search engines like google [18:<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 Postexposure Prophylaxis following Occupational Exposure to HIV Oral 200 mg twice daily. 199 Use in conjunction with 2 NRTIs (see Postexposure Prophylaxis following Occupational Exposure to HIV under Uses). 199 Initiate PEP as soon as possible following occupational exposure to HIV (preferably within hours); continue for 4 weeks, if tolerated. 199 Special Populations Hepatic Impairment Dosage adjustments 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 adjustments not necessary in HIV-infected adults coinfected with HBV and/or HCV. 1 (See Special Populations under Pharmacokinetics.) Renal Impairment Dosage adjustments 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 Etravirine 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, including drug rash with eosinophilia and systemic symptoms (DRESS) characterized by rash and systemic symptoms (sometimes involving organ dysfunction such as hepatic failure), 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 Mechanisms and long-term consequences of fat redistribution unknown; causal relationship not established. 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 jirovecii [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 routine use of etravirine for initial treatment regimens in antiretroviral-naive 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 Rash generally was mild to moderate and macular/papular rash, occurred the second week of therapy, and generally was self-limiting and resolved within 1 week with continued etravirine therapy. 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 Etravirine Metabolized by CYP isoenzymes 3A, 2C9, and 2C19. 1 Induces CYP3A; 1 inhibits 2C9 and 2C19. 1 Inhibits P-glycoprotein (P-gp). 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-gp. 1 Specific Drugs Drug Interaction Comments Abacavir No in vitro evidence of antagonistic antiretroviral effects 1 Avanafil Data not available 200 Concomitant use not recommended 200 Antiarrhythmics (amiodarone, disopyramide, flecainide, systemic lidocaine, mexiletine, propafenone, quinidine) Possible decreased antiarrhythmic agent concentrations 1 Use concomitantly with caution; monitor antiarrhythmic agent concentrations 1 Anticoagulants, oral Possible increased warfarin concentrations 1 200 Monitor INR; adjust warfarin dosage if needed 1 200 Anticonvulsants (carbamazepine, phenobarbital, phenytoin) Possible decreased etravirine concentrations and decreased antiretroviral efficacy; 1 200 decreased anticonvulsant concentrations 200 Concomitant use not recommended; 1 200 consider alternative anticonvulsants 200 Antifungals, azoles Fluconazole: Substantially increased etravirine concentrations and AUC; no clinically important change in fluconazole concentrations or AUC 1 200 Itraconazole: Possible increased etravirine concentrations and decreased itraconazole concentrations 1 200 Ketoconazole: Possible increased etravirine concentrations and decreased ketoconazole concentrations 1 200 Posaconazole: Possible increased etravirine concentrations; no change in posaconazole concentrations 1 200 Voriconazole: Substantially increased etravirine concentrations and AUC; increased voriconazole concentration and AUC 1 200 Fluconazole: Dosage adjustments not needed for either drug; use caution because of limited safety data regarding increased etravirine concentrations 1 200 Itraconazole: Adjustment of itraconazole dosage may be needed depending on other concomitantly administered drugs; 1 200 consider monitoring itraconazole concentrations and response to the antifungal 200 Ketoconazole: Adjustment of ketoconazole dosage may be needed depending on other concomitantly administered drugs 1 200 Posaconazole: Experts state dosage adjustments not needed; 200 manufacturer of etravirine states adjustment of posaconazole dosage may be needed depending on other concomitantly administered drugs 1 Voriconazole: Use caution because of limited safety data regarding increased etravirine concentrations; 1 200 dosage adjustments not needed; 1 200 consider monitoring voriconazole concentrations 200 Antimalarials Fixed combination of artemether and lumefantrine (artemether/lumefantrine): Decreased concentrations and AUC of artemether, active metabolite of artemether (dihydroartemisinin), and lumefantrine; 1 200 no clinically important effect on etravirine concentrations or AUC 1 Artemether/lumefantrine: Dosage adjustments not needed; use concomitantly with caution since effect on antimalarial efficacy not known; 1 closely monitor antimalarial efficacy 200 Antimycobacterials (rifabutin, rifampin, rifapentine) Rifabutin: Decreased concentrations of etravirine and rifabutin 1 200 Rifampin: Substantially decreased etravirine concentrations possible 1 200 Rifapentine: Substantially decreased etravirine concentrations possible 1 200 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 PI 1 200 Rifampin: Concomitant use not recommended 1 200 Rifapentine: Concomitant use not recommended 1 200 Atazanavir Atazanavir or ritonavir-boosted atazanavir: Increased etravirine concentrations; decreased atazanavir concentrations and possible decreased antiretroviral efficacy 1 200 No in vitro evidence of antagonistic antiretroviral effects 1 Atazanavir (with or without low-dose ritonavir): Do not use concomitantly 1 200 Benzodiazepines (alprazolam, diazepam) Alprazolam: Data not available 200 Diazepam: Possible increased diazepam concentrations 1 200 Alprazolam: Monitor for alprazolam therapeutic effects 200 Diazepam: Decreased diazepam dosage may be needed 1 200 Boceprevir Decreased etravirine AUC; increased boceprevir concentrations and AUC 200 Dosage adjustments not needed 200 Buprenorphine, buprenorphine/naloxone Decreased buprenorphine concentrations and AUC; no effect on norbuprenorphine or etravirine concentrations 1 200 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 patients 1 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 MAC 1 200 Clopidogrel Possible decreased concentrations of the active metabolite of clopidogrel 1 Avoid concomitant use if possible; 200 consider alternatives to clopidogrel 1 Corticosteroids (dexamethasone) Dexamethasone: Possible decreased etravirine concentrations and decreased antiretroviral efficacy 1 200 Use concomitantly with caution; consider alternatives to dexamethasone, especially when long-term corticosteroid use anticipated 1 200 Darunavir Ritonavir-boosted darunavir: Decreased etravirine AUC; no change in darunavir concentrations; safety and efficacy of concomitant use established in phase 3 clinical studies 1 2 3 200 No in vitro evidence of antagonistic antiretroviral effects 1 Ritonavir-boosted darunavir: Dosage adjustments not needed 1 200 Delavirdine Possible increased etravirine concentrations 1 Do not use concomitantly 1 Didanosine No effect on didanosine or etravirine concentrations 1 No in vitro evidence of antagonistic antiretroviral effects 1 Dosage adjustments not needed 1 Digoxin Possible increased digoxin concentrations; no change in etravirine concentrations 1 If digoxin and etravirine are initiated at the same time, initiate digoxin at the lowest dosage 1 If etravirine is initiated in a patient already receiving digoxin, dosage adjustments not needed for either drug 1 Monitor serum digoxin concentrations and adjust digoxin dosage to achieve desired clinical effect 1 Dolutegravir Substantially decreased dolutegravir concentrations and AUC; 200 236 no apparent effect on etravirine pharmacokinetics 236 Effect on dolutegravir pharmacokinetics is mitigated if etravirine and dolutegravir used concomitantly with lopinavir/ritonavir or ritonavir-boosted darunavir; 200 236 effect expected to be mitigated if etravirine and dolutegravir used concomitantly with ritonavir-boosted atazanavir 200 236 Do not use etravirine and dolutegravir concomitantly unless ritonavir-boosted atazanavir, ritonavir-boosted darunavir, or lopinavir/ritonavir also included in the regimen 200 236 HIV integrase strand transference inhibitor-naive (INSTI-naive) or INSTI-experienced without INSTI resistance: Use dolutegravir 50 mg once daily with etravirine and with ritonavir-boosted atazanavir, ritonavir-boosted darunavir, or lopinavir/ritonavir 200 INSTI-experienced with documented or suspected INSTI resistance: Use dolutegravir 50 mg twice daily with etravirine and with ritonavir-boosted atazanavir, ritonavir-boosted darunavir, or lopinavir/ritonavir 200 Efavirenz Decreased etravirine concentrations 1 200 and loss of antiretroviral efficacy 1 Do not use concomitantly 1 200 Elvitegravir and cobicistat Fixed combination of elvitegravir, cobicistat, emtricitabine, and tenofovir DF (EVG/COBI/TDF/FTC): Possible altered concentrations of elvitegravir, cobicistat, and/or etravirine 200 EVG/COBI/TDF/FTC: Do not use concomitantly 200 Emtricitabine No in vitro evidence of antagonistic antiretroviral effects 1 Enfuvirtide No in vitro evidence of antagonistic antiretroviral effects 1 Dosage adjustments not needed 1 Ergot alkaloids (dihydroergotamine, ergotamine, methylergonovine) Possible decreased ergot alkaloid concentrations; possible inadequate treatment effect 202 If methylergonovine used to treat postpartum hemorrhage in a woman receiving etravirine, additional uterotonic agents may be needed 202 Estrogens/progestins Hormonal contraceptives: Slight increase in ethinyl estradiol concentrations; no change in norethindrone concentrations 1 200 Dosage adjustments not needed with oral contraceptives containing ethinyl estradiol and norethindrone 1 200 Fosamprenavir Fosamprenavir or ritonavir-boosted fosamprenavir: Substantially increased concentrations of amprenavir (active metabolite of fosamprenavir) 1 200 No in vitro evidence of antagonistic antiretroviral effects 1 Fosamprenavir (with or without low-dose ritonavir): Do not use concomitantly 1 200 Histamine H 2 -receptor antagonists Ranitidine: Decreased etravirine concentrations 1 Ranitidine: Dosage adjustments not needed 1 HMG-CoA reductase inhibitors (statins) Atorvastatin: Decreased atorvastatin concentrations; no change in etravirine concentrations 1 200 Fluvastatin: Possible increased fluvastatin concentrations; no change in etravirine concentrations 1 200 Lovastatin: Possible decreased lovastatin concentrations 1 200 Pitavastatin: Possible increased pitavastatin concentrations 1 Pravastatin: Pharmacokinetic interaction not expected 1 200 Rosuvastatin: Pharmacokinetic interaction not expected 1 200 Simvastatin: Possible decreased simvastatin concentrations 1 200 Atorvastatin: Usual etravirine and atorvastatin dosages can be used; however, may need to adjust atorvastatin dosage based on clinical response 1 200 (do not exceed maximum recommended atorvastatin dosage) 200 Fluvastatin: May need to adjust fluvastatin dosage 1 200 Lovastatin: May need to adjust lovastatin dosage based on clinical response 1 200 (do not exceed maximum recommended lovastatin dosage); 200 if a ritonavir-boosted PI is included in the regimen, avoid use of lovastatin 200 Pitavastatin: May need to adjust pitavastatin dosage 1 Pravastatin: Dosage adjustments not needed 200 Rosuvastatin: Dosage adjustments not needed 200 Simvastatin: May need to adjust simvastatin dosage based on clinical response 1 200 (do not exceed maximum recommended simvastatin dosage); 200 if a ritonavir-boosted PI is included in the regimen, avoid use of simvastatin 200 Immunosuppressive agents (cyclosporine, sirolimus, tacrolimus) Potential for decreased immunosuppressive agent concentrations 1 Use concomitantly with caution; 1 therapeutic drug monitoring of immunosuppressive agent recommended; 200 consultation with a specialist may be needed 200 Indinavir Indinavir (without low-dose ritonavir): Possible decreased indinavir concentrations 1 No in vitro evidence of antagonistic antiretroviral effects 1 Do not use concomitantly without low-dose ritonavir 1 Lamivudine No in vitro evidence of antagonistic antiretroviral effects 1 Lopinavir/ritonavir Decreased etravirine concentrations and AUC; decreased lopinavir concentrations and AUC 1 200 No in vitro evidence of antagonistic antiretroviral effects 1 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 experts state that dosage adjustments not needed for either drug 1 200 Maraviroc Decreased maraviroc concentrations and AUC; 1 200 224 no clinically important effect on etravirine concentrations or AUC 1 No in vitro evidence of antagonistic antiretroviral effects 1 Recommended maraviroc dosage is 600 mg twice daily with usual etravirine dosage, provided regimen does not include a potent CYP3A inhibitor 1 200 224 Methadone No clinically important change in methadone or etravirine concentrations 1 8 200 Dosage adjustments not needed 1 8 200 Nelfinavir Nelfinavir (without low-dose ritonavir): Possible increased nelfinavir concentrations 1 No in vitro evidence of antagonistic antiretroviral effects 1 Do not use concomitantly with etravirine without low-dose ritonavir 1 Nevirapine Decreased etravirine concentrations 1 200 and loss of antiretroviral efficacy 1 Do not use concomitantly with etravirine 1 Paroxetine No change in etravirine or paroxetine concentrations 1 Dosage adjustments not needed 1 Proton pump inhibitors Omeprazole: Increased etravirine concentrations 1 Omeprazole: Dosage adjustments not needed 1 Raltegravir Decreased raltegravir concentrations and AUC; 1 225 no clinically important effect on etravirine pharmacokinetics; 1 225 clinical importance unknown 225 No in vitro evidence of antagonistic antiretroviral effects 1 Dosage adjustments not needed 1 200 Rilpivirine Possible decreased rilpivirine concentrations; no change in etravirine concentrations 226 No in vitro evidence of antagonistic antiretroviral effects 226 Do not use concomitantly 226 Ritonavir Full-dose ritonavir (600 mg twice daily): Substantial decrease in etravirine concentrations and possible loss of antiretroviral efficacy 1 No in vitro evidence of antagonistic antiretroviral effects 1 Full-dose ritonavir (600 mg twice daily): Do not use concomitantly with etravirine 1 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 recommended 1 200 Saquinavir Ritonavir-boosted saquinavir: Decreased etravirine AUC; no change in saquinavir concentrations 1 200 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 effects 1 Ritonavir-boosted saquinavir: Dosage adjustments not needed 1 200 Sildenafil Decreased sildenafil concentrations 1 200 Usual etravirine and sildenafil dosages can be used; sildenafil dosage may need to be increased based on clinical effect 1 200 Simeprevir Possible decreased simeprevir concentrations 187 200 Concomitant use not recommended 187 200 Stavudine No in vitro evidence of antagonistic antiretroviral effects 1 St. John s wort ( Hypericum perforatum ) Possible substantially decreased etravirine concentrations and loss of antiretroviral efficacy 1 200 Concomitant use not recommended 1 200 Tadalafil Possible decreased tadalafil concentrations 200 Tadalafil dosage may need to be increased based on clinical effect 200 Telaprevir Decreased telaprevir concentrations and AUC; no clinically important effect on etravirine concentrations or AUC 1 200 Insufficient data to make telaprevir dosage recommendations 1 200 Tenofovir Decreased etravirine concentrations; no change in tenofovir concentrations 1 No in vitro evidence of antagonistic antiretroviral effects 1 Dosage adjustments not needed 1 Tipranavir Ritonavir-boosted tipranavir: Decreased etravirine concentrations and possible decreased antiretroviral efficacy; increased tipranavir concentrations 1 200 No in vitro evidence of antagonistic antiretroviral effects 1 Ritonavir-boosted tipranavir: Do not use concomitantly 1 200 Vardenafil Possible decreased vardenafil concentrations 200 Vardenafil dosage may need to be increased based on clinical effect 200 Zidovudine No in vitro evidence of antagonistic antiretroviral effects 1 Etravirine 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 Crosses the placenta and has been detected in cord blood. 202 Not known whether distributed into human milk. 1 202 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. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Etravirine Routes Dosage Forms Strengths Brand Names Manufacturer Oral Tablets 25 mg Intelence Janssen 100 mg Intelence Janssen 200 mg Intelence Janssen AHFS DI Essentials. Copyright 2017, Selected Revisions October 30, 2014. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. Use is not currently included in the labeling approved by the US Food and Drug Administration. References 1. Janssen. Intelence (etravirine) tablets prescribing information. Titusville, NJ; 2013 Feb. 2. Madruga JV, Cahn P, Grinsztejn B et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1 infected patients in DUET-1: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet . 2007; 370:29-38. [PubMed 17617270] 3. Lazzarin A, Campbell T, Clotet B et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1 infected patients in DUET-2: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet . 2007; 370:39-48. [PubMed 17617271] 4. Vingerhoets J, Azijn H, Fransen E et al. TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experiments. J Virol . 2005; 79:12773-82. [PubMed 16188980] 6. Tibotec Therapeutics, Bridgewater, NJ: Personal communication. 8. Schöller-Gyüre M, van den Brink W, Kakuda TN et al. Pharmacokinetic and pharmacodynamic study of the concomitant administration of methadone and TMC125 in HIV-negative volunteers. J Clin Pharmacol . 2008; 48:322-9. 10. Anderson MS, Kakuda TN, Hanley W et al. Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects. Antimicrob Agents Chemother . 2008; 52:4228-32. [PubMed 18838586] 11. Schöller-Gyüre M, Boffito M, Pozniak AL et al. Effects of different meal compositions and fasted state on the oral bioavailability of etravirine. Pharmacotherapy . 2008; 28:1215-22. [PubMed 18823217] 12. Schöller-Gyüre M, Kakuda TN, De Smedt G et al. Effects of hepatic impairment on the steady-state pharmacokinetics of etravirine 200 mg BID: an open-label, multiple-dose, controlled Phase I study in adults. Clin Ther . 2010; 32:328-37. [PubMed 20206790] 187. Janssen Products LP. Olysio (simeprevir) capsules prescribing information. Titusville, NJ; 2013 Nov. 199. Kuhar DT, Henderson DK, Struble KA et al. Updated US Public Health Service guidelines for the management of occupational exposures to human immunodeficiency virus and recommendations for postexposure prophylaxis. Infect Control Hosp Epidemiol . 2013; 34:875-92. [PubMed 23917901] 200. Panel on Antiretroviral Guidelines for Adults and Adolescents, US Department of Health and Human Services (HHS). Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents (May 1, 2014). Updates may be available at HHS AIDS Information (AIDSinfo) website. 201. Panel on Antiretroviral Therapy and Medical Management of HIV-infected Children, US Department of Health and Human Services (HHS). Guidelines for the use of antiretroviral agents in pediatric HIV infection (February 12, 2014). Updates may be available at HHS AIDS Information (AIDSinfo) website. 202. Panel on Treatment of HIV-Infected Pregnant Women and Prevention of Perinatal Transmission, US Department of Health and Human Services (HHS). Recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV transmission in the United States (March 28, 2014). Updates may be available at HHS AIDS Information (AIDSinfo) website. 224. ViiV Healthcare. Selzentry (maraviroc) tablets prescribing information. Research Triangle Park, NC; 2012 Aug. 225. Merck Sharp & Dohme. Isentress (raltegravir) film-coated tablets and chewable tablets prescribing information. Whitehouse Station, NJ; 2012 Aug. 226. Tibotec Therapeutics. Edurant (rilpivirine) tablets prescribing information. Raritan, NJ; 2012 Aug. 236. ViiV Healthcare. Tivicay (dolutegravir) tablets prescribing information. Research Triangle Park, NC; 2014 May. Next Interactions Print this page Add to My Med List More about etravirine Side Effects During Pregnancy or Breastfeeding Dosage Information Dr ideal
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