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
ADR of protease inhibitors
GI distress, hyperglycemia, insulin resistance, hyperlipidemia, CAD, fat accumulation, hepatotoxicity
Metabolism by and inhibits CYP 3A4 (ritonavir most)
Metabolism induced by rifampin and phenytoin
Absorption reduced with rising gastric pH d/t H2-blockers and PPIs
saquinavir
PI
ADR: n/v/d
darunavir
PI
ADR: n/v, rash
indinavir
PI
ADR: n/v, nephrolithiasis
nelfinavir
PI
ADR: nausea, diarrhea
fosamprenavir
PI
ADR: nausea, rash
atazanavir
PI
ADR: increased bilirubin