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PHARM 2 > Antivirals > Flashcards

Antivirals Flashcards

1
Q

Tx of respiratory viral infections

A

neuraminidase inhibitors
inhibitors of viral uncoating
synthetic guanosine analog

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2
Q

oseltamivir

A

neuraminidase inhib

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3
Q

zanamivir

A

neuraminidase inhib

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4
Q

amantadine

A

inhibts viral uncoating

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5
Q

rimantadine

A

inhibitors of viral uncoating

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6
Q

ribavirin

A

synthetic guanosine analog

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7
Q

neuraminidase inhibitors

A

oseltamivir, zanamivir

work against type A and B influenza - prophylaxis OR after onset of sxs

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8
Q

neuraminidase inhib MOA

A

neuraminidase cleaves hemaglutinin residues from surface receptors - allows cleavage and budding of virus

–> INHIBITION of virion release d/t halted viral replication

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9
Q

olsetamivir vs zanamivir

A

olsetamivir: ORAL - hydrolyzed in liver
zanamivir: INHALE or INTRANASAL - less bioavail`

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10
Q

zanamivir AE

A

airway irritation - avoid in pt with asthma and COPD

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11
Q

Ion channel blockers

A

amantadine, rimantadine

only active on influenza type A
- not recommended as first line tx anymore b/c resistance

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12
Q

ion channel blocker MOA

A

blocks viral membrane protein - M2 (H+ channel)

- channel needed for fusion of viral with cell membrane to endosome

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13
Q

amantadine vs rimantadatine? which crosses BBB

A

amantadine = crosses BBB
- excreted in urine

greater AE with amantadine

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14
Q

ion channel blockers contraindications

A

pregnancy

nursing

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15
Q

ribavarin use

A

active against RNA/DNA viruses - broad spec

used in combo with IFN-alpha or HCV tx

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16
Q

ribavarin MOA

A

convert to ribavirin - triphosphate = inhibits GTP formation - no viral mRNA capping

inhib RNA dep RNA polym = inhib of protein synthesiss

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17
Q

ribavarin AE

A

dose dependent transient anemia
GI
CNS

PREGNANCY X - teratogen, can also affect those nearby, doesn’t need to be ingested by only 1 person

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18
Q

hepatic viral infection tx

A

1) IFN-alpha
2) nucleotide analog
3) protease inhibitors

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19
Q

ifn alpha

A

glycoproteins/cytokines - alpha and beta produced by many cell types

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20
Q

IFN-a MOA

A

naturally occuring

an be peglyated

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21
Q

nucleoside analogs

A

lamiduvidne

entecavir

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22
Q

lamidvudine

A

protect against hep B and HIV - in triphosphate form

monophosph form = incorporated into DNA (via HBV polymerase) – chain termination

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23
Q

entecarvir use

A

effective against lamivudine resistant HBV and HIV strains

phosphorylated form = competes for viral polymerase - inhibitiors blocks reverse transcriptase

STOPS ASSEMBLY and maturation

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24
Q

entecavir AE

A

monitor after discontinuation for severe hepatitis exacerbation

25
Q

Protease inhibitors

A

boceprevir
telaprevir

tx HCV in pt previously failed tx with IFN-a and ribavarin
- given in combo with IFN-a and ribavrin

26
Q

boceprevir

A

protease inhib

27
Q

telaprevir

A

protease inhib

28
Q

protease inhib MOA

A

binds reversibly to nonstructural protein 3 - serine protease and inhibts replication of HCV

29
Q

protease inhib AE

A

fatigue
anemia
nausea
dysgeusia

30
Q

Herpes Tx

A

purine/pyrimidine analogs
foscarnet

inhibition of RNA and DNA synthesis

31
Q

Acyclovir

A

active against HSV1 and 2, VZV, HSV4

prophylactic in immunocompromised transplant pt

CMV is resistant (Doesn’t encode thymidine kinase)

32
Q

DOC in HSV encephalitis

A

acyclovir

33
Q

prodrug of acyclovir

A

valacyclovir

34
Q

acyclovir MOA

A

3 phosphorylation steps

monophosph by herpes virus encoded thymidine kinase

host completes phosphorylation to di and triphosph

competes with dGTP = once incorporation – chain terminates - inhib of viral DNA polym

35
Q

acyclovir resistance

A

no cross resistance

1) deficient thymdine kinases
2) altered viral DNA pol - dec affinity for acyclovir

36
Q

which has greater oral bioavailbility, ayclovir or valacyclovir

A

valacyclovir

37
Q

acyclovir AE

A

topical admin = irritation locally

oral = HA, n/v/d

IV: renal failure - minimize with slow infusion and prior hydration

38
Q

DOC for CMV retinitis and prophylaxis

A

ganciclovir

39
Q

ganciclovir

A

prodrug - valganciclovir (greater oral bioavail)

aycclovir analog - but has more acitivity against CMV

40
Q

ganciclovir MOA

A

phosphorylated by viral (UL97) and cell kinases

DNA chain terminator and DAN pol inhib

41
Q

ganciclovir resistance

A

dec intracellular phosphorylation

mutations to phosphotransferase

42
Q

ganciclovir excretion

A

urine

43
Q

ganciclovir AE

A

myelosuppresion
dose dependent neutropenia

CONTRAINDIC in PREGNANCY

44
Q

cidofovir

A

CMV induced retinitis in HIV/AIDS

NOT phoshporylated by viral kinases

requires activ by host cell kinases

active against HSV and ganciclovir resis HSV

45
Q

cidofovir MOA

A

DNA chain terminator and DNA pol inhib

46
Q

cidofovoir resistance

A

viral DNA pol mutations

47
Q

cidofovir AE

A

nephrotoxicity

48
Q

penciclovir

A

HSV1, 2 and VZV use

topical tx of HSV (cold sores)

49
Q

penciclovir MOA

A

monophosphorylated by viral thymidine kinase

further phosph –> triphosphate form

Inhibits HSV DNA pol/chain temrinator

50
Q

penciclovir AE

A

mild erythema

51
Q

Trifluridine

A

active against HSV 1 and 2, vaccina virus

52
Q

DOC HSV keratoconjunctivitis and reccurent epithelial keratitis

A

trifluridine

53
Q

trifluridine MOA

A

triphosph form incorportated into viral DNA = fragmentation

54
Q

trifluridine PK

A

short t 1/2 - reapply frequently

55
Q

foscarnet

A

analog of inorganic pyrophosphate

NO phosphorylation required

56
Q

Tx

  • CMV retinitis in immunocompromised
  • aycylovir resistant HSV
  • CMV retinitis
  • ganciclovir resistant CMV and VZV
A

foscarnet

57
Q

foscarnet MOA

A

analog of anion pyrophosphate - selectively inhibits pyrophosphate binding site on viral DNA pol

58
Q

foscarnet AE

A

nephrotoxicity
electrolyte disturbances: Ca, Mg, K, PO4
CNS - hallucinations, seizures, HA

PHARM 2 (18 decks)

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