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Pharmacology I Final Exam > Antiretrovirals (HIV) > Flashcards

Antiretrovirals (HIV) Flashcards

1
Q

What is the DOC of the NRTIs?

A

Emtricitabine + Tenofovir

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2
Q

What is the DOC of the NNRTIs? What is the patient is pregnant?

A

Efavirenz

- If pregnant, Rilpivirine

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3
Q

What is the DOC of the PIs?

What do most of the PIs end with?

A

Darunavir

  • Most end in “avir” (except Abacavir from NRTIs)
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4
Q

What is the DOC of the IIs?

A

Dolutegravir

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5
Q

What is the MOA of all NRTIs?

A

Nucleoside analogue → Inhibit reverse transcriptase

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6
Q

What is the toxicity of all NRTIs (2)?

A
  • Lactic acidosis

- Hepatotoxicity

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7
Q

What is the primary toxicity associated with Emtricitabine + Tenofovir (not including normal NRTI toxicities of lactic acidosis and hepatotoxicity)?

A

Flatulence

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8
Q

What is the primary toxicity associated with Zidovudine (not including normal NRTI toxicities of lactic acidosis and hepatotoxicity)?

A

Myelosuppression

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9
Q

What medication is used to treat AIDS dementia, and what characteristic does this mean the medication has?

A

Zidovudine has good CNS penetration

- Used to treat AIDS dementia

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10
Q

What two NRTIs are also used to treat Hep B (can treat HIV and Hep B co-infection)?

A
  • Tenofovir (+ Emtricitabine)

- Lamivudine

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11
Q

What MUST be considered when starting Abacavir?

What type of inhibitor is it?

A

If patient is HLA-B-5701 positive

NRTI

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12
Q

With what medication should you consider genotyping for HLA-B-5701? If they are positive, what should be your next step in the treatment plan?

A

Abacavir

- STOP it and NEVER restart it (could be fatal)

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13
Q

What are the two primary toxicities associated with Abacavir?

What type of inhibitor is it?

A
  • Hypersensitivity
  • Increased risk for SJS (if HLA-B-5701 positive)

NRTI

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14
Q

What is the MOA for all NNRTIs?

A

Bind directly to reverse transcriptase and inhibits it

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15
Q

What are the two primary toxicities associated with Efavirenz?

What type of inhibitor is it?

A
  • TERATOGENIC (use Rilpivirine instead)
  • Drug interactions (induces CYPs)

NNRTI

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16
Q

What are the four primary toxicities associated with all PIs?

A
  • Drug interactions
  • Altered body fat distribution
  • Insulin resistance
  • Increased serum cholesterol
17
Q

Why are drug interactions and PIs such a big issue??? (think how it is metabolized and what it may be given with)

Give an example of a CYP3A4 inducer and a CYP3A4 inhibitor.

A

PIs are metabolized by CYP3A4 so if using a PI to treat HIV, avoid any other drugs that induce/inhibit CYP3A4
- Otherwise, PI drug levels decrease if induced or increase if inhibited

  • Inducer example: Rifampin
  • Inhibitor example: Erythromycin
18
Q

What is the purpose of Ritonavir? What three drugs can it NOT be given with?

A

Ritonavir is a “BOOST” and inhibits CYP3A4 so it will protect the PIs from any inducers (cancels out inducer so PI levels remain normal/not decreased)

  • Saquinavir
  • Indinavir
  • Tipranavir
19
Q

What is the primary toxicity associated with Darunavir?

What type of inhibitor is it?

A

Sulfa moiety (cannot give if Sulfa allergy)

PI

20
Q

What medication is used as an alternative to Darunavir?
What is an advantage of this medication?

What type of inhibitor is it?

A

Atazenavir
- Less altered body fat distribution

PI

21
Q

What is the primary toxicity associated with Saquinavir? What medication should it NOT be given with, and why?

What type of inhibitor is it?

A

QT prolongation
- Do NOT combine with Ritonavir (worsens toxicity)

PI

22
Q

What medication is ALWAYS combined with Ritonavir, and why?

What type of inhibitor is it?

A

Lopinavir + Ritonavir (increased bioavailability)

PI

23
Q

What are the two primary toxicities associated with Indinavir? What medication should it NOT be given with, and why?

What type of inhibitor is it?

A
  • Nephrolithiasis
  • Hyperbilirubinemia (HYDRATE)
  • Do NOT combine with Ritonavir (cross-resistance with Ritonavir)

PI

24
Q

What are the two primary toxicities associated with Tipranavir? What medication should it NOT be given with, and why?

What type of inhibitor is it?

A
  • Sulfa moiety (cannot give if Sulfa allergy)
  • Hepatotoxicity
  • Do NOT combine with Ritonavir (increased bleeding)

PI

25
Q

What are the two FIs, and what is each of their MOAs?

A

Enfuvirtide (Fuzeon)
- MOA: binds to gp41 subunit

Maraviroc
- MOA: binds to CCR-5 ONLY (check receptor type)

26
Q

What is the MOA of Dolutegravir?

What type of inhibitor is it?

A

Inhibit integrase

II

Pharmacology I Final Exam (8 decks)

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