HIV drugs Flashcards

1
Q

What are the anti-retroviral subsets?

A
  1. NRTI’s
  2. NNRTI’s
  3. Protease inhibitors
  4. Integrase inhibitors
  5. Fusion inhibitors
  6. CCR5 antagonists
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2
Q

What are the two reverse transcriptase inhibitors?

A

Nucleoside

Non-nucleoside

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3
Q

What are the nucleoside reverse transcriptase inhibitors?

A
  1. Zidovudine
  2. Lamivudine
  3. Abacavir
  4. Emtricitabine
  5. Tenofovir
  6. Didanosine
  7. Stavudine
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4
Q

What is the mnemonic for the NRTI’s?

A

STALEDZ

  • makes the viral DNA go stale
  • BY inhibiting reverse transcriptase.
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5
Q

What is the MOA of NRTI’s?

A

Inhibit reverse transcriptase and can be incorporated into viral DNA chain and cause termination.

Analog or inhibitor so more nucleosides cannot be added.

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6
Q

What is unique about tenofovir?

A

NucleoTide reverse transcriptase inhibitor

- thus does not need to be phosphorylated to be incorporated into DNA

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7
Q

What is the difference between nucleosides and nucleotides?

A
  • Sides have nitrogenous bases with sugar (Ribose or Deoxy)

- Tides contain both of those as well as a phosphate group

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8
Q

What are the NNRTI’s? What is the mnemonic?

A
  1. Nevirapine
  2. Etravirine
  3. Efavirenz
  4. Rilpivirine
  5. Delavirdine

NEERD

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9
Q

What is the MOA of NNRTI’s?

A

Bind directly to the reverse transcriptase at a site distinct from NRTI’s and inhibit it.
- no phosphorylation required

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10
Q

What are the protease inhibitors?

A
  1. Atazanavir
  2. Darunavir
  3. Fosamprenavir
  4. Indinavir
  5. Lopinavir
  6. Ritonavir
  7. Saquinavir
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11
Q

What is common about protease inhibitors name?

A
  • Navirs

Navir tease a protease

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12
Q

What is the MOA of protease inhibitors?

A

Prevent post translational cleavage of Gag-Pol polyprotein.

- these proteases are needed to cleave mRNA into functional products

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13
Q

What are the fusion inhibitors?

A

Enfuviritide

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14
Q

What is the integrase inhibitor?

A

Raltegravir

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15
Q

What is the CCR5 antagonist and what is its subtype?

A

Maraviroc

- Fusion inhibitor

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16
Q

What is the MOA of maraviroc?

A

Binds specifically and selectively to CCR5 which blocks the binding of HIV to host cells

17
Q

What is the MOA of Raltegravir?

A

Inhibits integrase with is essential for HIV replication

18
Q

What is the MOA of of Enfuvirtide?

A

36 amino-acid synthetic peptide that binds to gp41 and prevents the conformational change.
- this is needed for fusion facilitation