with caution, administer 2 hr before or 4 hr after.Concurrent use with H2 antagonists may ↓ blood levels and effectiveness; use with caution, administer 12 hr before or 4 hr after.Blood levels may be ↑ by clarithromyin, erythromycin, or troleandomycin ; consider azithromycin.Concurrent use with drugs that ↑ risk of torsades de pointes may ↑ risk of serious arrhythmias.Concurrent use of other non-nucleoside reverse transcriptase inhibitors may alter blood levels and should be avoided.May alter blood levels of methadone ; monitor clinical effects.Concurrent use of St. John's wort ↓ blood levels and effectiveness, ↑ resistance; concurrent use contraindicated.


Oral (Adults) 25 mg once daily.


Tablets: 25 mg
In combination with: emtricitabine and tenofovir (Complera). See combination drugs.

Nursing implications

Nursing assessment

  • Assess for change in severity of HIV symptoms and for symptoms of opportunistic infections during therapy.
  • Monitor closely for notable changes in behavior that could indicate the emergence or worsening of suicidal thoughts or behavior or depression.
  • Lab Test Considerations: Monitor viral load and CD4 cell count regularly during therapy.
    • Monitor liver function tests before and periodically during therapy in patients with underlying liver disease, hepatitis B or C, or marked ↑ transaminase. May cause ↑ serum creatinine, AST, ALT, total bilirubin, total cholesterol, LDL, and triglycerides.

Potential Nursing Diagnoses

Risk for infection (Indications)
Noncompliance (Patient/Family Teaching)


  • Oral: Administer once daily with a meal.

Patient/Family Teaching

  • Emphasize the importance of taking rilpivirine as directed, at the same time each day. It must always be used in combination with other antiretroviral drugs. Do not take more than prescribed amount and do not stop taking without consulting health care professional. Take missed doses with a meal if remembered <12 hr of the time it is usually taken, then return to regular schedule. If more than 12 hr from time dose is usually taken, omit dose and resume dosing schedule; do not double doses. Advise patient to read Patient Information prior to starting therapy and with each Rx refill in case of changes.
  • Advise patient to take antacids 2 hr before or 4 hr after and H2 antagonists 12 hr before or 4 hr after rilpivirine.
  • Instruct patient that rilpivirine should not be shared with others.
  • Inform patient that rilpivirine does not cure AIDS or prevent associated or opportunistic infections. Rilpivirine does not reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Caution patient to use a condom and to avoid sharing needles or donating blood to prevent spreading the AIDS virus to others. Advise patient that the long-term effects of rilpivirine are unknown at this time.
  • Inform patients and families of risk of suicidal thoughts and behavior and advise that behavioral changes, emergency or worsening signs and symptoms of depression, unusual changes in mood, or emergence of suicidal thoughts, behavior, or thoughts of self-harm should be reported to health care professional immediately.
  • Immune reconstitution syndrome may trigger opportunistic infections or autoimmune disorders. Notify health care professional if symptoms occur.
  • May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially St. John's wort.
  • Inform patient that changes in body fat (increased fat in upper back and neck, breast, and around back, chest, and stomach area; loss of fats from legs, arms, and face) may occur.
  • Advise patients to notify health care professional if pregnancy is planned or suspected. Advise patient to avoid breast feeding during rilpivirine therapy.
  • Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects.

Evaluation/Desired Outcomes

  • Delayed progression of AIDS and decreased opportunistic infections in patients with HIV.
  • Decrease in viral load and increase in CD4 cell counts.
Drug Guide, © 2015 Farlex and Partners
References in periodicals archive ?
Francies et al., "Simultaneous estimation of Emtricitabine, Tenofovir disoproxil fumarate and Rilpivirine in bulk form by RP-HPLC method," Journal of Pharmacy Research, vol.
In the two trials, rilpivirine was compared with efavirenz, which is also approved for the treatment of HIV infection.
Subject to regulatory approval, Gilead will assume the lead role in the manufacturing, registration, distribution and commercialization of the fixed-dose combination of Truvada and rilpivirine worldwide (excluding the developing world and Japan.) Tibotec will be responsible for the commercialization of rilpivirine as a stand-alone product and will hold rights to co-promote the fixed-dose combination in these areas.
The company has submitted a new drug application to the US FDA for the two-drug regimen to treat HIV-1 infection in adults whose viral load is suppressed and who are not resistant to cabotegravir or rilpivirine. Cabotegravir, which is ViiV Healthcare's investigational integrase inhibitor, is not approved by regulatory authorities anywhere in the world.
"Therefore, the efficacy, safety, and pharmacokinetic outcomes of long-acting cabotegravir plus rilpivirine in different subpopulations infected with HIV-1 needs further evaluation," the investigators concluded.
The results showed virologic failure to be the only parameter by which rilpivirine fell short of efavirenz, with rilpivirine's rate nearly twice that of efavirenz, Dr.
This application to the EMA follows the recent submission of a New Drug Application (NDA) for the 2DR of cabotegravir and rilpivirine, as well as cabotegravir oral tablets, to the US Food and Drug Administration (FDA) in April 2019.
The studies indicated that 84% of participants who switched from their current three- or four-drug antiretroviral regimen to a two-drug regimen of dolutegravir (ViiV Healthcare) and rilpivirine (Janssen Sciences Ireland UC, part of the Janssen Pharmaceutical Companies of Johnson & Johnson) maintained viral suppression (viral load of up to 50 copies/mL).
The Janssen Pharmaceutical Companies of Johnson & Johnson confirmed that the long-acting two-drug injectable regimen of rilpivirine and cabotegravir met its primary endpoints in two Phase 3 studies - the Antiretroviral Therapy as Long-Acting Suppression, or ATLAS, trial and the First Long-Acting Injectable Regimen, or FLAIR, trial.
Emtricitabine and tenofovir alafenamide are from Gilead and rilpivirine is from Janssen Sciences Ireland UC, one of the Janssen Pharmaceutical Companies of Johnson & Johnson.
[38] There are no data for rilpivirine in children.