Trade Names:Sustiva- Capsules 50 mg- Capsules 200 mg- Tablets 600 mg
Noncompetitive inhibition of HIV-1 reverse transcriptase.
C max is 1.6 to 9.1 mcM. T max is 3 to 5 h. Food significantly increases the AUC and C max . Should be taken on an empty stomach.
Approximately 99.5% to 99.75% is protein bound, predominantly to albumin.
Metabolized in the liver by CYP-450 (primarily CYP3A4 and CYP2B6) to inactive metabolites.
The half-life is 52 to 76 h (single dose) and 40 to 55 h (multiple doses). Approximately 14% to 34% is excreted in the urine (less than 1% as unchanged drug), and 16% to 61% is excreted in the feces.
Pharmacokinetics have not been studied. Because less than 1% is excreted unchanged in the urine, the impact of renal function impairment should be minimal.Hepatic Function Impairment
Pharmacokinetics have not been adequately studied.Gender
Pharmacokinetics similar between men and women.Race
Pharmacokinetics similar between racial groups studied.
Treatment of HIV-1 infection in combination with other antiretroviral agents.
Concomitant use with astemizole, bepridil, cisapride, ergot derivatives, midazolam, pimozide, St. John's wort, triazolam, or voriconazole (in standard doses); hypersensitivity to any component of the product.
PO 600 mg/day in combination with other antiretroviral agents.Children 10 to less than 15 kg
PO 200 mg/day in combination with other antiretroviral agents.Children 15 to less than 20 kg
PO 250 mg/day in combination with other antiretroviral agents.Children 20 to less than 25 kg
PO 300 mg/day in combination with other antiretroviral agents.Children 25 to less than 32.5 kg
PO 350 mg/day in combination with other antiretroviral agents.Children 32.5 to less than 40 kg
PO 400 mg/day in combination with other antiretroviral agents.Children at least 40 kg
PO 600 mg/day in combination with other antiretroviral agents.Coadministration With VoriconazoleAdults
PO When coadministered with voriconazole, increase the voriconazole maintenance dosage to 400 mg every 12 h, and decrease the efavirenz dosage to 300 mg once daily, using the capsule formulation.
Store at room temperature, between 59° and 86°F.
May elevate levels of these drugs, which may increase the risk of arrhythmias, hematologic abnormalities, or other potentially serious adverse reactions. Coadministration is contraindicated.Atazanavir, calcium channel blockers (eg, diltiazem, felodipine, nicardipine, nifedipine, verapamil), clarithromycin, fosamprenavir, HMG-CoA reductase inhibitors (atorvastatin, pravastatin, simvastatin), indinavir, itraconazole, ketoconazole, lopinavir, methadone, rifabutin, saquinavir, sertraline
Efavirenz may decrease plasma concentrations of these agents, which could reduce their efficacy.Carbamazepine, phenobarbital, phenytoin
Plasma concentrations of the anticonvulsant may decrease.Carbamazepine, phenobarbital, phenytoin, rifampin
May decrease plasma levels of efavirenz, which may reduce antiviral activity.Ethinyl estradiol, nelfinavir, ritonavir
Efavirenz may increase plasma concentrations, which could increase activity or toxicity of these agents.Food
Efavirenz plasma concentrations may be elevated, increasing the risk of adverse reactions. Efavirenz should be taken on an empty stomach, preferably at bedtime.Ritonavir
May increase efavirenz plasma levels, which could increase adverse reactions.St. John's wort
May reduce efavirenz plasma concentrations, which may decrease the clinical efficacy. Coadministration is contraindicated.Voriconazole
Contraindicated at standard doses. Voriconazole doses should be increased while efavirenz doses should be decreased.Warfarin
Plasma concentrations may be increased or decreased.
False-positive urine assay screening test for cannabinoid may occur.
Flushing, palpitations (postmarketing).
Depression (19%); dizziness/light-headedness/fainting (16%); anxiety (13%); headache (11%); fatigue (8%); insomnia, nervousness (7%); impaired concentration (5%); abnormal dreams (3%); somnolence (2%); abnormal coordination, aggressive reactions, agitation, asthenia, ataxia, cerebellar coordination and balance disturbances, convulsions, delusions, emotional lability, hypoesthesia, mania, neuropathy, neurosis, paranoia, paresthesia, psychosis, suicide, tremor (postmarketing).
Rash (46%); pruritus (9%); erythema multiforme, exfoliative dermatitis, nail disorder, necrosis requiring surgery, photoallergic dermatitis, skin discoloration, Stevens-Johnson syndrome, toxic epidermal necrolysis (postmarketing).
Abnormal vision, tinnitus (postmarketing).
Diarrhea (39%); vomiting (12%); nausea (10%); vomiting (6%); dyspepsia (4%); abdominal pain (3%); constipation, malabsorption (postmarketing).
Hepatic enzyme increase, hepatic failure, hepatitis (postmarketing).
Elevated triglycerides (11%); decreased neutrophils (10%); elevated ALT, AST, and gamma-glutamyltransferase (8%); increased amylase (6%); increased glucose (5%).
Hypercholesterolemia, hypertriglyceridemia, redistribution of body fat (postmarketing).
Arthralgia, myalgia, myopathy (postmarketing).
Cough (16%); dyspnea (postmarketing).
Fever (21%); aches/discomfort (14%); pain (13%); allergic reactions (postmarketing).
Consider monitoring cholesterol and triglycerides. Monitor LFTs in patients with history of hepatitis B and/or C.
Category D .
Undetermined. HIV-infected mothers should not breast-feed their infants.
Use with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.
Use with caution.
Use with caution in patients with history of seizures. Convulsions have been reported.
Reported in 53% of patients.
Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement, peripheral wasting, facial wasting, breast enlargement, and cushingoid appearance, may occur.
Monitor liver enzymes in patients with known or suspected history of hepatitis B or C infection and in patients receiving medication associated with liver toxicity.
May occur, necessitating further evaluation and treatment.
Increases in total cholesterol and triglycerides have been reported.
Resistant virus may emerge rapidly.
Serious adverse psychiatric experiences have been reported. Patients with a history of psychiatric disorders may be at greater risk. There have been occasional reports of death by suicide, delusions, and psychosis-like behavior.
Reported in 26% of adults and 46% of children.
Increased CNS symptoms, involuntary muscle contractions.
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