Efavirenz (15 brand names, 2 dosage forms, 1 route)
Available dosage forms: TABLET, CAPSULE.
Routes of administration: ORAL.
Brand Names
- ATRIPLA
- EFAVIRENZ
- EFAVIRENZ 200MG SCORED TABLETS
- EFAVIRENZ, EMTRICITABINE, AND TENOFOVIR DISOPROXIL FUMARATE
- EFAVIRENZ, LAMIVUDINE AND TENOFOVIR DISOPROXIL FUMARATE
- EFAVIRENZ, LAMIVUDINE, AND TENOFOVIR DISOPROXIL FUMARATE
- EFAVIRENZ; EMTRICITABINE AND TENOFOVIR DISOPROXIL FUMARATE
- EFAVIRENZ; EMTRICITABINE; TENOFOVIR DISOPROXIL FUMARATE
- EFAVIRENZ; LAMIVUDINE; TENOFOVIR DISOPROXIL FUMARATE
- LAMIVUDINE; ZIDOVUDINE
- LAMIVUDINE; ZIDOVUDINE; EFAVIRENZ
- STAVUDINE; LAMIVUDINE; EFAVIRENZ
- SUSTIVA
- SYMFI
- SYMFI LO
Boxed Warning
Severe acute exacerbations of hepatitis B virus (HBV) have been reported in patients who are coinfected with HIV-1 and HBV and have discontinued products containing emtricitabine (FTC) and/or tenofovir disoproxil fumarate (TDF), which are components of efavirenz, emtricitabine and tenofovir disoproxil fumarate. Closely monitor hepatic function with both clinical and laboratory follow-up for at least several months in patients who are coinfected with HIV-1 and HBV and discontinue efavirenz, emtricitabine and tenofovir disoproxil fumarate. If appropriate, initiation of anti-hepatitis B therapy may be warranted [see Warnings and Precautions (5.1) ] .
Indications and Usage
Efavirenz, emtricitabine and tenofovir disoproxil fumarate tabletsare indicated as a complete regimen or in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 40 kg.
Contraindications
Efavirenz, emtricitabine and tenofovir disoproxil fumarate tablets are contraindicated in patients with previously demonstrated clinically significant hypersensitivity (e.g., Stevens-Johnson syndrome, erythema multiforme, or toxic skin eruptions) to efavirenz, a component of efavirenz, emtricitabine and tenofovir disoproxil fumarate tablets [see Warnings and Precautions (5.2)] . Efavirenz, emtricitabine and tenofovir disoproxil fumarate tablets are contraindicated to be coadministered with voriconazole or elbasvir/grazoprevir [see Drug Interactions (7.3) and Clinical Pharmacology (12.3)].
Adverse Reactions
The following adverse reactions are discussed in other sections of the labeling: Severe Acute Exacerbations of Hepatitis B in Patients Coinfected with HIV-1 and HBV [see Warnings and Precautions (5.1)]. Rash [see Warnings and Precautions (5.2)]. Hepatotoxicity [see Warnings and Precautions (5.3)]. Psychiatric Symptoms [see Warnings and Precautions (5.5)]. Nervous System Symptoms [see Warnings and Precautions (5.6)]. New Onset or Worsening Renal Impairment [see Warnings and Precautions (5.7)]. Embryo-Fetal Toxicity [see Warnings and Precautions (5.8)]. Bone Loss and Mineralization Defects [see Warnings and Precautions (5.9)]. Convulsions [see Warnings and Precautions (5.10)]. Lactic Acidosis/Severe Hepatomegaly with Steatosis [see Warnings and Precautions (5.11)]. Immune Reconstitution Syndrome [see Warnings and Precautions (5.12)]. Fat Redistribution [see Warnings and Precautions (5.13)].
Mechanism of Action
Efavirenz, emtricitabine and tenofovir disoproxil fumarate is a fixed-dose combination of antiviral drugs EFV, FTC, and TDF [see Microbiology (12.4)].
Overdosage
If overdose occurs, the patient should be monitored for evidence of toxicity, and standard supportive treatment applied as necessary. Administration of activated charcoal may be used to aid removal of unabsorbed EFV. Hemodialysis can remove both FTC and TDF (refer to detailed information below) but is unlikely to significantly remove EFV from the blood. Efavirenz: Some patients accidentally taking 600 mg twice daily have reported increased nervous system symptoms. One patient experienced involuntary muscle contractions. Emtricitabine: Hemodialysis treatment removes approximately 30% of the FTC dose over a 3-hour dialysis period starting within 1.5 hours of FTC dosing (blood flow rate of 400 mL/min and a dialysate flow rate of 600 mL/min). It is not known whether FTC can be removed by peritoneal dialysis. Tenofovir DF: Tenofovir is efficiently removed by hemodialysis with an extraction coefficient of approximately 54%. Following a single 300 mg dose of TDF, a 4-hour hemodialysis session removed approximately 10% of the administered tenofovir dose.