B3-071B Anti HIV Chemotherapy

Question 1

mechanism: Maraviroc

Answer 1

fusion inhibitor, prevents CCR5 and gp120 binding

Question 2

before administering Maraviroc, do a ______ to eval for CCR5 or CXCR4

Answer 2

tropism assay

Question 3

Side effect: maraviroc

Answer 3

severe hepatotoxicity

Question 4

is maraviroc common?

Answer 4

no

Question 5

mechanism: enfuvirtide

Answer 5

fusion inhibitor; inhibits gp41 and prevents fusion of membranes

Question 6

blocks infection of new cells

Answer 6

enfuvirtide

Question 7

limited to patients who no longer respond to other regimens

Answer 7

enfuvirtide

Question 8

mechanism: zidovudine

Answer 8

thymidine analog

Question 9

NRTIs ________ inhibit reverse transcriptase

Answer 9

competitively

Question 10

Zidovudine exhibits __________, due to specificity for HIV RT

Answer 10

selective toxicity

Question 11

Zidovudine can reduce

Answer 11

mother-to-newborn transmission

Question 12

mechanism: abacavir

Answer 12

guanosine analog

Question 13

abacavir is metabolized

Answer 13

by alcohol dehydrogenase (EtOH interaction)

Question 14

resistance to abacavir develops _____

Answer 14

slowly

Question 15

Abacavir can cause a Type _____ hypersensitivity

Answer 15

I

Question 16

abacavir hypersensitivity is caused by the _______ allele

Answer 16

HLA-B5701

**testing is done on all patients prior to administration, but only 50% react

Question 17

tenofovir is often combined with

Answer 17

emtricitabine

Question 18

tenofovir can cause

Answer 18

renal toxicity (disoproxil)

Question 19

tenofovir and emtricitabine are used for

Answer 19

HIV pre-exposure prophylaxis

Question 20

post exposure prophylaxis

Answer 20

tenofovir and emtricitabine + integrase inhibitor of protease inhibitor

Question 21

lamivudine mechanism

Answer 21

cytosine analog

Question 22

mechanism: emtricitabine

Answer 22

fluorinated analog of lamivudine

Question 23

NNRTIs ________ inhibit reverse transcriptase

Answer 23

non-competitively (allosteric inhibition)

Question 24

nevirapine is an ______ of CYP3A

Answer 24

inducer

Question 25

efavirenz is an ________ of CYP34A

Answer 25

inducer and inhibitor (drug-drug interactions)

Question 26

side effects: efavirenz

Answer 26

dizziness, drowsiness, nightmares, headaches, confusion, amnesia

Question 27

why is Efavirenz considered second line?

Answer 27

CNS side effects are severe

Question 28

Doravirine is metabolized by

Answer 28

CYP34A

Question 29

intergrase inhibitors provide a ______ viral target

Answer 29

unique

Question 30

raltegravir is an

Answer 30

intergrase inhibitor

Question 31

dolutegravir is eleminated by

Answer 31

glucuronidation minor role for CYP34A

Question 32

bictegravir is only available in

Answer 32

a fixed combination pill with emtricitabine and tenofovir

Question 33

bictegravir aka

Answer 33

Biktarvy

Question 34

cabotegravir must be

Answer 34

dosed with rilpirivine

Question 35

protease inhibitors inhibit _____ protease

Answer 35

aspartyl

Question 36

adverse effects of protease inhibitors

Answer 36

diarrhea nausea lipodystrophy insulin resistance

Question 37

Saquinavir

Answer 37

1st HIV protease inhibitor

Question 38

indinavir adverse effect

Answer 38

nephrolithiasis

Question 39

ritonavir

Answer 39

potent CYP34A inhibitor **boosts concentration of other proteases

Question 40

darunavir/ritonavir is administered with a

Answer 40

subtherapeutic dose of ritonavir, inhibits CYP34A

Question 41

cobicistat

Answer 41

no antiviral activity, CYP3A inhibitor **boosts concentration of other proteases

Question 42

atazanavir

Answer 42

is not associated with typical protease inhibitor side effects

Question 43

ART usually consists of

Answer 43

3-4 anti retroviral drugs 2 NRTIs + protease inhibitor

Question 44

CYP3A4 substrates

Answer 44

delavirdine, efavirenz, nevirapine, all protease inhibitors

Question 45

CYP34A inducers

Answer 45

efavirenz, nevirapine, amprenavir

Question 46

CYP34A inhibitors

Answer 46

delavirdine, efavirenz, all protease inhibitors

Question 47

unique targets of ART

Answer 47

reverse transcriptase integrase HIV protease