Non-Nucleoside Analogue Reverse Transcriptase Inhibitors (NNRTIs)
Last Updated: May 22, 2018; Last Reviewed: May 22, 2018
Etravirine (ETR, Intelence, TMC 125)
|Etravirine (ETR, Intelence, TMC 125)
For additional information see Drugs@FDA: http://www.accessdata.fda.gov/scripts/cder/daf/
|Tablets: 25 mg, 100 mg, and 200 mg
||Selected Adverse Events
- Not approved for use in neonates/infants.
- Not approved for use in children aged <6 years. Studies in infants and children aged 2 months to 6 years are under way.
Antiretroviral-Experienced Children and Adolescents Aged 6–18 Years and Weighing ≥16 kg
|16 kg to <20 kg
||100 mg twice daily
|20 kg to <25 kg
||125 mg twice daily
|25 kg to <30 kg
||150 mg twice daily
||200 mg twice daily
Adult Dose (Antiretroviral-Experienced Patients):
- 200 mg twice daily following a meal
- Rash, including Stevens-Johnson syndrome
- Hypersensitivity with rash, constitutional findings, and sometimes organ dysfunction, including hepatic failure
Instructions for Dispersing Etravirine Tablets in Liquid:
- Always administer etravirine following a meal. Area under the curve of etravirine is decreased by about 50% when the drug is taken on an empty stomach. The type of food does not affect the exposure to etravirine.
- Etravirine tablets are sensitive to moisture; store at room temperature in original container with desiccant.
- Patients who are unable to swallow etravirine tablets may disperse the tablets in liquid.
- Place the tablet(s) in 5 mL (1 teaspoon) of water, or enough liquid to cover the medication, and stir well until the water looks milky. If desired, add more water or, alternatively, orange juice or milk. Note: Patients should not place the tablets in orange juice or milk without first adding water. The use of grapefruit juice, warm (>40°C) drinks, or carbonated beverages should be avoided.
- Drink immediately, then rinse the glass several times with water, orange juice, or milk and completely swallow the rinse each time to make sure the entire dose is consumed.
Etravirine Dosing in Patients with Hepatic Impairment:
- Etravirine is an inducer of cytochrome P450 3A4 (CYP3A4) and an inhibitor of CYP2C9, CYP2C19, and P-glycoprotein. It is a substrate for CYP3A4, 2C9, and 2C19.
- Etravirine is involved in multiple interactions with antiretroviral agents and other drugs (see text below).
Etravirine Dosing in Patients with Renal Impairment:
- No dose adjustment is necessary for patients with mild-to-moderate hepatic insufficiency. No dosing information is available for patients with severe hepatic impairment.
- Dose adjustment is not required in patients with renal impairment.