Trade Names:Intelence- Tablets 100 mg
Binds directly to reverse transcriptase and blocks RNA- and DNA-dependent DNA polymerase activities by disrupting the enzyme's catalytic site.
T max following oral administration is about 2.5 to 4 h. Bioavailability is unknown. Systemic exposure is decreased about 50% when taken under fasting conditions.
Protein binding is approximately 99.9%, primarily to albumin.
Etravirine is metabolized by CYP2C9, CYP2C19, and CYP3A4. The major metabolites are 90% less active than etravirine.
Elimination is 93.7% in the feces and 1.2% in the urine. 81.2% to 86.4% of the dose recovered in the feces is unchanged etravirine. Mean terminal t ½ is 41 h.
Etravirine is primarily metabolized by the liver; however, steady-state pharmacokinetics were similar in subjects with healthy, mildly impaired, and moderately impaired hepatic function. The effect of severe hepatic function impairment has not been studied.Age
No difference in pharmacokinetics within the range of 18 to 77 years of age.Gender
No pharmacokinetic difference has been noted between men and women.Race
No pharmacokinetic difference has been demonstrated based on race.Renal function impairment
Pharmacokinetics have not been studied.
Treatment of HIV-1 infection in combination with other antiretroviral agents.
PO 200 mg twice daily following a meal.
Store at 59° to 86°F. Protect from moisture.
Etravirine may decrease plasma levels of these agents. Use with caution.Atazanavir, indinavir
Plasma levels may be decreased by etravirine. Do not administer without low-dose ritonavir.Atazanavir/Ritonavir
Atazanavir minimum plasma levels may be reduced while etravirine plasma levels may be increased.Carbamazepine, phenobarbital, phenytoin, rifampin, rifapentine
May induce etravirine metabolism, decreasing plasma levels and resulting in loss of efficacy. Do not coadminister.Clarithromycin
Systemic exposure to clarithromycin may be decreased while exposure to the active metabolite, 14-hydroxy-clarithromycin, may be increased. Consider azithromycin as alternative treatment against Mycobacterium avium complex.Darunavir/Ritonavir, saquinavir/ritonavir
Etravirine systemic exposure may be reduced. Dosage adjustments do not appear necessary. If etravirine is administered with darunavir/ritonavir or saquinavir/ritonavir, do not coadminister rifabutin because etravirine exposure will be reduced.Delavirdine
Etravirine plasma levels may be increased. Do not coadminister.Dexamethasone, efavirenz, nevirapine, St. John's wort, tipranavir/ritonavir
Etravirine plasma levels may be decreased, resulting in loss of efficacy. Do not coadminister. Coadminister dexamethasone with caution or use an alternative agent.Diazepam, fluvastatin
Plasma levels may be increased by etravirine.Fluconazole, itraconazole, ketoconazole, posaconazole
May inhibit etravirine metabolism, resulting in elevated plasma levels. In addition, etravirine may increase itraconazole and ketoconazole metabolism, resulting in decreased plasma levels of these agents.Fosamprenavir, nelfinavir
Plasma levels of amprenavir and nelfinavir may be elevated. Do not administer these protease inhibitors with etravirine without low-dose ritonavir.Fosamprenavir/Ritonavir
Systemic exposure to amprenavir may be increased. Do not coadminister this combination with etravirine.Lopinavir/Ritonavir
Systemic exposure to etravirine may be increased. Coadminister with caution.Rifabutin
If etravirine is not coadministered with a protease inhibitor plus ritonavir, rifabutin 300 mg daily is recommended.Ritonavir
Ritonavir 600 mg twice daily may decrease etravirine plasma levels, resulting in a loss of efficacy. Do not coadminister ritonavir 600 mg twice daily.Voriconazole
Etravirine and voriconazole plasma levels may be increased.Warfarin
Warfarin plasma levels may be increased. Monitor anticoagulant parameters.
None well documented.
Hypertension (3%); angina pectoris, atrial fibrillation, MI, syncope (less than 2%).
Fatigue, headache, peripheral neuropathy (3%); abnormal dreams, amnesia, anxiety, confusional state, convulsion, disorientation, hyperinsomnia, hypoesthesia, insomnia, nervousness, nightmares, paresthesia, sleep disorder, sluggishness, somnolence, tremor (less than 2%).
Rash (17%); dry skin, hyperhidrosis, lipohypertrophy, night sweats, prurigo, swelling face (less than 2%); erythema multiforme, hypersensitivity rash, Stevens-Johnson syndrome.
Blurred vision, vertigo (less than 2%).
Nausea (14%); diarrhea (5%); abdominal pain (3%); vomiting (2%); abdominal distention, constipation, dry mouth, flatulence, gastritis, gastroesophageal reflux disease, hematemesis, pancreatitis, retching, stomatitis (less than 2%).
Gynecomastia, renal failure (less than 2%).
Anemia, hemolytic anemia (less than 2%).
Cytolytic hepatitis, hepatic stenosis, hepatitis, hepatomegaly (less than 2%).
Elevated creatinine, glucose, lipase, LDL, pancreatic amylase, total cholesterol, and triglycerides; decreased hemoglobin, neutrophils, and platelet count.
Anorexia, diabetes mellitus, dyslipidemia (less than 2%).
Bronchospasm, external dyspnea (less than 2%).
Drug hypersensitivity, immune reconstitution syndrome (less than 2%).
Category B .
Undetermined. HIV-infected mothers should not breast-feed to avoid risking potential transmission of HIV to infant.
Safety and efficacy not established.
Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, breast enlargement, and cushingoid appearance, have been reported.
Has been reported in patients treated with combination antiretroviral therapy.
Severe and life-threatening skin reactions, including Stevens-Johnson syndrome, hypersensitivity reaction, and erythema multiforme, may occur.
Experience is limited.
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