etravirine (Rx)

Brand and Other Names:Intelence
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 25mg
  • 100mg
  • 200mg

HIV Infection

Treatment of HIV-1 infection in combination with ≥2 additional antiretroviral agents in treatment-experienced patients exhibiting viral replication with documented non-nucleoside reverse transcriptase inhibitor (NNRTI) resistance

200 mg PO q12hr

Renal Impairment

No dosage adjustment required

Hepatic Impairment

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

Severe (Child-Pugh class C): Pharmacokinetics have not been evaluated

Dosage Forms & Strengths

tablet

  • 25mg
  • 100mg
  • 200mg

HIV Infection

Treatment of HIV-1 infection in combination with ≥2 additional antiretroviral agents in treatment-experienced patients ≥2 years exhibiting viral replication with documented non-nucleoside reverse transcriptase inhibitor (NNRTI) resistance

<2 years: Safety and efficacy not established

2 to <18 years and ≥10 kg

  • 10 to <20 kg: 100 mg PO q12hr
  • 20 to <25 kg: 125 mg PO q12hr
  • 25 to <30 kg: 150 mg PO q12hr
  • ≥30 kg: 200 mg PO q12hr
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Interactions

Interaction Checker

and etravirine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Rash (16.9%)

            Nausea (13.9%)

            Increased LDL (13%)

            1-10%

            GI disorders (2.3-5.2%)

            Fatigue (3.3%)

            Peripheral neuropathy (4%)

            Increased creatinine (2%)

            Diarrhea (2%)

            <1%

            Stevens-Johnson syndrome

            Erythema multiforme

            Angina

            Angioedema

            Toxic epidermal necrolysis (including reports of fatalities)

            Hypersensitivity reactions (including cases of hepatic failure)

            Postmarketing Reports

            Immune system disorders: Severe hypersensitivity reactions including DRESS and cases of hepatic failure

            Musculoskeletal and connective tissue disorders: Rhabdomyolysis

            Skin and subcutaneous tissue disorders: Fatal cases of toxic epidermal necrolysis

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            Warnings

            Contraindications

            None

            Cautions

            Hypersensitivity

            Risk of severe skin reactions (eg, Stevens-Johnson Syndrome, erythema multiforme, toxic epidermal necrolysis)

            Hypersensitivity reactions including drug rash with eosinophilia and systemic symptoms (DRESS) reported; characterized by rash, constitutional findings, and sometimes organ dysfunction; discontinue if severe rash develops and initiate appropriate therapy

            Risk of immune reconstitution syndrome

            50% decrease in absorption when administered under fasting conditions: only take with meal

            Drug interactions overview

            • Etravirine is a CYP3A, CYP2C9, and CYP2C19 substrate; coadministration with CYP3A, CYP2C9, and CYP2C19 inhibitors or inducers may alter efficacy or adverse reaction profile of etravirine
            • Etravirine is a CYP3A inducer and CYP2C9, CYP2C19 and P-glycoprotein (Pgp) inhibitor; coadministration of CYP3A, CYP2C9, CYP2C19, or P-gp substrate may alter the efficacy or toxicity of the coadministered drug(s)
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            Pregnancy & Lactation

            Pregnancy

            An ART pregnancy registry has been established (1-800-258-4263); prospective pregnancy data from the Antiviral Pregnancy Registry (APR) not sufficient to adequately assess risk of birth defects or miscarriage

            Etravirine use during pregnancy evaluated in a limited number of individuals as reported by the APR, and available data show 1 birth defect in 66 first trimester exposures to etravirine-containing regimens

            Lactation

            The Centers for Disease Control and Prevention recommend HIV-1-infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV

            Based on limited data, etravirine has been shown to be present in human breast milk

            No data on the effects of etravirine on the breastfed infant, or the effects of etravirine on milk production Because of potential for HIV-1 transmission (in HIV-negative infants), developing viral resistance (in HIV-positive infants), and adverse reactions in breastfed infants similar to those seen in adults, instruct mothers not to breastfeed during treatment

            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

            Non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1

            Binds directly to reverse transcriptase and blocks RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme's catalytic sites

            Absorption

            AUC: 4380 ng·hr/mL

            Peak plasma time: 2.5-4 hr

            Effects of food

            • AUC to etravirine was decreased by about 50% when administered under fasting conditions, as compared to when administered following a meal
            • Meals contained a total caloric content ranging from 345-1160 kilocalories (17-70 grams fat)

            Distribution

            Protein Bound: 99.9%

            Metabolism

            Metabolized in liver by CYP3A4, CYP2C9, and CYP2C19

            Induces CYP3A4

            Inhibits CYP2C9 and CYP2C19

            Elimination

            Half-Life: 41 hr +/- 20 hr

            Excretion: Feces (93.7% [81.2% unchanged]); urine (1.2% [86.4% unchanged])

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            Administration

            Oral Administration

            Take ONLY after a meal

            Swallow tablets whole

            Unable to swallow tablet whole

            • Place tablet(s) in 5 mL (1 teaspoon) of water, or at least enough liquid to cover the medication; stir until water looks milky
            • Add ~15 mL (1 tablespoon) of liquid (eg, water, orange juice, or milk) Do not place tablets in orange juice or milk without first adding water
            • Avoid use of warm (temperature > 104°F [>40°C]) or carbonated beverages
            • Drink mixture immediately
            • Rinse glass several times with liquid and completely swallow the rinse each time to ensure patient takes the entire dose

            Storage

            Tablets: Store at 25°C (77°F); with excursions permitted to 15-30°C (59-86°F)

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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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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.