Non-HIV Drugs Flashcards

1
Q

What drugs are in the category of neuraminidase inhibitors?

A

Zanamavir

Oseltamivir

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2
Q

What is the mechanism of action of neuraminidase inhibitors?

A

Inhibits neuramidase – enzyme that cleaves bond between terminal sialic acid residues on host cell surface and progeny virus hemagglutinin (HA) protein

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3
Q

What is the clinical use of neuraminidase inhibitors?

A

Treatment and prophylaxis of influenza virus

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4
Q

What are side effects/toxicities of Zanamivir?

A

Nausea, allergy, diarrhea, respiratory distress

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5
Q

What are side effects/toxicities of Oseltamivir?

A

Seizure events, respiratory distress

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6
Q

What mechanisms of resistance are there for neuraminidase inhibitors?

A

Mutations in HA and/or NA

Cross resistance of Oseltamivir with Zanamavir

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7
Q

Who can use Zanamavir?

A

Not recommended for <7 yo or those with underlying respiratory disease

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8
Q

Who can use Oseltamivir?

A

Approved for treatment in >1 yo and prophylaxis in >13 yo

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9
Q

Who should use neuramidase inhibitors as prophylaxis?

A

High-risk children, people in contact with high-risk children

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10
Q

What is the method for administration for Zanamavir v. Oseltamivir?

A

Zanamavir - Inhalation

Oseltamivir - Oral

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11
Q

What is the primary method for preventing influenza?

A

Influenza vaccine

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12
Q

Who should not use the live attenuated influenza vaccine (Flumist)?

A

50 yo

People with medical condition that places them at high risk of influenza

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13
Q

What is the mechanism of action of Ribavirin?

A

Inhibits IMP dehydrogenase, preventing GMP synthesis (and therefore reducing ATP formation)

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14
Q

What are the clinical uses of Ribavirin?

A

Paramyxoviruses (RSV, parainfluenza)
Arenaviruses (Lassa fever)
Hepatitis C

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15
Q

What are side effects/toxicities of Ribavirin?

A

Hemolytic anemia with high dose or prolonged therapy (has longer half life in RBCs)
Myocardial infarction
Teratogenic

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16
Q

What are methods of administration of Ribavirin?

A

Inhalation (most common)
Oral (less effective)
IV (for Arenaviruses)

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17
Q

What is standard of care for HCV?

A

Ribavirin combined with Pegylated interferons

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18
Q

What comprises the new IFN-free regimen for HCV care?

A

Combination therapy of:

  • Ribavirin
  • Protease inhibitor
  • Polymerase inhibitor
  • Cyclophilin inhibitors
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19
Q

What are the goals of HBV therapy?

A

Prevent complications like cirrhosis, hepatic failure, and hepatocellular carcinoma

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20
Q

What therapies are approved for HBV?

A

IFNalpha, Peg-IFNalpha, 5 nucleoside analogs

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21
Q

What is the first line therapy for HBV?

A

Entecavir and Tenofovir

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22
Q

What therapy was successful in MERS-CoV and SARS studies in monkeys?

A

Ribavirin with IFNalpha2b

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23
Q

What are the acyclic and carbocyclic guanosine analogs?

A
Acyclovir
Valaciclovir
Famciclovir
Ganciclovir
Valganciclovir
24
Q

What is the mechanism of action of Acyclovir?

A

Guanosine analog
Monophosphorylated by viral thymidine kinase (TK)
Triphosphate formed by cellular enzymes to become acyclo-GTP
Inhibits viral DNA polymerase by chain termination

25
Q

What is the clinical spectrum of acyclovir?

A

Genital HSV infections
Chronic and recurrent mucocutaneous HSV or VZV infections
Neonatal herpes
HSV encephalitis

26
Q

What are side effects/toxicities of acyclovir?

A

Very low overall
Encephalopathy associated with renal insufficiency
Obstructive nephropathy with high IV doses

27
Q

What are methods of administration of acyclovir?

A

Oral (for genital lesions and recurrent HSV)
Topical (genital lesions)
IV (HSV encephalitis)
IV and oral (for neonatal HSV)

28
Q

What are mechanisms of resistance of acyclovir?

A

Mutations in viral TK and/or DNA polymerase

29
Q

What is the oral prodrug of acyclovir?

A

Valaciclovir

30
Q

What is mechanism of action of Famciclovir?

A

Same as acyclovir:
Guanosine analog
Monophosphorylated by viral thymidine kinase (TK)
Triphosphate formed by cellular enzymes to become acyclo-GTP
Inhibits viral DNA polymerase by chain termination

Not as effective at pol inhibition, but similar antiviral activity due to better phosphorylation by cellular enzymes

31
Q

What is the spectrum of clinical activity of Famciclovir?

A

Genital HSV

VZV

32
Q

What are the methods of administration of Famciclovir?

A

Oral

33
Q

What are mechanisms of resistance of Famciclovir?

A

Cross-resistance with acyclovir

34
Q

What compound is Famciclovir the prodrug of?

A

Penciclovir

35
Q

What is the mechanism of action of Ganciclovir?

A

Guanosine analog
Monophosphorylated by CMV viral kinase pUL97
Triphosphate formed by cellular enzymes to become ganciclovir-GTP
Inhibits viral DNA polymerase by chain termination

36
Q

What is the spectrum of clinical activity of Ganciclovir?

A

Life or sight-threatening CMV in immunosuppressed patients

Pneumonitis in BMT recipients

37
Q

What are side effects/toxicities of Ganciclovir?

A

Bone marrow suppression
Neutropenia
Thrombocytopenia
CNS effects (headache, behavioral changes, psychosis)

38
Q

What is method of administration of Ganciclovir?

A

IV

39
Q

What are mechanisms of resistance of Ganciclovir?

A

Mutations in CMV kinase pUL97 and/or DNA polymerase

40
Q

What is the oral prodrug of Ganciclovir?

A

Valganciclovir

41
Q

What is mechanism of action of Foscarnet?

A

Inhibits viral DNA pol and RT by interacting with pyrophosphate binding sites on these enzymes (distinct from Acyclovir sites)

42
Q

What is the spectrum of clinical activity of Foscarnet?

A

Acyclovir-resistant HSV and CMV retinitis in AIDS patients

43
Q

What are the side effects/toxicities of Foscarnet?

A
Risk of renal insufficiency
Anemia
Granulocytopenia
Tremor, seizures, irritability
Hypocalcemia
44
Q

What is the method of administration of Foscarnet?

A

IV

45
Q

What are mechanisms of resistance of Foscarnet?

A

Mutations in DNA polymerase

46
Q

What is the mechanism of action of Cidofovir?

A

Cytosine analog
Phosphorylated to active form by cellular enzymes (not viral)
Inhibits viral DNA polymerase by chain termination

47
Q

What is spectrum of clinical activity of Cidofovir?

A

CMV retinitis in AIDS patients

48
Q

What are side effects/toxicities of Cidofovir?

A

Irreversible renal toxicity (must be given with probenecid to protect kidneys)

49
Q

What is method of administration of cidofovir?

A

IV

50
Q

What are mechanisms of resistance of cidofovir?

A

Resistant strain may develop with treatment

51
Q

What disorders can immunoglobulins be used as prophylaxis for?

A

Hepatitis A
RSV infection in high risk children/babies
Rabies

52
Q

What disorders can immunoglobulins be used as treatment for?

A

HBV (post exposure of liver transplant)
CMV, Varicella, Measles
Rabies
Ebola

53
Q

What are methods of administration of immunoglobulins?

A

Subcutaneous
IM
IV

54
Q

What is the mechanism of action of antisense oligonucleotide Vitravene?

A

21 member oligonucleotide complementary to region of CMV IE (immediate early gene) that encodes several proteins required for virus replication

55
Q

What is the spectrum of clinical activity of antisense oligonucleotide Vitravene?

A

CMV retinitis in AIDS patients who are intolerant or have contraindication for other treatments

56
Q

What is method of administration of antisense oligonucleotide Vitravene?

A

Intravitreal injection