rilpivirine (Rx)

Brand and Other Names:Edurant
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 25mg
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HIV-1 Infection

Indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in treatment-naïve adult patients with HIV-1 RNA <100,000 copies/mL

25 mg PO qDay; administer with a meal

Renal & Hepatic Impairment

Renal impairment

  • Mild-to-moderate renal impairment: No dose adjustment required
  • Severe renal impairment or ESRD: Used with caution and with increased monitoring for adverse effects, plasma concentrations may be increased because of altered drug absorption, distribution, and metabolism secondary to renal dysfunction
  • Dialysis: Highly bound to plasma proteins, unlikely to be significantly removed by hemodialysis or peritoneal dialysis

Hepatic impairment

  • Mild-to-moderate hepatic impairment (Child-Pugh Classes A and B): No dose adjustment required
  • Severe hepatic impairment (Child-Pugh Class C): Has not been studied

Dosage Forms & Strengths

tablet

  • 25mg
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HIV-1 Infection

Indicated in combination with other antiretroviral agents for treatment of HIV-1 infection in treatment-naïve adolescents aged 12-17 yr with HIV-1 RNA ≤100,000 copies/mL

<12 years: Safety and efficacy not established

12-17 years (weight ≥35 kg): 25 mg PO qDay; administer with a meal (see Administration)

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Interactions

Interaction Checker

and rilpivirine

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Depressive disorders (4%)

            Insomnia (3%)

            Headache (3%)

            Rash (3%)

            Increased AST (2%; grade 3 or higher)

            ALT increased (19%)

            Abnormal dreams (1%)

            Nausea (1%)

            Suicidal ideation (4-8%)

            Abdominal pain (1%)

            Vomiting (1%)

            Fatigue (1%)

            Dizziness (1%)

            Posmarketing reports

            Severe skin and hypersensitivity reactions including DRESS (Drug Reaction with Eosinophilia and Systemic Symptoms)

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            Warnings

            Contraindications

            Hypersensitivity

            Coadministration with drugs (eg, CYP inducers like phenobarbital, dexamethasone, oxcarbazepine, phenytoin, or carbamazepine) where significant decreases in rilpivirine plasma concentrations may occur, which may result in loss of virologic response and possible resistance and cross-resistance to other NNRTIs

            Contraindicated with drugs that increase gastric pH (eg, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole) that may decrease rilpivirine absorption and result in decreased rilpivirine plasma concentrations

            Cautions

            Coadministration with other NNRTIs may either increase or decrease rilpivirine; avoid use with other NNRTIs

            Supratherapeutic doses (ie, 75 mg and 300 mg qDay) have been shown to prolong the QTc interval; caution when coadministered with a drug known to increase risk of Torsade de Pointes

            May increase risk for depressive disorders

            Hepatic adverse effects reported; patients with underlying hepatitis B or C, or marked increased transaminases prior to treatment may be at increased risk; monitor for hepatotoxicity before initiating and during treatment

            Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance” have been observed in patients receiving antiretroviral therapy

            Immune reconstitution syndrome: During initial phase of combination ART treatment, patients whose immune system responds may develop an inflammatory response to indolent or residual opportunistic infections (eg, Mycobacterium avium complex, CMV, Pneumocystis pneumonia, TB)

            Severe skin and hypersensitivity reactions reported, including cases of drug reaction with eosinophilia and systemic symptoms (DRESS), with rilpivirine-containing regimens; immediately discontinue treatment if hypersensitivity or rash with systemic symptoms or elevations in hepatic serum biochemistries develop and closely monitor clinical status, including hepatic serum biochemistries

            Use caution in patients taking major CYP3A inducers or drugs that increase gastric pH

            Virologic failure & resistance

            • More rilpivirine treated individuals with HIV-1 RNA >100,000 copies/mL at the start of therapy experienced virologic failure compared to those with <100,000 copies/mL
            • Observed virologic failure rate in rilpivirine treated individuals conferred a higher rate of overall treatment resistance and cross-resistance to the NNRTI class compared to efavirenz
            • More individuals treated with rilpivirine developed lamivudine/emtricitabine associated resistance compared to efavirenz
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            Pregnancy & Lactation

            Pregnancy Category: B; Antiretroviral Pregnancy Registry 1-800-258-4263

            Lactation: Unknown whether distributed in human breast milk; The CDC recommends that mothers should not breastfeed their infants because of risk of postnatal HIV transmission

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Antiviral agent; diarylpyrimidine non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1

            Inhibits HIV-1 replication by noncompetitive inhibition of HIV-1 reverse transcriptase

            Does not inhibit the human cellular DNA polymerases alpha, beta, and gamma  

            Absorption

            Bioavailability: Absolute bioavailability unknown

            Peak Plasma Time: 4-5 hr

            Peak Plasma Concentration: 80 ng/mL (mean)

            AUC: 2397 ng•h/mL (mean)

            Food: Exposure ~40% lower when taken in a fasted condition as compared to a normal caloric meal (533 kcal) or high-fat high-caloric meal (928 kcal); when taken with only a protein-rich nutritional drink, exposures were 50% lower than when taken with a meal

            Distribution

            Protein Bound: 99.7% (primarily to albumin)

            Metabolism

            Metabolized primarily by CYP3A

            Elimination

            Half-life: 50 hr

            Excretion: feces (85%), urine (6.1%) bile, other

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            Administration

            Oral Administration

            Must administer with a meal

            Must be able to take with a meal of at least 500 calories on a regular schedule (a protein drink alone does not constitute a meal)

            If coadministered with antacids should only be administered either at least 2 hr before or at least 4 hr after rilpivirine

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            Images

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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