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Pharmacology > Exam 3: HIV > Flashcards

Exam 3: HIV Flashcards

(42 cards)

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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)?

Study These Flashcards
A

Efavirenz and Rilpivirine

18
Q

What is the MOA of the NNRTIs?

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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?

20
Q

What are the side effects of Efavirenz?

Study These Flashcards
A
  • Drug interactions- CYP34A inducer

- Teratogenic

21
Q

What is the use of Rilpivirine?

Study These Flashcards
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?

Study These Flashcards
A

-Protease inhibitors, except Abacavir is the NRTI

23
Q

What is the MOA of protease inhibitors?

Study These Flashcards
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?

25
Why are protease inhibitors given with ritovanir?
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
What are the common toxicities associated with protease inhibitors?
- Altered body fat distribution - insulin resistance - increases serum cholesterol - spontaneous bleeding in patients with hemophilia A or B
27
What should ritonavir never be combined with?
Saquinavir because they both cause QT prolongation -drugs with disulfiram reactions (metronidazole and cephalosporins) because the formulation of Ritonavir contains ethanol
28
Why is ritonavir often combined with other protease inhibitors?
Because it inhibits CYP3A4 and protease inhibits are metabolized by CYP3A4 -Keeps drug from metabolizing too quickly.
29
What is the DOC of the protease inhibitors?
Darunavir
30
Who should Darunavir never be used for?
People with sulfa allergy
31
What are the common side effects seen with atazenavir?
- Less effect on body fat distribution than other protease inhibitors - Increase in bilirubin - Diarrhea, rash, nausea
32
What is Lopinavir always combined with?
Ritonavir to increase bioavailability
33
What are the common side effects seen with Indinavir?
Nephrolithiasis and hyperbilirubinemia (aggressive hydration recommended)
34
When is tipranavir used?
In combination with Ritonavir, Indicated for use in treatment-experienced HIV infected patients who harbor strains resistant to other protease inhibitors
35
When should tipranavir not be used?
- Patients with head trauma because it increases risk for intracranial hemorrhage - Patients with sulfa allergy
36
What are the two fusion inhibitor HIV drugs?
Enfuvirtide and maraviroc
37
What is the MOA of Enfuvirtude (fuzeon)?
Binds to the gp41 subunit of the viral envelope glycoproteins, prevents conformation change required for membrane fusion and viral entry
38
What is the only parenteral antiretroviral agent?
Enfuvirtide (Fuzeon)
39
What is the MOA of Maraviroc?
-Inhibits fusion of virus by binding to the CCR5 receptor of the CD4 T-Cell.
40
When is Maraviroc used?
-ONLY in patients with a CCR5-tropic HIV infection in which other treatment has not been effective
41
What kind of drug is Dolutegravir?
Integrase inhibitor -DOC in combination with NRTIs
42
When in Dolutegravir used?
Treatment-resistant patients where other drugs are no longer working

Pharmacology (25 decks)

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