rilpivirine

REMS

Treatment-nave patients with HIV infection with HIV-1 RNA 100,000 copies/mL at start of therapy.
Short-term treatment of HIV infection in patients with an HIV-1 RNA <50 copies/mL who on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine (in combination with cabotegravir) (to be used as either oral lead-in to assess the tolerability of rilpivirine prior to administration of cabotegravir/rilpivirine extended-release injection or oral therapy for patients who will miss planned injection dosing with cabotegravir/rilpivirine extended-release injection).

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/Excretion: Mostly metabolized by the liver (CYP3A enzyme system); 25% excreted in feces unchanged, <1% excreted unchanged in urine.

Half-life: 50 hr.

Contraindicated in:

Concurrent use of drugs that induce the CYP3A enzyme system or ↑ gastric pH (↓ blood levels and effectiveness, ↑ resistance)
Lactation: Breastfeeding not recommended in patients with HIV.

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 C
Concurrent use of antacids or H₂ antagonists (↓ levels and effectiveness)
Pedi: Children <12 yr (safety and effectiveness not established)
Geri: Consider ↓ hepatic/renal/cardiac function, concurrent diseases, and drug therapy.

Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), rash.

Endo: fat redistribution, Grave's disease.

GI: autoimmune hepatitis, hepatotoxicity.

MS: polymyositis.

Neuro: Guillain-Barré syndrome , depression (↑ in children), dizziness, headache, insomnia.

Misc: immune reconstitution syndrome.

Drug-Drug:

Drugs that induce the CYP3A enzyme system including carbamazepine, dexamethasone (more than a single dose), oxcarbazepine, phenobarbital, phenytoin, rifampin, or rifapentine↓ levels and effectiveness and promote virologic resistance; concurrent use contraindicated.
Proton pump inhibitors including esomeprazole, lansoprazole, omeprazole, pantoprazole, and rabeprazole↓ levels and effectiveness and may ↑ resistance; concurrent use contraindicated.
Concurrent use with antacids may ↓ levels and effectiveness; use with caution, administer at least 2 hr before or 4 hr after rilpivirine.
Concurrent use with H₂ antagonists may ↓ levels and effectiveness; use with caution, administer at least 12 hr before or 4 hr after rilpivirine.
Rifabutin may ↓ levels; ↑ rilpivirine dose during concurrent use
Efavirenz, etravirine, and nevirapine may ↓ levels; avoid concurrent use
Darunavir/ritonavir, lopinavir/ritonavir, atazanavir/ritonavir, fosamprenavir/ritonavir, saquinavir/ritonavir, tipranavir/ritonavir, atazanavir, fosamprenavir, indinavir, and nelfinavir may ↑ levels
Clarithromyin or erythromycin may ↑ levels; consider using azithromycin.
Fluconazole, itraconazole, ketoconazole, posaconazole, and voriconazole may ↑ levels; rilpivirine may ↓ ketoconazole levels
Concurrent use with drugs that ↑ risk of torsades de pointes may ↑ risk of serious arrhythmias.
May ↓ levels of methadone; monitor clinical effects.

Drug-Natural Products:

Concurrent use of St. John's wort↓ blood levels and effectiveness and promote virologic resistance; concurrent use contraindicated.

Treatment-Nave Patients with HIV Infection

PO (Adults and Children 12 yr and 35 kg): 25 mg once daily; Pregnant patients on stable rilpivirine regimen prior to pregnancy and virologically suppressed (HIV RNA <50 copies/mL) — 25 mg once daily; Concurrent rifabutin therapy — 50 mg once daily (↓ dose to 25 mg once daily when rifabutin discontinued).

Combination Therapy with Cabotegravir for HIV Infection

PO (Adults): Oral lead-in therapy to assess tolerability of rilpivirine — 25 mg once daily (with oral cabotegravir) for 28 days, then switch to cabotegravir/rilpivirine extended-release injection. To replace planned missed cabotegravir/rilpivirine extended-release injections (up to 2 consecutive monthly injections) — 25 mg once daily (with oral cabotegravir) initiated approximately 1 mo after last injection of cabotegravir/rilpivirine and then continued until day the cabotegravir/rilpivirine extended-release injection is restarted.

PO: Administer once daily with a meal.
- When administered with cabotegravir, administer rilpivirine with cabotegravir once daily at same time with a meal. Take last PO dose on same day as cabotegravir injection is started. If patient plans to miss a scheduled cabotegravir injection by >7 days, take daily PO therapy to replace up to 2 consecutive monthly injection visits. Take 1st PO dose 1 mo after last injection.

Therapeutic Classification: antiretrovirals

Pharmacologic Classification: non nucleoside reverse transcriptase inhibitors

Tablets: 25 mg;
In combination with: dolutegravir (Juluca); emtricitabine and tenofovir (Complera). See Appendix [not included in this PDA edition].

(blood levels)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	4–5 hr	24 hr

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.
Assess for rash periodically during therapy. May cause DRESS. Discontinue therapy if severe or if accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis, and/or eosinophilia.

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.

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 or rash 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.
Rep: Advise patient taking oral contraceptives to use a nonhormonal method of birth control during rilpivirine therapy. If pregnancy is suspected notify health care professional promptly. Encourage pregnant women to enroll in the Antiretroviral Pregnancy Registry by calling 1-800-258-4263. Advise female patient to avoid breastfeeding.
Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects.

Delayed progression of AIDS and decreased opportunistic infections in patients with HIV.
Decrease in viral load and increase in CD4 cell counts.

NDC Code^*

59676- Janssen Products, LP
59676-278- EDURANT 59676-278-01- 30 TABLET, FILM COATED in 1 BOTTLE (59676-278-01)

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