Etravirine


Concise Prescribing Info
Indications/Uses
HIV-1 infection.
Dosage/Direction for Use
Adult : PO Treatment-experienced patients: 200 mg bid given w/ other antiretrovirals.
Dosage Details
Oral
HIV-1 infection
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.
Adverse Reactions
Significant: Fat redistribution (e.g. Cushingoid appearance, central obesity, buffalo hump, peripheral and facial wasting, breast enlargement), immune reconstitution syndrome, osteonecrosis, mild to moderate rash.
Nervous: Fatigue, headache, peripheral neuropathy, malaise, drowsiness.
CV: MI, angina pectoris, HTN.
GI: Nausea, abdominal pain, diarrhoea, flatulence, gastritis, GERD, dry mouth, vomiting, pancreatitis.
Resp: Bronchospasm.
Hepatic: Hepatitis, increased liver enzymes.
Genitourinary: Renal failure.
Endocrine: DM, hyperglycaemia, hyperlipidaemia.
Haematologic: Anaemia.
Musculosckeletal: Rhabdomyolysis, myopathy.
Ophthalmologic: Blurred vision.
Dermatologic: Sweating.
Potentially Fatal: Rarely, Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis, drug rash w/ eosinophilia and systemic symptoms (DRESS), hepatic failure.
MonitoringParameters
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: 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

Click on icon to see table/diagram/image
Storage
Store at 25°C. Protect from moisture.
MIMS Class
ATC Classification
J05AG04 - etravirine ; Belongs to the class of non-nucleoside reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.
Disclaimer: This information is independently developed by MIMS based on Etravirine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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