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Boards First Aid and Kaplan > Antiviral Agents > Flashcards

Antiviral Agents Flashcards

1
Q

What is the MOA of enfuvirtide and maraviroc?

A

Inhibit viral adsorption/penetration into the host cell

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2
Q

What is the MOA of amantadine?

A

Inhibits uncoating

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3
Q

What is the MOA of polymerase inhibitors and reverse transcriptase inhibitors?

A

Inhibit nucleic acid synthesis

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4
Q

What is the MOA of protease inhibitors?

A

Inhibit protein synthesis and processing

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5
Q

What is the MOA of neuraminidase inhibitors?

A

Inhibit viral release from cells

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6
Q

Which antivirals inhibit DNA polymerases?

A
  • Acyclovir
  • Foscarnet
  • Ganicyclovir
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7
Q

Which antivirals inhibit RNA polymerases?

A
  • Foscarnet

- Ribavirin

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8
Q

Which antivirals inhibit viral reverse transcriptase?

A
  • Zidovudine, didanosine, zalcitabine, lamivudine, stavudine, and nevirapine (anything that ends in “-ine” (except amantadine)
  • Efavirenz
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9
Q

Which antivirals inhibit viral aspartate protease?

A

-Indinavir, ritonavir, saquinavir, nelfinavir

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10
Q

Which antivirals inhibit viral neuraminidase?

A

Zanamivir and oseltamivir

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11
Q

What is the MOA of acyclovir?

A
  • Monophosphorylated by thymidine kinase to become triphosphate
  • Acyclovir is BOTH a substrate and inhibitor of viral DNA polymerase
  • Acts as a DNA chain terminator because it lacks a ribosyl 3’ hydoxyl group
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12
Q

What are the mechanisms of resistance to acyclovir?

A
  • Changes in DNA polymerase

- Decreased activity of thymidine kinase-Half of resistant strains completely lack thymidine kinase

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13
Q

What is a good way to remember which antivirals are used to treat which infx?

A
  • avir-AIDS
  • ivir-Influenza
  • ovir-oh my god I have herpes
  • evir and uvir-Hep C
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14
Q

What are the clinical uses of acyclovir?

A

HSV and VZV

  • Reduces viral shedding in genital herpes-> dec acute neuritis in shingles but no effect on postherpetic neuralgia
  • Reduces sx early in chickenpox, prophylactic in immunocompromised
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15
Q

What are the side effects of acyclovir?

A
  • Crystalluria and neurotoxicity

- Minor with oral use, increased with IV

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16
Q

What is the MOA of ganicyclovir?

A

Similar to acyclovir-involves thymidine kinase in herpes and phosphotransferase (UL97) in CMV

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17
Q

What are the clinical uses of ganicyclovir?

A

HSV, VZV, and CMV

-Mostly used in prophylaxis and tx of CMV (CD4 < 50), including retinitis, in AIDS and tranplant pts

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18
Q

What are the side effects of ganicyclovir?

A

-Dose-limiting hematotoxicity (leukopenia and thrombocytopenia)

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19
Q

What is the MOA of foscarnet?

A

Inhibits viral DNA and RNA polymerases (not an antimetabolite though)

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20
Q

What are the clinical uses of foscarnet?

A

-Identical to ganicyclovir plus increased activity against acyclovir resistant strains of HSV

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21
Q

What are the side effects of foscarnet?

A

-Dose limiting nephrotoxicity with acute tubular necrosis, electrolyte imbalance with hypoCa (tremors and seizures)

22
Q

What is the MOA of the original reverse transcriptase inhibitors?

A

The original reverse transcriptase inhibitors are nucleoside antimetabolites (zidovudine is the prototype)
-Converted to active forms via phosphorylation

23
Q

Nucleoside reverse transcriptase inhibitors (NRTIs)

A
  • Components of most combination drug regimens used in HIV

- Used with a protease inhibitor

24
Q

What is HAART?

A

-Highly active antiretroviral therapy (HAART) has often resulted in decreased viral RNA, reversal of CD4 decline, and decreased opportunistic infections

25
Q

What are nNRTIs?

A
  • RTIs that DO NOT require metabolic activation (nevirapine, efavirenz)
  • Are not myelosuppressant
  • Inhibit reverse transcriptase at a different site than NRTIs
  • Additive or synergistic if used in combo w/ NRTIs and/or PIs
26
Q

What is the MOA of zidovudine (ZDV, azidothymidine/AZT)?

A

NRTI-phosphorylated nonspecifically to a triphosphate that can inhibit RT
-Inhibits natural nucleotides and can also be incorporated into viral DNA to cause chain termination

27
Q

What is the mechanism of resistance to zidovudine?

A

Resistance occurs by mutations (multiple) in the RT gene

28
Q

What are the side effects of zidovudine?

A

-Hematotoxicity (major and dose-limiting)

29
Q

What are the major side effects of didanosine?

A

Pancreatitis (major and dose-limiting)

30
Q

What are the side effects of lamivudine (3TC) and emtricitabine (FTC)?

A
  • Least toxic of the NRTIs, but some GI effects and neutropenia
  • Lamivudine is active in HBV
31
Q

What is the side effect common to most NRTIs?

A

Peripheral neuropathy

32
Q

What is the MOA of protease inhibitors?

A

-PIs inhibit aspartate protease (pol gene encoded)-viral enzyme that cleaves polypeptides to form the proteins of the HIV core

33
Q

What is the mechanism of resistance for PIs?

A

-Point mutations in the pol gene such that there is complete cross resistance between different PIs

34
Q

What are 2 examples of PIs?

A
  • Ritonavir (most common)

- Indinavir

35
Q

What is the main clinical use of ritonavir?

A

Used as a booster to increase the levels of other PIs

36
Q

What is the main side effect of ritonavir?

A
  • Induction of CYP1A2

- Inhibits CYP3A4 and CYP2D6-major CYP isoforms

37
Q

What is the side effect that can be caused by any PI?

A

Syndrome of disordered lipid and CHO metabolism with central adiposity and insulin resistance -> hyperglycemia

38
Q

What is the treatment combination used for HIV postexposure prophylaxis?

A

Emtricitabine + tenofovir + raltegravir

39
Q

What is the treatment combination used for HIV prophylaxis in pregnancy?

A

Ritonavir-boosted atazanavir or lopinavir
2 NRTIs
-Emtricitabine or lamivudine
-Zidovudine or tenofovir

40
Q

What is the MOA of integrase inhibitors?

A

Prevents integration of viral genome into host cell DNA

41
Q

What is an example of an integrase inhibitor?

A

Raltegravir

42
Q

Name 2 examples of fusion inhibitors

A
  • Enfurvirtide

- Maraviroc

43
Q

What is the MOA of enfurvirtide?

A

Binds to gp41-inhibits the fusion of HIV-1 to CD4 cells

44
Q

What is the MOA of maraviroc?

A

Blocks the binding of gp120 HIV protein to CCR5 on macrophage to prevent viral entry

45
Q

What is the MOA of zanamivir and oseltamivir?

A

Inhibit neuraminidases of influenza A and B

  • enzymes that prevent clumping of virions so that more particles are available for infecting host cells
  • Decreases the likelihood that the virus will penetrate uninfected cells
46
Q

What are the clinical uses of oseltamivir and zanamivir?

A

Prophylaxis

47
Q

What is the MOA of ribavirin?

A
  • Monophosphorylated form inhibits IMP dehydrogenase

- Triphosphate inhibits viral RNA polymerase and capping of viral RNA

48
Q

What are the clinical uses of ribavirin?

A
  • Adjunct to alpha-interferons in HCV
  • RSV
  • Lassa fever
  • Hantavirus
49
Q

What are the possible side effects of ribavirin?

A
  • Hematotoxic
  • Upper airway irritation
  • Teratogen
50
Q

What are the main drugs used in HCV treatment?

A
  • Sofosbuvir

- Simeprevir

51
Q

What is the MOA of sofosbuvir?

A

Nucleotide analog that inhibits RNA polymerase

-combined with ribavirin or alpha-interferon

52
Q

What is the MOA of simeprevir?

A

HCV protease inhibitor

-combined with ribavirin or alpha-interferon

Boards First Aid and Kaplan (19 decks)

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