NRTIs Flashcards

1
Q

What is the mechanism of action of the Nucleoside Reverse Transcriptase inhibitors (NRTIs)

A
  • They mimic DNA bases,
  • Acting as false substrates for reverse transcriptase
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2
Q

Which 2 NRTIs act as Thymidine?

A

Zidovudine (AZT) + Stavudine (d4T)

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3
Q

Which NRTI act as Guanosine?

A

Abacavir (ABC)

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4
Q

Which 2 NRTIs act as Cytidine?

A
  • Lamivudine (3TC) + emtricitabine (FTC)
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5
Q

Which 2 NRTIs act as Adenosines?

A
  • Tenofovir (TDF) + Dedanosine (ddI)
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6
Q

Which NRTI well penetrates CSF?

A

Zidovudine (AZT)

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7
Q

How do the NRTIs result to lactic acidosis in host cells?

A

They all inhibit mitochondrial DNA gamma, which is an enzyme that replicates the mitochondria of a host cell.

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8
Q

How does lactic acidosis manifest itself in the human body? How do you know u are having lactic acidosis?

A
  • Nausea
  • Vomiting
  • Abdominal pain
  • Extreme tiredness
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9
Q

What are the side effects from using Zidovudine (AZT)?

A
  • Anemia
    -Myelosuppression
  • Neutropenia
    -leucopenia
  • peripheral neuropathy (damage to peripheral nerves)
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10
Q

Wha are side effects of using stavudine (d4T)?

A
  • Neutropenia
  • Lipoatrophy
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11
Q

What are the side effects from using abacavir (ABC)?

A
  • Hypersensitivity reactions
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12
Q

What are the side effects from using Tenofovir (TDF)

A
  • Nephrotoxicity
  • Bone loss
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13
Q

What are side effects from using lamivudine (3TC) and Emtricitabine (FTC)?

A

Peripheral neurophathy

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14
Q

What’s the metabolism pathway of the NRTIs?

A

Zidovudine (AZT) and Abacavir (ABC) undergo glucuronidation in the liver.

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15
Q

Which drugs does Zidovudine interact with?

A
  • Ganciclovir
  • Valproate
  • Probenecid
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16
Q

What is the possible outcome from Zidovudine interaction with ganciclovir?

A
  • increased
    hematological toxicity
17
Q

What is the possible outcome from Zidovudine interaction with valproate?

A

increase
AZT levels

18
Q

What is the possible outcome from Zidovudine interaction with probenecid?

A

delayed
AZT excretion

19
Q

When to not use Zidovudine? (The drug’s CI)

A
  • Anemiac or patients with neutropenia
20
Q

What drugs does tenofovir interact with? And what are the outcomes?

A
  • ddI- increases levels of
    didanosine
  • ATV- decrease levels of
    atazanavir
  • Kaletra®- Increase TDF
    levels
21
Q

When is Tenofovir contraindicated?

A

On patients with nephrotoxicity

22
Q

What are the adverse effects from Tenofovir use?

A
  • Nephrotoxic,
  • Hepatomegaly-enlargement of the liver beyond its normal size,
  • HBV exacerbationswhen you stop using the drug