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Anti-microbes > Anti-HIV > Flashcards

Anti-HIV Flashcards

1
Q

What are the 5 NRTIs?

A

Abacavir, Emtricitabine, Lamivudine, Tenofovir & Zidovudine

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2
Q

What is the mechanism of action of NRTIs?

A

NRTIs are analogs of native ribosides, lacking a 3’-OH group.

Upon cell entry, they are phosphorylated and preferentially incorporated into the viral DNA by RT.

Since the 3’-OH group is not present, a 3’,5’-phosphodiester bond between an incoming nucleoside triphosphate and the growing DNA chain cannot be formed

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3
Q

What are the 4 classes of HIV drugs?

A
  1. Nucleoside Reverse Transcriptase Inhibitor (NRTI)
  2. Integrase inhibitor
  3. Protease inhibitor
  4. Non-NRTI (NNRTI)
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4
Q

What is the standard ARV regimen?

A

2 NRTIs + 1 integrase/protease inhibitor

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5
Q

What are the 2 cytosine analogs?

A

Emtricitabine & Lamivudine

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6
Q

Which ARV drugs have activity against Hep B?

A

Emtricitabine, Tenofovir & Lamivudine

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7
Q

What is the route of administration of all the ARV drugs?

A

PO

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8
Q

Which ARV drug is nephrotoxic?

A

Tenofovir

The tenofovir alafenamide formulation has less renal effects and is more favourable for those with renal impairment

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9
Q

What is the adenosine analog?

A

Tenofovir

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10
Q

What is the guanine analog?

A

Abacavir

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11
Q

What is the thymidine analog?

A

Zidovudine

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12
Q

What is the ARV drug that requires prior genotyping and which genotype is contraindicated?

A

Abacavir

Only used in HLA-B5701 negative individuals

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13
Q

What is the severe complication that may occue when HLA-B5701 positive individuals take abacavir?

A

Fatal hypersensitivity syndrome

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14
Q

What is the mechanism of action of the integrase inhibitors?

A

They bind to and inhibit the catalytic site of the HIV integrase, which terminates integration of HIV DNA into the host genome

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15
Q

What is the route of administration of the integrase inhibitors?

A

PO

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16
Q

What is the mechanism of action of protease inhibitors?

A

Protease inhibitors bind to the active site of HIV protease, preventing the enzyme from releasing the individual core proteins

17
Q

What are the potential DDIs when using protease inhibitors?

A

CYP450 substrates; hence are CYP450 inhibitors

18
Q

What is the purpose of Ritonavir & Cobicistat in combination with other protease inhibitors?

A

Pharmacokinetic enhancers as they have CYP450-inhibitory activity

19
Q

What is the mechanism of action of NNRTIs?

A

They bind to HIV RT at an allosteric site, infucing a conformational change that results in enzyme inhibition

20
Q

What is the issue with NNRTI treatment?

A

NNRTIs have low genetic barrier to resistance

21
Q

What is the recommended pre-exposure prophylaxis for HIV?

A

Emtricitabine + tenofovir daily for 1 month

22
Q

What is the recommended post-exposure prophylaxis for HIV?

A

2 NRTIs + integrase inhibitor within 72hrs, for 1 month

Anti-microbes (9 decks)

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