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Rilpivirine: Drug information

Rilpivirine: Drug information
(For additional information see "Rilpivirine: Patient drug information" and see "Rilpivirine: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Edurant
Brand Names: Canada
  • Edurant
Pharmacologic Category
  • Antiretroviral, Reverse Transcriptase Inhibitor, Non-nucleoside (Anti-HIV)
Dosing: Adult
HIV-1 infection, treatment

HIV-1 infection, treatment:

Treatment-naive patients: Oral:

Patients ≥35 kg: 25 mg once daily.

Note: Do not use rilpivirine-based regimens in patients with preantiretroviral therapy CD4 count <200 cells/mm3 and/or HIV RNA >100,000 copies/mL (Ref).

Pregnancy: 25 mg once daily in patients on stable regimen prior to pregnancy and who are virologically suppressed.

Combination treatment with cabotegravir, treatment-experienced patients: Oral:

Oral lead-in: 25 mg once daily, in combination with oral cabotegravir, for ~1 month (≥28 days) prior to initiation of cabotegravir and rilpivirine injections, to assess tolerability to rilpivirine. Note: Final oral dose should be taken on the same day as initiation of injections.

Oral bridging therapy: 25 mg once daily, in combination with oral cabotegravir, in patients who plan to miss a scheduled cabotegravir and rilpivirine injection visit by >7 days. Note: First oral dose should be initiated at approximately the same time as the planned missed injection dose and continued until the day injection dosing is restarted. Oral therapy may be used for up to 2 months to replace missed injection(s).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Mild or moderate renal impairment: No dosage adjustment necessary.

Severe or end-stage renal impairment (ESRD): Use with caution; no dosage adjustment necessary (Ref).

Hemodialysis/peritoneal dialysis: Due to extensive protein binding, significant removal by hemodialysis or peritoneal dialysis is unlikely.

Dosing: Hepatic Impairment: Adult

Mild to moderate impairment (Child-Pugh class A or B): No dosage adjustment necessary.

Severe impairment (Child-Pugh class C): There are no dosage adjustments provided in the manufacturer's labeling (has not been studied). The Canadian labeling recommends avoiding use due to lack of data.

Dosing: Pediatric

(For additional information see "Rilpivirine: Pediatric drug information")

HIV-1 infection, treatment; treatment-naive patients

HIV-1 infection, treatment; treatment-naive patients: Note: Use in combination with other antiretroviral (ARV) agents. Gene mutation and ARV resistance patterns should be evaluated (refer to https://www.iasusa.org/ for more information) when necessary. Do not use in patients with HIV RNA >100,000 copies/mL.

Children ≥12 years and Adolescents, weighing ≥35 kg: Oral: 25 mg once daily.

HIV-1 infection, treatment; treatment-experienced patients

HIV-1 infection, treatment; treatment-experienced patients:

Combination treatment with oral cabotegravir:

Children ≥12 years and Adolescents, weighing ≥35 kg:

Oral lead-in: Oral: 25 mg once daily for ~1 month (≥28 days) prior to initiation of cabotegravir and rilpivirine injections, to assess tolerability to rilpivirine. Note: Initiate injection therapy on the same day as the final oral dose.

Oral bridging therapy: Patients who plan to miss a scheduled rilpivirine and cabotegravir injection visit by >7 days: Oral: 25 mg once daily for up to 2 months. First oral dose should be taken approximately the same day as the planned missed injection dose and continued until the day injection dosing is restarted.

Combination treatment with other ARV agents (non-cabotegravir): Note: For use in virologically suppressed (HIV RNA <50 copies/mL) patients with no history of virologic failure or resistance to rilpivirine or other antiretrovirals in regimen (refer to https://www.iasusa.org/ for more information) (Ref).

Children ≥12 years and Adolescents, weighing ≥35 kg: Oral: 25 mg once daily (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

Children ≥12 years and Adolescents:

Mild to moderate renal impairment: No dosage adjustment necessary.

Severe or end-stage renal impairment: Use with caution; guidelines suggest no dosage adjustment necessary; monitor closely as exposure may be increased (Ref).

Hemodialysis/peritoneal dialysis: Due to extensive protein binding, significant removal by hemodialysis or peritoneal dialysis is unlikely.

Dosing: Hepatic Impairment: Pediatric

Children ≥12 years and Adolescents:

Mild to moderate impairment: No dosage adjustment necessary.

Severe impairment: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Central nervous system: Depression (5% to 9%; children and adolescents: 19%), headache (3%; children and adolescents: 19%), drowsiness (children and adolescents: 14%)

Endocrine & metabolic: Decreased plasma cortisol (7%; children and adolescents: 20%; decrease from baseline via ACTH stimulation test; clinical significance is unknown), increased serum cholesterol (7% to 17%), increased LDL cholesterol (5% to 14%)

Gastrointestinal: Nausea (1%; children and adolescents: 11%)

Hepatic: Increased serum ALT (1% to 18%), increased serum AST (1% to 16%)

1% to 10%:

Central nervous system: Dizziness (1%; children and adolescents: 8%), insomnia (3%), abnormal dreams (2%), fatigue (2%)

Dermatologic: Skin rash (3% to 6%)

Endocrine & metabolic: Increased serum triglycerides (2%)

Gastrointestinal: Abdominal pain (2%; children and adolescents: 8%), vomiting (1%; children and adolescents: 6%)

Hepatic: Increased serum bilirubin (1% to 5%)

Renal: Increased serum creatinine (1% to 6%)

<1%, postmarketing, and/or case reports (Limited to important or life-threatening): Angioedema, conjunctivitis, DRESS syndrome, facial edema, fever, hepatitis, hypersensitivity reaction, localized vesiculation, nephrotic syndrome, suicidal ideation

Contraindications

Coadministration with antiseizure medications (carbamazepine, oxcarbazepine, phenobarbital, phenytoin), antimycobacterials (rifampin, rifapentine), proton pump inhibitors (esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole), systemic dexamethasone (more than a single dose), or St John's wort.

Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to rilpivirine or any component of the formulation

Warnings/Precautions

Concerns related to adverse effects:

• Depressive disorders: May cause depression, depressed mood, dysphoria, major depression, mood changes, negative thoughts, suicide attempts, or suicidal ideation; if changes are noted, seek professional intervention immediately; reevaluate risk versus benefit of continued rilpivirine therapy.

• Hepatotoxicity: Has been reported during use. Patients with significant transaminase elevations or hepatitis B or C prior to treatment may be at greater risk for hepatic adverse events. Hepatotoxicity has occurred in a few adult patients with no prior hepatic disease or risk factors. Baseline and periodic laboratory LFT evaluation during therapy is recommended for patients with pre-existing risk factors; also consider LFT monitoring in patients without identifiable hepatic disease risk.

• Hypersensitivity: Hypersensitivity and severe skin reactions have been reported, including severe rash or rash accompanied by fever, blisters, mucosal involvement, conjunctivitis, facial edema, angioedema, hepatitis or eosinophilia, or drug reaction with eosinophilia and systemic symptoms. Some skin reactions were accompanied by constitutional symptoms (eg, fever); other skin reactions were associated with organ dysfunction (eg, hepatic serum biochemistry elevations). In clinical trials, treatment-related rashes ≥ grade 2 were reported in 3% of patients. Most rashes were grade 1 or 2 and occurred within the first 4 to 6 weeks of therapy. No grade 4 rashes were reported. Monitor laboratory parameters and clinical status; discontinue if any hypersensitivity or skin rash develop.

• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.

Warnings: Additional Pediatric Considerations

Safety was assessed in 36 pediatric patients 12 to <18 years of age in a phase 2 trial; the reported incidence of adverse reactions was higher in pediatric subjects than previously reported in adults; 52.8% overall; most were grade 1 or 2. Reported adverse reactions for pediatric patients (in at least 2 subjects, ages 12 to <18 years) include: Headache (19.4% vs 3% in adults), depression (19.4% vs 9% in adults), somnolence (13.9%), nausea (11.1% vs 1% in adults), dizziness (8.3% vs 1% in adults), abdominal pain (8.3% vs 2% in adults), vomiting (5.6% vs 1% in adults), and rash (5.6% vs 3% in adults). For depressive disorders, the incidence of grade 3 and 4 depressive disorders (regardless of causality) was 5.6% (vs 1% in adult studies). None of these pediatric patients discontinued therapy due to their depressive symptoms.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Edurant: 25 mg

Generic Equivalent Available: US

No

Pricing: US

Tablets (Edurant Oral)

25 mg (per each): $54.01

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Edurant: 25 mg

Administration: Adult

Oral: Administer with a normal- to high-calorie meal. Taking with a protein supplement drink alone does not increase absorption.

Administration: Pediatric

Oral: Swallow tablet whole with water. Administer with a normal- to high-calorie meal (≥500 kcal); administration with a protein supplement drink alone is not adequate (Ref).

Use: Labeled Indications

HIV-1 infection, treatment:

Treatment-naive patients: Treatment of HIV-1 infections in antiretroviral treatment-naive patients ≥12 years of age and weighing ≥35 kg, with HIV-1 RNA ≤100,000 copies/mL at the start of therapy in combination with other antiretroviral agents.

Combination treatment with cabotegravir, treatment-experienced patients: Short-term treatment of HIV-1 infection, in combination with cabotegravir, in patients ≥12 years of age and weighing ≥35 kg who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either rilpivirine or cabotegravir, as oral lead-in to assess tolerability of rilpivirine prior to initiating rilpivirine and cabotegravir injections or an oral bridging therapy for missed rilpivirine and cabotegravir injections.

Metabolism/Transport Effects

Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Antacids: May decrease the serum concentration of Rilpivirine. Management: Administer antacids at least 2 hours before or 4 hours after oral rilpivirine when used with most rilpivirine products. However, administer antacids at least 6 hours before or 4 hours after the rilpivirine/dolutegravir combination product. Risk D: Consider therapy modification

Antihepaciviral Combination Products: May increase the serum concentration of Rilpivirine. Risk X: Avoid combination

Betibeglogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Betibeglogene Autotemcel. Risk X: Avoid combination

CarBAMazepine: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination

CYP3A4 Inducers (Moderate): May decrease the serum concentration of Rilpivirine. Risk C: Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Rilpivirine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for reduced rilpivirine efficacy (eg, loss of virologic response or resistance). Risk X: Avoid combination

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Rilpivirine. Risk C: Monitor therapy

DexAMETHasone (Systemic): May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination

Didanosine: Rilpivirine may decrease the absorption of Didanosine. Didanosine may decrease the absorption of Rilpivirine. More specifically, simultaneous coadministration of these drugs creates a conflict between recommendations to administer with (rilpivirine) and without (didanosine) food. Management: Administer didanosine on an empty stomach at least 2 hours before or 4 hours after rilpivirine, due to the requirement that rilpivirine be administered with food. Risk D: Consider therapy modification

Elivaldogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Elivaldogene Autotemcel. Management: Avoid use of antiretroviral medications for at least one month, or for the amount of time required for elimination of the retroviral medication, prior to stem cell mobilization and until the all apheresis cycles are finished Risk X: Avoid combination

Ergonovine: Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the serum concentration of Ergonovine. Specifically, this would be most likely with delavrdine, while other Non-Nucleoside Reverse Transcriptase Inhibitors may be more likely to decrease the concentration of Ergonovine. Risk X: Avoid combination

Fosphenytoin: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination

Haloperidol: QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of Haloperidol. Risk C: Monitor therapy

Histamine H2 Receptor Antagonists: May decrease the serum concentration of Rilpivirine. Management: Administer histamine H2 receptor antagonists (H2RAs) at least 12 hours before or 4 hours after oral rilpivirine. Risk D: Consider therapy modification

Inhibitors of the Proton Pump (PPIs and PCABs): May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination

Ketoconazole (Systemic): May increase the serum concentration of Rilpivirine. Rilpivirine may decrease the serum concentration of Ketoconazole (Systemic). Risk C: Monitor therapy

Levoketoconazole: QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of Levoketoconazole. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy

Levomethadone: Reverse Transcriptase Inhibitors (Non-Nucleoside) may decrease the serum concentration of Levomethadone. Management: Levomethadone dosage adjustments will likely be required with efavirenz and nevirapine, and may be necessary with rilpivirine as well. Risk C: Monitor therapy

Lovotibeglogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Lovotibeglogene Autotemcel. Risk X: Avoid combination

Macrolide Antibiotics: May increase the serum concentration of Rilpivirine. Management: Consider the use of azithromycin or another non-macrolide alternative when appropriate to avoid this potential interaction. Risk D: Consider therapy modification

Methadone: Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the metabolism of Methadone. Management: Methadone dosage adjustments will likely be required with efavirenz and nevirapine, and may be necessary with rilpivirine as well. Risk C: Monitor therapy

Orlistat: May decrease the serum concentration of Antiretroviral Agents. Risk C: Monitor therapy

OXcarbazepine: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination

PHENobarbital: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination

Phenytoin: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination

Primidone: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination

QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy

Reverse Transcriptase Inhibitors (Non-Nucleoside): May enhance the adverse/toxic effect of other Reverse Transcriptase Inhibitors (Non-Nucleoside). Reverse Transcriptase Inhibitors (Non-Nucleoside) may decrease the serum concentration of other Reverse Transcriptase Inhibitors (Non-Nucleoside). Specifically, efavirenz and nevirapine may decrease the serum concentrations of other non-nucleoside reverse transcriptase inhibitors. Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the serum concentration of other Reverse Transcriptase Inhibitors (Non-Nucleoside). Specifically, delavirdine may increase the serum concentration of etravirine. Risk X: Avoid combination

Rifabutin: May decrease the serum concentration of Rilpivirine. Management: Increase rilpivirine dose to 50 mg/day during rifabutin treatment. Use of rifabutin with emtricitabine/rilpivirine/tenofovir alafenamide product is not recommended. Use with IV cabotegravir/rilpivirine is contraindicated. Risk D: Consider therapy modification

RifAMPin: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination

Rifapentine: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination

Saquinavir: Rilpivirine may enhance the arrhythmogenic effect of Saquinavir. Saquinavir may increase the serum concentration of Rilpivirine. Risk X: Avoid combination

St John's Wort: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination

Food Interactions

Absorption increased by ~40% when taken with a normal- to high-calorie meal. Management: Administer with a normal- to high-calorie meal. Administration with a protein supplement drink alone does not increase absorption.

Grapefruit products: Grapefruit products may inhibit CYP3A4-mediated metabolism of rilpivirine and increase its exposure.

Reproductive Considerations

Contraception is not required to initiate or continue antiretroviral therapy (ART).

The Health and Human Services perinatal HIV guidelines consider oral rilpivirine an alternative component of ART for patients with HIV who are not yet pregnant but are trying to conceive.

Maximum viral suppression sustained below the limits of detection prior to conception is recommended for all persons with HIV who are planning a pregnancy. Optimization of the health of the person who will become pregnant is recommended. Selection of or changes to a specific antiretroviral regimen prior to pregnancy should be done as part of a shared decision-making process. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth.

Health care providers caring for couples planning a pregnancy when one or both partners are diagnosed with HIV may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2023).

Pregnancy Considerations

Rilpivirine has moderate to high placental transfer.

No increased risk of overall teratogenic effects has been observed following first trimester exposure according to data collected by the antiretroviral pregnancy registry. Maternal antiretroviral therapy (ART) may be associated with adverse pregnancy outcomes including preterm birth, low birth weight, and small for gestational age infants. Actual risks may be influenced by maternal factors, such as disease severity, gestational age at initiation of therapy, and specific ART regimen; therefore, close fetal monitoring is recommended. Because there is clear benefit to appropriate treatment, maternal ART should not be withheld due to concerns for adverse neonatal outcomes. Long-term follow-up is recommended for all infants exposed to antiretroviral medications; children not diagnosed with HIV but who were exposed to ART in utero or as a neonate and develop significant organ system abnormalities of unknown etiology (particularly of the CNS or heart) should be evaluated for potential metabolic dysfunction.

The Health and Human Services (HHS) perinatal HIV guidelines consider oral rilpivirine an alternative ART for pregnant patients with HIV who are antiretroviral naive, who have had ART therapy in the past but are restarting, or who require a new ART regimen (due to poor tolerance or poor virologic response of current regimen). Patients who become pregnant while taking rilpivirine may continue if viral suppression is effective and the regimen is well tolerated.

The HHS perinatal HIV guidelines recommend rilpivirine as a component in alternative regimens for initial use in antiretroviral-naive pregnant patients with a pretreatment HIV RNA ≤100,000 copies/mL and CD4 cell count ≥200 cells/mm3.

The pharmacokinetics of oral rilpivirine in pregnancy are highly variable. Concentrations of rilpivirine may decrease in the second and third trimesters, however, use of higher doses has not been studied. Viral loads should be monitored more frequently in pregnant patients taking standard doses of rilpivirine.

ART is recommended for all pregnant people with HIV to maximize their health, maintain the viral load below the limit of detection, and reduce the risk of perinatal transmission. Selection of or changes to a specific antiretroviral regimen during pregnancy should be done as part of a shared decision-making process. Patients on fully suppressive regimens prior to pregnancy generally may continue the same regimen considering known pregnancy outcomes and pharmacokinetic data. Monitoring of patients who are pregnant is more frequent than in patients who are not pregnant. ART initiated during pregnancy can be modified after delivery. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth.

Data collection to monitor pregnancy and infant outcomes following exposure to ART is ongoing. Health care providers should enroll all patients exposed to antiretroviral medications during pregnancy in the Antiretroviral Pregnancy Registry (1-800-258-4263). Enrollment should be done as early in pregnancy as possible.

Health care providers caring for pregnant patients with HIV and their infants may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2023).

Breastfeeding Considerations

Rilpivirine is present in breast milk.

Data related to the presence of rilpivirine in breast milk are available from 2 lactating patients taking rilpivirine 25 mg once daily during pregnancy and postpartum. Single samples of breast milk and maternal plasma were sampled ~15 hours after a dose 1 month following delivery. Median concentrations of rilpivirine were 122 ng/mL (breast milk; range 107 to 140 ng/mL) and 113 ng/mL (maternal plasma; range 120 to 126 ng/mL). Rilpivirine was also detected in the infant plasma (4 ng/mL) when sampled 16 hours after the maternal dose. Authors of the study calculated the estimated infant dose of rilpivirine via breast milk to be 0.02 mg/kg/day (Aebi-Popp 2022).

Maintaining maximum viral suppression during pregnancy and postpartum decreases but does not eliminate the risk of HIV transmission via breast milk. In addition, multiclass-resistant virus has been detected in breastfeeding infants who acquire HIV despite maternal therapy. In the United States, where formula is usually accessible, affordable, safe, and sustainable, and the risk of infant mortality due to diarrhea and respiratory infections is low, the Health and Human Services perinatal HIV guidelines do not recommend breastfeeding for patients with HIV when safer infant feeding options are available. Persons with HIV who maintain an undetectable viral load while taking antiretroviral therapy (ART) should evaluate infant feeding options (formula, banked donor milk, or breastfeeding) as part of a shared decision-making process (if breastfeeding is being considered, see guidelines for measures to reduce the risk of HIV transmission). When the HIV status at delivery is not known, breast milk may be expressed and stored until a negative test is available. If HIV infection is diagnosed after breastfeeding has been initiated, breastfeeding should be discontinued immediately. Breastfeeding is not recommended for persons with HIV who are not taking ART and/or who do not have sustained viral suppression.

Information is available for counseling and managing patients with HIV who are considering breastfeeding (1-888-448-8765). In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth (HHS [perinatal] 2023).

Dietary Considerations

Take with a normal- to high-calorie meal. Administration with a protein supplement drink alone does not increase absorption.

Monitoring Parameters

Cholesterol, triglycerides, hepatic transaminases; signs of skin rash, fever, and/or hypersensitivity reactions, signs and symptoms of infection

Mechanism of Action

As a non-nucleoside reverse transcriptase inhibitor, rilpivirine has activity against HIV-1 by binding to reverse transcriptase. It consequently blocks the RNA-dependent and DNA-dependent DNA polymerase activities, including HIV-1 replication. It does not require intracellular phosphorylation for antiviral activity.

Pharmacokinetics (Adult Data Unless Noted)

Note: Pharmacokinetic data in pediatric patients 12 to <18 years reported to be similar to that in adult patients.

Absorption: Increased 40% with a meal (normal-to-high calorie)

Protein binding: 99.7% (primarily albumin)

Metabolism: Hepatic, primarily by CYP3A4

Half-life elimination: ~50 hours

Time to peak, plasma: 4 to 5 hours

Excretion: Feces (85%, ~25% as unchanged drug); urine (~6%; <1% as unchanged drug)

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Altered kidney function: Exposure was similar in HIV-1-infected subjects with mild renal impairment relative to HIV-1–infected subjects with healthy renal function; no dose adjustment is required. There is limited information regarding the pharmacokinetics in patients with moderate or severe renal impairment or in patients with ESRD. Concentrations may be increased because of alteration of drug absorption, distribution, and metabolism secondary to renal dysfunction. The potential impact is not expected to be of clinical relevance for subjects with moderate renal impairment; no dose adjustment is required.

Hepatic function impairment: The multiple-dose exposure was 47% higher in subjects with mild hepatic impairment and 5% higher in subjects with moderate hepatic impairment; no dose adjustment is required. Rilpivirine has not been studied in subjects with severe hepatic impairment.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AR) Argentina: Edurant;
  • (AT) Austria: Edurant;
  • (AU) Australia: Edurant;
  • (BE) Belgium: Edurant;
  • (BG) Bulgaria: Edurant;
  • (CH) Switzerland: Edurant;
  • (CO) Colombia: Edurant;
  • (CZ) Czech Republic: Edurant;
  • (DE) Germany: Edurant;
  • (EE) Estonia: Edurant;
  • (ES) Spain: Edurant;
  • (ET) Ethiopia: Edurant;
  • (FI) Finland: Edurant;
  • (FR) France: Edurant;
  • (GB) United Kingdom: Edurant;
  • (GR) Greece: Edurant;
  • (HK) Hong Kong: Edurant;
  • (HU) Hungary: Edurant;
  • (ID) Indonesia: Edurant;
  • (IE) Ireland: Edurant;
  • (IT) Italy: Edurant;
  • (KE) Kenya: Edurant;
  • (KR) Korea, Republic of: Edurant;
  • (KW) Kuwait: Edurant;
  • (LU) Luxembourg: Edurant;
  • (LV) Latvia: Edurant;
  • (MX) Mexico: Edurant;
  • (MY) Malaysia: Edurant;
  • (NG) Nigeria: Edurant;
  • (NL) Netherlands: Edurant;
  • (NO) Norway: Edurant;
  • (PH) Philippines: Edurant;
  • (PL) Poland: Edurant;
  • (PR) Puerto Rico: Edurant;
  • (PT) Portugal: Edurant;
  • (RO) Romania: Edurant;
  • (RU) Russian Federation: Edurant | Lakonivir;
  • (SE) Sweden: Edurant;
  • (SG) Singapore: Edurant;
  • (SI) Slovenia: Edurant;
  • (SK) Slovakia: Edurant;
  • (TH) Thailand: Edurant;
  • (TR) Turkey: Edurant;
  • (TW) Taiwan: Edurant;
  • (UG) Uganda: Edurant;
  • (ZA) South Africa: Edurant;
  • (ZW) Zimbabwe: Edurant
  1. Aebi-Popp K, Kahlert CR, Crisinel PA, et al; Swiss Mother and Child HIV Cohort Study (SHCS). Transfer of antiretroviral drugs into breastmilk: a prospective study from the Swiss Mother and Child HIV Cohort Study. J Antimicrob Chemother. 2022;77(12):3436-3442. doi:10.1093/jac/dkac337 [PubMed 36177836]
  2. Cohen CJ, Molina JM, Cahn P, et al, “Efficacy and Safety of Rilpivirine (TMC278) Versus Efavirenz at 48 Weeks in Treatment-Naive HIV-1-Infected Patients: Pooled Results from the Phase 3 Double-Blind Randomized ECHO and THRIVE Trials,” J Acquir Immune Defic Syndr, 2012, 60(1):33-42. [PubMed 22343174]
  3. Cohen CJ, Molina JM, Cassetti I, et al, “Week 96 Efficacy and Safety of Rilpivirine in Treatment-Naive HIV-1 Infected Patients in Two Phase II Randomized Trials,” AIDS, 2013, 7(6):939-50. [PubMed 23211772]
  4. Edurant (rilpivirine) [prescribing information]. Titusville, NJ: Janssen Therapeutics; October 2022.
  5. Edurant (rilpivirine) [product monograph]. Toronto, Ontario, Canada: Janssen Inc; January 2023.
  6. Fulco PP and McNicholl IR, “Etravirine and Rilpivirine: Nonnucleoside Reverse Transcriptase Inhibitors With Activity Against Human Immunodeficiency Virus Type 1 Strains Resistant to Previous Nonnucleoside Agents,” Pharmacotherapy, 2009, 29(3):281-94. [PubMed 19249947]
  7. MacArthur RD, “Clinical Trial Report: TMC278 (Rilpivirine) Versus Efavirenz as Initial Therapy in Treatment-Naïve, HIV-1-Infected Patients,” Curr Infect Dis Rep, 2011, 13(1):1-3. [PubMed 21308448]
  8. Molina JM, Clumeck N, Orkin C, et al, “Rilpivirine Efficacy, Virology and Safety in ARV Treatment-Naïve Patients With Viral Load ≤100,000 HIV-1 RNA c/mL: ECHO and THRIVE 96 Week Results,” J Int AIDS Soc, 2012, 15(6):18250. [PubMed 23234922]
  9. Nelson M, Amaya G, Clumeck N, et al, “Efficacy and Safety of Rilpivirine in Treatment-Naive HIV-1-Infected Patients With Hepatitis B Virus/Hepatitis C Virus Coinfection Enrolled in the Phase III Randomized, Double-Blind ECHO and THRIVE Trials,” J Antimicrob Chemother, 2012, 67(8):2020-8. [PubMed 22532465]
  10. Pozniak AL, Morales-Ramirez J, Katabira E, et al. Efficacy and Safety of TMC278 in Antiretroviral-Naïve HIV-1 Patients: Week 96 Results of a Phase IIb Randomized Trial. AIDS. 2010;24(1):55-65. [PubMed 19926964]
  11. Public Health Agency of Canada (PHAC), Canadian Guidelines on Sexually Transmitted Infection. Last modified December 2013. http://www.phac-aspc.gc.ca/std-mts/sti-its/index-eng.php. Accessed December 30, 2015.
  12. Refer to manufacturer's labeling.
  13. US Department of Health and Human Services (HHS) Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in adults and adolescents with HIV. http://www.aidsinfo.nih.gov/ContentFiles/AdultandAdolescentGL.pdf. Updated January 20, 2022. Accessed February 9, 2022.
  14. US Department of Health and Human Services (HHS) Panel on Antiretroviral Therapy and Medical Management of Children Living with HIV. Guidelines for the use of antiretroviral agents in pediatric HIV infection. https://clinicalinfo.hiv.gov/en/guidelines/pediatric-arv/whats-new-guidelines. Updated April 7, 2021. Accessed April 13, 2022.
  15. US Department of Health and Human Services (HHS) Panel on Treatment of HIV During Pregnancy and Prevention of Perinatal Transmission. Recommendations for the use of antiretroviral drugs during pregnancy and interventions to reduce perinatal HIV transmission in the United States. https://clinicalinfo.hiv.gov/en/guidelines/perinatal/whats-new. Updated January 31, 2023. Accessed February 23, 2023.
Topic 16494 Version 261.0

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