Contraindicated in:
Use Cautiously in:
CV: QT interval prolongation.
Derm: rash, ERYTHEMA MULTIFORME, STEVENS-JOHNSON SYNDROME (SJS).
Endo: Graves' disease.
F and E: diarrhea.
GI: ↑ amylase, ↑ liver enzymes, abdominal pain, autoimmune hepatitis, dyspepsia, HEPATOMEGALY WITH STEATOSIS, HEPATOTOXICITY, LACTIC ACIDOSIS, nausea, PANCREATITIS, vomiting.
GU: ACUTE RENAL FAILURE/FANCONI SYNDROME, hematuria.
Hemat: neutropenia.
Metab: fat redistribution, hyperlipidemia.
MS: ↑ creatine kinase, pain, ↓ bone mineral density, arthralgia, muscle weakness, myalgia, osteomalacia, polymyositis.
Neuro: depression, headache, Guillain-Barré syndrome, abnormal dreams, aggressive behavior, anxiety, ataxia, catatonia, delusions, dizziness, drowsiness, encephalopathy, fatigue, hallucinations, impaired concentration, insomnia, manic episodes, nervousness, paranoia, peripheral neuropathy, psychoses, sedation, SEIZURES, SUICIDAL THOUGHTS/BEHAVIORS.
Misc: fever, immune reconstitution syndrome.
Drug-Drug:
(Generic available)
Therapeutic Classification: antiretrovirals
Pharmacologic Classification: non nucleoside reverse transcriptase inhibitors, nucleoside reverse transcriptase inhibitors
Efavirenz
Absorption: 50% absorbed when ingested following a high-fat meal.
Distribution: Unknown.
Protein Binding: >99%.
Metabolism/Excretion: Mostly metabolized by the liver by the CYP3A and CYP2B6 isoenzymes. 1661% excreted in feces as unchanged drug, 1434% excreted in urine (primarily as metabolites).
Half-life: Following single dose: 5276 hr. Following multiple doses: 4055 hr.
Lamivudine
Absorption: 86% absorbed after oral administration.
Distribution: Unknown.
Metabolism/Excretion: Mostly excreted unchanged in urine; <5% metabolized by the liver.
Half-life: 57 hr.
Tenofovir Disoproxil Fumarate
Absorption: Tenofovir disoproxil fumarate is a prodrug, which is split into tenofovir, the active component; absorption enhanced by food.
Distribution: Unknown.
Metabolism/Excretion: 7080% excreted unchanged in urine by glomerular filtration and active tubular secretion.
Half-life: 17 hr.
(plasma concentrations)
ROUTE | ONSET | PEAK | DURATION |
---|---|---|---|
Efavirenz (PO) | rapid | 35 hr | 24 hr |
Lamivudine (PO) | unknown | 0.9 hr | 24 hr |
Tenofovir (PO) | unknown | 2 hr | 24 hr |