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SBL Exam 2 > HIV Pharmacology > Flashcards

HIV Pharmacology Flashcards

(75 cards)

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1
Q

Describe the treatment goals of Antiretroviral therapy

A

maximal and durable suppression of of plasma viremia delays, improves or preserves CD4 T cell numbers

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2
Q

What are the predictors of virologic success in HIV patients

A 
low baseline viremia 
high potency of ARV regimen 
Tolerability of Regimen 
Convenience of regimen 
Compliance
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3
Q

What do Nucleoside Reverse Transcriptase Inhibitors inhibit?

A

Reverse transcriptase by direct inhibition.

They are incorporated into DNA being made from HIV RNA and stops the process

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4
Q

What process must NRTIs go through to become activated?

A

phosphorylation

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5
Q

What determines NRTI toxicity and where are NRTIs universally toxic

A

the ability of NRTI to target only HIV reverse transcriptase without inhibiting host cell DNA polymerase

mitochondrial toxicity

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6
Q

Name the Thymidine analogue NRTIs

A

zidovudine (AZT)
stavudine

this is also the first line drug

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7
Q

Name the cytidine analogue NRTIs

A

Emtricitabine

Lamivudine

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8
Q

Name the guanosine analogue NRTI

A

abacavir

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9
Q

Name the adenosine analogue NRTI

A

tenofovir

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10
Q

True or false: ALL NRTI can select for resistance mutations

A

True

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11
Q

What are the toxicities associated with NRTI class

A

Lactic acidosis syndrome
peripheral neuropathy
pancreatitis

All due to mitochondrial toxicity

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12
Q

Which NRTI the only option for IV administration

A

zidovudine (AZT)

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13
Q

What are specific toxicities are possible with zidovudine

A

Bone marrow suppression
Skeletal muscle myopathy
Hepatic steatosis (potentially fatal)

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14
Q

What are the major toxicities associated with stavudine

A

peripheral neuropathy
NRTI most associated with lipodystrophy
Lactic Acidosis and hepatic steatosis

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15
Q

how effective is emtricitabine as a monotherapy to resistance

A

low

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16
Q

What other virus is emtricitabine effective against

A

HBV

DC of this drug can cause rebound effects

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17
Q

What other NRTI drug can emtricitabine be combined with as a superior combination

A

tenofovir

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18
Q

Describe the pharmacokinetics of emtricitabine

A

long intracellular half life (a current NRTI of choice)

excreted primarily as unchanged drug in urine

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19
Q

Describe the toxicity of emicitrabine

A

one of the lease toxic antiretroviral but prolonged use leads to hyperpigmentation of skin especially in palms and soles (most common in AA)

*Allison’s drug of choice

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20
Q

What antiviral drug was lamivudine co-formulated with?

A

tenofovir

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21
Q

Describe the pharmacokinetics of lamviduine

A

long intracellular half-life and excreted primarily as unchanged in urine

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22
Q

Describe the toxicity of lamivudine

A

one of the least toxic

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23
Q

What NRTI is the only guanosine analogue

A

abacavir

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24
Q

Is abacavir effective against HBV

A

nope

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25
What genotype is fatally incompatible with abacavir
HLA-B*5701 - potential hypersensitivity syndrome
26
How is abacavir eliminated from the body
NOT CYP substrate. uses dehydrogenases and is glucuronidated
27
Describe the hypersensitivity syndrome in those who take abacavir
fever abdominal/GI pain maculopapular (looking at you allison) rash *avoid in people with CAD due to hyplerlipidemia
28
How does tenofovir work as an NRTI
it is a nucleotide reverse transcriptase inhibitor It is also approved to treat HBV
29
Describe the pharmacokinetics of tenofovir disoproxil fumarate
intracellular half-life of 10-50 hrs excreted primarily as unchanged in urine
30
Describe the toxicities of tenofovir disoproxil fumarate
nephrotoxicity with acute tubular necrosis -> fanconi syndrome decreased bone mineral density
31
how is Tenofovir alafenamide transported differently than tenofovir disoproxil fumarate
lower doses mean lower plasma concentrations but higher intracellular concentrations *less renal toxicity than TDF
32
Describe how most ART treatments are built
NRTI backbone with two each targeting a different base (ie emtricitabine + tenofovir) with another drug from another class
33
Why would emtricitabine and lamivudine not be prescribed together as an NRTI backbone?
both inhibit the same bases
34
what combination of drugs is recommended for treatment of naive patients unless HIV load is high
lamivudine and dolutegravir
35
Describe the mechanism of action of integrase strand transfer inhibitors
Prevent the insertion of reverse transcribed DNA from viral RNA into host genome
36
What drugs belong to the ISTI class
raltegravir dolutegravir bictegravir
37
How is raltegravir eliminated
9 hour half life eliminated in urine and feces as unchanged drug also undergoes glucuronidation
38
describe dolutegravir and bictegravir's barrier to drug resistance
it has a high barrier to drug resistance
39
Describe the toxicities of dolutegravir
rare skin hypersensitivity possible immune reconstitution syndrome avoid in pregnancy
40
how can the availability of bictegravir be affected
inducers or inhibitors of CYP3A4 but needs very potent agents to alter effects relatively stable
41
Describe the mechanism of action of protease inhibitors
prevent the cleaving of the HIV virion propeptide into a functional viron.
42
How do protease inhibitors inhibit viral aspartyl proteases but not human aspartyl proteases
virus protease is a homodimer while human are monomer
43
What enzyme is most responsible for metabolism of protease inhibitors
CYP3A4 ritonavir is used to boost CYP3A4 activity
44
List all the drugs in the protease inhibitor class
``` saquinavir indinavir darunavir atazanavir Lopinavir ```
45
Describe the toxicity of saquinavir
GI distress | long term -> lipodystrophy
46
Why is indinavir no longer recommended or prescribed
unique crystalluria/renal stones
47
describe the specific mechanism of action of darunavir
a non-peptidic protease inhibitor
48
what is the offlable use of darunavir
post-exposure prophylaxis
49
Describe the pharmacokinetics of darunavir
15 hour half life when boosted CYP3A4 80% excreted in feces 40% unchanged drug Current PI of choice
50
Describe the toxicities of darunavir
GI distress cholesterolemia fat redistribution syndrome immune reconstitution syndrome sulfa drug -> hypersensitivity
51
describe the toxicities of atazanavir
GI problems Elevated unconjugated bilirubin not associated with hepatitis hypersensitivity immune reconstitutions
52
Which drug is prescribed after other PI -containing regimens fail
Lopinavir
53
Which drugs are CYP3A4 inhibtors
ritonavir | cobicistat
54
Describe the mechanism of action Non-nucleoside reverse transcriptase inhibitors
denatures the viral reverse transcriptase to inhibit the process. Binds the p66 subunit which induces conformational change; non-competitive antagonist
55
Which type of HIV is NNRTI effective against
HIV-1
56
how does resistance develop in NNRTI
a single aa substitution is enough. a single exposure to nevirapine in absence of other drugs is enough to induce resistance in 1/3 of HIV infected people
57
What are the drugs in the NNRTI class
``` nevirapine efavirenz etravirine rilpivirine doravirine ```
58
What is a consideration with respect to birth control when taking nevirapine
reduces level of oral contraceptives so alternative method is needed itching rashes most common side effect
59
Describe the toxicity of efavirenz
CNS toxicity/psychiatric side effects was considered teratogenic but not anymore?
60
When should efavirenz not be prescribed
don't add to failing regiment
61
describe a unique function in the etravirine drug
it still works after mutations that disrupt activity of other NNRTI
62
Describe the toxicity of etravine
fat redistribution immune reconstruction syndrome rash is common and resolves spontaneously Stevens-johnson syndrome is possible
63
Which NNRTI is the newest
doravirine still not top choice though
64
Describe the mechanism of action of the Entry Blockers - HIV Fusion Inhibitor
Prevents the binding of the HIV virion binding CD4 t cell area.
65
What class of medication does enfuvirtide belong to
HIV fusion inhibitor
66
What are the main effects of enfuvirtide
inhibits infection of CD4 by free virus particles inhibits cell-to-cell transmission in vitro
67
Which drug would be most appropriate if you needed to include a drug effective against HIV-2 A. enfuvirtide B.Doravirine C. Lopinavir D. Rilpivirine
C. Lopinavir
68
Describe the mechanism of action of the CCR5 blockers
prevent the binding of the gp120 and gp41 to the CD4 and CCR5 binding region
69
Which class of medication does maraviroc belong to
CCR5 blocker
70
What must be done before prescribing maravoc to ensure effectiveness?
phenotypic test to determine if CCR5 or CXCR4 tropism. NOT effective against CXCR4. test is very expensive. it the gucci of tests
71
how is maravoc eliminated
CYP3A4 metabolism with renal excretion
72
Who is ART recommended for?
Everyone!! and immediately
73
True or False: a person who has a viral load of <200 copies/mL can have unprotected sex without transmitting their HIV
technically true but contingent on heavy heavy adherence. Slipping up in compliance will cause bounce back viral load in your load
74
What are the 3 ART considerations
1. Always use combo therapy 2. current emphasis on tolerance and convenience 3. based on realization that therapy must be life long
75
If a treatment fails, what should be considered
1. Adherence 2. drug-drug/drug-food 3. tolerability 4. HIV RNA level adding one new drug to a failed regimen is NOT recommended

SBL Exam 2 (7 decks)

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