HIV Pharm - NRTIs Flashcards

1
Q

General MOA for NRTIs

A

(-) incorporation of native nucleotides and terminate DNA elongation

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2
Q

General MOA for NRTIs

A

(-) incorporation of native nucleotides and terminate DNA elongation

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3
Q

NRTIs must enter the cell and become _______

A

Phosphorylated

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4
Q

NRTIs (-)

A

Reverse transcriptase

– Takes RNA to DNA

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5
Q

NRTIs must (-) Reverse Transcriptase without (-) DNA?

A

Polymerase of the host cell

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6
Q

Some NRTIs (-) _____ DNA polymerase ___

A

Mitochondrial DNA Polymerase Gamma

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7
Q

The widely used NRTIs that (-) Mitochondrial DNA Polymerase Gamma have ____ affinity for gamma

A

LOW affinity

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8
Q

Zidovudine interferes with?

A

Thymidine incorporation

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9
Q

Adverse side effects of Zidovudine?

A

Bone marrow suppression
Myopathy
Hepatic Steatosis

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10
Q

What was the first ART drug discovered?

A

Zidovudine

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11
Q

Stavudine interferes with?

A

Thymidine incorporation

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12
Q

Adverse side effects of Stavudine?

A

Peripheral neuropathy and fat wasting

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13
Q

What NRTIs interfere with Thymidine incorporation?

A

Zidovudine

Stavudine

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14
Q

Zidovudine and Stavudine and ____ used now

A

Less used now

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15
Q

Emtricitabine inteferes with?

A

Cytosine incorporation

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16
Q

Emtricitabine has a ____ barrier to resistance if monotherapy

A

LOW

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17
Q

Emtricitabine half life and metabolism?

A

Long half life and excreted UNCHANGED in urine

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18
Q

Emtricitabine is one of the least toxic agents! What is one possible side effect?

A

Hyperpigmentation of the palms/soles with prolonged use

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19
Q

Iamivudine interferes with?

A

Cytosine incorporation

20
Q

Iamivudine has a ___ barrier to resistance if monotherapy

21
Q

Iamivudine half life and metabolism?

A

Long half life and excreted UNCHANGED in urine

22
Q

Iamivudine is one of the least toxic agents! What is it similar to?

A

Emtricitabine

23
Q

Emtricitabine is similar to?

A

Iamivudine

24
Q

What NRTIs interfere with Cytosine incorporation?

A

Emtricitabine

Iamivudine

25
What agent is often used with Iamivudine to treat naive patients?
Dolutegravir
26
What agent is often used with Iamivudine to treat naive patients?
Dolutegravir
27
What NRTI interferes with Guanine incorporation?
Abacavir
28
Abacavir interferes with?
Guanine incorporation
29
Abacavir should not be used with patients with what locus?
HLA-B*5701
30
In patients with HLA-B*5701 locus, what does Abacavir cause?
Aberrant TNF release | = Potentially fatal hypersensitivity syndrome
31
Adverse effects of Abacavir?
Potentially fatal hypersensitivity syndrome | Avoided in CAD patients
32
Tenofovir Disoproxil Fumarate interferes with?
Adenosine incorporation
33
Adverse effects of Tenofovir Disoproxil Fumarate?
Nephrotoxicity that can cause Fanconi Syndrome | Decreased bone mineral density
34
Tenofovir Alafenamide interferes with?
Adenosine incorporation
35
Adverse effects of Tenofovir Alafenamide?
LESS renal and bone toxicity than Tenofovir Disoproxil Fumarate -- Can cause slight weight gain
36
What NRTIs interfere with Adenosine incorporation?
Tenofovir Disoproxil Fumarate | Tenofovir Alafenamide
37
What NRTI that interferes with Adenosine incorporation causes slight weight gain but less renal and bone toxicity?
Tenofovir Alafenamide
38
What NRTI that interferes with Adenosine incorporation causes nephrotoxicity and decreased bone mineral density?
Tenofovir Disproxil Fumarate
39
What NRTI that interferes with Guanine incorporation causes aberrant TNF release in some patients?
Abacavir
40
What NRTI that interferes with Cytosine incorporation can cause sole/palm hyperpigmentation with prolonged use?
Emtricitabine
41
ART involves 2 NRTIs that each target?
A different base
42
ART involves 2 NRTIs that each target?
A different base
43
What is the best combo of NRTIs?
Emtricitabine + Tenofovir
44
What is the best combo of NRTIs?
Emtricitabine + Tenofovir
45
What is the best combo of NRTIs?
Emtricitabine + Tenofovir