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Year 2 Pharmacology > Antiviral drugs > Flashcards

Antiviral drugs Flashcards

1
Q

antiviral treatments for herpesviruses are indicated for which members of the herpresvirus family?

A

VZV
HSV-1
HSV-2
CMV

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2
Q

what type of drug is acyclovir?

A

nucleoside analogue

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3
Q

what is the MOA of acyclovir?

A

competitive inhibitor of the viral genome DNA pol

chain termination upon incorporation into viral DNA

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4
Q

what is required for acyclovir MOA?

A

phosphorylation of viral thymidine kinase enzyme

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5
Q

what is the bioavailability of acyclovir?

A

low

15-20%

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6
Q

what are the indications of acyclovir?

A

oral - genital herpes, varicella zoster

IV - neonate infections, severe disseminated mucocutaneous disease, HSV encephalitis, VZV in compromised patients

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7
Q

what are the adverse effects of acyclovir?

A

nausea, headache, diarrhea

crystalline nephrotoxicity

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8
Q

acyclovir use is cautioned in what condition?

A

concomitant adminstration of nephrotoxic agents

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9
Q

what is valacyclovir?

A

prodrug of acyclovir

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10
Q

what is the advantage of valacyclovir?

A

3-5x greater oral bioavailability

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11
Q

what are the therapeutic indications for valacylcovir?

A

primary and recurrent genital herpes
varicella in older children and adults
zoster
orolabial herpes

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12
Q

what type of drug is foscarnet?

A

analogue of pyrophosphate

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13
Q

what is the MOA of foscarnet?

A

occupies site where pyrophosphate normally resides and blocks pyrophosphate release - blocks catalytic cycle

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14
Q

does foscarnet require prior phosphorylation by thymidine kinase?

A

no

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15
Q

what is the route of administration for foscarnet?

A

IV only

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16
Q

what are the indications for foscarnet?

A

HSV and VZV resistance (to acyclovir)

CMV retinitis, CMV colitis, CMV esophagitis

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17
Q

what are the adverse effects of foscarnet?

A

renal impairment

blood chem - changes Ca, P, Mg levels

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18
Q

foscarnet use is cautioned in what condition?

A

concurrent administration of nephrotoxic drugs

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19
Q

what type of drug is ganciclovir?

A

acyclic guanosine analogue

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20
Q

what is the MOA of ganciclovir?

A

competitive inhibitor viral DNA pol

chain termination upon incorporation into viral DNA

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21
Q

does ganciclovir require prior phosphorylation by viral kinase?

A

yes

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22
Q

what are the therapeutic indications for ganciclovir?

A

CMV retinitis / colitis / pneumonitis / esophagitis

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23
Q

what are the adverse effects of ganciclovir?

A

myelosuppression
bone marrow / CNS toxicity
phlebitis / rash / anemia / fever

24
Q

what type of drug is valganciclovir?

A

prodrug of ganciclovir

25
Q

what are the therapeutic indications for valganciclovir?

A

CMV retinitis

prevention of CMV disease post-transplantation

26
Q

what type of drug is trifluridine?

A

fluorinated nucleoside

27
Q

what is the MOA of trifluridine?

A

competitive inhibitor of thymidine for incorporation into newly synthesized genomes

28
Q

does trifluridine require prior phosphorylation for activation?

A

yes

29
Q

what type of drug is oseltamivir?

A

sialic acid analogue

30
Q

what is the MOA of oseltamivir?

A

binds to active site of neuraminidase to inhibit its function

inhibits spread of progeny virions through the respiratory tract

31
Q

what is the bioavailability of oseltamivir?

A

80%

32
Q

what is the MOR of oseltamivir?

A

point mutations in H and N genes

33
Q

what are the therapeutic indications for oseltamivir?

A

influenza A and B

children 1 yo and older

34
Q

what type of drug is zanamivir?

A

sialic acid analogue

35
Q

what is the MOA of zanamivir?

A

same as oseltamivir

binds to active site of neuraminidase to inhibit its function

inhibits spread of progeny virions through the respiratory tract

36
Q

how is zanamivir administered?

A

inhalation

37
Q

what are the therapeutic indications for zanamivir?

A

influenza A and B

children 7 yo and older

38
Q

what type of drug is peramivir?

A

neuraminidase inhibitor

39
Q

what are the therapeutic indications for peramivir?

A

acute uncomplicated flu in patients who have been symptomatic for no more than 48 hours

40
Q

what type of drugs are amantadine and rimantadine?

A

symmetric tricyclic amines

41
Q

what is the MOA of amantadine and rimantadine?

A

inhibits activity of INFLUENZA A M2 protein - ion channel forming protein required for nucleocapsid release

42
Q

what are the therapeutic indications for amantadine and rimantadine?

A

flu within 48 hours to shorten duration

43
Q

what is the most common cause of bronchiolitis and pneumonia in children under 1 year?

A

respiratory syncytial virus (RSV)

44
Q

when is ribavirin treatment indicated?

A

premature infants
immunocompromised
patients with chronic lung or congenital heart disease

45
Q

what type of drug is ribavirin?

A

guanosine analogue

46
Q

what is the MOA of ribavirin?

A

interferes with synthesis of GTP
inhibits viral mRNA capping
inhibits RdRp of RSV and hep C virus

47
Q

what is the major adverse effects of ribavirin?

A

hemolytic anemia

48
Q

what are the contraindications for ribavirin?

A

pregnancy
anemia
ischemic vascular disease
renal disease

49
Q

what are the protease inhibitors of HCV?

A

paritaprevir

simprevir

50
Q

what is the MOA of paritaprevir and simprevir?

A

protease inhibitors

51
Q

what are the NS5A inhibitors of HCV?

A

ledipasivir

omvitasivir

52
Q

what is the MOA of ledipasivir and omvitasivir?

A

HCV NS5A inhibitors

53
Q

what are the RNA polymerase inhibitors for HCV?

A

sofosbuvir

dasabuvir

54
Q

what is the MOA of sofosbuvir and dasabuvir for HCV?

A

RNA polymerase inhibitors

55
Q

what needs to be screened for prior to simepravir use? why?

A

NS3 Q80K polymorphism

resistance

56
Q

what is unique about dasabuvir MOA?

A

non-nucleoside inhibitor of the RNA-dependent RNA pol

Year 2 Pharmacology (70 decks)

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