antiretroviral Flashcards
who are the analog inhibitors
protease inhibitors , mimic hydrolysis transition state = sp3 tetrahedral
What is ritonavir
its used in combo with lopinavir
doesnt have antiretroviral activity but inhibits lopinavir metabolism by cyp3a4
Antiretrovirals with dipeptide or tripeptide structures
protease inhibitors
Darunavir , lopinavir
where do INSTIs bind in the IN enzyme
diketo acids are needed for binding
near the acidic catalytic residues (raltegravir)
if IN enzyme develops mutations/resistance to the diketo acids where would this occur
near the conserved residues in the IN enzyme
what is special about maraviroc structure
it has a tropane ring system
(fusion of pyrrolidine and piperidine)
which antiretroviral is classified as CCR5 receptor antagonist
Maraviroc
which antiretroviral is not recommend as an initial treatment for naive patients (patients who have been diagnosed with HIV first the first time)?
Maraviroc
fusion inhibitor
enfuvirtide
only used for patients with multi-drug resistant virus
emtrictibine and lamvudine rare AE
skin discoloration
pancreatitis
superior viral load suppression and transmission
tenofovir
NNRTIs are active against
only HIV 1
Zidovudine uses
mainly in peds, to prevent transfer of HIV from mother to fetus
which antiretroviral drug could be used for a patient with high lipid profile
An INSTIs ex raltegravir or dolutegravir
AE of NNRTIs
SJS
boosters are contraindicated in
women of child bearing age and pregnant women bc drug levels may decrease
NRTIs main problem
the fact that they have high affinity to DNA polymerase y which is mitochondrial enzyme results in inhibiting it and causing myopathy, granulocytopenia , pancretitis , anemia , peripheral neuropathy
lamvudine, emtricitbine , tenfovir dont cause this
when can we give TDF
if patient is in end stage kidney disease and is on hemodialysis
AE f TDF
1) kidney injury
-Proximal tubular dysfunction (fanconi)
2) Bone loss
whats both a blessing and a curse for NNRTIs
the fact that they have a long half life is an advantage but if regimen is stopped it could lead to functional NNRTI monotherpay which leads to resistance
boosters
ritonavir and Cobicistatis(chemically similar to ritonavir)
PIs and INSTIs are usually coadminstered with them (low dose) to increase half life, peak troughs, cmax, reduce dosing
disadvantages of AZT
Inferior virologic potency
dosed twice daily
AE reactions
first FDA approved antiretroviral drug
Zidovudine AZT
