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)
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