Antivirals Flashcards

1
Q

HSV/ VZV- correspond to what HHVs

A

1,2,3

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2
Q

First line Tx for HSV, VZV

A

Acylovir, Valacyclovir, Penciclovir, Famicilovir

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3
Q

Alternative Tx for HSV and VZV

A

Cidofovir, Foscarnet, Vidarabine

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4
Q

Acyclovir- Drug class

A

Nucleoside analog

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5
Q

Acyclovir- MOA

A

viral thymidine kinase converts Acyclovir to acylco GMP –> inhibits viral DNA pol, chain termination

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6
Q

Acyclovir- Features

A

High selectivity, poor solubility and oral availability

Topical, IV, Oral- not absorbed well orally

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7
Q

Acyclovir MOR

A

viral TK or viral DNA polymerase mutation

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8
Q

Acyclovir t1/2

A

3 hr- short half life

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9
Q

Acyclovir AE

A

Acyclovir has poor solubility, ensure adequate hydration to prevent crystalluria

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10
Q

Valcyclovir- Structure

A

Ester of Acyclovir

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11
Q

Valcyclovir advantages

A

Increased water solubility increases bioavailability

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12
Q

Penciclovir Advantage

A

increases oral bioavailability, prolonged intracellular half life

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13
Q

Pencilovir Chain termination

A

Not an obligate chain terminator

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14
Q

Famciclovir Structure

A

Ester of Penciclovir

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15
Q

Famcilovir Advantage

A

More water soluble & Inc half life

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16
Q

Cidofovir structure

A

Nuleotide analog of Cytidine Monophosphate

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17
Q

Cidofovir activation

A

independent of the virus

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18
Q

Cidofovir MOA

A

viral DNA polymerase inhibitor –> chain termination

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19
Q

CIdofovir- Admin

A

IV

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20
Q

Cidofovir- Uses

A

Resistant HHV1,2,3 and CMV (HHV5)

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21
Q

Cidofovir AE

A

dose limiting renal toxicity ensure is pre hydrated with IV saline

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22
Q

Cidofovir + Probenacid

A

Give probenacid to dec renal elimination of Cidofovir

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23
Q

Foscarnet Structure

A

Pyrophosphate analog

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24
Q

Foscarnet MOA

A

binds to pyrophosphate binding site of viral DNA pol –> inhibits it

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25
Q

Foscarnet AE

A

renal toxicity, prevent via hydration

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26
Q

Foscarnet resistance

A

mutation in viral DNA polymerase

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27
Q

Vidarabine Structure

A

Adenosine analog

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28
Q

Vidarabine MOA

A

viral TK coverts it to Ara- MP –> Ara- ATP inhibits viral DNA pol BUT NOT A CHAIN TERMINATOR

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29
Q

VIdarabine MOR

A

mutation in viral DNA pol

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30
Q

Vidarabine uses

A

Topical treatment for herpes keratitis. Limited systemic value b/c of metabolic inactivation and high toxicity

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31
Q

Tx for CMV

A

Cidofovir, Ganciclovir, Valganciclovir

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32
Q

Ganciclovir structure

A

similar to acyclovir but altered to be an inhibitor of UL97

33
Q

Ganciclovir Features

A

Poor oral bioavailability

34
Q

Ganciclovir AE

A

myelosuppresion that is potentiated when given with Zidovudine (AZT)

35
Q

Gancilovir Resistance

A

UL97 or DNA polymerase mutation

36
Q

Valgancilovir structure

A

Ester of Ganciclovir

37
Q

Valganciclovir advantages

A

Increased bioavailability compared to Ganciclovir

38
Q

HBV Tx 1st line, 2nd line

A

1st line- Lamivudine, IFN alpha

2nd line- Adefovir

39
Q

Lamivudine structure

A

Cytidine analog

40
Q

Lamivudine MOA

A

NRTI + chain terminator

41
Q

Lamivudine AE

A

fairly non toxic

42
Q

Lamivudine resistance

A

rapid and common

43
Q

Adefovir Structure

A

AMP nucleotide

44
Q

Adefovir MOA

A

nucletoide RTI

45
Q

Adefovir use

A

alternative CMV tx if resistant to lamivudine

46
Q

Adefovir resistance

A

None up to 1 yr

47
Q

Adefovir AE

A

Dose limiting renal toxicity

48
Q

IFN alpa MOA

A

immune cytokine that activates non selective immunity (macrophages and NK cells) and stops replication in virally infected cells

49
Q

IFN alpha AE

A

Feel sick- fever, flu like, injection site reactions. Bone marrow suppression

50
Q

IFN alpha CI

A

autoimmune disease, hepatic decompensation

51
Q

HCV tx- 1st line, 2nd line

A

1st line- IFN alpha

2nd line- add Ribavirin

52
Q

IFN alpha in HCV

A

prophylaxis and chronic infection

53
Q

Ribavirin use only with?

A

IFN alpha

54
Q

Ribavirin structure

A

guanidine/ adenosine dual analog

55
Q

Ribarvirin MOA

A

inserts itself into mRNA and causes hypermutation NOT A CHAIN TERMINATOR

56
Q

Ribavirin admin

A

oral

57
Q

Ribavirin elim

A

renal

58
Q

Ribavirin AE

A

dose limiting renal toxicity b/c stored in RBC for entire 90 day life span

59
Q

Ribavirin CI

A

Pregnancy

60
Q

Influenza A tx- 1st line, 2nd line

A

1st line- Oseltamivir

2nd line- zanamivir, amantadine, rimantadine

61
Q

Amantadine MOA

A

M2 blocker

62
Q

Amantadine uses

A

only prophylactic and treatment of suspected influenza A infection

63
Q

Amantadine resistance

A

frequent but strain dependent

64
Q

Amantadine AE

A

Crosses BBB and is dopaminergic- agitation, hallucination, cardiac arrhythmias, death if OD

65
Q

Rimantadine MOA

A

M2 inhibitor

66
Q

Rimantadine uses

A

prophylaxis and Tx and influenza A infection

67
Q

Rimantadine AE

A

GI, but less BBB penetration than amantadine so less CNS side effects

68
Q

Oseltamavir Name

A

Tamiflu

69
Q

Oseltanavir MOA

A

Sialic acid analog that blocks neurominidase for prophylaxis and early tx

70
Q

Oseltanavir resistance

A

high

71
Q

Oseltanavir uses

A

Influenza A and B

72
Q

Zanamavir MOA

A

sialic acid analog that blocks neuriminidase for propyxlaxis and early tx

73
Q

Zanamavir admin

A

Nasal

74
Q

Zanamavir AE

A

respiratory toxicity- bronchospasm

75
Q

Zanamvir CI

A

Pulmonary disease

76
Q

Influenza B tx

A

oseltamavir and zanamavir

77
Q

Acylovir, Valacyclovir, Penciclovir, Famicilovir- MOA

A

Nucleoside activated by viral TYR kinase, inhibit viral DNA pol–> chain termination

78
Q

Valganciclovir Toxicity

A

Same as Gancilovir- myelosuppression potentiated by Zidovudine

79
Q

Lamivudine uses

A

Also used for HAART