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D&D Infectious Disease FINAL > Pharm - HIV pharmacotherapy part 2 > Flashcards

Pharm - HIV pharmacotherapy part 2 Flashcards

1
Q

true or false

Efavirenz is an NNRTI that can be used in pregnancy

A

FALSE

it is an NNRTI but cannot be used in pregnancy

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2
Q

efavirenz is a potent ___ agent

A

HIV-1

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3
Q

name some AE of efavirenz

A

CNS psychiatric events (depression, mania, disturbing dreams, insomnia)

hepatotoxicity (increased liver enzymes)

increased cholesterol

rare - SJS

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4
Q

true or false

nevirapine is an NNRTI that can be used in pregnancy

A

true

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5
Q

AE of nevirapine

A

rash (if becomes severe, discontinue - can be life threatening)

hepatotoxicity

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6
Q

true or false

nevirapine as an excellent oral PK profile and is also effective in preventing transmission of HIV

A

true

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7
Q

name a second gen NNRTI

what is an advantage?

A

etravirine

has better resistance profile

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8
Q

counseling point for etravirine

A

take with food! better absorption

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9
Q

AE etravirine

A

serious rash and allergy, elevated triglyceride and cholesterol, IRIS

also DDI because substrate and inducer of CYP3A4 and CYP2C9 AND 2C19 inhibitor

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10
Q

rilpivirine is an NNRTI ONLY for which patients?

A

treatment naive, 12 and older, greater than 100,000 virus copies/mL

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11
Q

important counseling point for rilpivirine

A

take with meals, but NOT with antacids, H2 antagonists, or PPIS

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12
Q

AE rilpivirine

A

rash, depression, hepatotoxicity, fat redistribution, QT prolongation

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13
Q

name an NNRTI that is CONTRAINDICATED with CYP3A4 inducers

A

doravirine

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14
Q

what is an advantage of doravirine over other NNRTIs

A

It is less hepatotoxic and has a better lipid profile than the others

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15
Q

which 3 NNRTIS are considered 2nd generation

A

etravirine
rilipivirine
doravirine

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16
Q

name 3 protease inhibitors

A

atazanavir
darunavir
ritonavir

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17
Q

explain the MOA of protease inhibitors

A

prevent the breakdown of polyprotein into smaller proteins which come together to form a new virus

inhibits aspartyl protease.

normally, protease breaks the peptide bond between phenylalanine and proline. but when protease is blocked it can;t do this and protein maturation is affected

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18
Q

protease inhibitors mimic what structure

A

peptide

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19
Q

true or false

protease inhibitors for HIV have much less affinity for human proteases

A

TRUE - this is good - prevent side effects

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20
Q

true or false

protease inhibitors are administered alone

A

FALSE

bc of mutations and resistance - need multiple drugs

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21
Q

some AE of protease inhibitors

A

dyslipidemia (cushingoid appearance)

cardiac conduction issues (WT prolongation)

hepatotoxicity

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22
Q

DDI concern with protease inhibitors

A

they are metabolized by CYP3A4 and are substrates of P-gp efflux pump

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23
Q

only PI contraindicated in pregnancy

A

fosamprenavir + ritonavir

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24
Q

atazanavir counseling point

A

take with meals. acidic medium is good for absorption

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25
Q

true or false

atazanavir is recommended in pregnancy

A

TRUE

only one that isnt is the oral solution of fosamprenavir + ritonavir

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26
Q

how is the AE of atazanavir unlike other protease inhibitors?

A

NO dyslipidemia!!

also hyperbilirubinemia is a concern (jaundice)

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27
Q

darunavir is a protease inhibitor that must be coadministered with ______

A

ritonavir

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28
Q

AE concern with darunavir

A

has sulfa group!!!! watch out for hypersensitivity

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29
Q

true or false

darunavir has less frequent dyslipidemia than other protease inhibitors

A

true

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30
Q

fosamprenavir is a prodrug of _______

A

amprenavir

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31
Q

what is fosamprenavir administered with

A

low dose ritonavir

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32
Q

which 2 protease inhibitors have a hypersensitivity concern due to their sulfa group

A

darunavir
fosamprenavir

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33
Q

WHY is fosamprenavir + low dose ritonavir not given in young children and in pregnancy?

A

the oral solution has propylene glycol

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34
Q

true or false

ritonavir is recommended in pregnancy

A

TRUE

alone, it’s fine

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35
Q

which 2 drug levels should be monitored with ritonavir and why

A

theophylline and digoxin - have narrow TIs and their levels may increase

36
Q

ritonavir is not given with -___ due to _____

A

saquinavir

QT prolongation

37
Q

name an entry inhibitor

A

maraviroc

38
Q

name a fusion inhibitor

A

enfuvirtide

enFU (fusion)

“tide” - peptide

39
Q

explain the MOA of maraviroc

A

it’s an entry inhibitor

binds CCR5, preventing it from binding to gp120, which thus prevents fusion and entry of the virus

Just the cd4 receptor attachment is not enough to get in!!!

40
Q

true or false

maraviroc is an ALLOSTERIC CCR5 receptor antagonist

A

true

41
Q

maraviroc can only be given in what type of HIV?

A

HIV1 and CCR5+
and in combo with other drug(s)

42
Q

maraviroc should be given with caution in what patients

A

hepatic compromised and CV issues

43
Q

2 mechanisms of maraviroc resistance

A

-mutation in the v3 loop of the gp120 protein

-virus changing to the CXCR4 tropism. maraviroc only works against ccr5

44
Q

AE of maraviroc

A

cough, upper resp tract infections, hepatotoxicity, allergic rxns

45
Q

explain the mechanism of enfuvirtide

A

fusion inhibitor. it’s a 36 amino acid peptide that blocks the interaction between the gp41 glycoprotein. does this by binding to a hydrophobic groove

this prevents the formation of a 6-HELIX BUNDLE, which is CRITICAL for membrane fusion and viral entry

46
Q

name 3 clinical-like effects of enfuvirtide

A

-inhibits infection of cd4 cells

-inhibits cell to cell transmission of hiv

-retains activity against viruses that have become resistant to other classes!!!!

47
Q

enfuvirtide is mainly given to what patients/

A

treatment experienced in combo with other retroviral

even if other classes are resistant, this drug isn’t!!!

48
Q

how is enfuvirtide administered and what is an advantage and disadvantage

A

SUBQ

advantage - absorbed slowly so dont need to inject a lot (it’s a chronic condition)

disadvantage - more painful. also, if poor circulation, there will be poor absorption

49
Q

resistance mechanism to enfuvirtide

any cross ressitance?

A

mutations in gp41

NO cross resistance with other agents

50
Q

true or false

enfuvirtide is administered orally

A

FALSE

subq

cannot give oral – it’s a 36 amino acid peptide and we have peptidase in our GI

51
Q

name an attachment inhibitor

A

fostemsavir

52
Q

name a post attachment inhibitor

A

ibalizumab

53
Q

true or false

fostemsavir is an attachment inhibitor and is a prodrug

A

TRUE

prodrug of temsavir

54
Q

fostemsavir is a _______ attachment inhibitor

A

gp120-directed

55
Q

explain the MOA of fostemsavir

A

metabolized to temsavir in vitro, which directly binds the gp120 subunit in the HIV-1 envelope which inhibits the interaction between the virus and the CD4 receptors, thus preventing ATTACHMENT to the host cell

56
Q

3 AE fostemsavir

A

hepatotoxicity
QT prolongation
IRIS

57
Q

explain MOA ibalizumab

A

CD4-directed POST-attachment HIV-1 inhibitor

binds CD4 domain 2

prevents binding to CCR5/CXCR4 (coreceptors)

58
Q

how is ibalizumab administered

A

IV once every 2 weeks

for treatment experienced pts with MDR HIV-1

59
Q

AE ibalizumab

A

rash, IRIS

60
Q

what does INSTI stand for

A

integrase strand transfer inhibitors

61
Q

name 3 INSTIS

A

dolutegravir
raltegravir
biictegravir

62
Q

true or false

INSTIS are active against both HIV 1 and HIV 2

A

true

63
Q

AE of INSTIS

A

generally well tolerated - do not affect lipid metabolism

however, rare events of hypersensitivity reactions and rhabdomyolysis

64
Q

MOA of integrase inhibitors (INSTIs)

A

normally, integrase would cut host DNA and integrate viral DNA

however, INSTIS bind to HIV integrase and prevent the DNA strand transfer and the viral DNA cannot be integrated and viral protein cannot be produced to make more HIV virus

65
Q

counseling points dolutegravir

A

no antacids, laxatives, Fe or Ca supplements - chelation and decreased absorption

66
Q

which INSTI is NOT affected by CYP3A4

A

raltegravir

67
Q

all of the INSTIS have what metabolism

A

glucuronide formation by UGT1A1

68
Q

raltegravir should be given with caution with ____

A

antacids - polyvalent cations can bind them

69
Q

raltegravir AE

A

srs hypersensitivity like SJS

same AE as other INSTIS - fat redistribution, etc

70
Q

AE bictegravir

A

IRIS, lactic acidosis/hepatomegaly with steatosis, SJS, nephrotoxicity

71
Q

name a capsid inhibitor

A

lenaCAPavir

72
Q

explain MOA lenacapavir

A

selective inhibitor of HIV-1 capsid function

directly binds between capsid protein (p24) subunits in hexamers

this affects capsid functions such as:
-nuclear uptake of HIV proviral DNA
-virus assembly and release
-capsid core formation

73
Q

what is cobicistat

A

a pharmacokinetic enhancer - potent inhibitor of CYP3A4

74
Q

cobicistat is only used with what class of antiretrovirals for HIV? specifically which 2?

A

protease inhibitors

atazanavir
darunavir

to increase the systemic exposure of them

75
Q

which of the following drugs is an INSTI

tenofovir
lopinavir
raltegravir
zidovudine

A

raltegravir

tenofovir = NRTI
lopinavir = protease inhibitor
zidovudine = NRTI

76
Q

which of the following is an NRTI

zidovudine
darunavir
raltegravir
maraviroc

A

zidovudine

darunavir = protease inhibitor
raltegravir = INSTI
maraviroc = attachment/entry inhibitor

77
Q

fusion inhibitors prevent…

A

the virus from fusing with the host cell membrane

78
Q

NNRTIs block reverse transcriptase by…..

A

DIRECTLY BINDING to reverse transcriptase - causing a structural change

NOT at the enzymatic site - at an allosteric site that induces conformational change

79
Q

which is a protease inhibitor

efavirenz
ritonavir
tenofovir
enfuvirtide

A

ritonavir

efavirenz = NNRTI
tenofovir = NRTI
enfuvirtide = fusion inhibitor

80
Q

which HIV drug is an entry inhibitor that blocks CCR5 co receptor, preventing HIV from entering the hose cell

A

MARAVIROC

81
Q

how do protease inhibitors work in treating HIV infection

A

inhibit the enzyme that cuts viral protein into functional units

82
Q

which is NOT a prodrug

tenofovir
zidovudine
emtricitabine
efavirenz

A

efavirenz - an NNRTI

all the others are NRTIS

83
Q

name a prodrug that needs TWO additional phosphorylation steps

A

tenofovir

84
Q

what is a nucleoside analog

A

a nucleotide without phosphate groups

85
Q

drug has no direct antiviral effect but increases plasma levels of protease inhibitors by inhibiting CYP3A4. also reduces the daily pill burden

what drug is this

A

cobicistat

86
Q
A

D&D Infectious Disease FINAL (21 decks)

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