Rilpivirine (Monograph)

Brand names: Edurant, Edurant PED
Drug class: HIV Nonnucleoside Reverse Transcriptase Inhibitors

Medically reviewed by Drugs.com on Apr 10, 2025. Written by ASHP.

Introduction

Antiretroviral; HIV nonnucleoside reverse transcriptase inhibitor (NNRTI).^{1 4 8}

Uses for Rilpivirine

Treatment of HIV Infection

Treatment of HIV-1 infection in treatment-naïve patients ≥2 years of age and weighing ≥14 kg with baseline plasma HIV-1 RNA levels ≤100,000 copies/mL;^{1 2 3 10 11 24 25 26 27 28 29 30 200 201 202} used in conjunction with other antiretrovirals.¹

Short-term treatment of HIV-1 infection, in combination with oral cabotegravir, in adults and adolescents ≥12 years of age and weighing ≥35 kg who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine.^{1 14 17 19 18 20 22 21 23}

In the HHS Adult and Adolescent HIV treatment guideline, rilpivirine is not recommended for initial therapy in the majority of patients with HIV due to the availability of other effective regimens without virologic and immunologic prerequisites to treatment initiation, the presence of substantial drug-drug interactions, and its low genetic barrier to resistance.²⁰⁰ The guideline panel continues to recommend rilpivirine/tenofovir alafenamide/emtricitabine as part of other initial antiretroviral regimens for certain clinical scenarios (e.g., patients with pre-treatment viral loads <100,000 copies/mL and CD4⁺ counts >200 cells/mm³.²⁰⁰

Postexposure Prophylaxis following Occupational Exposure to HIV (PEP)

Postexposure prophylaxis of HIV infection following occupational exposure^{† [off-label]} (PEP) in health-care personnel and others exposed via percutaneous injury (e.g., needlestick, cut with sharp object) or mucous membrane or nonintact skin (e.g., chapped, abraded, dermatitis) contact with blood, tissue, or other body fluids that might contain HIV.¹⁹⁹ Used in conjunction with other ARVs.¹⁹⁹ Rilpivirine in combination with 2 NRTIs is among several alternative regimens recommended in guidelines for PEP when the preferred regimen cannot be used.¹⁹⁹

Postexposure Prophylaxis following Nonoccupational Exposure to HIV (nPEP)

Postexposure prophylaxis of HIV infection following nonoccupational exposure^{† [off-label]} (nPEP) in individuals exposed to blood, genital secretions, or other potentially infectious body fluids that might contain HIV when the exposure represents a substantial risk for HIV transmission.^{32 31 198} Used in conjunction with other ARVs.¹⁹⁸ Rilpivirine in combination with 2 NRTIs is among several alternative regimens recommended in guidelines for nPEP.¹⁹⁸ A fixed dose combination containing rilpivirine, emtricitabine, and tenofovir disoproxil fumarate (Complera) is used for nPEP in this setting.^{31 32 198} See the full prescribing information for use of Complera.²³³

Rilpivirine Dosage and Administration

General

Pretreatment Screening

• Assess liver function tests prior to therapy initiation in patients with underlying hepatic disease such as hepatitis B (HBV) and/or C (HCV) co-infection or marked elevations in aminotransferases.¹

Patient Monitoring

• Monitor liver function tests during therapy in patients with underlying hepatic disease such as HBV and/or HCV co-infection or marked elevations in aminotransferases.¹ Consider monitoring liver function tests if no underlying hepatic dysfunction or risk factors.¹

Dispensing and Administration Precautions

• Rilpivirine is commercially available as a single entity and in various fixed-combination preparations containing additional ARV agents.^{13 14 233 244} Refer to the full prescribing information for specific, distinct uses of the combination products.^{13 14 233 244} Since the antiretroviral agents contained in the fixed combination preparations also may be available in single-entity or other fixed-combination preparations, exercise care to ensure that therapy is not duplicated if a fixed combination is used in conjunction with other ARVs.^{13 14 233 244}

• The Institute for Safe Medication Practices (ISMP) list of error-prone abbreviations, symbols, and dose designations states that the use of abbreviations for antiretroviral medications (e.g., DOR, TAF, TDF) during the medication use process should be avoided as their use has been associated with serious medication errors.²⁴⁵

Administration

Oral Administration

Available as oral tablets (Edurant) and tablets for oral suspension (Edurant PED); administer both formulations once daily with a meal.¹ Administer rilpivirine tablets to adults and pediatric patients weighing ≥25 kg.¹ Administer rilpivirine tablets for oral suspension only to pediatric patients weighing ≥14 kg to <25 kg.¹

Rilpivirine oral tablets and tablets for oral suspension have differing pharmacokinetic profiles; therefore, do not substitute the tablets and tablets for oral suspension on a milligram-per-milligram basis.¹

Disperse rilpivirine tablets for oral suspension in drinking water and immediately consume with a meal.¹ If not consumed immediately, discard the suspension and prepare a new dose.¹ Do not crush, chew, or swallow whole rilpivirine tablets for oral suspension.¹

In order to properly prepare the tablets for oral suspension for administration, place an appropriate number of tablets in a cup and add 5 mL of room temperature drinking water.¹ Swirl cup carefully for 1—2 minutes; oral suspension should begin to have a cloudy appearance.¹ After swirling cup for 1—2 minutes, consume the oral suspension immediately or further dilute the suspension with 5 mL of drinking water, orange juice, or applesauce to assist in administration.¹ All the medicine within the cup should be consumed immediately; a spoon may be used if needed.¹

Food enhances rilpivirine bioavailability.¹

If a dose of rilpivirine is missed within 12 hours of the time it is usually taken, take the missed dose as soon as possible with a meal.¹ If a dose of rilpivirine is missed by more than 12 hours, then skip the missed dose and resume the normal dosing schedule.¹

Rilpivirine must be used in conjunction with other antiretrovirals.¹

Fixed Combinations Containing Rilpivirine

Rilpivirine hydrochloride is commercially available in fixed-combination tablets containing dolutegravir sodium and rilpivirine (Juluca); emtricitabine, rilpivirine, and tenofovir alafenamide (Odefsey); and emtricitabine, rilpivirine, and tenofovir disoproxil fumarate (Complera).^{13 233 244} Rilpivirine is also commercially available as an extended-release injectable suspension kit containing copackaged cabotegravir and rilpivirine (Cabenuva).¹⁴ See the full prescribing information for administration of each of these combination products.^{13 14 233 244}

Dosage

Available as rilpivirine hydrochloride; dosage expressed in terms of rilpivirine.¹

Pediatric Patients

Treatment of HIV Infection in Antiretroviral-naïve Pediatric Patients

Oral

Patients ≥2 years of age weighing ≥14 kg: dosage based on body weight.¹ Table 1 provides recommended dosage regimens.¹

Treatment of HIV Infection in Antiretroviral-experienced Pediatric Patients in Combination with Cabotegravir

Oral

Adolescents ≥12 years of age weighing ≥35 kg: 25 mg once daily.¹

Take in combination with cabotegravir (Vocabria) 30 mg once daily.^{1 17}

Use oral lead-in therapy with rilpivirine (Edurant) and cabotegravir (Vocabria) for 1 month (at least 28 days) to assess rilpivirine tolerability prior to cabotegravir/rilpivirine (Cabenuva) injections.^{1 14 17}

Administer last oral dose on same day cabotegravir/rilpivirine (Cabenuva) injection dosing initiated.^{1 14 17}

If scheduled monthly injection of cabotegravir/rilpivirine (Cabenuva) is planned to be missed by >7 days, daily oral rilpivirine (Edurant) and cabotegravir (Vocabria) can be taken together for up to 2 months to replace missed injections.^{1 14 17}

Recommended oral daily dose is one 25-mg tablet of rilpivirine and one 30-mg tablet of cabotegravir.¹ Initiate first dose of oral therapy approximately same time as planned missed injection; continue until day injection dosing is restarted.^{1 14 17} For durations longer than 2 months, use alternative oral regimen.^{1 14 17}

If scheduled every-2-month injection of cabotegravir/rilpivirine (Cabenuva) is planned to be missed by >7 days, daily oral rilpivirine (Edurant) and cabotegravir (Vocabria) can be taken together for up to 2 months to replace 1 missed scheduled every-2-month injection.^{1 14}

Recommended oral daily dose is one 25-mg tablet of rilpivirine and one 30-mg tablet of cabotegravir.¹ Initiate first dose of oral therapy approximately same time as planned missed injection; continue until day injection dosing is restarted.^{1 14 17} For durations longer than 2 months, use alternative oral regimen.^{1 14 17}

Adults

Treatment of HIV Infection in Antiretroviral-naïve Adults

Oral

25 mg once daily.¹

Treatment of HIV Infection in Antiretroviral-experienced Adults in Combination with Cabotegravir

Oral

25 mg once daily.¹

Take in combination with cabotegravir (Vocabria) 30 mg once daily.^{1 17}

Use oral lead-in therapy with rilpivirine (Edurant) and cabotegravir (Vocabria) for 1 month (at least 28 days) to assess rilpivirine tolerability prior to cabotegravir/rilpivirine (Cabenuva) injections.^{1 14 17}

Administer last oral dose on same day cabotegravir/rilpivirine (Cabenuva) injection dosing initiated.^{1 14 17}

If scheduled monthly injection of cabotegravir/rilpivirine (Cabenuva) is planned to be missed by >7 days, daily oral rilpivirine (Edurant) and cabotegravir (Vocabria) can be taken together for up to 2 months to replace missed injections.^{1 14 17}

Recommended oral daily dose is one 25-mg tablet of rilpivirine and one 30-mg tablet of cabotegravir.¹ Initiate first dose of oral therapy approximately same time as planned missed injection; continue until day injection dosing is restarted.^{1 14 17} For durations longer than 2 months, use alternative oral regimen.^{1 14 17}

If scheduled every-2-month injection of cabotegravir/rilpivirine (Cabenuva) is planned to be missed by >7 days, daily oral rilpivirine (Edurant) and cabotegravir (Vocabria) can be taken together for up to 2 months to replace 1 missed scheduled every-2-month injection.^{1 14}

Recommended oral daily dose is one 25-mg tablet of rilpivirine and one 30-mg tablet of cabotegravir.¹ Initiate first dose of oral therapy approximately same time as planned missed injection; continue until day injection dosing is restarted.^{1 14 17} For durations longer than 2 months, use alternative oral regimen.^{1 14 17}

Postexposure Prophylaxis following Occupational Exposure to HIV (PEP)† [off-label]

Oral

25 mg once daily.¹⁹⁹ Use in conjunction with 2 NRTIs .¹⁹⁹

Initiate PEP as soon as possible following occupational exposure to HIV (preferably within hours);¹⁹⁹ continue for 4 weeks, if tolerated.¹⁹⁹

Postexposure Prophylaxis following Nonoccupational Exposure to HIV (nPEP)† [off-label]

Oral

Emtricitabine/rilpivirine/tenofovir DF (Complera): 1 tablet (200 mg of emtricitabine, 25 mg of rilpivirine, and 300 mg of tenofovir DF) once daily.¹⁹⁸ Use as a complete regimen for nPEP.¹⁹⁸

Initiate nPEP as soon as possible (within 72 hours) following nonoccupational exposure that represents a substantial risk for HIV transmission and continue for 28 days.¹⁹⁸

nPEP not recommended if exposed individual seeks care >72 hours after exposure.¹⁹⁸

Dosage Modification with Rifabutin Coadministration

If rilpivirine (Edurant) is coadministered with rifabutin, increase rilpivirine dosage to 50 mg once daily.¹ If rifabutin coadministration is halted, decrease rilpivirine dosage to 25 mg once daily.¹

Special Populations

Hepatic Impairment

Administer usual dosage in patients with mild or moderate hepatic impairment (Child-Pugh class A or B); not studied in those with severe hepatic impairment (Child-Pugh class C).¹

Renal Impairment

Administer usual dosage in patients with mild or moderate renal impairment.¹ Manufacturer makes no specific dosage recommendations for those with severe renal impairment or end-stage renal disease (ESRD); use with caution.¹

Geriatric Patients

Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.¹

Cautions for Rilpivirine

Contraindications

• Concomitant use with drugs that induce CYP3A or elevate gastric pH contraindicated since substantially decreased plasma rilpivirine concentrations may occur and may result in loss of virologic response and development of resistance to rilpivirine and/or class resistance to other NNRTIs.¹

Warnings/Precautions

Skin and Hypersensitivity Reactions

Severe skin and hypersensitivity reactions, including drug reaction with eosinophilia and systemic symptoms (DRESS), reported.¹ Some skin reactions were accompanied by constitutional symptoms such as fever; others were associated with organ dysfunction, including elevated hepatic enzyme serum concentrations.¹ Rash generally was grade 1 or 2 and occurred in the first 4–6 weeks of therapy.¹

Immediately discontinue rilpivirine if signs or symptoms of severe skin or hypersensitivity reactions develop (e.g., severe rash or rash accompanied by fever, blisters, mucosal involvement, conjunctivitis, facial edema, angioedema, hepatitis, or eosinophilia).¹ Monitor clinical status, including laboratory parameters, and initiate appropriate therapy.¹

Hepatotoxicity

Adverse hepatic effects reported; hepatotoxicity reported in some patients without preexisting hepatic disease or other risk factors.¹

HIV-infected patients with HBV or HCV coinfection or marked elevations in aminotransferase concentrations prior to rilpivirine treatment may be at increased risk for development or worsening of aminotransferase concentration elevations.¹

In patients with underlying hepatic disease (e.g., HBV or HCV infection, elevated aminotransferase concentrations), perform laboratory tests to evaluate hepatic function prior to and during rilpivirine treatment (single entity or fixed combinations).¹

Consider liver enzyme monitoring in patients without preexisting hepatic disease or other risk factors.¹

Depressive Disorders

Depressive disorders (e.g., depressed mood, depression, dysphoria, major depression, altered mood, negative thoughts, suicide attempt, suicidal ideation) reported.¹

Advise patients experiencing severe depressive symptoms to seek immediate medical evaluation to determine the likelihood that symptoms are related to rilpivirine and to determine if benefits of continued rilpivirine outweigh risks.¹

Risk of Adverse Reactions or Loss of Virologic Response Due to Drug Interactions

Concomitant use with certain drugs (e.g., drugs that may reduce rilpivirine concentrations, drugs known to increase risk of torsade de pointes) is contraindicated or requires particular caution.¹ Some drug interactions may lead to loss of virologic effect of rilpivirine and the possible development of resistance.¹ Consider the potential for drug interactions with concomitant medications prior to and during treatment with rilpivirine.¹

Immune Reconstitution Syndrome

During initial treatment, HIV-infected patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium, M. tuberculosis, cytomegalovirus [CMV], Pneumocystis jirovecii [formerly P. carinii]); this may necessitate further evaluation and treatment.¹

Autoimmune disorders (e.g., Graves' disease, polymyositis, Guillain-Barré syndrome, autoimmune hepatitis) also reported to occur in the setting of immune reconstitution; time to onset is more variable and can occur many months after initiation of ARV therapy.¹

Formulations Are Not Substitutable

Rilpivirine tablets (Edurant) and tablets for oral suspension (Edurant PED) have differing pharmacokinetic profiles and are not substitutable on a milligram-per-milligram basis.¹ When a pediatric patient weighs ≥25 kg, they must switch from rilpivirine tablets for oral suspension (Edurant PED) to one 25 mg tablet rilpivirine tablet (Edurant) daily.¹ Incorrect dosing of a given formulation may lead to a loss of therapeutic effect and possible resistance development or the occurrence of clinically significant adverse reactions due to increased rilpivirine exposure.¹

Specific Populations

Pregnancy

Human data indicate no increased risk of birth defects.¹ No dosage adjustments necessary in females stable on a rilpivirine-containing regimen prior to pregnancy and who are virologically suppressed (<50 copies/mL).¹ Monitor viral load closely in pregnant females; lower rilpivirine exposures have been observed in pregnant individuals.¹

Antiretroviral Pregnancy Registry at 800-258-4263 or [Web].¹

Lactation

Rilpivirine is present in human milk; however, there are no data on the effects of rilpivirine on the breastfed infant or on milk production.¹

The HHS perinatal HIV transmission guideline provides updated recommendations on infant feeding.²⁰² The guideline states that patients with HIV should receive evidence-based, patient-centered counseling to support shared decision making about infant feeding.²⁰² During counseling, patients should be informed that feeding with appropriate formula or pasteurized donor human milk from a milk bank eliminates the risk of postnatal HIV transmission to the infant.²⁰² Additionally, achieving and maintaining viral suppression with antiretroviral therapy during pregnancy and postpartum reduces the risk of breastfeeding HIV transmission to <1%, but does not completely eliminate the risk.²⁰² Replacement feeding with formula or banked pasteurized donor milk is recommended when patients with HIV are not on antiretroviral therapy and/or do not have a suppressed viral load during pregnancy (at a minimum throughout the third trimester), as well as at delivery.²⁰²

Pediatric Use

Safety and efficacy of rilpivirine tablets (Edurant) and tablets for oral suspension (Edurant PED) established for treatment of HIV-1 infection in treatment-naïve pediatric patients ≥2 years of age and weighing ≥14 kg.¹

Rilpivirine tablets for oral suspension (Edurant PED) not recommended for use in pediatric patients <2 years of age or weighing <14 kg.¹

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether they respond differently than younger adults.¹

Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.¹

Hepatic Impairment

Not studied in patients with severe hepatic impairment (Child-Pugh class C).¹

Higher incidence of increased serum aminotransferase concentrations reported in HIV-infected patients coinfected with HBV and/or HCV compared with those without coinfection.¹

Renal Impairment

Use with caution and increased monitoring for adverse effects in patients with severe renal impairment or ESRD; increased rilpivirine concentrations possible due to alterations in absorption, distribution, or metabolism.¹

Common Adverse Effects

Adverse effects of at least moderate to severe intensity (≥2%): depressive disorders, insomnia, headache, rash.¹

Drug Interactions

Rilpivirine is metabolized by CYP3A.¹

The following drug interactions are based on studies using single-entity rilpivirine.¹ When rilpivirine fixed combinations are used, interactions associated with each drug in the fixed combination should be considered.^{13 14 233 244}

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

CYP3A inducers: Possible decreased rilpivirine concentrations and possible loss of virologic response and development of resistance to rilpivirine or the NNRTI class.¹

CYP3A inhibitors: Possible increased rilpivirine concentrations.¹

CYP substrates: Recommended rilpivirine dosage (25 mg once daily) unlikely to have clinically important pharmacokinetic interactions.¹

Drugs that Increase Gastric pH

Possible decreased rilpivirine concentrations, loss of virologic response, and development of drug resistance or NNRTI class resistance.¹

Drugs that Prolong the QT Interval

Only limited data available to date regarding potential for pharmacodynamic interaction if used concomitantly with drugs known to prolong QT interval and increase the risk of torsade de pointes.¹ In healthy individuals, rilpivirine dosages of 75 or 300 mg daily (substantially higher than recommended dosage) resulted in clinically important prolongation of QT_c interval.¹

Use caution if rilpivirine used concomitantly with drugs known to increase risk of torsade de pointes.¹

Specific Drugs

Rilpivirine Pharmacokinetics

Absorption

Bioavailability

Absolute oral bioavailability unknown.¹

Peak plasma rilpivirine concentrations attained within approximately 4–5 hours.¹

Food

Systemic exposure is approximately 40 or 50% lower if rilpivirine tablets are administered under fasting conditions or with only a protein-rich nutritional drink, respectively, compared with following a standard meal (533 kcal) or high-caloric meal (928 kcal).^{1 4}

Systemic exposure is 31 or 28% lower if rilpivirine tablets for oral suspension are dispersed in drinking water in fasted conditions or after yogurt consumption, respectively, compared with following a meal in adults containing 533 kcal.¹

Distribution

Extent

Distribution into compartments other than plasma (e.g., CSF, genital tract secretions) not evaluated.¹

Distributed into human milk.¹

Plasma Protein Binding

Approximately 99.7% (in vitro), principally albumin.¹

Approximately 99% during second and third trimesters and postpartum period.¹

Elimination

Metabolism

Metabolized principally in the liver by CYP3A.¹

Elimination Route

Following oral administration of a single dose, 85% of rilpivirine dose eliminated in feces (75% as metabolites) and 6% eliminated in urine (<1% as unchanged rilpivirine).¹

Because rilpivirine is highly bound to plasma proteins, clinically important removal by peritoneal dialysis or hemodialysis is unlikely.¹

Half-life

Terminal elimination half-life is about 50 hours.¹

Special Populations

Mild or moderate hepatic impairment (Child-Pugh class A or B) increases rilpivirine exposure by 47 or 5%, respectively.¹

Coinfection with HIV and HBV or HCV does not alter rilpivirine exposure.¹

Mild renal impairment does not alter rilpivirine exposure.¹ Only limited data available for patients with moderate or severe renal impairment; rilpivirine concentrations may be increased as a result of altered absorption, distribution, or elimination.¹

Pharmacokinetics in treatment-naïve HIV-1-infected pediatric patients 2 to <18 years of age and weighing ≥16 kg receiving the recommended weight-based dosing regimen of rilpivirine tablets and tablets for oral suspension are similar or slightly higher than those observed in treatment-naïve adult patients.¹

Sex differences in pharmacokinetics not observed.¹

Race not expected to affect rilpivirine exposure.¹

Total exposure to rilpivirine 30—40% lower in pregnant females.¹ Not clinically relevant if virologically suppressed (<50 copies/mL).¹

Stability

Storage

Oral

Tablets

20—25°C (excursions permitted to 15–30°C); store in original container.¹

Tablets for oral suspension

20—25°C (excursions permitted to 15–30°C); store in original container.¹

Actions and Spectrum

• Inhibits replication of HIV-1 by interfering with viral RNA- and DNA-directed polymerase activities of reverse transcriptase.^{1 7 8}

• Rilpivirine is a diarylpyrimidine NNRTI; structural flexibility of these drugs allows for binding to the allosteric NNRTI binding pocket in a variety of conformations.^{5 6 7}

• Unlike other currently available NNRTIs, rilpivirine contains a cyanovinyl group that contributes to potency and maintains the drug’s binding ability despite emergence of some resistance mutations in HIV-1 reverse transcriptase.^{4 5 7 9}

• Active in vitro against wild-type HIV-1, but has limited activity against HIV type 2 (HIV-2).^{1 6} Active in vitro against some clinical HIV-1 isolates resistant to other commercially available NNRTIs (efavirenz, nevirapine).^{1 6 8}

• Rilpivirine-resistant strains have been selected in cell culture and have emerged during clinical use.^{1 3 6 10}

• Cross-resistance can occur between rilpivirine and other commercially available NNRTIs.^{1 6 10 11} Up to 90% of rilpivirine-resistant isolates that developed in patients receiving rilpivirine in clinical studies were resistant to etravirine.⁸

• Patients in clinical studies experiencing virologic failure while receiving a rilpivirine regimen were more likely to develop NNRTI-class resistance and treatment-emergent resistance to NRTIs than patients receiving an efavirenz regimen.^{1 8}

Advice to Patients

• Advise patients to read the FDA-approved patient labeling (Patient Information and Instructions for Use).¹

• Advise patients of the critical nature of compliance with HIV therapy and importance of remaining under the care of a clinician.¹ Stress importance of taking rilpivirine as prescribed; do not alter or discontinue antiretroviral regimen without consulting clinician.¹

• Counsel patients on the importance of using single-entity rilpivirine in conjunction with other antiretrovirals—not for monotherapy.¹

• Advise patients to inform their clinician immediately of any signs or symptoms of infection as inflammation from previous infection may occur soon after combination antiretroviral therapy is initiated.¹

• Inform patients that rilpivirine tablets (Edurant) and tablets for oral suspension (Edurant PED) are not substitutable on a milligram-per-milligram basis.¹ Advise patients that switching from rilpivirine tablets for oral suspension to rilpivirine tablets requires a dosage adjustment and that patients should visually inspect tablets to ensure the correct formulation is dispensed each time the prescription is filled.¹

• Advise patients of the importance of taking rilpivirine once daily with a meal; a protein drink or yogurt alone does not constitute a meal.¹ Food enhances absorption of rilpivirine.¹

• Inform patients that rilpivirine tablets for oral suspension (Edurant PED) should be dispersed in drinking water and should not be crushed, chewed, or swallowed whole.¹

• Counsel patients that if a missed dose of single-entity rilpivirine is remembered within 12 hours, take the dose with a meal as soon as possible and take next dose at regularly scheduled time.¹ If the missed dose is remembered more than 12 hours after the scheduled time, omit the missed dose and take next dose at regularly scheduled time.¹ Advise patients that doses that are larger or smaller than the prescribed dosage should not be taken at any time.¹

• Advise patients that skin reactions ranging from mild to severe, including DRESS, reported with rilpivirine-containing antiretroviral regimens.¹ Instruct patients to immediately stop taking rilpivirine (single entity or fixed combinations) and contact a clinician if a rash develops and is also associated with fever, blisters, mucosal involvement, eye inflammation (conjunctivitis), swelling of the face, eyes, lips, mouth, tongue, or throat which may lead to difficulty swallowing or breathing, or any signs and symptoms of liver problems as it may be a sign of a more serious problem.¹

• Advise patients that depressive disorders (e.g., depressed mood, depression, dysphoria, major depression, altered mood, negative thoughts, suicide attempt, suicidal ideation) have been reported.¹ Stress importance of immediately contacting clinician if depressive symptoms (e.g., feeling sad, hopeless, anxious, or restless; hurting oneself; having thoughts of hurting oneself) occur.¹

• Advise patients that hepatotoxicity has been reported in patients receiving rilpivirine.¹

• Advise patients to inform their clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and herbal products (e.g., St. John’s wort), and any concomitant illnesses.¹

• Stress importance of patients informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹ Inform patients that there is a pregnancy registry that monitors outcomes in patients exposed to rilpivirine during pregnancy.¹

• Advise patients of other important precautionary information.¹

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Frequently asked questions

• What is the difference between HIV treatments Odefsey and Complera?
• What drugs are contained in HIV treatment Juluca?

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