Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Pharmacology > EXAM #4: ANTIRETROVIRALS > Flashcards

EXAM #4: ANTIRETROVIRALS Flashcards

1
Q

What does NRTI stand for?

A

Nucelotide Reverse Transcriptase Inhibitor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

List the NRTIs.

A 
Zidovudine 
Lamivudine 
Abacavir 
Tenofovir disoproxil
Emtricitabine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is the MOA of the NRTIs?

A

Analogs of nucleotides that inhibit nucleotide binding to REVERSE TRANSCRIPTASE and cause DNA chain termination

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is required for conversion of the NRTIs into their active form?

A

Cellular kinases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What infection aside from HIV can be treated with NRTIs?

A

HBV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What are the adverse effects common to the NRTIs?

A

1) Lactic acidosis
2) Fatty liver disease
3) Lipodystrophy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is Abacavir?

A

Guanosine analog NRTI

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What specific adverse effects are associated with Abacavir?

A

Allergic reaction

Think “A” for allergic reaction*

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is the allergic reaction in with Abacavir associated with?

A

HLA-B5707–must do genetic testing first!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What type of drug is Lamivudine?

A

Cytosine analog NRTI

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is unique about the toxicity associated with Lamivudine?

A

LEAST toxic of the antiretrovirals

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is the unique clinical utility associated with Lamivudine?

A

Safe in pregnancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What type of drug is Emtricitabine?

A

Fluorinated analog of Lamivudine–NRTI

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What specific adverse effect is associated with Emtricitabine?

A

Hyperpigmentation of the palms and soles

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

When is Emtricitabine contraindicated?

A

1) Young children
2) Pregnant women
3) Hepatic or renal failure

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What type of drug is Tenofovir?

A

Nucleotide analog of adenosine–NRTI

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

How is Tenofovir administered?

A

Orally; however, not that is is normally given as “Tenofovir disoproxil” that has more oral bioavalibility

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What adverse effects are associated with Tenofovir?

A

1) Bone marrow toxicity (Faconi anemia)

2) Decreased bone density and fetal growth

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What type of drug is Zidovudine or AZT?

A

Deoxythymidine analog NRTI

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What unique adverse effects are associated with Zidovudine?

A

Myelosuppression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What is the unique clinical indication for Zidovudine?

A

Post-exposure prophylaxis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What does NNRTI stand for?

A

Non-nucleoside Reverse Transcriptase Inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What is the MOA of the NNRTIs?

A

Binds to Reverse Transcriptase at a site OTHER THAN THE ACTIVE SITE and inhibits the enzyme

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

How do the NNRTIs compare to NRTIs?

A

NNRTIs do NOT require phosphorylation for activation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
What strain of HIV are the NNRTIs NOT active against?
HIV-2
26
What adverse reactions are common to the NNRTIs?
1) Rash 2) Steven Johnson Syndrome 3) Hepatotoxicity 4) Major drug-drug interactions b/c of CYP450
27
List the NNRTIs.
asdf
28
What specific adverse effects are associated with Efavirnez?
1) Teratogenic 2) Adverse CNS effects 3) CYP 450 inducer
29
When is Efavirnez contraindicated?
Pregnancy
30
What specific toxicity is associated with Nevirapine?
Hepatitis
31
What is unique about the clinical indications for Nevirapine?
Can be used to prevent VERTICAL transmission
32
What is the MOA of the protease inhibitors in HIV therapy?
Block the protease necessary for maturation of virion proteins
33
What adverse effects are associated with the Protease Inhibitors?
1) Hyperlipidemia 2) Iipodystrophy 3) Hepatotoxicity 4) GI intolerance 5) Increased bleeding risk 6) Drug-drug interactions via CYP p450
34
List the Protease Inhibitors.
asdf
35
What type of drug is contraindicated with Atazanavir?
PPIs--requires acid for absorption
36
What major adverse effects are associated with Atazanavir?
1) Peripheral neuropathy 2) Hyperbilirubinemia 3) Adverse cardiac effects
37
What effect does Atazanavir have on the CYP p450 enzymes?
Inhibition
38
What is the effect of Ritonavir on liver metabolism?
Potent INHIBITOR or CYP p450 enzymes
39
How is Ritonavir used clinically?
"Booster" to increase the half-life of co-administered drugs
40
How is Darunavir administered?
Orally + pharmacokinetic enhancer e.g. Ritonavir
41
What are the specific adverse effects seen with Darunavir?
1) Increased liver enzymes | 2) Increased serum amylase
42
What is Darunavir specifically good for treating?
Drug resistant HIV-1
43
What is the MOA of the CCR5 Receptor Antagonists?
Blocks interaction of HIV (gp120) with the CCR5 co-receptor
44
What drug is a CCR5 receptor antagonist?
Maraviroc
45
What is the major toxicity associated with Maraviroc?
Increased cardiac events in those with underlying heart disease
46
What is the mechanism of resistance to Maraviroc?
Change in HIV tropism i.e. switch from CCR5 to CXCR4 tropism
47
What are the indications for Maraviroc?
HIV "experienced" patients with a tropsim for CCR5
48
What is the mechanism of the Fusion Inhibitors?
Blockade of the gp41 fusion protein
49
What is the Fusion inhibitor?
Enfurvirtide
50
What is the only anti-viral that is given parenterally?
Enfurvirtide *Given SubQ
51
What are the adverse effects associated with Enfurvirtide?
1) Injection site reaction 2) Allergy to drug 3) Increased risk for bacterial pneumonia
52
What is the clinical utility of Enfurvirtide?
HIV experienced patients with resistance
53
What is the MOA of the Integrase Inhibitors?
Inhibit viral integration into the host genome
54
List the Integrase Inhibitors.
Raltegravir Elvitegravir Dolutegravir
55
What major toxicities are associated with Raltegravir?
1) Mypoathy | 2) Rhabdomyolysis
56
How is Elvitegravir administered?
Orally with a CYP p450 inhibitor e.g. ritonavir
57
What specific adverse effect is associated with Elvitegravir ?
Elevated lipase enzymes
58
What are the adverse effects associated with Dolutegravir?
1) Hypersensitivity reaction | 2) Elevation of liver enzymes
59
What is unique about Dolutegravir in terms of resistance?
Retains activity against strains that are resistant to other integrase inhibitors
60
How much does a patient need to weigh to be given Dolutegravir?
At least 40 kg
61
When do you initiate ARV therapy?
ALL HIV infected individuals
62
At what point is there the strongest recommendation for ART initiation?
CD4+ T-cell count less than 350
63
What is the standard of care for ART?
Combination of at LEAST 3 antiretroviral drugs/classes
64
What is the preferred combination of ART for initial therapy?
1) Protease inhibitor (Ritonavir) 2) 2x NRTIs OR 1) Integrase Inhibitor 2) 2x NRTIs

Pharmacology (64 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions