elvitegravir (Rx)

Brand and Other Names:Vitekta
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 85mg
  • 150mg
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HIV Infection

For use in combination with an HIV protease inhibitor coadministered with ritonavir and with other antiretroviral drug(s) indicated for the treatment of HIV-1 infection in antiretroviral treatment-experienced adults

Elvitegravir 85-mg dose

  • 85 mg PO qDay plus atazanavir 300 mg qDay plus ritonavir 100 mg qDay
  • 85 mg PO qDay plus lopinavir 400 mg PO BID plus ritonavir 100 mg BID

Elvitegravir 150-mg dose

  • 150 mg PO qDay plus darunavir 600 mg PO BID plus ritonavir 100 mg BID
  • 150 mg PO qDay plus fosamprenavir 700 mg PO BID plus ritonavir 100 mg BID
  • 150 mg PO qDay plus tipranavir 500 mg PO BID plus ritonavir 200 mg BID

Dosage Modifications

Coadministration with rifabutin: Decrease rifabutin dose by ~75%; (eg, rifabutin 300 mg/day reduced to 150 mg every other day or 3 times per week)

Dosing Considerations

Limitation of use

  • No comparative pharmacokinetic or clinical data exist evaluating elvitegravir with cobicistat as single entities compared with Stribild
  • Elvitegravir coadministered with protease inhibitors and cobicistat is not recommended
  • Coadministration of elvitegravir with dosage regimens or HIV-1 protease inhibitors other than those listed above is not recommended

Administration

Must be taken with food

Elvitegravir plasma concentrations are lower with antacids, owing to the formation of ionic complexes in the GI tract and not to changes in gastric pH; separate elvitegravir and antacid administration by at least 2 hr

Safety and efficacy not established

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Interactions

Interaction Checker

and elvitegravir

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            2-10%

            Diarrhea (7%)

            Total bilirubin, >2.5 x ULN (6%)

            Hematuria, >75 RBC/HPF (6%)

            Serum amylase, >2 x ULN (6%)

            Creatine kinase, ≥10 x ULN (6%)

            Total cholesterol, >300 mg/dL (5%)

            Total triglycerides, >250 mg/dL (5%)

            Hyperglycemia, >250 mg/dL (5%)

            Urine glucose, +4 (4%)

            Nausea (4%)

            Headache (3%) GGT, >5 x ULN (3%)

            Neutrophils, <750/mm³ (3%)

            ALT or AST, >5 x ULN (2%)

            <2%

            Gastrointestinal disorders: Abdominal pain, dyspepsia, vomiting

            General disorders and administration site conditions: Fatigue

            Psychiatric disorders: Depression, insomnia, suicidal ideation and suicide attempt (<1%, most in subjects with a preexisting history of depression or psychiatric illness)

            Skin and subcutaneous tissue disorders: Rash

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            Warnings

            Contraindications

            None for elvitegravir; consult prescribing information for ritonavir and coadministered protease inhibitor

            Immune reconstitution syndrome reported with combination ARTs, consisting of anti-inflammatory response to indolent or residual opportunistic infections (eg, Mycobacterium avium infection, CMV, Pneumocystis jirovecii pneumonia [PCP], tuberculosis)

            Autoimmune disorders (eg, Graves disease, polymyositis, and Guillain-Barré syndrome) have also been reported to occur with immune reconstitution syndrome

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            Pregnancy & Lactation

            Pregnancy Category: B

            Antiretroviral Pregnancy Registry: 1-800-258-4263

            Lactation: Unknown whether distributed in breast milk

            In the United States, the CDC recommends that HIV-infected mothers not breastfeed their infants, to avoid risking postnatal transmission of HIV

            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

            Integrase strand transfer inhibitor (INSTI)

            Integrase is an HIV-1 encoded enzyme that is required for viral replication; inhibition of integrase prevents the integration of HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the viral infection

            Absorption

            Peak plasma time: 4 hr

            Peak plasma concentration: 1.2-1.5 mcg/mL

            Trough plasma concentration: 0.35-0.42 mcg/mL

            AUC: 18 mcg•h/mL

            Food increases mean systemic exposure of elvitegravir by 34%

            A high fat meal (~800 kcal, 50% fat) increases mean systemic exposure of elvitegravir by 87%

            Distribution

            Protein bound: 98-99%

            Metabolism

            Metabolized by CYP3A4

            Also undergoes glucuronidation via UGT1A1/3 enzymes

            Elimination

            Half-life: 8.7 hr (administered with ritonavir)

            Excretion: 94.8% feces, 6.7% urine

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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.

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            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
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            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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