antiretroviral

Question 1

who are the analog inhibitors

Answer 1

protease inhibitors , mimic hydrolysis transition state = sp3 tetrahedral

Question 2

What is ritonavir

Answer 2

its used in combo with lopinavir

doesnt have antiretroviral activity but inhibits lopinavir metabolism by cyp3a4

Question 3

Antiretrovirals with dipeptide or tripeptide structures

Answer 3

protease inhibitors

Darunavir , lopinavir

Question 4

where do INSTIs bind in the IN enzyme

Answer 4

diketo acids are needed for binding

near the acidic catalytic residues (raltegravir)

Question 5

if IN enzyme develops mutations/resistance to the diketo acids where would this occur

Answer 5

near the conserved residues in the IN enzyme

Question 6

what is special about maraviroc structure

Answer 6

it has a tropane ring system

(fusion of pyrrolidine and piperidine)

Question 7

which antiretroviral is classified as CCR5 receptor antagonist

Answer 7

Maraviroc

Question 8

which antiretroviral is not recommend as an initial treatment for naive patients (patients who have been diagnosed with HIV first the first time)?

Answer 8

Maraviroc

Question 9

fusion inhibitor

Answer 9

enfuvirtide

only used for patients with multi-drug resistant virus

Question 10

emtrictibine and lamvudine rare AE

Answer 10

skin discoloration
pancreatitis

Question 11

superior viral load suppression and transmission

Answer 11

tenofovir

Question 12

NNRTIs are active against

Answer 12

only HIV 1

Question 13

Zidovudine uses

Answer 13

mainly in peds, to prevent transfer of HIV from mother to fetus

Question 14

which antiretroviral drug could be used for a patient with high lipid profile

Answer 14

An INSTIs ex raltegravir or dolutegravir

Question 15

AE of NNRTIs

Answer 15

SJS

Question 16

boosters are contraindicated in

Answer 16

women of child bearing age and pregnant women bc drug levels may decrease

Question 17

NRTIs main problem

Answer 17

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

Question 18

when can we give TDF

Answer 18

if patient is in end stage kidney disease and is on hemodialysis

Question 19

AE f TDF

Answer 19

1) kidney injury

-Proximal tubular dysfunction (fanconi)

2) Bone loss

Question 20

whats both a blessing and a curse for NNRTIs

Answer 20

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

Question 21

boosters

Answer 21

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

Question 22

disadvantages of AZT

Answer 22

Inferior virologic potency

dosed twice daily

AE reactions

Question 23

first FDA approved antiretroviral drug

Answer 23

Zidovudine AZT