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

A

LOW

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
Q

What agent is often used with Iamivudine to treat naive patients?

A

Dolutegravir

26
Q

What agent is often used with Iamivudine to treat naive patients?

A

Dolutegravir

27
Q

What NRTI interferes with Guanine incorporation?

A

Abacavir

28
Q

Abacavir interferes with?

A

Guanine incorporation

29
Q

Abacavir should not be used with patients with what locus?

A

HLA-B*5701

30
Q

In patients with HLA-B*5701 locus, what does Abacavir cause?

A

Aberrant TNF release

= Potentially fatal hypersensitivity syndrome

31
Q

Adverse effects of Abacavir?

A

Potentially fatal hypersensitivity syndrome

Avoided in CAD patients

32
Q

Tenofovir Disoproxil Fumarate interferes with?

A

Adenosine incorporation

33
Q

Adverse effects of Tenofovir Disoproxil Fumarate?

A

Nephrotoxicity that can cause Fanconi Syndrome

Decreased bone mineral density

34
Q

Tenofovir Alafenamide interferes with?

A

Adenosine incorporation

35
Q

Adverse effects of Tenofovir Alafenamide?

A

LESS renal and bone toxicity than Tenofovir Disoproxil Fumarate
– Can cause slight weight gain

36
Q

What NRTIs interfere with Adenosine incorporation?

A

Tenofovir Disoproxil Fumarate

Tenofovir Alafenamide

37
Q

What NRTI that interferes with Adenosine incorporation causes slight weight gain but less renal and bone toxicity?

A

Tenofovir Alafenamide

38
Q

What NRTI that interferes with Adenosine incorporation causes nephrotoxicity and decreased bone mineral density?

A

Tenofovir Disproxil Fumarate

39
Q

What NRTI that interferes with Guanine incorporation causes aberrant TNF release in some patients?

A

Abacavir

40
Q

What NRTI that interferes with Cytosine incorporation can cause sole/palm hyperpigmentation with prolonged use?

A

Emtricitabine

41
Q

ART involves 2 NRTIs that each target?

A

A different base

42
Q

ART involves 2 NRTIs that each target?

A

A different base

43
Q

What is the best combo of NRTIs?

A

Emtricitabine + Tenofovir

44
Q

What is the best combo of NRTIs?

A

Emtricitabine + Tenofovir

45
Q

What is the best combo of NRTIs?

A

Emtricitabine + Tenofovir