HIV pharmacology Flashcards
Classes of drugs used for HIV
- NRTI
- NNRTI
- PI
- INSTI
- viral fusion/entry inhibitors
MOA of NRTIs
host cell purine and pyrimidine kinase enzymes must convert them into nucleotide triphosphates inside of HIV infected CD4+ cells so then gets added to viral DNA which stops the reverse transcription
Black box warning for NRTIs
Why does this happen
possibility of lactic acidosis syndrome which is potentially fatal
similarities b/t HIV reverse transcriptase and host mitochondrial DNA polymerase gamma leading to deficient proteins needed for oxidative phosphorylation
Which 3 NRTIs cause the most damage to mitochondrial polymerase
- didanosine
- Stavudine
- Zidovudine
NRTIs that are LESS BAD for mitochondrial polymerases
- Tenofovir
- Lamivudine
- Emtricitabine
- Abacavir
Which NRTI also causes pancreatitis
Stavudine
NRTI treatment should be suspended in the setting of what?
- rapidly rising aminotransferase levels
- progressive hepatomegaly
- metabolic acidosis of unknown cause
Which NRTI starts out with a phosphate and is therefore a nucleoTide instead of nucleoSide and doesn’t rely on the virus to add a phosphate
Tenofovir
What is the complication that is a result of Tenofovir being a nucleoTide instead of a side
nephrotoxicity
In patients with renal insufficiency, what alternative NRTI is preferred over Tenofovir
Abacavir
How many NRTIs do you want to use at the same time
2
What is the distinct complication associated with Abacavir
idiosyncratic, multisystem inflammatory reaction
What genetics are associated with the hypersensitivity reaction that happens sometimes with Abacavir
HLA-B*5701
NRTI combos to AVOID
- Zidovudine and Stavudine
- Lamivudine and Emtricitabine
- Stavudine and didanosine
- Didanosine and Tenofovir
- any 3 drug combo
Preferred initial combo for naive HIV patient
Tenofovir and Emtricitabine
