Dosing and uses of Intelence (etravirine)
Adult dosage forms and strengths
tablet
- 100mg
- 200mg
HIV Infection
Indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in antiretroviral treatment-experienced patients, who have evidence of viral replication and HIV-1 strains resistant to a non-nucleoside reverse transcriptase inhibitor (NNRTI) and other antiretroviral agents
200 mg PO q12hr
Administration
Take ONLY after a meaL
If unable to swallow tablet whole, may disperse tablet(s) in 5 mL of water, stir dispersion well; may add more water or alternatively orange juice or milk; do not mix with grapefruit juice, warm liquids, or carbonated beverages
Drink dispersion immediately
Rinse glass several times with water, orange juice, or milk and completely swallow the rinse each time to ensure the entire dose is taken
Renal Impairment
No dosage adjustment required
Hepatic Impairment
Mild-to-moderate (Child-Pugh class A or B): No dosage adjustment required
Severe impairment (Child-Pugh class C): Not studied
Pediatric dosage forms and strengths
tablet
- 25mg (scored)
- 100mg
- 200mg
HIV Infection
Indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in antiretroviral treatment-experienced patients, who have evidence of viral replication and HIV-1 strains resistant to a non-nucleoside reverse transcriptase inhibitor (NNRTI) and other antiretroviral agents
<6 years
- Safety and efficacy not established
>6 years
- <16 kg: Safety and efficacy not established
- 16 kg to <20 kg: 100 mg PO q12hr
- 20 kg to <25 kg: 125 mg PO q12hr
- 25 kg to <30 kg: 150 mg PO q12hr
- 30 kg or greater: 200 mg PO q12hr
Administration
Take ONLY after a meaL
If unable to swallow tablet whole, may disperse tablet(s) in 5 mL of water, stir dispersion well; may add more water or alternatively orange juice or milk; do not mix with grapefruit juice, warm liquids, or carbonated beverages
Drink dispersion immediately
Rinse glass several times with water, orange juice, or milk and completely swallow the rinse each time to ensure the entire dose is taken
Intelence (etravirine) adverse (side) effects
>10%
Rash (16.9%)
Nausea (13.9%)
Increased LDL (13%)
1-10%
GI disorders (2.3-5.2%)
Fatigue (3.3%)
Peripheral neuropathy (4%)
Increased creatinine (2%)
Diarrhea (2%)
<1%
Stevens-Johnson syndrome
Erythema multiforme
Angina
Angioedema
Toxic epidermal necrolysis (including reports of fatalities)
Hypersensitivity reactions (including cases of hepatic failure)
Postmarketing Reports
Immune system disorders: Severe hypersensitivity reactions including DRESS and cases of hepatic failure
Musculoskeletal and connective tissue disorders: Rhabdomyolysis
Skin and subcutaneous tissue disorders: Fatal cases of toxic epidermal necrolysis
Warnings
Contraindications
Coadministration with drugs (eg, CYP inducers) where significant decreases in etravirine plasma concentrations may occur, which may result in loss of virologic response and possible resistance and cross-resistance to other NNRTIs
Cautions
Hypersensitivity
Risk of severe skin reactions, including Stevens-Johnson Syndrome, erythema multiforme, toxic epidermal necrolysis (sometimes accompanied by hepatic failure)
Hypersensitivity reactions including Drug Rash with Eosinophilia and Systemic Symptoms (DRESS) have also been reported and were characterized by rash, constitutional findings, and sometimes organ dysfunction
Discontinue if severe rash develops and initiate appropriate therapy
Risk of immune reconstitution syndrome
50% decrease in absorption when administered under fasting conditions: only take with meaL
Do not coadminister with other NNRTIs
Pregnancy and lactation
Pregnancy category: B
Lactation: It is not known whether etravirine is excreted in milk. It should not be administered to nursing mothers. The CDC advises HIV-infected women not to breast-feed to avoid postnatal transmission of HIV.
Pregnancy Registry: Physicians are encouraged to enroll pregnant women exposed to etravirine by calling 1-800-258-4263.
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Intelence (etravirine)
Mechanism of action
Non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1
Absorption
Peak Plasma Time: 3-5 hr
Distribution
Protein Bound: 99.9%
Metabolism
Metabolized in liver by CYP3A4, CYP2C9, and CYP2C19
Induces CYP3A4
Inhibits CYP2C9 and CYP2C19
Elimination
Half-Life: 41 hr +/- 20 hr
Excretion: Feces 93.7%; urine 1.2%
