Week 6: HIV drugs Flashcards
Name Nucleoside Reverse Transcriptase Inhibitors
Zidovudine (AZT), Lamivudine, Abacavir, Emtricitabine
Name NucleoTIDE Reverse Transcriptase Inhibitor
Tenofovir
Name Non-nucleoside reverse transcriptase inhibitor
Etravirine, Efavirenz, Rilpivirine
Name Protase Inhibitors
Atazanavir, Darunavir
Name integrase inhibitor
Raltegravir
Name Fusion inhibitor
Enfuvirtide (T-20)
Name CCR5 antagonist
Maraviroc
What is the goal of HIV treatment?
fully undetectable levels of virus
What is the mechanism of NRTIs?
competitively inhibit reverse transcriptase and can be incorporated into viral DNA chain and cause termination
T/F: NRTIs require phosphorylation by cellular enzymes to be active
True
What are AE of NRTIs?
lactic acidosis with hepatic steatosis; most likely due to mitochondrial toxicity
What are AE of zidovudine?
granulocytopenia and anemia in 45% of patients, CNS disturbances
What are AE of Abacavir?
hypersensitivity reactions (Test for HLA-B*5701)
What is MOA of Tenofovir (nucleotide RTI)
same as NRTI
What are AE of tenofovir?
nausea, vomiting, diarrhea and POTENTIAL FOR RENAL FAILURE
What is MOA of nnRTI (etravirine, efavirenz, rilpivirine)
bind directly to RT at a site different from NRTI, preventing enzyme from producing viral DNA
Do NNRTIs have cross resistance with NRTIs and protease inhibitors?
No
What are AE of NNRTIs?
varying levels of GI intolerance and skin rash, can affect cytochrome P450
What can you not use rilpivirine?
patients with pretreatment viral loads of >100,000 copies/ml
What is mechanism of protease inhibitors?
Prevents maturation of full assembled virus, preventing buddying of the virus and therefore preventing further infections
What are AE of Protease inhibitors?
GI, hepatotoxicity, hyperglycemia and insulin resistance, dyslipidemia, CYP3A4
What is the better use of ritonavir?
Inhibits CYP3A4 to increase serum levels of other drugs
What is MOA of cobicistat?
pharmacokinetic enhancer that inhibits CYP3A4 and intestinal transport proteins; acts as a booster of protease inhibitors
What is MOA of enfuvirtide (FI)
Prevents conformational change of gp41 upon binding of HIV particle to cell
What is MOA of integrase inhibitors (Raltegravir)
Inhibits strand transfer into host DNA
What is MOA of CCR5 antagonist (Maraviroc)
Blocks CCR5, a major co-receptor used by HIV-1 to gain entry into host cells
What is AE of CCR5 antagonist?
pyrexia, rash, postural dizziness
What is HAART the result of? What is it?
long term use of combination anti-retroviral therapies usually RTIs in combo with PI. Results in lipodystrophy (central adiposity, hyperlipidemia, insulin resistance and DM)
