- MOA: binds to reverse transcriptase and blocks the RNA-dependent and DNA-dependent DNA polymerase activities including HIV-1 replication.
- Class effects: all drugs in this class can cause a rash that is sometimes severe (most common with nevirapine); can cause increase LFT's, and have a low genetic barrier to resistance (single mutation). Mainly cleared by the liver.
- Pts with achlorhydria (little to no gastric acid in the stomach) should take with acidic beverage; separate dose from antacids by 1 hour.
- Strong hepatic inhibitors.
- Take on an empty stomach, preferably at bedtime.
- Preg Cat D: not to be used in pregnant women (particularly the 1st trimester)
- 2C9 and 3A4 inhibitors (moderate)
- 3A4 inducer (strong)
efavirenz + emtricitabine + tenofovir
- Take after a full meal.
- S/e: rash, peripheral neuropathy, HTN
- Monitor LFT's frequently.
- BBW: severe hepatotoxic reaction (liver failure, death); risk is great in the first 6 weeks. Severe, life-threatening skin reaction (SJS, TENS); intensive monitoring in the first 18 weeks of tx.
- 3A4 inducer.