Efavirenz

Efavirenz in combination with other antiretroviral agents is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults and in pediatric patients at least 3 months old and weighing at least 3.5 kg. Efavirenz is a non-nucleoside reverse transcriptase inhibitor indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 infection in adults and in pediatric patients at least 3 months old and weighing at least 3.5 kg.( 1 )

• Efavirenz should be taken orally once daily on an empty stomach, preferably at bedtime. • Recommended adult dose: 600 mg. • With rifampin, increase efavirenz dose to 800 mg once daily for patients weighing 50 kg or more. • Pediatric dosing is based on weight
• Hepatic Function Monitor hepatic function prior to and during treatment with efavirenz [ see Warnings and Precautions ]
• Efavirenz is not recommended in patients with moderate or severe hepatic impairment (Child Pugh B or C) [ see Warnings and Precautions and Use in Specific Populations ]
• Adults The recommended dosage of efavirenz is 600 mg orally, once daily, in combination with a protease inhibitor and/or nucleoside analogue reverse transcriptase inhibitors (NRTIs)
• It is recommended that efavirenz be taken on an empty stomach, preferably at bedtime
• The increased efavirenz concentrations observed following administration of efavirenz with food may lead to an increase in frequency of adverse reactions [see Clinical Pharmacology ]
• Dosing at bedtime may improve the tolerability of nervous system symptoms [see Warnings and Precautions , Adverse Reactions , and Patient Counseling Information ]
• Efavirenz capsules or tablets should be swallowed intact with liquid
• Concomitant Antiretroviral Therapy Efavirenz must be given in combination with other antiretroviral medications [see Indications and Usage , Warnings and Precautions , Drug Interactions , and Clinical Pharmacology ]. …

• Efavirenz Tablets, USP 600 mg 600-mg tablets are yellow, biconvex, capsule-shaped, film-coated tablets, engraved with "ML 12" on one side and plain on the other side. •Tablets: 600 mg ( 3 )

• The safety, pharmacokinetic profile, and virologic and immunologic responses of efavirenz were evaluated in antiretroviral-naive and -experienced HIV-1 infected
• Pediatric patients 3 months to 21 years of age in three open-label clinical trials [see Adverse Reactions ,Clinical Pharmacology , and Clinical Studies ]. …

Clinical studies of efavirenz did not include sufficient numbers of subjects aged 65 years and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other therapy.

• Advise the patient to read the FDA-approved patient labeling (Patient Information and Instructions for Use)
• Drug Interactions A statement to patients and healthcare providers is included on the product's bottle labels: ALERT : Find out about medicines that should NOT be taken with efavirenz tablets
• Efavirenz tablets may interact with some drugs; therefore, advise patients to report to their doctor the use of any other prescription, nonprescription medication
• General Information for Patients Infom patients that efavirenz tablets is not a cure for HIV-1 infection and patients may continue to experience illnesses associated with HIV-1 infection, including opportunistic infections. …

• Efavirenz is contraindicated in patients with previously demonstrated clinically significant hypersensitivity (e.g., Stevens-Johnson syndrome, erythema multiforme, or toxic skin eruptions) to any of the components of this product. • Coadministration of efavirenz with elbasvir and grazoprevir is contraindicated [ see Warnings and Precautions ( 5.1 ) and Drug Interactions ( 7.1 ) ]. …

Coadministration of efavirenz can alter the concentrations of other drugs and other drugs may alter the concentrations of efavirenz. The potential for drug-drug interactions should be considered before and during therapy. ( 7 ) 7.1 Potential for efavirenz to Affect other Drugs Efavirenz has been shown in vivo to induce CYP3A and CYP2B6. Other compounds that are substrates of CYP3A or CYP2B6 may have decreased plasma concentrations when coadministered with efavirenz 7.2 Potential for Other Drugs to Affect efavirenz Drugs that induce CYP3A activity (e.g., phenobarbital, rifampin, rifabutin) would be expected to increase the clearance of efavirenz resulting in lowered plasma concentrations [see …

• QTc prolongation : Consider alternatives to efavirenz in patients taking other medications with a known risk of Torsade de Pointes or in patients at higher risk of Torsade de Pointes. ( 5.2 ) • Do not 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. ( 5.3 ) •Not recommended with ATRIPLA, which contains efavirenz, emtricitabine, and tenofovir disoproxil fumarate, unless needed for dose adjustment when coadministered with rifampin. ( 5.4 ) • Serious psychiatric symptoms : Immediate medical evaluation is recommended for serious psychiatric symptoms such as severe depression or suicidal ideation. …

The most significant adverse reactions observed in patients treated with efavirenz are: •psychiatric symptoms [see Warnings and Precautions ( 5.5 )], •nervous system symptoms [see Warnings and Precautions ( 5.6 )], •rash [see Warnings and Precautions ( 5.8 )]. •hepatotoxicity [see Warnings and Precautions ( 5.9 )] Most common adverse reactions (>5%, moderate-severe) are impaired concentration, abnormal dreams, rash, dizziness, nausea, headache, fatigue, insomnia, and vomiting.( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Macleods Pharmaceutical Ltd at 1-888-943-3210 or 1-855-926-3384 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . …

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to efavirenz during pregnancy. Physicians are encouraged to register patients by calling the Antiretroviral Pregnancy Registry at 1-800-258-4263. …

Some patients accidentally taking 600 mg twice daily have reported increased nervous system symptoms. One patient experienced involuntary muscle contractions. Treatment of overdose with efavirenz should consist of general supportive measures, including monitoring of vital signs and observation of the patient's clinical status. Administration of activated charcoal may be used to aid removal of unabsorbed drug. There is no specific antidote for overdose with efavirenz. Since efavirenz is highly protein bound, dialysis is unlikely to significantly remove the drug from blood.

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