Antiretroviral therapy for HIV Flashcards
MOA of NRTI
competitive inhibition of reverse transcriptase to prevent formation of viral DNA from viral RNA
*DNA chain termination
ADRs of NRTIs
potential for lactic acidosis, hepatic steatosis, lipodystrophy
*No significant drug interactions
zidovudine (AZT)
nucleoside RTI
ADR: marrow suppression
didanosine (ddI)
nucleoside RTI
ADR: pancreatitis, neuropathy
stavudine (D4T)
nucleoside RTI
ADR: all shared ADRs of NRTIs increased; neuropathy
lamivudine (3TC)
nucleoside RTI
ADR: headache
emtricitabine (FTC)
nucleoside RTI
ADR: headache, diarrhea
abacavir (ABC)
nucleoside RTI
ADR: hypersensitivity reaction
tenofovir (TDF)
*nucleotide RTI
ADR: diarrhea, n/v, Fanconi syndrome (dz of prox renal tubules -> glucose, amino acids, uric acid, phosphate, bicarb passed into urine, instead of reabsorbed)
MOA of NNRTI
direct, non-nucleoside inhibitors of RT; doesn’t require metabolic conversion, not incorporated into viral DNA, additive effect to NRTI
ADR of NNRTI
rash, may -> Stevens-Johnson syndrome
significant drug interactions
nevirapine
NNRTI
ADR: rash, SJS, hepatotoxicity (esp CD4 > 250), modest CYP 3A4 inducer, may precipitate withdrawal in methadone maintenance patients
delaviridine
NNRTI
ADR: rash, SJS, HA, strong CYP 3A inhibitor
*rarely used d/t low potency
efavirenz
NNRTI
ADR: rash, SJS, neuropsych reaction, mod CYP 3A4 inducer, teratogenic
etravirine
NNRTI
ADR: rash, SJS, hyperlipidemia, modest CYP 3A4 inducer; CYP 2C9 and 2C19 inhibitor
rilpivirine
NNRTI
ADR: rash, HA, prolonged QT interval
MOA protease inhibitors
prevents viral protease from forming functional viral proteins necessary to mature viral particle and viral replication