54: Antiviral Drugs Flashcards

1
Q

productive =

clinically silent =

A

lytic
latent

only the lytic stage is suppressed by antivirals, so treatment goals are to speed time to healing and increase time between outbreaks

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2
Q

the herpesvirus diseases are…

A

herpes simplex 1 and 2
varicella zoster virus
cytomegalovirus

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3
Q

MOA acyclovir

A

nucleoside analogue that requires initial phosphorylation by the viral thymidine kinase enzyme

competitive inhibitor of viral DNA pol –> chain termination upon incorporation into viral DNA

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4
Q

acyclovir resistance

A

mutation of thymidine kinase gene required for activation

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5
Q

indications for acyclovir

A

oral = genital herpes, varicella zoster

IV = severe or disseminated mucocutaneous disease, neonate infections, HSV encephalitis, VZV in immunocompromised pts

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6
Q

adverse effects acyclovir

A

nausea, headache, diarrhea

reversible crystalline nephrotoxicity with neurological effects –> caution when administered concurrently with nephrotoxic agents

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7
Q

prodrug of acyclovir

A

metabolizes to acyclovir in liver and intestines –> greater oral bioavailability

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8
Q

therapeutic indications for valacyclovir

A

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

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9
Q

MOA foscarnet

A

occupies the site when pyrophosphate normally resides and blocks pyrophosphate release –> blocks catalytic cycle

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10
Q

foscarnet _______ prior phosphorlyation by thymidine kinase in order to act

A

does not require *

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11
Q

indications for foscarnet

A

*only IV

HSV and VZV infections that are resistant to acyclovir

CMV retinitis, CMV colitis, CMZ esophagitis

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12
Q

adverse effect foscarnet

A

renal impairment –> avoid concurrent admin of drugs with nephrotoxicity

also changes in Ca, Ph, K, or Mg levels

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13
Q

MOA ganciclovir

A

acyclic guanosine analogue that requires initial phosphorylation by viral kinase enzyme

competitive inhibitor of viral DNA pol –> chain termination upon incorporation into viral DNA

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14
Q

which is more active against CMV- ganciclovir or acyclovir?

A

ganciclovir

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15
Q

therapeutic indications ganciclovir

A

IV - CMV retinitis and CMV colitis, pneumonitis, and esophagitis

IV followed by oral - reduce risk of CMV disease in transplant recipients

intraocular injection or implant - CMV retinitis

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16
Q

adverse effect ganciclovir

A

myelosuppression

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17
Q

prodrug of ganciclovir

A

valganciclovir

metabolized into ganciclovir in liver and intestines –> higher oral bioavailability

18
Q

therapeutiv indications valganciclovir

A

CMV retinitis

prevention of CMV disease in pts with heart, kidney and kidney-pancreas transplants

19
Q

MOA trifluridine

A

phosphorylated by cellular enzymes

competitive inhibitor of thymidine for incorporation into newly synthesized genomes

20
Q

therapeutic indications for trifluridine

A

not systemic

ocular admin to treat keratoconjunctivitis and recurrent epithelial keratitis due to HSV-1 and HSV-2

21
Q

MOA tamiflu

A

sialic acid analogue that is metabolized to active compound by hepatic esterases

binds to active site of neuraminidse to inhibit its function. inhibits spread of progeny virion sthrough respiratory tract

22
Q

indications for oseltamivir

A

flu A and B virus within 48 hrs

23
Q

MOA zanamivir

A

sialic acid analogue with same MOA as oseltamivi r

24
Q

administration zanmivir

A

oropharynx and lungs by inhalation

25
Q

contraindications for zanmivir

A

pre-existing pulmonary disease

only approved 7yo and up

26
Q

MOA peramvir

A

neuraminidase inhibitor administered IV

27
Q

MOA amantadine and rimantadine

A

symmetric tricyclic amines that inhibit the activity of FLU A M2 PRTN (ion channels forming prtn requried for nucleocapsid release)

28
Q

most common cause bronchiolitis and pneumonia in children under 1 yr

A

RSV

common cold in adults and older children

29
Q

treatment for severe LRT illness in premees, immunocompromised, chronic lung or heart disease

A

ribavirin

30
Q

MOA ribavirin

A

guanosine analogue that is phosphorylated by cellular adenosine kinase. interferes with synthesis of guanosine triphosphate, inhibit viral mRNA cappin, inhibits RdRp of RSV and hep C virus

aerosol route for RSV treatment, orally as part of combo for hep C

31
Q

therapeutic indications for ribavirin

A

aerosolized for severe respiratory illness due to RSV in certain populations

oral with pegylated interferon and other hcv inhibitors for chronic hep C infections

32
Q

adverse effects and contraindications ribavirin

A

hemolytic anemia

pregnancy and anemia contra

33
Q

which hep C genotype is less responsive to treatment?

A

genotype 1

hep C is transmitted through percutaneous exposure, contaminated blood exposure and sexual transmission

34
Q

hep C –>

A

chronic hepatitis

35
Q

MOA paritaprevir

A

HCV protease inhibitor (HCV NS3/4A - necessary for cleavage of immature viral polypeptides into mature)

36
Q

MOA simeprevir

A

HCV protease inhibitor (NS3/4A)

37
Q

what do you need to check before simeprevir use?

A

screen pts for presence of NS3 Q80K polymorphism (reduces response)

38
Q

MOA ledipasvir

A

nucleoside analogue HCV Ns5VA inhibitor - necessary for viral RNA replication and virion assembly

used orally in combo with sofosbuvir

39
Q

MOA ombitasvir

A

HCV Ns5A inhibitor

used in combo orally with paritaprevir and ritonavir

40
Q

MOA sofosbuvir

A

nucleotide analogue prodrug that is incorporated into newly synthesized RNA by RNA pol –> premature chain termination

41
Q

bad drug mixes with sofosbuvir

A

rifampin, st. johns wort

lead to significantly reduced plasma concentration of drug

42
Q

MOA dasbuvir

A

non-nucleoside inhibitor of RNA dependent RNA pol – causes viral life cycle to halt before synthesis of RNA genome

orally used with ombitasvir, paritaprevir, and ritonavir