B3-071B Anti HIV Chemotherapy Flashcards

1
Q

mechanism: Maraviroc

A

fusion inhibitor, prevents CCR5 and gp120 binding

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2
Q

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

A

tropism assay

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3
Q

Side effect: maraviroc

A

severe hepatotoxicity

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4
Q

is maraviroc common?

A

no

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5
Q

mechanism: enfuvirtide

A

fusion inhibitor; inhibits gp41 and prevents fusion of membranes

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6
Q

blocks infection of new cells

A

enfuvirtide

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7
Q

limited to patients who no longer respond to other regimens

A

enfuvirtide

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8
Q

mechanism: zidovudine

A

thymidine analog

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9
Q

NRTIs ________ inhibit reverse transcriptase

A

competitively

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10
Q

Zidovudine exhibits __________, due to specificity for HIV RT

A

selective toxicity

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11
Q

Zidovudine can reduce

A

mother-to-newborn transmission

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12
Q

mechanism: abacavir

A

guanosine analog

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13
Q

abacavir is metabolized

A

by alcohol dehydrogenase (EtOH interaction)

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14
Q

resistance to abacavir develops _____

A

slowly

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15
Q

Abacavir can cause a Type _____ hypersensitivity

A

I

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16
Q

abacavir hypersensitivity is caused by the _______ allele

A

HLA-B5701

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

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17
Q

tenofovir is often combined with

A

emtricitabine

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18
Q

tenofovir can cause

A

renal toxicity (disoproxil)

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19
Q

tenofovir and emtricitabine are used for

A

HIV pre-exposure prophylaxis

20
Q

post exposure prophylaxis

A

tenofovir and emtricitabine + integrase inhibitor of protease inhibitor

21
Q

lamivudine mechanism

A

cytosine analog

22
Q

mechanism: emtricitabine

A

fluorinated analog of lamivudine

23
Q

NNRTIs ________ inhibit reverse transcriptase

A

non-competitively (allosteric inhibition)

24
Q

nevirapine is an ______ of CYP3A

A

inducer

25
Q

efavirenz is an ________ of CYP34A

A

inducer and inhibitor (drug-drug interactions)

26
Q

side effects: efavirenz

A

dizziness, drowsiness, nightmares, headaches, confusion, amnesia

27
Q

why is Efavirenz considered second line?

A

CNS side effects are severe

28
Q

Doravirine is metabolized by

A

CYP34A

29
Q

intergrase inhibitors provide a ______ viral target

A

unique

30
Q

raltegravir is an

A

intergrase inhibitor

31
Q

dolutegravir is eleminated by

A

glucuronidation

minor role for CYP34A

32
Q

bictegravir is only available in

A

a fixed combination pill with emtricitabine and tenofovir

33
Q

bictegravir aka

A

Biktarvy

34
Q

cabotegravir must be

A

dosed with rilpirivine

35
Q

protease inhibitors inhibit _____ protease

A

aspartyl

36
Q

adverse effects of protease inhibitors

A

diarrhea
nausea
lipodystrophy
insulin resistance

37
Q

Saquinavir

A

1st HIV protease inhibitor

38
Q

indinavir adverse effect

A

nephrolithiasis

39
Q

ritonavir

A

potent CYP34A inhibitor

**boosts concentration of other proteases

40
Q

darunavir/ritonavir is administered with a

A

subtherapeutic dose of ritonavir, inhibits CYP34A

41
Q

cobicistat

A

no antiviral activity, CYP3A inhibitor

**boosts concentration of other proteases

42
Q

atazanavir

A

is not associated with typical protease inhibitor side effects

43
Q

ART usually consists of

A

3-4 anti retroviral drugs

2 NRTIs + protease inhibitor

44
Q

CYP3A4 substrates

A

delavirdine, efavirenz, nevirapine, all protease inhibitors

45
Q

CYP34A inducers

A

efavirenz, nevirapine, amprenavir

46
Q

CYP34A inhibitors

A

delavirdine, efavirenz, all protease inhibitors

47
Q

unique targets of ART

A

reverse transcriptase
integrase
HIV protease