Drugs for HIV Flashcards

1
Q

Name the 8 Nucleoside Reverse Transcriptase Inhibitors (NRTI)

A
  • Zidovudine
  • Lamivudine
  • Emtricitabine
  • Tenofovir
  • Didanosine
  • Zalcitabine
  • Stavudine
  • Abacavir
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2
Q

MOA of Nucleoside Reverse Transcriptase Inhibitors (NRTI)

A
  • Nucleoside analogue
  • inhibits viral reverse transcriptase
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3
Q

route of administration of Zidovudine

A

oral

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4
Q

distribution of Zidovudine

A

good CNS penetration

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5
Q

Use of Zidovudine

A
  • lessen opportunistic infections
  • safe in pregnancy: decreases risk of transmission during pregnancy and during labor
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6
Q

Toxicity of Zidovudine

A
  • CNS
  • lactic acidosis or hepatotoxicity
  • Myelosuppression: neutropenia, anemia
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7
Q

If resistance develops to Zidovudine, what drug can be added to treatment regimen (alternate first choice)

A

Lamivudine

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8
Q

MOA of Zidovudine

A

Thymidine analogue

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9
Q

MOA of Lamivudine

A
  • Cytosine analogue
  • inhibits HIV reverse transcriptase
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10
Q

route of administration of Lamivudine

A

oral

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11
Q

toxicity of Lamivudine

A

low toxicity, very well tolerated

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12
Q

MOA of Tenofovir

A
  • Adenosine analogue
  • inhibit reverse transcriptase
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13
Q

MOA of Emtricitabine

A
  • cytosine inhibitor
  • inhibit reverse transcriptase
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14
Q

route of administration of Tenofovir and Emtricitabine

A

oral

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15
Q

DOC NRTI for treatment of HIV

A

Tenofovir and Emtricitabine

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16
Q

side effects of Tenofovir and Emtricitabine

A

flatulence

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17
Q

MOA of Didanosine

A

adenosine analogue

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18
Q

Toxicity of Didanosine, Stavudine, and Zalcitabine

A

peripheral neuropathy

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19
Q

toxicity of Abacavir

A
  • serious hypersensitivity
    • discontinue drug and DO NOT restart
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20
Q

what are serious side effects that can occur with all NRTIs

A
  • lactic acidosis
  • hepatotoxicity
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21
Q

name the 3 non-nucleotide reverse transcriptase inhibitors

A
  • Efavirenz
  • Nevirapine
  • Delavirdine
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22
Q

MOA of non-nucleotide reverse transcriptase inhibitors

A
  • bind directly to inhibit viral reverse transcriptase
  • do not require phosphorylation for activity
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23
Q

DOC: NNRTI for initial therapy of HIV

A

Efavirenz

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24
Q

route of administration of Efavirenz

A

oral

25
Q

combine Efavirenz with ?

A

nucleoside analogues

26
Q

toxicities of Efavirenz

A
  • Drug interaction: induces and inhibits CYP3A
  • teratogenic: avoid in pregnancy
27
Q

route of administration of Neviparine

A

oral

28
Q

DOC: NNRTI for intial therapy of HIV in pregnant females

A

Neviparine

*effective in the prevention of transmission of HIV from mother to newborn

29
Q

toxicities of Neviparine

A
  • stevens-johnson syndrome
  • hepatitis
30
Q

route of administration of Delavirdine

A

oral

31
Q

toxicities of Delavirdine

A
  • inhibits CYP3A4
  • rash
  • teratogenic: avoid in pregnancy
32
Q

Name the 7 protease inhibitors used in treatment of HIV

A
  • Atazanavir
  • Darunavir
  • Ritonavir
  • Saquinavir
  • Lopinavir/ritonavir
  • Indinavir
  • Tipranavir
33
Q

route of administration of protease inhibitors

A

oral

34
Q

combine protease inhibitors with?

A
  1. NRTIs
  2. ritonavir: bc protease inhibitors are metabolized by CYP3A4 and rionavir inhibits CYP3A4
35
Q

when giving your patient protease inhibitors, what should you specifically tell them to not take?

A

St. John’s Wort

36
Q

common toxicities of protease inhibitors

A
  • altered body fat distribution
  • insulin resistance
  • increases serum cholesterol: do not combine with statins
  • spontaneous bleeding: hemophilia A or B
37
Q

DOC: protease inhibitor in treatment of HIV

A

Atazenavir

38
Q

toxicity specific to Atazenavir

A
  • increase biliruben
  • diarrhea, rash, nausea
  • less effect on body fat distribution
39
Q

DO second choice: protease inhibitor in treatment of HIV

A

Darunavir: combine with ritonavir

40
Q

contraindication of Darunavir

A
  • contains a sulfonamide moiety: do not use in patients with sulfa allergy
41
Q

Use of Ritonavir

A
  • inhibits CYP3A4: combined with other protease inhibitors to increase thier bioavailability
42
Q

Ritonavir should not be combined with which because together they cause QT elongation

A

Saquinavir

43
Q

Ritonavir contains alcohol and so should not be combined with

A
  • disulfiram
  • metronidazole
44
Q

There is a cross resistance between ritonavir and ?

A

Indinavir

45
Q

toxicity of Indinavir

A
  • nephrolithiasis
  • hyperbilirubinemia
46
Q

Use of Tipranavir

A
  • non-peptide PI
  • indicated for use in treatment -experienced HIV-1-infected patients who harbor strains resistant to other PIs
47
Q

Tipranavir is combined with

A

ritonavir

48
Q

toxicity of Tipranavir + ritonavir

A
  • intracranial hemorrhage - avoid in pts with head trauma
  • sulfonamide moiety
  • hepatotoxic
49
Q

MOA of Enfuvirtide

A
  • fusion inhibitor
  • binds to gp41 subunit of viral envelope glycoprotein
50
Q

route of administration of Enfuvirtide

A

subcutaneous: only parenteral antiretroviral agent

51
Q

good thing about Enfuvirtide

A

no cross resistance with other antiretroviral agents

52
Q

adverse effects of Enfuvirtide

A

increases likelihood of bacterial pneumonia

53
Q

MOA of Maraviroc

A
  • inhibits virus fusion
  • binds to CCR5 receptor of CD4 T-cell
54
Q

use of Maraviroc

A

only use in patients with CCR5-tropic HIV infection in whom other treatment has not been effective

55
Q

MOA of Raltegravir

A

integrase inhibitor: inhibits transfer of viral DNA to host cell DNA

56
Q

MOA: zalcitabine

A

cytosine analogue

57
Q

MOA: stavudine

A

thymidine analogue

58
Q

MOA: abacavir

A

guanosine analogue