HIV Antiretrovirals Flashcards
NRTIs - 2 agents
Emtricitabine (FTC)
Tenofovir (TDF)
NRTIs - Adverse Effects
Toxicity results from inhibition of mitochondrial DNA polymerase gamma; serious adverse events include:
Anemia Granulocytopenia Myopathy Neuropathy Lactic Acidosis Steatosis
NNRTIs - Adverse Effects
Pregnancy Category D
Rash
GI upset
CNS effects - Dizziness, headache, inability to concentrate
Induction of CYP3A4 (decreased methadone levels)
NNRTIs - 2 Agents
Efavirenz (EFV)
Ertravirine - remains effective in treatment-experienced patients with resistance to older NNRTIs
Atripla
Emtricitabine + Tenofovir + Efavirenz
Protease Inhibitors - Agents
Atazanavir
Darunavir
Protease Inhibitors - Adverse Effects
Metabolized by CYP3A4 - lots of DDIs
Rash - can be severe (SJ-like) with Darunavir
GI upset
Metabolic effects - hyperlipidemia, insulin resistance, hyperlipidemia, lipodystrophy
Hepatotoxicity - especially in pts with HBV/HCV
Ritonavir
Potent inhibitor of CYP3A4
Co-administered with protease inhibitors to increase drug plasma levels - “Ritonavir boosting”
Integrase Inhibitors - Agents
Raltegravir
Integrase Inhibitors - Adverse Effects
Generally well tolerated; minor adverse effects:
Diarrhea
Nausea
Headache
Rare myopathy, rhabdomyolysis
Entry Inhibitor - Agent
Maraviroc
Entry Inhibitor - Adverse Effects
Minor adverse effects: Cough Fever URI Dizziness Rash
Indications for use of Maraviroc
Treatment-experienced adults with R5-tropic HIV-1 (requires tropism test); not used for initial therapy
Fusion Inhibitor - Agent
Enfurvirtide
Fusion Inhibitor - Adverse Effects
Injection site reactions
Eosinophilia
Hypersensitivity
Increased risk of bacterial pneumonia