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

Pharm - HIV pharmacotherapy part 2 Flashcards

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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
true or false atazanavir is recommended in pregnancy
TRUE only one that isnt is the oral solution of fosamprenavir + ritonavir
26
how is the AE of atazanavir unlike other protease inhibitors?
NO dyslipidemia!! also hyperbilirubinemia is a concern (jaundice)
27
darunavir is a protease inhibitor that must be coadministered with ______
ritonavir
28
AE concern with darunavir
has sulfa group!!!! watch out for hypersensitivity
29
true or false darunavir has less frequent dyslipidemia than other protease inhibitors
true
30
fosamprenavir is a prodrug of _______
amprenavir
31
what is fosamprenavir administered with
low dose ritonavir
32
which 2 protease inhibitors have a hypersensitivity concern due to their sulfa group
darunavir fosamprenavir
33
WHY is fosamprenavir + low dose ritonavir not given in young children and in pregnancy?
the oral solution has propylene glycol
34
true or false ritonavir is recommended in pregnancy
TRUE alone, it's fine
35
which 2 drug levels should be monitored with ritonavir and why
theophylline and digoxin - have narrow TIs and their levels may increase
36
ritonavir is not given with -___ due to _____
saquinavir QT prolongation
37
name an entry inhibitor
maraviroc
38
name a fusion inhibitor
enfuvirtide enFU (fusion) "tide" - peptide
39
explain the MOA of maraviroc
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
true or false maraviroc is an ALLOSTERIC CCR5 receptor antagonist
true
41
maraviroc can only be given in what type of HIV?
HIV1 and CCR5+ and in combo with other drug(s)
42
maraviroc should be given with caution in what patients
hepatic compromised and CV issues
43
2 mechanisms of maraviroc resistance
-mutation in the v3 loop of the gp120 protein -virus changing to the CXCR4 tropism. maraviroc only works against ccr5
44
AE of maraviroc
cough, upper resp tract infections, hepatotoxicity, allergic rxns
45
explain the mechanism of enfuvirtide
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
name 3 clinical-like effects of enfuvirtide
-inhibits infection of cd4 cells -inhibits cell to cell transmission of hiv -retains activity against viruses that have become resistant to other classes!!!!
47
enfuvirtide is mainly given to what patients/
treatment experienced in combo with other retroviral even if other classes are resistant, this drug isn't!!!
48
how is enfuvirtide administered and what is an advantage and disadvantage
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
resistance mechanism to enfuvirtide any cross ressitance?
mutations in gp41 NO cross resistance with other agents
50
true or false enfuvirtide is administered orally
FALSE subq cannot give oral -- it's a 36 amino acid peptide and we have peptidase in our GI
51
name an attachment inhibitor
fostemsavir
52
name a post attachment inhibitor
ibalizumab
53
true or false fostemsavir is an attachment inhibitor and is a prodrug
TRUE prodrug of temsavir
54
fostemsavir is a _______ attachment inhibitor
gp120-directed
55
explain the MOA of fostemsavir
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
3 AE fostemsavir
hepatotoxicity QT prolongation IRIS
57
explain MOA ibalizumab
CD4-directed POST-attachment HIV-1 inhibitor binds CD4 domain 2 prevents binding to CCR5/CXCR4 (coreceptors)
58
how is ibalizumab administered
IV once every 2 weeks for treatment experienced pts with MDR HIV-1
59
AE ibalizumab
rash, IRIS
60
what does INSTI stand for
integrase strand transfer inhibitors
61
name 3 INSTIS
dolutegravir raltegravir biictegravir
62
true or false INSTIS are active against both HIV 1 and HIV 2
true
63
AE of INSTIS
generally well tolerated - do not affect lipid metabolism however, rare events of hypersensitivity reactions and rhabdomyolysis
64
MOA of integrase inhibitors (INSTIs)
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
counseling points dolutegravir
no antacids, laxatives, Fe or Ca supplements - chelation and decreased absorption
66
which INSTI is NOT affected by CYP3A4
raltegravir
67
all of the INSTIS have what metabolism
glucuronide formation by UGT1A1
68
raltegravir should be given with caution with ____
antacids - polyvalent cations can bind them
69
raltegravir AE
srs hypersensitivity like SJS same AE as other INSTIS - fat redistribution, etc
70
AE bictegravir
IRIS, lactic acidosis/hepatomegaly with steatosis, SJS, nephrotoxicity
71
name a capsid inhibitor
lenaCAPavir
72
explain MOA lenacapavir
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
what is cobicistat
a pharmacokinetic enhancer - potent inhibitor of CYP3A4
74
cobicistat is only used with what class of antiretrovirals for HIV? specifically which 2?
protease inhibitors atazanavir darunavir to increase the systemic exposure of them
75
which of the following drugs is an INSTI tenofovir lopinavir raltegravir zidovudine
raltegravir tenofovir = NRTI lopinavir = protease inhibitor zidovudine = NRTI
76
which of the following is an NRTI zidovudine darunavir raltegravir maraviroc
zidovudine darunavir = protease inhibitor raltegravir = INSTI maraviroc = attachment/entry inhibitor
77
fusion inhibitors prevent...
the virus from fusing with the host cell membrane
78
NNRTIs block reverse transcriptase by.....
DIRECTLY BINDING to reverse transcriptase - causing a structural change NOT at the enzymatic site - at an allosteric site that induces conformational change
79
which is a protease inhibitor efavirenz ritonavir tenofovir enfuvirtide
ritonavir efavirenz = NNRTI tenofovir = NRTI enfuvirtide = fusion inhibitor
80
which HIV drug is an entry inhibitor that blocks CCR5 co receptor, preventing HIV from entering the hose cell
MARAVIROC
81
how do protease inhibitors work in treating HIV infection
inhibit the enzyme that cuts viral protein into functional units
82
which is NOT a prodrug tenofovir zidovudine emtricitabine efavirenz
efavirenz - an NNRTI all the others are NRTIS
83
name a prodrug that needs TWO additional phosphorylation steps
tenofovir
84
what is a nucleoside analog
a nucleotide without phosphate groups
85
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
cobicistat
86

D&D Infectious Disease FINAL (21 decks)

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