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Flashcards in Antivirals Deck (79)
1

HSV/ VZV- correspond to what HHVs

1,2,3

2

First line Tx for HSV, VZV

Acylovir, Valacyclovir, Penciclovir, Famicilovir

3

Alternative Tx for HSV and VZV

Cidofovir, Foscarnet, Vidarabine

4

Acyclovir- Drug class

Nucleoside analog

5

Acyclovir- MOA

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

6

Acyclovir- Features

High selectivity, poor solubility and oral availability
Topical, IV, Oral- not absorbed well orally

7

Acyclovir MOR

viral TK or viral DNA polymerase mutation

8

Acyclovir t1/2

3 hr- short half life

9

Acyclovir AE

Acyclovir has poor solubility, ensure adequate hydration to prevent crystalluria

10

Valcyclovir- Structure

Ester of Acyclovir

11

Valcyclovir advantages

Increased water solubility increases bioavailability

12

Penciclovir Advantage

increases oral bioavailability, prolonged intracellular half life

13

Pencilovir Chain termination

Not an obligate chain terminator

14

Famciclovir Structure

Ester of Penciclovir

15

Famcilovir Advantage

More water soluble & Inc half life

16

Cidofovir structure

Nuleotide analog of Cytidine Monophosphate

17

Cidofovir activation

independent of the virus

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Cidofovir MOA

viral DNA polymerase inhibitor --> chain termination

19

CIdofovir- Admin

IV

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Cidofovir- Uses

Resistant HHV1,2,3 and CMV (HHV5)

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Cidofovir AE

dose limiting renal toxicity ensure is pre hydrated with IV saline

22

Cidofovir + Probenacid

Give probenacid to dec renal elimination of Cidofovir

23

Foscarnet Structure

Pyrophosphate analog

24

Foscarnet MOA

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

25

Foscarnet AE

renal toxicity, prevent via hydration

26

Foscarnet resistance

mutation in viral DNA polymerase

27

Vidarabine Structure

Adenosine analog

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Vidarabine MOA

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

29

VIdarabine MOR

mutation in viral DNA pol

30

Vidarabine uses

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

31

Tx for CMV

Cidofovir, Ganciclovir, Valganciclovir

32

Ganciclovir structure

similar to acyclovir but altered to be an inhibitor of UL97

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Ganciclovir Features

Poor oral bioavailability

34

Ganciclovir AE

myelosuppresion that is potentiated when given with Zidovudine (AZT)

35

Gancilovir Resistance

UL97 or DNA polymerase mutation

36

Valgancilovir structure

Ester of Ganciclovir

37

Valganciclovir advantages

Increased bioavailability compared to Ganciclovir

38

HBV Tx 1st line, 2nd line

1st line- Lamivudine, IFN alpha
2nd line- Adefovir

39

Lamivudine structure

Cytidine analog

40

Lamivudine MOA

NRTI + chain terminator

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Lamivudine AE

fairly non toxic

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Lamivudine resistance

rapid and common

43

Adefovir Structure

AMP nucleotide

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Adefovir MOA

nucletoide RTI

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Adefovir use

alternative CMV tx if resistant to lamivudine

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Adefovir resistance

None up to 1 yr

47

Adefovir AE

Dose limiting renal toxicity

48

IFN alpa MOA

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

49

IFN alpha AE

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

50

IFN alpha CI

autoimmune disease, hepatic decompensation

51

HCV tx- 1st line, 2nd line

1st line- IFN alpha
2nd line- add Ribavirin

52

IFN alpha in HCV

prophylaxis and chronic infection

53

Ribavirin use only with?

IFN alpha

54

Ribavirin structure

guanidine/ adenosine dual analog

55

Ribarvirin MOA

inserts itself into mRNA and causes hypermutation NOT A CHAIN TERMINATOR

56

Ribavirin admin

oral

57

Ribavirin elim

renal

58

Ribavirin AE

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

59

Ribavirin CI

Pregnancy

60

Influenza A tx- 1st line, 2nd line

1st line- Oseltamivir
2nd line- zanamivir, amantadine, rimantadine

61

Amantadine MOA

M2 blocker

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Amantadine uses

only prophylactic and treatment of suspected influenza A infection

63

Amantadine resistance

frequent but strain dependent

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Amantadine AE

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

65

Rimantadine MOA

M2 inhibitor

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Rimantadine uses

prophylaxis and Tx and influenza A infection

67

Rimantadine AE

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

68

Oseltamavir Name

Tamiflu

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Oseltanavir MOA

Sialic acid analog that blocks neurominidase for prophylaxis and early tx

70

Oseltanavir resistance

high

71

Oseltanavir uses

Influenza A and B

72

Zanamavir MOA

sialic acid analog that blocks neuriminidase for propyxlaxis and early tx

73

Zanamavir admin

Nasal

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Zanamavir AE

respiratory toxicity- bronchospasm

75

Zanamvir CI

Pulmonary disease

76

Influenza B tx

oseltamavir and zanamavir

77

Acylovir, Valacyclovir, Penciclovir, Famicilovir- MOA

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

78

Valganciclovir Toxicity

Same as Gancilovir- myelosuppression potentiated by Zidovudine

79

Lamivudine uses

Also used for HAART