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Pharmacology I Exam 3 > Antiretrovirals > Flashcards

Antiretrovirals Flashcards

1
Q

How is Zidovudine administered?

A

Oral

Short acting; given 5X per day

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2
Q

What is the MOA for NRTIs?

A

Nucleoside analogue

Inserts itself into growing chain and inhibits viral reverse transcriptase leading to DNA termination

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3
Q

What is significant about the penetration of Zidovudine?

A

Good CNS penetration

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4
Q

What are the uses for Zidovudine?

A

Maintain CD4 count; lessen opportunistic infections

DOC:
HIV in Pregnancy (+ Lamivudine)
AIDS dementia

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5
Q

What are toxicities of Zidovudine?

A
  • Lactic acidosis or hepatoxicity
  • Myelosuppresion: neutropenia, anemia (caution when bone marrow compromised or using ganciclovir, ribavirin)
  • HA, nausea, vomiting, insomnia
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6
Q

What are the uses of Tenofovir and Emtricitabine?

A

DOC:

HIV (given together)

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7
Q

What are the toxicities of Tenofovir and Emtricitabine?

A
  • Flatulence

- Lactic acidosis or hepatoxicity

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8
Q

What drug should you not use with Tenofovir and Emtricitabine?

A

Do not use with Lamivudine as similar mechanism and resistance profiles

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9
Q

What are the uses of Lamivudine?

A

DOC:

  • Co-infection of HIV and Hep B
  • HIV in pregnancy (+ Zidovudine)

Monotherapy in HBV

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10
Q

What are the toxicities of Lamivudine?

A
  • Lactic acidosis or hepatoxicity

- HA, fatigue, insomnia, GI

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11
Q

What drugs must you combine with Abacavir?

A

Lamivudine or Zidovudine

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12
Q

What are toxicities of Abacavir?

A
  • Serious hypersensitivity (screen for HLA-B-5701 as if positive for this allele, has higher chance for SJS)
  • Lactic acidosis or hepatoxicity
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13
Q

What are special considerations for Abacavir?

A

Screen for HLA-B-5701 as if positive for this allele, has higher chance for SJS

If hypersensitivity occurs, stop drug and do not restart it as it could be fatal

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14
Q

What is the MOA for NNRTIs?

A

Bind directly to inhibit viral reverse transcriptase and prevent conversion of RNA to DNA (no phosphorylation)

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15
Q

What are the uses for Efavirenz?

A

DOC:

Initial HIV treatment

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16
Q

What are toxicities of Efavirenz?

A
  • Drug interactions – induces CYP3A4
  • Decreases effectiveness of oral birth control and methadone
  • Teratogenic!
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17
Q

What are contraindications to Efavirenz?

A

Pregnancy

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18
Q

What are the uses for Rilpivirine?

A

DOC:

Initial HIV therapy in pregnant patients

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19
Q

What are contraindications for Rilpivirine?

A

Patients with hepatitis co-infection as may increase liver enzymes

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20
Q

What is the MOA of all protease inhibitors?

A

Inhibit proteases which inhibits the production of smaller proteins and ultimately decreases viral loads as they cannot replicate

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21
Q

What are the drug reactions associated with protease inhibitors?

A

Protease inhibitors are metabolized by CYP3A4 and have interactions with drugs that induce CYP3A4 such as Rifampin and Rifabutin

22
Q

What protease inhibitor is given with other protease inhibitors and why?

A

Ritonavir is often given in combination because it is a potent inhibitor of CYP3A4 which increases PI levels for lower dose/less frequent dosing

23
Q

What should you not use with protease inhibitors and why?

A

Should not use St. John’s Wort as it increases the metabolism of protease inhibitors

Should not combine with statins as protease inhibitors already increase serum cholesterol

24
Q

What are common toxicities associated with all protease inhibitors?

A
  • Altered body fat distribution
  • Insulin resistance
  • Increase in serum cholesterol (do not combine with statins)
  • Spontaneous bleeding
25
Q

What are the uses of Ritonavir?

A

Boosts bioavailability of other protease inhibitors

26
Q

What are toxicities of Ritonavir?

A
  • Inhibits CYP3A4 – combine with other protease inhibitors to increase their bioavailability
  • Prolonged QT (if combined with saquinavir)
  • Contains ethanol (do not give with metronidazole or cephalosporins)
27
Q

What are the toxicities of Darunavir?

A
  • Rash, nausea, diarrhea, HA, bad dreams

- Contains sulfonamide moiety

28
Q

What are contraindications for Darunavir?

A

Patients with sulfa allergy as drug contains sulfa moiety

29
Q

What are the toxicities of Atazenavir?

A
  • Less effect on body fat distribution
  • May increase bilirubin due to inhibition of UGT
  • Diarrhea, rash, nausea, hypoglycemia
30
Q

What are contraindications to Atazenavir?

A

Infants (inhibits UGT and can increase bilirubin)

31
Q

What are contradindications of Saquinavir?

A
  • QT prolongation (DO NOT combine with ritonavir)

- GI side effects

32
Q

What are toxicities of Lopinavir/Ritonavir?

A
  • Diarrhea, nausea

- Liver enzyme elevation if pre-existing hepatic disease

33
Q

What are toxicities of Indinavir?

A
  • Nephrolithiasis
  • Hyperbilirubinemia due to urinary crystallization
  • Need aggressive hydration
34
Q

What other protease inhibitor should not be given with Ritonavir and why?

A

Do not combine Saquinavir with Ritonavir as they will cause QT prolongation

35
Q

What is the MOA for Enfuvirtide (Fuzeon)?

A

Fusion inhibitor

Bind to gp41 subunit of viral envelope glycoprotein; prevents conformational change required for membrane fusion and viral entry into target cells

36
Q

What are uses of Enfuvirtide (Fuzeon)?

A

Advanced disease who are treatment-experienced

Combine with other antiretrovirals

37
Q

What are toxicities of Enfuvirtide (Fuzeon)?

A

Increased likelihood of bacterial pneumonia

38
Q

What is the MOA for Maraviroc?

A

Fusion inhibitor

Inhibits fusion of virus by binding to CCR5 receptor of CD4 T-cell – one of two chemokine receptors needed for HIV entry into cell

39
Q

What are uses of Maraviroc?

A

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

40
Q

What is the MOA for Dolutegravir?

A

Integrase inhibitor

Blocks integrase enzyme needed for replication

41
Q

What are uses for Dolutegravir?

A

Used in treatment resistant patients where other drugs are no longer working

42
Q

What is the NRTI DOC for HIV?

A

Tenofovir + Emtricitabine

43
Q

What is the NRTI DOC for pregnant HIV patients?

A

Zidovudine + Lamivudine

44
Q

What is the NRTI DOC for co-infection of HIV and Hepatitis B?

A

Lamivudine

45
Q

What is the NNRTI DOC for HIV?

A

Efavirenz

46
Q

What is the NNRTI DOC for pregnant HIV patients?

A

Rilpivirine

47
Q

What is the Protease Inhibitor DOC for HIV?

A

Darunavir

48
Q

What is the Protease Inhibitor 2nd DOC for HIV?

A

Atazenavir

49
Q

What is the Integrase Inhibitor DOC for HIV?

A

Dolutegravir

50
Q

What antiretroviral regiment is given for a treatment-naive patient?

What does this consist of?

A

HAART

Two NRTIs
A third drug from one of three drug classes: 
- NNRTI
- Protease Inhibitor (PI)
- Integrase Inhibitor
51
Q

What is the Protease Inhibitor 2nd DOC for HIV?

A

Atazenavir

Pharmacology I Exam 3 (8 decks)

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