II. Indications
-
HIV Infection with Anti-Retroviral Therapy experienced patients (combination therapy)
- Indicated in HIV resistance (especially K103N) to first-generation NNRTI (Efavirenz or Nevirapine)
- NNRTIs carry a high risk of induced HIV resistance
- Never use NNRTIs as monotherapy in HIV Infection
III. Mechanism
- See Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)
- Second generation, diarylpyrimidine NNRTI
IV. Dosing
- Indicated as part of combination therapy in Anti-Retroviral Therapy experienced patients
- Adult (or child weight >=30 kg)
- Take 200 mg orally twice daily after meals
- Child (age >= 2 years)
- Weight 10 to 20 kg: 100 mg orally twice daily after meals
- Weight 20 to 25 kg: 125 mg orally twice daily after meals
- Weight 25 to 30 kg: 150 mg orally twice daily after meals
- Weight >=30 kg: 200 mg orally twice daily after meals (adult dose)
V. Adverse Effects
- See NNRTI for class related adverse effects
- Rash (20% of patients)
- Stop the agent and do not rechallenge
- Higher risk in women (30%) than men (18%)
- Risk of serious reactions (1-2%)
- Stevens-Johnson Syndrome
- Toxic Epidermal Necrolysis
- Eythema multiforme
- Nausea
- Peripheral Neuropathy
- Hypertension
- Hepatotoxicity
- Obtain Liver Function Tests (LFTs) at baseline and periodically
-
Hyperlipidemia
- Obtain baseline lipid panel and periodically
VI. Safety
- Avoid in Lactation
- Unknown safety in pregnancy (registry exists)
- Has been used in pregnancy for Anti-Retroviral Therapy experienced patients (resistance to other NNRTIs)
VII. Drug Interactions
- Many significant Drug Interactions
- Use formal Drug Interaction application to review
- CYP3A4 Inducer and CYP3A4 Substrate
- CYP2C9 Inhibitor and CYP2C9 Substrate
- CYP2C19 Inhibitor and CYP2C19 Substrate
VIII. Resources
Images: Related links to external sites (from Bing)
Related Studies
| etravirine (on 6/22/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| ETRAVIRINE 200 MG TABLET | Generic | $17.71 each |
| intelence (on 4/20/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| INTELENCE 200 MG TABLET | Generic | $17.71 each |
Ontology: etravirine (C1456409)
| Definition (NCI) | A diarylpyrimidine non-nucleoside reverse transcriptase inhibitor. Etravirine is designed to be active against HIV isolates with mutations that confer resistance to the two most commonly prescribed first-generation NNRTIs. It can bind the enzyme reverse transcriptase (RT) in multiple conformations, both for native and mutant RT, thereby blocking the enzymatic activity of RT. |
| Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
| MSH | C451734 |
| SnomedCT | 432121008, 432221004 |
| LNC | LP68431-3, MTHU028135 |
| English | Etravirine (substance), Etravirine, Etravirine (product), etravirine (medication), etravirine [Chemical/Ingredient], ETRAVIRINE, 4-(6-Amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yloxy)-3,5-dimethylbenzonitrile, ETV, etravirine |
| Spanish | etravirina (producto), etravirina, etravirina (sustancia) |
