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Pharmacology > Exam 3: HIV > Flashcards

Exam 3: HIV Flashcards

1
Q

What are the 4 mechanisms for HIV drugs?

A

1) Reverse transcriptase inhibitors
2) protease inhibitors
3) Fusion inhibitor
4) Integrase inhibitor

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2
Q

What are the 5 drugs that are nucleoside analogue reverse transcriptase inhibitors (NRTI)?

A
  • Zidovudine
  • Emtricitabine
  • Tenofovir
  • Lamivudine
  • Abacavir
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3
Q

What is the first choice combination of NRTI?

A

Emtricitabine and tenofovir

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4
Q

What is the 2nd choice combination for NTRI?

A

Lamivudine and abacavir

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5
Q

What is the MOA of NRTIs?

A

Nucleoside analogue that requires 3 phosphorylations, is incorporated into DNA and inhibits viral reverse transcriptase

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6
Q

Which HIV drug is useful in AIDs dementia? Why?

A

Zidovudine because it has good CNS penetration

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7
Q

What is Zidovudine normally combined with? Why?

A

Lamivudine because zidovudine Monotherapy develops resistance quickly.

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8
Q

What is the use of Zidovudine?

A
  • Maintain CD4 count and lessen opportunistic infections

- Safe in pregnancy

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9
Q

What are the toxicities associated with zidovudine?

A
  • Headache, nausea, vomiting, insomnia
  • Lactic acidosis or hepatotoxicity
  • Myelosuppression: neutropenia and anemia (caution with other drugs that may cause this)
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10
Q

How can you combat the neutropenia and anemia caused by Zidovudine?

A
  • Epogen can increased RBCs

- Neupogen can increase WBCs

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11
Q

What it is the MOA for Tenofovir and Emtricitabine?

A

Nucleoside analogue that inhibits reverse transcriptase

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12
Q

What is the first line treatment of HIV?

A

Tenofovir and Emtricitabine

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13
Q

What is the MOA for Lamivudine?

A

Cytosine analogue that inhibits HIV reverse transcriptase and HBV polymerase

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14
Q

What is the MOA of Abacavir?

A

Guanosine analogue that is used in combination with lamivudine OR Zidovudine

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15
Q

What are the toxicities associated with Abacavir?

A
  • Serious hypersensitivity
  • HLA-B27 patients may develop SJS
  • If hypersensitivity reaction occurs, DO NOT GIVE DRUG AGAIN
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16
Q

What are the serious side effects that can occur with any of the NRTIs?

A

Lactic acidosis and Hepatotoxicity

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17
Q

What are the two non-nucleotide reverse transcriptase inhibitors (NNRTIs)?

A

Efavirenz and Rilpivirine

18
Q

What is the MOA of the NNRTIs?

A
  • Bind directly to inhibit viral reverse transcriptase and prevent conversion of RNA to DNA
  • Does not require phosphorylation
19
Q

Which of the NNRTIs is the DOC that is used in initial therapy of HIV?

A

Efavirenz

20
Q

What are the side effects of Efavirenz?

A
  • Drug interactions- CYP34A inducer

- Teratogenic

21
Q

What is the use of Rilpivirine?

A

Used instead of efavirenz in pregnant patients

22
Q

If a drug ends in “avir” what class does it belong in? What is the exception to this?

A

-Protease inhibitors, except Abacavir is the NRTI

23
Q

What is the MOA of protease inhibitors?

A

-Bind to protease and inhibit their function of digesting long viral polypeptides into smaller, mature functional proteins.
Viral particles are unable to mature and become infectious

24
Q

How are protease inhibitors metabolized?

A

CYP34A

25
Q

Why are protease inhibitors given with ritovanir?

A

Ritovanir is a potent inhibitor of CYP34A, which is important because protease inhibitors are given with NNRTIs, which are CYP34A inducers. Without the inhibitor, the protease inhibitors would be metabolized too quickly

26
Q

What are the common toxicities associated with protease inhibitors?

A
  • Altered body fat distribution
  • insulin resistance
  • increases serum cholesterol
  • spontaneous bleeding in patients with hemophilia A or B
27
Q

What should ritonavir never be combined with?

A

Saquinavir because they both cause QT prolongation

-drugs with disulfiram reactions (metronidazole and cephalosporins) because the formulation of Ritonavir contains ethanol

28
Q

Why is ritonavir often combined with other protease inhibitors?

A

Because it inhibits CYP3A4 and protease inhibits are metabolized by CYP3A4 -Keeps drug from metabolizing too quickly.

29
Q

What is the DOC of the protease inhibitors?

A

Darunavir

30
Q

Who should Darunavir never be used for?

A

People with sulfa allergy

31
Q

What are the common side effects seen with atazenavir?

A
  • Less effect on body fat distribution than other protease inhibitors
  • Increase in bilirubin
  • Diarrhea, rash, nausea
32
Q

What is Lopinavir always combined with?

A

Ritonavir to increase bioavailability

33
Q

What are the common side effects seen with Indinavir?

A

Nephrolithiasis and hyperbilirubinemia (aggressive hydration recommended)

34
Q

When is tipranavir used?

A

In combination with Ritonavir, Indicated for use in treatment-experienced HIV infected patients who harbor strains resistant to other protease inhibitors

35
Q

When should tipranavir not be used?

A
  • Patients with head trauma because it increases risk for intracranial hemorrhage
  • Patients with sulfa allergy
36
Q

What are the two fusion inhibitor HIV drugs?

A

Enfuvirtide and maraviroc

37
Q

What is the MOA of Enfuvirtude (fuzeon)?

A

Binds to the gp41 subunit of the viral envelope glycoproteins, prevents conformation change required for membrane fusion and viral entry

38
Q

What is the only parenteral antiretroviral agent?

A

Enfuvirtide (Fuzeon)

39
Q

What is the MOA of Maraviroc?

A

-Inhibits fusion of virus by binding to the CCR5 receptor of the CD4 T-Cell.

40
Q

When is Maraviroc used?

A

-ONLY in patients with a CCR5-tropic HIV infection in which other treatment has not been effective

41
Q

What kind of drug is Dolutegravir?

A

Integrase inhibitor

-DOC in combination with NRTIs

42
Q

When in Dolutegravir used?

A

Treatment-resistant patients where other drugs are no longer working

Pharmacology (25 decks)

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