Class: Antiretroviral Agent, Reverse Transcriptase Inhibitor
Dosage Forms. Capsule: 50 mg, 200 mg; Tablet: 600 mg
Common FDA Label Indication, Dosing, and Titration.
1. Treatment of HIV-1 infections in combination with at least two other antiretroviral agents: Adults and children ≥40 kg, 600 mg po daily; Children <40 kg, weight based and used in combination with ritonavir
Off Label Uses. None
MOA. Binds to HIV reverse transcriptase, blocking the RNA-dependent and DNA-dependent DNA polymerase activities including HIV-1 replication
Drug Characteristics: Efavirenz
Medication Safety Issues: Efavirenz
Drug Interactions: Efavirenz
Adverse Reactions: Efavirenz
Efficacy Monitoring Parameters. HIV viral load, CD4 count, HIV resistance testing prior to starting therapy.
Toxicity Monitoring Parameters. Liver function tests, bilirubin, CBCs, lipid panel.
Key Patient Counseling Points. Multiple, potentially serious drug interactions, do not take new medications, OTCs, or herbals without consulting healthcare provider. Take on an empty stomach at bedtime. Do not open, chew, or crush capsule. Does not prevent transmission of HIV, practice safe sex. May cause drowsiness, avoid driving and concurrent CNS depressants.
Clinical Pearls. Not recommended for children less than 3 y of age. Efavirenz is the non-nucleoside reverse transcriptase inhibitor of choice for initial combination therapy for HIV.