HIV treatment Flashcards
HAART therapy
2 NRTIs + 1 NNRTI or 1 protease inhibitor or 1 integrase inhibitor
protease inhibitors drugs (general)
end in -“nadir”
protease inhibitor moa
prevents cleavage of the polypeptide products of HIV mRNA into their functional parts; this prevents maturation of new viruses
protease inhibitor toxicity
hyperglycemia, GI intolerance, lipodystrophy, nephropathy, hematuria, diabetes mellitus;
ritonavir other use
increase concentrations of other drugs by inhibiting CYPs
Nucleoside reverse transcriptase inhibitors
abacavir, didanosine, emtricitabine, lamivudine, stavudine, tenofovir, zidovudine,
NRTI moa
competitively inhibit nucleotide binding to reverse transcriptase and terminating the DNA chain due to their lack of a 3’OH group; NRTIs are nucleosides need to be activated except tenofovir which is a nucleotide
zidovudine use
general prophylaxis and during pregnancy to decrease the risk of fetal transmission
NRTI toxicity
bone marrow suppression (can be reversed with G-CSF and erythropoietin), peripheral neuropathy, lactic acidosis, rash,
zidovudine - anemia
didanosine - pancreatitis
NNRTIs
efavirenz, nevirapine, delvirdine
NNRTI moa
bind to reverse transcriptase at site different from NRTIs; do not require phosphorylation to be active or compete with nucleotides;
NNRTI toxicity
rash and hepatotoxicity common to all NNRTIs;
vivid dreams and CNS symptoms are common with efavirenz;
delavirdine and efavirenz are contraindicated in pregnancy
raltegravir moa
inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase
raltegravir toxicity
hypercholesterolemia
enfuvirtide moa
binds gp41, inhibiting viral entry
