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Sheehy Flashcards

1
Q

What kind of virus is HIV?

A

Retrovirus

SsRNA is reverse transcribed into DNA and inserted into the host cell genome

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2
Q

MOA of Maraviroc

A

Binds specifically and selectively to CCR5 to prevent viral entry into the host cell (entry inhibitor)

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3
Q

AE of Maraviroc

A

Generally well tolerated

Systemic allergic reaction followed by hepatoxicity

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4
Q

MOA of Enfuvirtide

A

Binds to gp41 preventing the conformational and structural changes needed to allow fusion of the viral envelope with the host cell membrane

(Fusion inhibitor)

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5
Q

How must enfuvirtide be administered?

A

SubQ

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6
Q

What drug class is included in treatment for all patients beginning antiretroviral therapy?

A

NRTIs (nucleoside/nucleotide reverse transcriptase inhibitors)

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7
Q

MOA of NRTIs

A

Competitive inhibition of HIV reverse transcriptase

Leads to premature chain termination due to inhibition of binding with the incoming nucleotide

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8
Q

What is the one nucleotide RTI?

A

Tenofovir

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9
Q

What are the 6 nucleoside reverse transcriptase inhibitors?

A

Abacavir, didanosine, lamivudine, emtricatibine, stavudine, zidovudine

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10
Q

What drug is also metabolized by alcohol dehydrogenase?

A

Abacavir

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11
Q

What analog is abacavir

A

Guanosine

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12
Q

AEs of abacavir

A

Skin rash in 50% (do not reintroduce abacavir if hypersensitivity is observed)

Constitutional sx, abdominal, and respiratory (dyspnea, pharyngitis, cough)

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13
Q

What analog is didanosine?

A

Deoxyadenosine

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14
Q

AEs of didanosine

A

Dose dependent pancreatitis

Retinal changes with optic neuritis

Increased risk of lactic acidosis and hepatic steatosis when combine with stavudine

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15
Q

What analog is lamivudine

A

Cytosine

[active against HIV and HBV]

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16
Q

Which two drugs select for the same point mutation in HIV reverse transcriptase?

A

Lamivudine and emtricitabine

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17
Q

What analog is emtricitabine

A

Fluorinated analog of lamivudine (which is a cytosine analog) with a long intracellular half-life allowing for once daily dosing

Also active against HIV and HBV

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18
Q

AEs of emtricitabine

A

Hyperpigmentation of the palms or soles (especially in AA’s)

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19
Q

What analog is stavudine

A

Thymidine

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20
Q

AEs of stavudine

A

Dose dependent peripheral sensory neuropathy

Dyslipidemia (more common with stavudine than other NRTIs)

Increased risk of lactic acidosis and hepatic steatosis when combined with didanosine

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21
Q

What analog is zidovudine

A

Deoxythymidine

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22
Q

AEs of zidovudine

A

Macrocytic anemia, neutropenia, GI intolerance, HA, insomnia

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23
Q

What was the first antiretroviral drug to be approved

A

Zidovudine

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24
Q

What analog is tenofovir

A

Acyclic nucleotide analog of adenosine

Active against both HIV and HBV

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25
What 2 drugs enhance oral absorption of tenofovir
Disoproxil and alafenamide
26
AEs of tenofovir
Generally well tolerated Flatulence
27
MOA of NN (non-nucleoside)RTIs
Binds directly to HIV reverse transcriptase in site distant from active site Binding causes conformational change in enzyme and leads to reduced activity (Noncompetitive inhibitors)
28
Why is monotherapy with NNRTIs not preferred?
Resistance can rapidly develop
29
How are NNRTIs metabolized
By CYP450, so lots of drug interactions
30
What are the 3 first generation NNRTIs
Delavirdine Efavirenz Nevirapine
31
What are the 2 second generation NNRTIs
Etravirine Rilpivirine
32
AEs of delaviridine
Skin rash Increased aminotransferase levels
33
How is delavirdine metabolized
Extensively by CYP3A & CYP2D6
34
What are the benefits of efavirenz
Can be given once daily due to increased half life Typically given in a combo pill of tenofovir and emtricitabine for a once daily pill
35
What is efavirenz metabolized by
CYP3A4 & CYP2B6
36
AEs of efavirenz
CNS: dizziness, drowsiness, insomnia, NIGHTMARES, HA Also skin rash
37
What drug is used to prevent transmission of HIV from mother to child
Nevirapine
38
What is nevirapine metabolized by
CYP3A
39
AEs of nevirapine
Rash which can be dose limiting Liver toxicity
40
What drug was designed to overcome HIV resistance to first generation NNRTIs
Etravirine
41
Etravirine is an inducer and inhibitor of which enzymes
Inducer: CYP3A4 Inhibitor: CYP2C9 & CYP2C19
42
AEs of rilpivirine
Rash, DEPRESSION, headache, insomnia, increased serum aminotransferases High doses associated with QT prolongation **
43
MOA of INSTIs
Integrase strand transfer inhibitors Binds HIV integrase and inhibits the strand transfer and prevents ligation of reverse-transcribed HIV DNA into the chromosomes of the host cell
44
What are the most common AEs in INSTIs
HA and GI effects
45
What are the 3 INSTIs
Dolutegravir Elvitegravir Raltegravir
46
What are preferred drug combos for treatment naive patients
Tenofovir/emtricitabine/dolutegravir Abacavir/lamivudine/dolutegravir
47
What is the only available form of elvitegravir
A combo pill of elvitegravir, cobicistat, emtricitabine, tenofovir
48
What is the half life for raltegravir
9 hours
49
What is the MOA of protease inhibitors
Block HIV protease and prevent maturation of the final structural proteins that make up the mature virion core
50
AEs of protease inhibitors
GI intolerance Lipodystrophy (hyperglycemia, hyperlipidemia, lipoatrophy, fat deposition) Redistribution and accumulation of body fat
51
What are protease inhibitors metabolized by
CYP3A4
52
Which drug has the most pronounced inhibitory effect on CYP3A4? The least?
Most: Ritonavir Least: Saquinavir
53
Which drug inhibits CYP3A4, CYP2C9, UGT1A1?
Atazanavir
54
What drug has to be co-administered with ritonavir or cobicistat
Darunavir
55
Which drugs can lead to a potential hypersensitivity reaction in someone who has a sulfa allergy?
Darunavir, fosamprenavir, tipranavir
56
AEs of indinavir
Unconjugated hyperbilirubinemia and nephrolithiasis
57
Which protease inhibitor is a very potent CYP450 inhibitor
Ritonavir
58
Which protease inhibitor is indicated in patients resistant to other protease inhibitors
Tipranavir Which is normally combined with ritonavir
59
AEs of tipranavir
Abd sx Urticarial or maculopapular rash
60
What combo of drugs make up a highly active antiretroviral therapy (HAART)
2 NRTIS + 1 protease inhibitor OR 1 NNRTI OR 1 INSTI

HIV Pharm (1 decks)

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