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
what are the therapeutic indications for valganciclovir?
CMV retinitis | prevention of CMV disease post-transplantation
26
what type of drug is trifluridine?
fluorinated nucleoside
27
what is the MOA of trifluridine?
competitive inhibitor of thymidine for incorporation into newly synthesized genomes
28
does trifluridine require prior phosphorylation for activation?
yes
29
what type of drug is oseltamivir?
sialic acid analogue
30
what is the MOA of oseltamivir?
binds to active site of neuraminidase to inhibit its function inhibits spread of progeny virions through the respiratory tract
31
what is the bioavailability of oseltamivir?
80%
32
what is the MOR of oseltamivir?
point mutations in H and N genes
33
what are the therapeutic indications for oseltamivir?
influenza A and B | children 1 yo and older
34
what type of drug is zanamivir?
sialic acid analogue
35
what is the MOA of zanamivir?
same as oseltamivir binds to active site of neuraminidase to inhibit its function inhibits spread of progeny virions through the respiratory tract
36
how is zanamivir administered?
inhalation
37
what are the therapeutic indications for zanamivir?
influenza A and B | children 7 yo and older
38
what type of drug is peramivir?
neuraminidase inhibitor
39
what are the therapeutic indications for peramivir?
acute uncomplicated flu in patients who have been symptomatic for no more than 48 hours
40
what type of drugs are amantadine and rimantadine?
symmetric tricyclic amines
41
what is the MOA of amantadine and rimantadine?
inhibits activity of INFLUENZA A M2 protein - ion channel forming protein required for nucleocapsid release
42
what are the therapeutic indications for amantadine and rimantadine?
flu within 48 hours to shorten duration
43
what is the most common cause of bronchiolitis and pneumonia in children under 1 year?
respiratory syncytial virus (RSV)
44
when is ribavirin treatment indicated?
premature infants immunocompromised patients with chronic lung or congenital heart disease
45
what type of drug is ribavirin?
guanosine analogue
46
what is the MOA of ribavirin?
interferes with synthesis of GTP inhibits viral mRNA capping inhibits RdRp of RSV and hep C virus
47
what is the major adverse effects of ribavirin?
hemolytic anemia
48
what are the contraindications for ribavirin?
pregnancy anemia ischemic vascular disease renal disease
49
what are the protease inhibitors of HCV?
paritaprevir | simprevir
50
what is the MOA of paritaprevir and simprevir?
protease inhibitors
51
what are the NS5A inhibitors of HCV?
ledipasivir | omvitasivir
52
what is the MOA of ledipasivir and omvitasivir?
HCV NS5A inhibitors
53
what are the RNA polymerase inhibitors for HCV?
sofosbuvir | dasabuvir
54
what is the MOA of sofosbuvir and dasabuvir for HCV?
RNA polymerase inhibitors
55
what needs to be screened for prior to simepravir use? why?
NS3 Q80K polymorphism resistance
56
what is unique about dasabuvir MOA?
non-nucleoside inhibitor of the RNA-dependent RNA pol