Intelence

Generic Name: Etravirine
Class: Nonnucleoside Reverse Transcriptase Inhibitors
VA Class: AM800
Chemical Name: 4-{[6-amino-5-bromo-2-((4-cyanophenyl)amino)-4-pyrimidinyl]oxy}-3,5-dimethylbenzonitrile
Molecular Formula: C₂₀H₁₅BrN₆O
CAS Number: 269055-15-4

Introduction

Antiretroviral; nonnucleoside reverse transcriptase inhibitor (NNRTI).^{1 2 3 200}

Uses for Intelence

Treatment of HIV Infection

Treatment of HIV-1 infection in conjunction with other antiretrovirals.¹

Use only in antiretroviral-experienced (previously treated) patients with evidence of HIV-1 replication and HIV-1 strains resistant to an NNRTI and other antiretrovirals.^{1 2 3}

Slideshow: Top Prevention Tips: Springtime Allergies

Consider the following factors when initiating etravirine: Because of concerns regarding cross-resistance, use individual’s prior antiretroviral treatment and viral resistance testing to guide therapy;¹ use in conjunction with other active antiretrovirals is associated with greater likelihood of treatment response;¹ regimen that includes only etravirine and nucleoside reverse transcriptase inhibitors (NRTIs) not recommended in those who experienced virologic failure while receiving a previous NNRTI-containing regimen.¹

Concomitant use of etravirine and another NNRTI (e.g., delavirdine, efavirenz, nevirapine, rilpivirine) not recommended.^{1 200 226}

Safety and efficacy not established in antiretroviral-naive (have not previously received antiretroviral therapy) adults or pediatric patients;¹ do not use in initial treatment regimens in such patients.^{200 201}

Intelence Dosage and Administration

Administration

Oral Administration

Administer orally after a meal.¹ Food enhances bioavailability.^{1 11} (See Food under Pharmacokinetics.)

Swallow tablets whole with a liquid (e.g., water);¹ do not chew.¹

For patients unable to swallow tablets whole, administer as a dispersion.¹ Place dose of tablets in 5 mL of water (enough water to cover the tablets) and stir until a uniform, milky dispersion occurs.¹ If desired, add more water or, alternatively, orange juice or milk;¹ do not use grapefruit juice or carbonated or warm (>40°C) beverage.¹ Consume dispersion promptly; to ensure consumption of entire dose, rinse the glass several times with water, orange juice, or milk and swallow each rinse.¹

Dosage

Must be given in conjunction with other antiretrovirals.¹

Pediatric Patients

Treatment of HIV Infection

Antiretroviral-experienced Pediatric Patients

Oral

To avoid medication errors, use extra care in calculating dose, transcribing medication order, dispensing prescription, and providing dosing instructions.¹

Children 6 years to <18 years of age weighing ≥16 kg: Dosage is based on weight and should not exceed recommended adult dosage.¹ (See Table 1.)

Table 1. Dosage of Etravirine for Pediatric Patients 6 Years to <18 Years of Age Weighing ≥16 kg

Body Weight	Dosage
16 to <20 kg	100 mg twice daily
20 to <25 kg	125 mg twice daily
25 to <30 kg	150 mg twice daily
≥30 kg	200 mg twice daily

Adults

Treatment of HIV Infection

Antiretroviral-experienced Adults

Oral

200 mg twice daily.¹ Give dose as a single 200-mg tablet or two 100-mg tablets.¹

Special Populations

Hepatic Impairment

Dosage adjustment not necessary in patients with mild or moderate hepatic impairment (Child-Pugh class A or B).^{1 12 200} Pharmacokinetics not studied in patients with severe hepatic impairment (Child-Pugh class C);¹ dosage recommendations not available for such patients.²⁰⁰ (See Special Populations under Pharmacokinetics.)

Dosage adjustment not necessary in HIV-infected adults coinfected with HBV and/or HCV.¹ (See Special Populations under Pharmacokinetics.)

Renal Impairment

Dosage adjustment not necessary.^{1 200} (See Special Populations under Pharmacokinetics.)

Geriatric Patients

Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.¹

Cautions for Intelence

Contraindications

• Manufacturer states none known.¹

Warnings/Precautions

Sensitivity Reactions

Severe, potentially life-threatening and fatal skin reactions, including Stevens-Johnson syndrome, toxic epidermal necrolysis, and erythema multiforme, reported.¹ Hypersensitivity reactions with rash and systemic symptoms also reported.¹

If severe hypersensitivity reactions (e.g., severe rash or rash with fever, malaise, fatigue, muscle or joint pain, blisters, oral lesions, conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema) occur, immediately discontinue etravirine and initiate appropriate therapy.¹ Monitor clinical status and liver transaminase concentrations.¹

Rash of mild to moderate intensity also reported;^{1 2 3} generally occurs within first few weeks of therapy and resolves with continued therapy (median duration 12–16 days).^{1 2 3}

Manufacturer states that history of rash while receiving other NNRTIs does not appear to increase the risk for etravirine-related rash.¹

Adipogenic Effects

Possible redistribution or accumulation of body fat, including central obesity, dorsocervical fat enlargement (“buffalo hump”), peripheral wasting, facial wasting, breast enlargement, and general cushingoid appearance.¹

Immune Reconstitution Syndrome

During initial treatment, patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium, M. tuberculosis, cytomegalovirus [CMV], Pneumocystis jiroveci [formerly P. carinii]); this may necessitate further evaluation and treatment.¹

Autoimmune disorders (e.g., Graves' disease, polymyositis, Guillain-Barré syndrome) reported to occur in the setting of immune reconstitution; time to onset is more variable and can occur many months after initiation of antiretroviral therapy.¹

Specific Populations

Pregnancy

Category B.¹

Antiretroviral Pregnancy Registry at 800-258-4263 or .^{1 202}

Experts state safety and pharmacokinetic data insufficient to recommend etravirine in pregnant women.²⁰²

Lactation

Not known whether distributed into human milk.¹

Instruct HIV-infected women not to breast-feed because of risk of HIV transmission and risk of adverse effects in the infant.^{1 202}

Pediatric Use

Safety and efficacy not established in pediatric patients <6 years of age.¹

Safety, efficacy, and pharmacokinetics evaluated in antiretroviral-experienced pediatric patients 6 years to <18 years of age weighing ≥16 kg;¹ adverse effects were similar to those reported in adults (e.g., rash, diarrhea), although rash reported more frequently in pediatric patients.¹

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether they respond differently than younger adults.¹

Hepatic Impairment

Not studied in patients with severe hepatic impairment (Child-Pugh class C).¹

Renal Impairment

Minimal renal clearance; decrease in clearance not expected in patients with renal impairment.¹

Common Adverse Effects

Rash, peripheral neuropathy.¹

Interactions for Intelence

Metabolized by CYP isoenzymes 3A, 2C9, and 2C19.¹ Induces CYP3A;¹ inhibits 2C9 and 2C19.¹ Inhibits P-glycoprotein.¹

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Potential pharmacokinetic interactions with drugs that induce or inhibit CYP3A, 2C9, or 2C19 with possible altered metabolism of etravirine.^{1 200}

Potential pharmacokinetic interaction with drugs that are substrates for CYP3A, 2C9, or 2C19 with possible altered metabolism of such drugs.^{1 200}

Drugs Affected by P-glycoprotein Transport

Potential pharmacokinetic interaction with drugs that are substrates for P-glycoprotein.¹

Specific Drugs

Drug	Interaction	Comments
Abacavir	No in vitro evidence of antagonistic antiretroviral effects 1
Antiarrhythmics (amiodarone, disopyramide, flecainide, systemic lidocaine, mexiletine, propafenone, quinidine)	Possible decreased antiarrhythmic agent concentrations1	Use concomitantly with caution; monitor antiarrhythmic agent concentrations1
Anticoagulants, oral	Possible increased warfarin concentrations1 200	Monitor INR; adjust warfarin dosage if needed1 200
Anticonvulsants (carbamazepine, phenobarbital, phenytoin)	Possible decreased etravirine concentrations and decreased antiretroviral efficacy;1 200 decreased anticonvulsant concentrations200	Concomitant use not recommended;1 200 consider alternative anticonvulsants200
Antifungals, azoles	Fluconazole: Substantially increased etravirine concentrations; no change in fluconazole concentrations1 200 Itraconazole: Possible increased etravirine concentrations and decreased itraconazole concentrations1 200 Ketoconazole: Possible increased etravirine concentrations and decreased ketoconazole concentrations1 200 Posaconazole: Possible increased etravirine concentrations; no change in posaconazole concentrations1 200 Voriconazole: Increased etravirine and voriconazole concentrations1 200	Fluconazole: Dosage adjustments not needed for either drug; use caution because of limited safety data regarding increased etravirine concentrations1 200 Itraconazole: Adjustment of itraconazole dosage may be needed depending on other concomitantly administered drugs;1 200 consider monitoring itraconazole concentrations and response to the antifungal200 Ketoconazole: Adjustment of ketoconazole dosage may be needed depending on other concomitantly administered drugs1 200 Posaconazole: Some experts state dosage adjustments not needed;200 manufacturer of etravirine states adjustment of posaconazole dosage may be needed depending on other concomitantly administered drugs1 Voriconazole: Use caution because of limited safety data regarding increased etravirine concentrations;1 200 dosage adjustments not needed;1 200 consider monitoring voriconazole concentrations200
Antimycobacterials (rifabutin, rifampin, rifapentine)	Rifabutin: Decreased concentrations of etravirine and rifabutin1 200 Rifampin: Substantially decreased etravirine concentrations possible1 200 Rifapentine: Substantially decreased etravirine concentrations possible1 200	Rifabutin: Recommended rifabutin dosage is 300 mg daily in patients receiving etravirine without a ritonavir-boosted PI;1 200 rifabutin not recommended in patients receiving etravirine with a ritonavir-boosted PI1 200 Rifampin: Concomitant use not recommended1 200 Rifapentine: Concomitant use not recommended1 200
Atazanavir	Atazanavir or ritonavir-boosted atazanavir: Increased etravirine concentrations; decreased atazanavir concentrations and possible decreased antiretroviral efficacy1 200 No in vitro evidence of antagonistic antiretroviral effects1	Atazanavir (with or without low-dose ritonavir): Do not use concomitantly1 200
Benzodiazepines (alprazolam, diazepam)	Alprazolam: Data not available200 Diazepam: Possible increased diazepam concentrations1 200	Alprazolam: Monitor for alprazolam therapeutic effects200 Diazepam: Decreased diazepam dosage may be needed1 200
Buprenorphine, buprenorphine/naloxone	Decreased buprenorphine concentrations and AUC; no effect on norbuprenorphine or etravirine concentrations1 200	Routine buprenorphine or buprenorphine/naloxone dosage adjustments not needed;1 200 monitor for withdrawal symptoms since buprenorphine or buprenorphine/naloxone maintenance dosage adjustment may be needed in some patients1
Clarithromycin	Increased etravirine concentrations; decreased clarithromycin concentrations and increased concentrations of the major metabolite (14-hydroxyclarithromycin)1 200	Consider an alternative to clarithromycin (e.g., azithromycin) for treatment or prophylaxis of MAC1 200
Clopidogrel	Possible decreased concentrations of the active metabolite of clopidogrel1	Avoid concomitant use if possible;200 consider alternatives to clopidogrel1
Corticosteroids (dexamethasone)	Dexamethasone: Possible decreased etravirine concentrations and decreased antiretroviral efficacy1 200	Use concomitantly with caution; consider alternatives to dexamethasone, especially when long-term corticosteroid use anticipated1 200
Darunavir	Ritonavir-boosted darunavir: Decreased etravirine AUC; no change in darunavir concentrations; safety and efficacy of concomitant use established in phase 3 clinical studies1 2 3 200 No in vitro evidence of antagonistic antiretroviral effects1	Ritonavir-boosted darunavir: Dosage adjustments not needed1 200
Delavirdine	Possible increased etravirine concentrations1	Do not use concomitantly1
Didanosine	No effect on didanosine or etravirine concentrations1 No in vitro evidence of antagonistic antiretroviral effects1	Dosage adjustments not needed1
Digoxin	Possible increased digoxin concentrations; no change in etravirine concentrations1	If digoxin and etravirine are initiated at the same time, initiate digoxin at the lowest dosage1 If etravirine is initiated in a patient already receiving digoxin, dosage adjustment of either drug not needed1 Monitor serum digoxin concentrations and adjust digoxin dosage to achieve desired clinical effect1
Efavirenz	Decreased etravirine concentrations1 200 and loss of antiretroviral efficacy1	Do not use concomitantly1 200
Emtricitabine	No in vitro evidence of antagonistic antiretroviral effects1
Enfuvirtide	No in vitro evidence of antagonistic antiretroviral effects1	Dosage adjustments not needed1
Estrogens/progestins	Hormonal contraceptives: Slight increase in ethinyl estradiol concentrations; no change in norethindrone concentrations1 200	Dosage adjustments not needed with oral contraceptives containing ethinyl estradiol and norethindrone1 200
Fosamprenavir	Fosamprenavir or ritonavir-boosted fosamprenavir: Substantially increased concentrations of amprenavir (active metabolite of fosamprenavir)1 200 No in vitro evidence of antagonistic antiretroviral effects1	Fosamprenavir (with or without low-dose ritonavir): Do not use concomitantly1 200
Histamine H2-receptor antagonists	Ranitidine: Decreased etravirine concentrations1	Ranitidine: Dosage adjustments not needed1
HMG-CoA reductase inhibitors (statins)	Atorvastatin: Decreased atorvastatin concentrations; no change in etravirine concentrations1 200 Fluvastatin: Possible increased fluvastatin concentrations; no change in etravirine concentrations1 200 Lovastatin: Possible decreased lovastatin concentrations1 200 Pitavastatin: Possible increased pitavastatin concentrations1 Pravastatin: Pharmacokinetic interaction not expected1 200 Rosuvastatin: Pharmacokinetic interaction not expected1 200 Simvastatin: Possible decreased simvastatin concentrations1 200	Atorvastatin: Usual etravirine and atorvastatin dosages can be used; however, may need to adjust atorvastatin dosage based on clinical response1 200 (do not exceed maximum recommended atorvastatin dosage)200 Fluvastatin: May need to adjust fluvastatin dosage1 200 Lovastatin: May need to adjust lovastatin dosage based on clinical response1 200 (do not exceed maximum recommended lovastatin dosage);200 if a ritonavir-boosted PI is included in the regimen, avoid use of lovastatin200 Pitavastatin: May need to adjust pitavastatin dosage1 Pravastatin: Dosage adjustments not needed200 Rosuvastatin: Dosage adjustments not needed200 Simvastatin: May need to adjust simvastatin dosage based on clinical response1 200 (do not exceed maximum recommended simvastatin dosage);200 if a ritonavir-boosted PI is included in the regimen, avoid use of simvastatin200
Immunosuppressive agents (cyclosporine, sirolimus, tacrolimus)	Potential for decreased immunosuppressive agent concentrations1	Use concomitantly with caution1
Indinavir	Indinavir (without low-dose ritonavir): Possible decreased indinavir concentrations1 No in vitro evidence of antagonistic antiretroviral effects1	Do not use concomitantly without low-dose ritonavir1
Lamivudine	No in vitro evidence of antagonistic antiretroviral effects 1
Lopinavir/ritonavir	Decreased etravirine concentrations and AUC; decreased lopinavir concentrations and AUC1 200 No in vitro evidence of antagonistic antiretroviral effects1	Because decrease in etravirine systemic exposure in patients receiving concomitant lopinavir/ritonavir is similar to that in patients receiving etravirine and concomitant ritonavir-boosted darunavir (a combination found to be safe and effective), manufacturer and some experts state that dosage adjustments not needed for either drug1 200
Maraviroc	Decreased maraviroc concentrations and AUC;1 200 224 no clinically important effect on etravirine concentrations or AUC1 No in vitro evidence of antagonistic antiretroviral effects1	Recommended maraviroc dosage is 600 mg twice daily with usual etravirine dosage, provided regimen does not include a potent CYP3A inhibitor1 200 224
Methadone	No clinically important change in methadone or etravirine concentrations1 8 200	Dosage adjustments not needed1 8 200
Nelfinavir	Nelfinavir (without low-dose ritonavir): Possible increased nelfinavir concentrations1 No in vitro evidence of antagonistic antiretroviral effects1	Do not use concomitantly with etravirine without low-dose ritonavir1
Nevirapine	Decreased etravirine concentrations1 200 and loss of antiretroviral efficacy1	Do not use concomitantly with etravirine1
Paroxetine	No change in etravirine or paroxetine concentrations1	Dosage adjustments not needed1
Proton pump inhibitors	Omeprazole: Increased etravirine concentrations1	Omeprazole: Dosage adjustments not needed1
Raltegravir	Decreased raltegravir concentrations and AUC;1 225 no clinically important effect on etravirine pharmacokinetics;1 225 clinical importance unknown225 No in vitro evidence of antagonistic antiretroviral effects1	Dosage adjustments not needed1 200
Rilpivirine	Possible decreased rilpivirine concentrations; no change in etravirine concentrations226 No in vitro evidence of antagonistic antiretroviral effects 226	Do not use concomitantly226
Ritonavir	Full-dose ritonavir (600 mg twice daily): Substantial decrease in etravirine concentrations and possible loss of antiretroviral efficacy1 No in vitro evidence of antagonistic antiretroviral effects 1	Full-dose ritonavir (600 mg twice daily): Do not use concomitantly with etravirine1 Low-dose ritonavir (usually 100 mg once or twice daily): Etravirine may be used concomitantly with certain ritonavir-boosted PI regimens (i.e., ritonavir-boosted darunavir, lopinavir/ritonavir, ritonavir-boosted saquinavir);1 concomitant use with ritonavir-boosted atazanavir, ritonavir-boosted fosamprenavir, or ritonavir-boosted tipranavir not recommended1 200
Saquinavir	Ritonavir-boosted saquinavir: Decreased etravirine AUC; no change in saquinavir concentrations1 200 Decrease in systemic exposure to etravirine is similar to that in patients receiving etravirine in conjunction with ritonavir-boosted darunavir (a combination found to be safe and effective)1 200 No in vitro evidence of antagonistic antiretroviral effects1	Ritonavir-boosted saquinavir: Dosage adjustments not needed1 200
Sildenafil	Decreased sildenafil concentrations1 200	Usual etravirine and sildenafil dosages can be used; sildenafil dosage may need to be increased based on clinical effect1 200
Stavudine	No in vitro evidence of antagonistic antiretroviral effects1
St. John’s wort (Hypericum perforatum)	Possible substantially decreased etravirine concentrations and loss of antiretroviral efficacy1 200	Concomitant use not recommended1 200
Tadalafil	Possible decreased tadalafil concentrations200	Tadalafil dosage may need to be increased based on clinical effect200
Tenofovir	Decreased etravirine concentrations; no change in tenofovir concentrations1 No in vitro evidence of antagonistic antiretroviral effects1	Dosage adjustments not needed1
Tipranavir	Ritonavir-boosted tipranavir: Decreased etravirine concentrations and possible decreased antiretroviral efficacy; increased tipranavir concentrations1 200 No in vitro evidence of antagonistic antiretroviral effects1	Ritonavir-boosted tipranavir: Do not use concomitantly1 200
Vardenafil	Possible decreased vardenafil concentrations200	Vardenafil dosage may need to be increased based on clinical effect200
Zidovudine	No in vitro evidence of antagonistic antiretroviral effects1

Intelence Pharmacokinetics

Absorption

Bioavailability

Absolute oral bioavailability is unknown.¹

Following oral administration in adults, peak plasma concentrations attained within approximately 2.5–4 hours.^{1 11}

Food

Systemic exposure is decreased by about 50% if etravirine is administered under fasting conditions compared with administration after a meal.^{1 11}

Effect of food on etravirine bioavailability was studied using various meals (standard, light, enhanced-fiber, high-fat);¹¹ magnitude of the food effect is similar with all meal types.^{1 11}

Distribution

Extent

Distribution into compartments other than plasma (e.g., CSF, genital tract secretions) not evaluated.¹

Not known whether etravirine crosses the placenta²⁰² or is distributed into human milk.¹

Plasma Protein Binding

99.9%, principally albumin and alpha 1-acid glycoprotein.¹

Elimination

Metabolism

Metabolized principally in the liver by CYP isoenzymes 3A, 2C9, and 2C19.¹

In cell culture, the major metabolites are at least 90% less active than etravirine against wild-type HIV-1.¹

Elimination Route

Following oral administration of a single dose in adults, the majority (93.7%) is eliminated in feces as unchanged etravirine (81.2–86.4%).¹ Up to 1.2% of the dose is eliminated in urine as metabolites.¹

Unlikely to be removed by hemodialysis or peritoneal dialysis.¹

Half-life

Mean terminal elimination half-life in adults is about 41 hours.¹

Special Populations

Renal impairment: Pharmacokinetics not studied; alterations not expected because renal clearance is minimal.¹

Hepatic impairment: Pharmacokinetics not altered in patients with mild or moderate hepatic impairment (Child-Pugh class A or B);^{1 12} not studied in patients with severe hepatic impairment (Child-Pugh class C).¹

HIV-infected individuals coinfected with HBV and/or HCV: Reduced clearance reported.¹

Geriatric individuals: Studies in those up to 77 years of age indicate no substantial differences in pharmacokinetics relative to younger adults.¹

Pediatric patients 6 years to <18 years of age weighing ≥16 kg: Weight-based dosage (approximately 5.2 mg/kg twice daily) results in systemic etravirine exposures similar to those reported in adults receiving 200 mg twice daily.¹

Pregnant patients: Pharmacokinetics not studied.¹

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).¹ Tight container; protect from moisture.¹ Dispense and store in original container; do not remove desiccant from bottle.¹

Actions and Spectrum

• Inhibits replication of HIV-1 by interfering with viral RNA- and DNA-directed polymerase activities of reverse transcriptase.^{1 4}

• Highly active against wild-type HIV-1; active against some clinical HIV-1 isolates resistant to some other NNRTIs (delavirdine, efavirenz, nevirapine).^{1 3 4 200}

• Different resistance profile than other NNRTIs; certain single mutations that result in class resistance to other NNRTIs may not necessarily result in etravirine resistance.^{2 3 4}

• Cross-resistance may occur between etravirine and other commercially available NNRTIs (delavirdine, etravirine, nevirapine, rilpivirine),^{1 4 200 226} and is expected in patients who have virologic failure while receiving a regimen that contains etravirine.¹

Advice to Patients

• Critical nature of compliance with HIV therapy and importance of remaining under the care of a clinician.^{1 200} Importance of taking as prescribed; do not alter or discontinue antiretroviral regimen without consulting clinician.¹

• Importance of using in conjunction with other antiretrovirals—not for monotherapy.^{1 200}

• Antiretroviral therapy is not a cure for HIV infection; opportunistic infections and other complications associated with HIV disease may still occur.¹

• Advise patients that sustained decreases in plasma HIV RNA have been associated with reduced risk of progression to AIDS and death.¹

• Advise patients that effective antiretroviral regimens can decrease HIV concentrations in blood and genital secretions and strict adherence to such regimens in conjunction with risk-reduction measures may decrease, but cannot absolutely eliminate, the risk of secondary transmission of HIV to others.²⁰⁰ Importance of continuing to practice safer sex (e.g., using latex or polyurethane condoms to minimize sexual contact with body fluids), never sharing personal items that can have blood or body fluids on them (e.g., toothbrushes, razor blades), and never reusing or sharing needles.^{1 200}

• Importance of reading patient information provided by the manufacturer.¹

• Importance of taking etravirine twice daily after a meal.¹ Food enhances absorption of the drug;^{1 11} magnitude of the food effect is similar with all meal types (standard, light, enhanced-fiber, high-fat).^{1 11}

• Advise patients to swallow the tablets whole with liquid (e.g., water) without chewing.¹ Patients unable to swallow tablets whole may disperse the tablets in 5 mL of water (enough to cover the tablets); after dispersion in water, orange juice or milk may be added to the mixture.¹ Ingest the liquid containing the dispersed etravirine tablets immediately, then rinse the glass several times with water, orange juice, or milk and drink the rinse each time to ensure entire dose is ingested.¹

• If a missed dose is remembered within 6 hours of the usually scheduled time, it should be taken after a meal as soon as possible and the next dose taken at the regularly scheduled time.¹ If missed dose is remembered >6 hours after the scheduled time, the dose should be omitted and the next dose taken at the regularly scheduled time.¹

• Advise patients that severe and potentially life-threatening rash has occurred (usually within the first few weeks of etravirine therapy).¹ Importance of immediately contacting clinician if rash occurs.¹ Importance of immediately discontinuing etravirine and seeking medical care if rash associated with systemic symptoms (e.g., fever, generally ill feeling, extreme tiredness, muscle or joint aches, blisters, oral lesions, eye inflammation, swelling of the face, eyes, lips, or mouth, breathing difficulties, yellowing of the eyes or skin, dark or tea colored urine, pale colored stools, nausea, vomiting, loss of appetite, or right upper quadrant tenderness/pain) occurs.¹

• Advise patients that redistribution/accumulation of body fat may occur with antiretroviral therapy, with as yet unknown long-term health effects.¹

• Advise patients to contact their clinician if signs or symptoms of an infection occur.¹

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and herbal supplements (e.g., St. John’s wort), and any concomitant illnesses.¹

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹ Advise HIV-infected women not to breast-feed.¹

• Importance of advising patients of other important precautionary information.¹ (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Etravirine

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets	100 mg	Intelence	Janssen
		200 mg	Intelence	Janssen

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2013. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Intelence 100MG Tablets (JANSSEN PRODUCTS): 120/$876.00 or 360/$2,519.00

Intelence 200MG Tablets (JANSSEN PRODUCTS): 60/$871.03 or 180/$2,567.01