antiviral pharmacology/medchem

Question 1

immune globulin use

Answer 1

acute, serious infections
post exposure prophylaxis
used with nucleoside antiviral

Question 2

herpes genome

Answer 2

dsDNA

Question 3

influenza genome

Answer 3

(-) ssRNA

Question 4

viruses that use host polymerase

Answer 4

DNA viruses
herpes (human and simplex)
varicella
epstein-barr
CMV

Question 5

acyclovir MoA

Answer 5

guanosine analog prodrug

terminates DNA chain synthesis

Question 6

what converts acyclovir to active drug

Answer 6

• viral thymidine kinase does first phosphorylation

- guanosine monophosphate kinase does rest

Question 7

resistance mechanisms to acyclovir and valacyclovir

Answer 7

• deficient thymidine kinase
• altered thymidine kinase
• altered DNA polymerase

Question 8

gancyclovir activity against

Answer 8

CMV
HSV
VZV
HHV

Question 9

ganciclovir toxicity

Answer 9

high because its less specific to viral thymidine kinase

-potential for bone marrow toxicity

Question 10

famciclovir features

Answer 10

• prodrug of penciclovir which increases bioavailability

- similar to acyclovir but longer duration

Question 11

cidofovir MoA

Answer 11

cytosine analog that inhibits DNA synthesis

No viral TK needed

Question 12

cidofovir dose limiting toxicity

Answer 12

nephrotoxicity

Question 13

cidofovir route

Answer 13

IV only due to poor bioavailability

Question 14

foscarnet MoA

Answer 14

inhibits DNA polymerase by blocking nucleotide binding, with no need of triphosphate (thus TK) like acyclovir and others

Question 15

foscarnet side effects

Answer 15

headache
tremor
seizures
hallucinations
*all due to chelation of calcium*

Question 16

foscarnet dose limiting toxicity

Answer 16

nephrotoxicity

hypocalcemia

Question 17

foscarnet route

Answer 17

IV only

Question 18

idoxuridine and trifluridine (thymidine analogs) MoA

Answer 18

is phosphorylated then inhibits DNA synthesis by inhibiting thymidylic phosphorylase

Question 19

fomivirsen use

Answer 19

CMV retinitis

Question 20

fomivirsen MoA

Answer 20

inhibits replication through specific and nonspecific mechanisms like virus binding

Question 21

fomivirsen route

Answer 21

eye injection (intravitreal)

Question 22

docosanol use

Answer 22

cold sores

Question 23

imiquimod use

Answer 23

HPV infections

Question 24

imiquimod MoA

Answer 24

not fully understood, does induce secretion of pro-inflammatory cytokines

Question 25

influenza strain that causes pandemics

Answer 25

A only

Question 26

influenza nomenclature

Answer 26

H (hemagglutinin - 16 subtypes) | N (neuraminidase - 9 subtypes)

Question 27

neuraminidase inhibitor drugs

Answer 27

zanamivir | oseltamivir (prodrug)

Question 28

neuraminidase inhibitor MoA

Answer 28

inhibits cleavage of sialic acid and the release of virus from the infected cell

Question 29

neuraminidase inhibitor adverse effects

Answer 29

bronchospasm unusual psychiatric behavior d/n Uncommon though

Question 30

viral uncoating inhibitor use

Answer 30

influenza A

Question 31

viral uncoating inhibitor drugs

Answer 31

amantadine | rimantadine

Question 32

viral uncoating inhibitor MoA

Answer 32

inhibits M2 ion channel in flu virus and uncoating of virus in endosome

Question 33

viral uncoating inhibitors adverse effects

Answer 33

GI and CNS

Question 34

hepatitis C genome

Answer 34

(+) ssRNA

Question 35

hepatitis B genome

Answer 35

dsDNA-RT

Question 36

hepatitis strain with no vaccine

Answer 36

C

Question 37

hep A transmission

Answer 37

fecal-oral

Question 38

hep C transmission

Answer 38

injection drug use | blood exposure

Question 39

interferon use

Answer 39

in combination with ribavirin for hep C | not very useful however

Question 40

ribavirin use

Answer 40

combo therapy for hep C

Question 41

ribavirin MoA

Answer 41

- inhibits capping of 5' end of mRNA | - inhibits inosine monophosphate deyhdrogenase in DNA production

Question 42

ribavirin adverse effects

Answer 42

- hemolytic anemia - bone marrow suppression - possibly teratogenic

Question 43

NS5A inhibitor MoA

Answer 43

inhibits the scaffolding protein that allows for the building of complex protein structures for use in the hep C virus

Question 44

NS5A (replication complex) inhibitor drugs

Answer 44

``` daclatasvir velpastasvir pibrentasvir elbasvir ledipasvir ```

Question 45

NS5A inhibitor adverse effects

Answer 45

headache fatigue nausea

Question 46

HCV protease (NS3/A4) inhibitor drugs

Answer 46

glecaprevir paritaprevir grazoprevir

Question 47

HCV protease inhibitor adverse effects

Answer 47

anemia | skin rashes

Question 48

HCV polymerase (NS5B) inhibitors

Answer 48

sofosbuvir

Question 49

HCV polymerase inhibitor drug interaction

Answer 49

serious bradycardia with amiodarone

Question 50

hep B transmission

Answer 50

contact with blood or body fluids of infected person

Question 51

unique DNA construct for hep B

Answer 51

covalently closed circular DNA (cccDNA)

Question 52

HIV drugs used for hepatitis (NI inhibitors)

Answer 52

tenofovir | entecavir

Question 53

valacyclovir features

Answer 53

- great oral bioavailability | - cleaved to active drug by valacyclovirase before portal circulation

Question 54

idoxuridine and trifluridine toxicity

Answer 54

bone marrow toxicity | -not very specific for virus so we get a lot into our DNA

Question 55

which drugs have the phosphonate group

Answer 55

cytidine analogs cidofovir deoxycytidine

Question 56

why aren't adamantanse used much

Answer 56

near universal resistance

Question 57

hemagglutinin

Answer 57

influenza component that binds to human glycoprotein containing sialic acid

Question 58

NI inhibitors MoA

Answer 58

- compete with adenosine to cause chain termination | - prodrug

Question 59

HCV polymerase inhibitor (NS5B) MoA

Answer 59

inhibit nucleoside biosynthesis and mRNA capping

Question 60

HCV protease inhibitors MoA

Answer 60

bind non-covalently to serine in the active site