efavirenz (Rx)

Brand and Other Names:Sustiva
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 50mg
  • 200mg

tablet

  • 600mg
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HIV Infection

Indicated in combination with other antiretroviral agents for HIV-1 infection

600 mg PO qDay; used in combination with protease inhibitor and/or NRTIs

Dosage Modifications

Coadministration with voriconazole: Increase voriconazole maintenance dose to 400 mg q12hr and decrease efavirenz dose to 300 mg qDay (using capsule formulation)

Coadministration with rifampin: If weight >50 kg, increase efavirenz to 800 mg qDay

Renal impairment: No dosage adjustment needed

Hepatic impairment

  • Mild (Child-Pugh Class A): Dose adjustment not necessary; use caution
  • Moderate-to-severe (Child Pugh Class B or C): Not recommended

Dosage Forms & Strengths

capsule

  • 50mg
  • 200mg

tablet

  • 600mg
more...

HIV Infection

NOTE: The NIH pediatric HIV treatment guideline (March 2016) differs from the prescribing information and recommends that efavirenz generally should NOT be used in children aged <3 yr

Indicated in combination with other antiretroviral agents for HIV-1 infection in pediatric patients >3 months old and weighing ≥3.5 kg

<3 months: Safety and efficacy not established

≥3 months (prescribing information)

  • 3.5 kg to <5 kg: 100 mg PO qDay
  • 5 to <7.5 kg: 150 mg PO qDay
  • 7.5 to <15 kg: 200 mg PO qDay
  • 15 to <20 kg: 250 mg PO qDay
  • 20 to <25 kg: 300 mg PO qDay
  • 25 to <32.5 kg: 350 mg PO qDay
  • 32.5 to <40 kg: 400 mg PO qDay
  • ≥40 kg: 600 mg PO qDay

NIH pediatric HIV treatment guidelines (March 2016)

  • Investigational dosing for 3 months to <3 years based on CYP 2B6 genotype
  • Extensive metabolizers (ie, CYP 2B6 516 GG and GT genotype)
    • 3 to <5 kg: 200 mg PO qDay
    • 5 to <7 kg: 300 mg PO qDay
    • 7 to <14 kg: 400 mg PO qDay
    • 14 to <17 kg: 500 mg PO qDay
    • ≥17 kg: 600 mg PO qDay
  • Slow metabolizers (ie, CYP 2B6 516 TT genotype)
    • 3 to <7 kg: 50 mg PO qDay
    • 7 to <14 kg: 100 mg PO qDay
    • ≥14kg: 150 mg PO qDay
  • ≥3 years
    • 10 to <15 kg: 200 mg PO qDay
    • 15 to <20 kg: 250 mg PO qDay
    • 20 to <25 kg: 300 mg PO qDay
    • 25 to <32.5 kg: 350 mg PO qDay
    • 32.5 to <40 kg: 400 mg PO qDay
    • ≥40 kg: 600 mg PO qDay

Dosage Modifications

Coadministration with voriconazole: If weight >40 kg and age >12 yr, increase voriconazole maintenance dose to 400 mg q12hr and decrease efavirenz dose to 300 mg qDay (using capsule formulation)

Coadministration with rifampin: If weight >40 kg, increase efavirenz to 800 mg qDay

Renal impairment: No dosage adjustment needed

Hepatic impairment

  • Mild (Child-Pugh Class A): Dose adjustment not necessary; use caution
  • Moderate-to-severe (Child Pugh Class B or C): Not recommended
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Interactions

Interaction Checker

and efavirenz

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Total cholesterol increased (20-40%)

            Diarrhea (3-14%, children up to 39%)

            HDL increased (25-35%)

            Dizziness (28.1%)

            Rash (5-26%)

            Fever (children 21%)

            Depression (19%)

            Insomnia (16.3%)

            Cough (children 16%)

            Vomiting (3-12%)

            Anxiety (2-13%)

            Nausea (2-12%)

            1-10%

            Neutropenia (2-10%)

            Pruitis (9%)

            Impaired concentration (8.3%)

            Transaminases increased (2-8%)

            Somnolence (7.0%)

            Abnormal dreams (6.2%)

            Amylase increased (6%)

            Hyperglycemia (2-5%)

            Dyspepsia (4%)

            Abdominal pain (2-3%)

            Anorexia (2%)

            Hallucinations (1.2%)

            Postmarketing Reports

            Serious psychiatric events: severe depression (2.4%), suicidal ideation (0.7%), nonfatal suicide attempts (0.5%), aggressive behavior (0.4%), paranoid reactions (0.4% ), manic reactions (0.2%)

            Stevens-Johnson syndrome

            Erythema multiforme

            Exfoliative dermatitis

            Hepatotoxicity

            Pancreatitis

            Cardiac arrhythmias

            Prolonged sedation, or respiratory depression

            Vertigo

            Catatonia

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            Warnings

            Contraindications

            Previously demonstrated clinically significant hypersensitivity (eg, Stevens-Johnson syndrome, erythema multiforme, or toxic skin eruptions)

            Coadministration of efavirenz with elbasvir and grazoprevir

            Cautions

            Hepatic impairment; not recommended for patients with moderate or severe hepatic impairment because there are insufficient data to determine whether dose adjustment is necessary

            Monitor liver function tests before and during treatment in patients with underlying hepatic disease, including hepatitis B or C coinfection, marked transaminase elevations, or who are taking medications associated with liver toxicity; among reported cases of hepatic failure, a few occurred in patients with no pre-existing hepatic disease; weigh risk/benefit if AST/ALT >5 xULN; discontinue therapy if elevation of serum transaminases is accompanied by clinical signs or symptoms of hepatitis or hepatic decompensation

            Redistribution of fat may occur (cushingoid appearance)

            Risk of serious psychiatric events (eg, depression, suicidality, paranoia, manic episodes); immediate medical evaluation recommended for serious psychiatric symptoms such as severe depression or suicidal ideation; there have been occasional postmarketing reports of death by suicide, delusions, psychosis-like behavior and catatonia; a causal relationship to the use of efavirenz cannot be determined from these reports

            CNS symptoms reported (eg, dizziness, insomnia, impaired concentration, somnolence, abnormal dreams, and hallucinations); nervous system symptoms (NSS) are frequent and usually begin 1-2 days after initiating therapy and resolve in 2-4 weeks; dosing at bedtime may improve tolerability; NSS are not predictive of onset of psychiatric symptoms

            Risk of skin rash - discontinue if severe rash associated wtih blistering, desquamation, mucosal involvement, or fever

            Use caution in history of seizures

            Total cholesterol and triglyceride elevations may occur; monitor before therapy and periodically thereafter

            Women should avoid pregnancy; use 2 forms of contraception including a barrier method; postmarketing reports of contraceptive failure in patients on efavirenz while on an implantable hormonal contraceptive; avoid administration in first trimester of pregnancy as fetal harm may occur

            Risk of immune reconstitution syndrome if used in combination with other antiretroviral drugs; immune reconstitution syndrome may necessitate further evaluation and treatment

            Autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) reported in the setting of immune reconstitution, however, the time to onset is more variable, and can occur many months after initiation of treatment

            Not for use as a single agent or add on as a sole agent to a failing regimen; consider potential for cross-resistance when choosing other agents

            Not recommended with ATRIPLA, which contains efavirenz, emtricitabine, and tenofovir disoproxil fumarate, unless needed for dose adjustment when coadministered with rifampin

            Postmarketing cases of catatonia reported, which may be associated with increased efavirenz exposure; patients with serious psychiatric adverse experiences should seek immediate medical evaluation to assess possibility that symptoms may be related to therapy, and if so, to determine whether risks of continued therapy outweigh the benefits

            Consider alternatives in patients taking other medications with known risk of Torsade de Pointes or in patients at higher risk of Torsade de Pointes

            Interactions

            • Efavirenz plasma concentrations may be altered by substrates, inhibitors, or inducers of CYP3A
            • Likewise, efavirenz may alter plasma concentrations of drugs metabolized by CYP3A or CYP2B6
            • The most prominent effect of efavirenz at steady-state is induction of CYP3A and CYP2B6
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            Pregnancy & Lactation

            Pregnancy Category: D

            Lactation: Unknown if distributed in human milk; the CDC advises HIV-infected women not to breastfeed to avoid 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

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

            Absorption

            Peak Plasma Time: 2.5-4 hr

            Metabolism

            Metabolized by liver CYP3A4 and CYP2B6

            Inhibits: CYP2C9; CYP2C19, and CYP3A4 (in vitro)

            Induces: CYP3A4 (in vivo)

            Elimination

            Half-Life: 41 hr ± 20 hr

            Excretion: Urine (14-34%); feces (16-61%)

            Distribution

            Protein binding: 99% (albumin)

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            Administration

            Oral Administration

            Swallow capsule or table whole; do not break tablet

            Take only on empty stomach, preferably at bedtime

            Capsule sprinkle method

            • If unable to swallow capsule or tablet, capsule contents may be mixed with a small amount of food (ie ~2 teaspoonfuls) or room temperature formula (ie, 10 mL)
            • Consume food/formula mixture within 30 minutes of mixing
            • Do not consume additional food for at least 2 hr after administration
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            Formulary

            FormularyPatient Discounts

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

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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.
            • 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.