Etravirine

Etravirine is a prescription medication used for the treatment of human immunodeficiency virus-1 (HIV-1) infection in combination with two or more additional antiretroviral agents in treatment-experienced patients exhibiting viral replication with documented non-nucleoside reverse transcriptase inhibitor (NNRTI) resistance.

• Etravirine is available under the following different brand names: Intelence

Common side effects of Etravirine include:

• nausea
• rash
• numbness or tingly feeling in the hands or feet
• dizziness
• drowsiness
• blurred vision
• upset stomach
• constipation
• heartburn
• dry mouth
• unusual dreams
• changes in the shape or location of body fat (especially in the arms, legs, face, neck, breasts, and waist)

Serious side effects of Etravirine include:

• rash
• redness, bumps, or blisters on the skin or in the mouth
• redness or swelling of the eyes
• swelling of the face
• sore throat, cough, fever, chills, or other signs of infection
• general ill feeling
• tiredness
• muscle or joint aches
• yellowing of the skin or eyes
• dark-colored urine
• pale-colored stools
• pain in the upper right part of the stomach
• loss of appetite

Rare side effects of Etravirine include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Tablet

• 25 mg
• 100 mg
• 200 mg

HIV Infection

Adult dosage

• 200 mg orally every 12 hours

Pediatric dosage

• Children aged below 2 years: Safety and efficacy not established.
• Children aged between 2 to 19 years and weighing 10 kg and more.
• Children weighing between 10 to 19 kg: 100 mg orally every 12 hours.
• Children weighing between 20 to 24 kg: 125 mg orally every 12 hours.
• Children weighing between 25 to 29 kg: 150 mg orally every 12 hours.
• Children weighing 30 kg and more: 200 mg orally every 12 hours.

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Etravirine has severe interactions with at least 32 other drugs
• Etravirine has serious interactions with at least 139 other drugs
• Etravirine has moderate interactions with at least 262 other drugs
• Etravirine has minor interactions with at least 69 other drugs

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Etravirine?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Etravirine?”

Cautions

• Hypersensitivity
  • Risk for severe skin reactions (eg, Stevens-Johnson Syndrome, erythema multiforme, toxic epidermal necrolysis)
  • Hypersensitivity reactions (including drug rash with eosinophilia and systemic symptoms) reported, characterized by rash, constitutional findings, and sometimes organ dysfunction; discontinue if severe rash develops and initiate appropriate therapy
• Risk for immune reconstitution syndrome
  • 50% decrease in absorption when administered under fasting conditions; take Etravirine only with a meal
• Drug interactions overview
  • Etravirine is a substrate of CYP3A, CYP2C9, and CYP2C19; coadministration with inhibitors or inducers of CYP3A, CYP2C9, and CYP2C19 may alter the efficacy or adverse reaction profile of Etravirine
  • Etravirine induces CYP3A and inhibits CYP2C9, CYP2C19, and P-glycoprotein (P-gp); coadministration of Etravirine with drugs that are substrates of CYP3A, CYP2C9, and CYP2C19 or are transported by P-gp may alter the efficacy or toxicity of the coadministered drug(s)

Pregnancy and Lactation

• An ART pregnancy registry has been established (1-800-258-4263); prospective pregnancy data from the Antiviral Pregnancy Registry (APR) are not sufficient to adequately assess the risk for birth defects or miscarriage
• Etravirine use during pregnancy was evaluated in a limited number of individuals as reported by the APR, and available data show 1 birth defect in 66 first-trimester exposures to Etravirine-containing regimens.
• Lactation
  • The CDC recommends that mothers infected with HIV-1 should not breastfeed their infants to avoid risking postnatal transmission of HIV
  • Based on limited data, etravirine is present in human breast milk
  • No data available on the effects of etravirine on the breastfed infant or milk production; instruct mothers not to breastfeed during treatment because of the potential for HIV-1 transmission (in HIV-negative infants), developing viral resistance (in HIV-positive infants), and adverse reactions in breastfed infants like those seen in adults