Adult: In combination w/ other antiretroviral agents: Treatment-experienced patients: 200 mg bid. Child: >6 yr In combination w/ other antiretroviral agents: Treatment-experienced patients: ≥16-<20 kg: 100 mg bid; ≥20-<25 kg: 125 mg bid; ≥25-<30 150 mg bid; ≥30 kg: Same as adult dose.
Hepatic Impairment
Severe (Child-Pugh Class C): Contraindicated.
Administration
Should be taken with food. Swallow whole, do not chew/crush. For patients w/ swallowing difficulties, disperse tab thoroughly in a glass of water & drink immediately. Rinse the glass w/ water several times & drink each rinse completely.
Contraindications
Hypersensitivity to etravirine. Severe hepatic (Child-Pugh Class C) impairment. Lactation.
Special Precautions
Patient w/ hepatitis B or C. Not indicated for use in treatment-naive patients. Mild to moderate hepatic impairment. Pregnancy.
Monitor viral load, CD4 count, cholesterol, triglycerides, hepatic transaminases (if signs or symptoms of hypersensitivity develops), signs and symptoms of infection and skin rash.
Drug Interactions
May decrease plasma concentrations and therapeutic effects of indinavir, antiarrhythmics (e.g. amiodarone, quinidine, flecainide, systemic lidocaine, disopyramide, mexiletine, propafenone), itraconazole, ketoconazole, lovastatin, rosuvastatin, simvastatin, immunosuppressants (e.g. ciclosporin, sirolimus, tacrolimus). May increase plasma concentrations of warfarin, diazepam, digoxin. Decreased plasma concentrations w/ carbamazepine, phenobarbital, phenytoin, rifampicin, rifapentine, dexamethasone. May inhibit metabolism of clopidogrel.
Food Interaction
Increased absorption w/ food. Decreased plasma concentration and therapeutic effect w/ St John’s wort.
Action
Description: Mechanism of Action: Etravirine, a non-nucleoside reverse transcriptase inhibitor (NNRTI), binds to HIV-1 reverse transcriptase and subsequently blocks viral RNA- and DNA-dependent DNA polymerase activities including replication. Pharmacokinetics: Absorption: Readily absorbed. Increased absorption w/ food. Time to peak plasma concentrations: 2.5-4 hr. Distribution: Crosses placenta. Plasma protein binding: 99.9%, primarily to albumin and α1-acid glycoprotein. Metabolism: Extensively metabolised in the liver by CYP3A4, CYP2C9, and CYP2C19 enzymes to less active metabolites. Excretion: Via faeces (94%, up to 86% as unchanged drug); urine (1% as metabolites). Terminal elimination half-life: Approx 41 hr.
Chemical Structure
Etravirine Source: National Center for Biotechnology Information. PubChem Database. Etravirine, CID=193962, https://pubchem.ncbi.nlm.nih.gov/compound/Etravirine (accessed on Jan. 23, 2020)
J05AG04 - etravirine ; Belongs to the class of non-nucleoside reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.
References
Anon. Etravirine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/03/2017.Buckingham R (ed). Etravirine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/03/2017.Intelence Tablet (Janssen Products LP) . DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/03/2017.Joint Formulary Committee. Etravirine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/03/2017.McEvoy GK, Snow EK, Miller J et al (eds). Etravirine. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 03/03/2017.
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