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Drugs reference index «Etravirine»


Pronunciation: (E-tra-VIR-een)Class: Antiretroviral, NNRTI

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.

Special Populations

Hepatic Function Impairment

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.


No difference in pharmacokinetics within the range of 18 to 77 years of age.


No pharmacokinetic difference has been noted between men and women.


No pharmacokinetic difference has been demonstrated based on race.

Renal function impairment

Pharmacokinetics have not been studied.

Indications and Usage

Treatment of HIV-1 infection in combination with other antiretroviral agents.


Standard considerations.

Dosage and Administration


PO 200 mg twice daily following a meal.


Store at 59° to 86°F. Protect from moisture.

Drug Interactions

Amiodarone, atorvastatin, bepridil, cyclosporine, disopyramide, flecainide, lidocaine (systemic), lovastatin, mexiletine, propafenone, quinidine, sildenafil, simvastatin, sirolimus, tacrolimus, tadalafil, vardenafil

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 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.


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.


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.


Systemic exposure to amprenavir may be increased. Do not coadminister this combination with etravirine.


Systemic exposure to etravirine may be increased. Coadminister with caution.


If etravirine is not coadministered with a protease inhibitor plus ritonavir, rifabutin 300 mg daily is recommended.


Ritonavir 600 mg twice daily may decrease etravirine plasma levels, resulting in a loss of efficacy. Do not coadminister ritonavir 600 mg twice daily.


Etravirine and voriconazole plasma levels may be increased.


Warfarin plasma levels may be increased. Monitor anticoagulant parameters.

Laboratory Test Interactions

None well documented.

Adverse Reactions


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%).

Lab Tests

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.

Fat redistribution

Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, breast enlargement, and cushingoid appearance, have been reported.

Immune reconstitution syndrome

Has been reported in patients treated with combination antiretroviral therapy.

Skin reactions

Severe and life-threatening skin reactions, including Stevens-Johnson syndrome, hypersensitivity reaction, and erythema multiforme, may occur.



Experience is limited.

Patient Information

  • Warn patient that this drug is not to be used by itself, but in combination with other antiretroviral agents, and not to change the dose or stop taking any other antiviral agents unless advised by health care provider.
  • Advise patient not to take etravirine on an empty stomach and that the type of food is not important.
  • Advise patients to take tablets whole with a liquid such as water and not to chew the tablets. If the tablets cannot be swallowed whole, the tablets may be placed in a glass of water, stirred well until water looks milky, then drunk immediately, rinsing the glass with water several times, swallowing the rinse each time to make sure the entire dose is taken.
  • Advise patient that etravirine may cause changes in body fat distribution and that the cause and long-term health effects of these changes are not known at this time. Advise patient to report changes in body fat distribution to heath care provider.
  • Advise patient that etravirine does not completely eliminate HIV virus and, therefore, does not reduce the risk of transmitting HIV to others. Appropriate precautions (eg, practicing safer sex using a latex or polyurethane condom) must be followed.
  • Advise patients that if a dose is missed within 6 h of the time they usually take the dose, to take the missed dose following a meal as soon as possible. Then, take the next dose at the regularly scheduled time. If a dose is missed by more than 6 h of the usual administration time, the patient should wait and take the next dose at the regularly scheduled time. The dose should not be doubled to make up for the missed dose.

Copyright © 2009 Wolters Kluwer Health.

  • Etravirine MedFacts Consumer Leaflet (Wolters Kluwer)
  • etravirine Advanced Consumer (Micromedex) - Includes Dosage Information
  • Intelence Prescribing Information (FDA)
  • Intelence Consumer Overview

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