Antivirals Flashcards

1
Q

what are the antivirals for influenza

A

neuraminidase inhibitors: Oseltamivir and Zanamivir

M2 inhibitors: Amantadine and Rimantadine

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2
Q

in depth mechanism of neuraminidase inhibitors (name them)

A

Oseltamivir and Zanamivir

neuraminidase cleaves sialic acid residues from viral and surface proteins of infected cells –> promotes virion release and prevents clumping of newly released virions

the above drugs inhibits this process

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3
Q

which strain of flu do the neuraminidase treat (name them)

A

Oseltamivir and Zanamivir

Influenza A and B

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4
Q

most common adverse effects of Oseltamivir

A

nausea, vomiting, diarrhea, abdominal pain, insomnia, vertigo, and neuropsychiatric issues

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5
Q

adverse effects of Zanamivir

A

it’s inhaled so usually well tolerated

acute bronchospasm in those with breathing difficulties (asthma and COPD)

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6
Q

mechanism of M2 inhibitors (name them)

A

Amantadine and Rimantadine

inhibits replication of influenza virus by inhibiting M2

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7
Q

what strain of influenza do the M2 inhibitors work on (name them)

A

Amantadine and Rimantadine

Influenza A because it is the only one that has the M2 protein

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8
Q

adverse effects of M2 inhibitors (name them)

A

Amantadine and Rimantadine

anxiety, disorientation, headache

neuro effects are less severe and more frequent with rimantadine

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9
Q

which set of anti flu medication would you give to pregnant women

A

neuraminidase inhibitors

Oseltamivir and Zanamivir

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10
Q

what are the antivirals for hepatitis

A

Interferon
Ribavirin
Nucleoside/Nucleotide Analogues: Entecavir and Lamivudine
Protease Inhibitors: Boceprevir and Telaprevir

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11
Q

what is the selective antiviral action of IFNalpha due to

A

activation of host cell ribonuclease that preferentially degrades mRNA

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12
Q

adverse effects of interferons

A

flu like symptoms, neurological problems, and depression in those with pre-existing mood disorders

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13
Q

what is ribavirin’s antiviral activity reversed by

A

guanosine

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14
Q

mechanism of ribavirin

A

inhibitor of influenza RNA polymerase and mRNA guanylyltransferase

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15
Q

two drugs used together for treatment of HCV

A

Ribavirin and IFNalpha

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16
Q

adverse effects of ribavirin

A

sudden deterioration of resp function
cardiovascular effects
hemolytic anemia
SEVERE depression, suicidal ideation, relapse of drug abuse

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17
Q

contraindication of ribavirin

A

Pregnant women and their male partners

Pre-existing Psychiatric Disorders

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18
Q

what are the protease inhibitors used for treatment in hepatitis

A

Boceprevir and Telaprevir

19
Q

mechanism of boceprevir

A

binds reversibly to HCV nonstructural 3 protein thereby inhibiting viral replication

20
Q

adverse effect of boceprevir

A

flu like illness
anemia – fatigue
nausea
dysgeusia – distortion of sense of taste

21
Q

mechanism of telaprevir

A

same as boceprevir - binds reversibly to HCV nonstructural 3 protein thereby inhibiting viral replication

22
Q

adverse effects of telaprevir

A

anemia, leucopenia, neutropenia, rash

Stevens Johnson rash

23
Q

mechanism of the nucleos(t)ide analogues used for treatment of hepatitis (name them)

A

Lamivudine and Entecavir

competitive inhibition of HBV DNA polymerase

also have anti HIV properties

24
Q

mechanism of Lamivudine

A

cytosine analogue that is phosphorylated to its active 5 triphosphate metabolite before incorporation into viral DNA by HBV polymerase then causes chain termination

25
Q

mechanism of Entecavir

A

guanosine analogue inhibits three functions of HBV DNA polymerase:

  • priming of the HBV DNA polymerase
  • reverse transcription of the negative strand from the pregenomic RNA
  • synthesis of positive strand HBV
26
Q

antiviral drugs for Herpes

A
Acyclovir
Ganciclovir
Penciclovir
Cidofivir
Foscarnet
Trifluridine
27
Q

what is acyclovir used to treat

A

guanosine analogue used to treat HSV and VZV

28
Q

mechanism of acyclovir

A

turned into acyclovir triphosphate by viral thymidine kinase and human enzymes –> competitive substrate for viral DNA polymerase –> incorporated into DNA chain –> terminate DNA replication

29
Q

how is acyclovir’s bioavailability increased

A

use of valacyclovir, valyl ester formulation of acyclovir

30
Q

big adverse effect of acyclovir

A

nephrotoxicity

31
Q

what is ganciclovir used to treat

A

acyclic 2’-deoxyguanosine analogue used in the treatment of CMV herpes

32
Q

mechanism of ganciclovir

A

it is triphosphorylated with first phosphate addition by viral UL97-encoded kinase and other two by human cellular enzymes then incorporated onto DNA chain –> termination of DNA replication

33
Q

what is ganciclovir used to treat

A

CMV retinitis in AIDs patient
Herpes simplex keratitis
CMV prophylaxis in transplant patient

34
Q

most common side effect of ganciclovir

A

reversible bone marrow suppression

35
Q

mechanism of penciclovir

A

guanine analogue that gets triphosphorylated then inhibits DNA polymerase activity since it is a competitive inhibitor for deoxyguanosine triphosphate

36
Q

what does penciclovir treat

A

HSV-1, HSV-2, and VZV

37
Q

major clinical indication for cidofovir

A

CMV retinitis especially those resistant against ganciclovir

38
Q

mechanism of foscarnet

A

non nucleoside pyrophosphate analogue that inhibits pyrophosphate binding to DNA polymerase hence suppressing HSV-1, HSV-2, and CMV replication

39
Q

most common adverse effect of all these antiviral herpes drug

A

nephrotoxicity

40
Q

special adverse effect of foscarnet

A

other than nephrotoxicity, electrolyte imbalance

41
Q

mechanism of Trifluridine

A

thymidine analogue that inhibits thymidylate synthetase and incorporates into viral DNA in place of thymidine

42
Q

use of trifluridine

A

opthalmic ointment so used for keratoconjunctivitis and recurrent epithelial keratitis caused by herpes

43
Q

adverse effect of trifluridine

A

transient irritation of eye

palpebral edema