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Final D&D > Antiviral Agents > Flashcards

Antiviral Agents Flashcards

1
Q

Amantadine Rimantadine

Mechanism of Action ?

A

inhibit viral uncoating by block of viral M2 proton channel

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2
Q

Amantadine and Rimantidine

Pharmacokinetics?

A

good po, accumulates in lungs
renal [A] or hepatic [R]
elimination

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3
Q

Amantadine Rimantadine

Adverse Reactions?

A

GI upset insomnia, confusion, headache (decrease CNS effects with rimantadine)

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4
Q

Oseltamivir, Zanamivir, Peramivir

Mechanism of Action?

A

inhibit viral neuraminidase to decrease viral budding ( decrease infectivity)

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5
Q

Oseltamivir, Zanamivir, Peramivir

Pharmacokinetics?

A

oseltamivir (orally as prodrug)
zanamivir (inhalation)
peramivir (intravenous)
all renally excreted

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6
Q

Oseltamivir, Zanamivir, Peramivir

Adverse Reaction?

A

nausea/vomiting (oseltamivir)

bronchospasm (zanamivir)

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7
Q

Acyclovir[155] , Valacyclovir [113], Penciclovir, [Famciclovir]
Mechanism of Action?

A

phosphorylated by viral thymidine kinase  inhibits viral DNA polymerase plus chain termination

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8
Q 
Acyclovir[155]	,
Valacyclovir [113], 
Penciclovir,    
 [Famciclovir]	
Pharmacokinetics?
A

VAL / FAM: 80%(prodrugs),
P: topical only]
renal excretion

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9
Q

Acyclovir[155] , Valacyclovir [113], Penciclovir, [Famciclovir]
Adverse Reaction?

A 
minor toxicities (headache, n/v)
higher levels with valacyclovir may increase risk of CNS / renal side effects
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10
Q

Docosanol (OTC)

Mechanism of Action?

A

inhibits fusion between plasma membrane and HSV envelope

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11
Q

Docosanol (OTC)

Pharmacokinetics?

A

topically applied 5 X daily

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12
Q

Docosanol (OTC)

Adverse Reaction?

A

well tolerated

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13
Q

Cidofovir

Mechanism of Action?

A

nucleotide analog, phosphory lated to active form by host kinases, inhibits viral DNA poly

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14
Q

Cidofovir

Pharmacokinetics?

A

long intracellular t1/2 (17-35h) given IV weekly / biweekly

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15
Q

Cidofovir

Adverse Reaction?

A

nephrotoxicity (decreased

by probenecid use) rash in HIV patients

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16
Q

Foscarnet

Mechanism of Action?

A

pyrophosphate analog, (no activation step), inhibits viral/DNA/RNA polymerase and RT

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17
Q

Foscarnet

Pharmacokinetics?

A

poor oral bioavailability

requires continuous infusion

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18
Q

Foscarnet

Adverse Reaction?

A

renal impairment, severe n/v electrolyte imbalance (esp. hypocalcemia)

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19
Q

Ribavirin

Mechanism of Action?

A

triphosphorylated to active form inhibits IMP dehydrogenase,

viral RNA-dep RNA polymerase

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20
Q

Ribavirin

Pharmacokinetics?

A

aerosol administration
well-absorbed orally
long intracellular t1/2

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21
Q

Ribavirin

Adverse Reaction?

A

low aerosol toxicity, but teratogen,
systemic toxicity includes anemia,
bone marrow depression

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22
Q

Amphotericin

Mechanism of Action?

A

binds to ergosterol, forming pores in membranes with loss of vital intracellular constituents

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23
Q

Amphotericin

Pharmacokinetics?

A

IV or tropical only

Slow excretion by kidney plus hepato-biliary (t1/2 15d)

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24
Q

Amphotericin

Adverse Reaction?

A

acute: fever/chills on infusion

nephrotoxicity (80%), anemia

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25
Q

Nystatin

Mechanism of Action?

A

same as amphotericin

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26
Q

Nystatin

Pharmacokinetics?

A

topical only

not absorbed orally

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27
Q

Nystatin

Adverse Reaction?

A

well tolerated given topically

mild GI upset (if swallowed)

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28
Q

Caspofungin

Mechanism of Action?

A

inhibits synthesis of cell wall component, disrupting assembly

29
Q

Caspofungin

Pharmacokinetics?

A

IV infusion only

level decrease by P450 inducers

30
Q

Caspofungin

Adverse Reaction?

A

infusion related symptoms (via histamine –> rash, pruritus, n/v)

31
Q

Triazoles

Mechanism of Action?

A

like imidazoles, but more selective inhibition of fungal P450

32
Q

Fluconazole [62]

Pharmacokinetics?

A

IV/po, renal excretion

enters CNS

33
Q

Imidazoles

Mechanism of Action?

A

inhibit P450 ergosterol synthesis,

altering membrane permeability

34
Q

Ketoconazole

Pharmacokinetics?

A

IV / po / topical

hepatic metabolism

35
Q

Ketoconazole

Adverser Reaction?

A

anorexia, n/v, hepatotoxicity inhibits CYP450 drug metabolism andandrogen-GCbiosynthesis

36
Q

Clotrimazole

Pharmacokinetics?

A

topical only

37
Q

Terbinafine

Mechanism of Action?

A

inhibits squalene oxidase reducing ergosterol synthesis

38
Q

Terbinafine

Pharmacokinetics?

A

po and topical

metabolized by hepatic P450

39
Q

Terbinafine

Adverse Reaction?

A

headache, diarrhea, rash

inhibition of CYP450

40
Q

Flucytosine

Mechanism of Action?

A

Converted to 5FU in fungi –> inhibits thymidylate synthetase and DNA synthesis

41
Q

Flucytosine

Pharmacokinetics?

A

Well-absorbed and distributed renally elminated (decrease dose if renal impairment)

42
Q

Flucytosine

Adverser Reaction?

A

n/v, skin rashes (prolonged use –> bone marrow depression)

43
Q

Griseofulvin

Mechanism of Action?

A

binds to fungal microtubules

inhibiting mitosis

44
Q

Griseofulvin

Pharmacokinetics?

A

poor po absorption, improved by microsizing particle, fatty meal

45
Q

Griseofulvin

Adverser Reaction?

A

hypersensitivity reactions, GI distress, headache, confusion.

46
Q

Fluconazole [62]

Adverser Reaction?

A 
well tolerated (GI upset)
lesser effect on CYP450 metabolism
47
Q

Amantadine Rimantadine

Spectrum / Uses?

A

prophylaxis/treatment of influenza A [emergence of resistance has been high]

48
Q

Oseltamivir, Zanamivir, Peramivir

Spectrum / Uses?

A

prophylaxis/treatment of influenza A, B, C

49
Q

Acyclovir[155] , Valacyclovir [113], Penciclovir, [Famciclovir]
Spectrum / Uses?

A

HSV-1/HSV-2 (mucosal, genital, encephalitis), also varicella-zoster (higher doses)

50
Q

Docosanol (OTC)

Spectrum / Uses?

A

HSV-1 labialis

51
Q

Ganciclovir [Valganciclovir valyl ester prodrug]

Spectrum / Uses?

A

HSV, VZV, CMV (more active, but more toxic than acyclovir) sight-threatening CMV retinitis

52
Q

Ganciclovir [Valganciclovir valyl ester prodrug]

Mechanism of Action

A

phosphorylated by viral thymidine kinase to active form that inhibits viral DNA polymerase

53
Q

Ganciclovir [Valganciclovir valyl ester prodrug]

Pharmacokinetics

A

poor oral absorption (good w/valganciclovir)
distributes to CNS
renal excretion

54
Q

Ganciclovir [Valganciclovir valyl ester prodrug]

Adverse Reactions

A

bone marrow depression

bone marrow depression

55
Q

Cidofovir

Spectrum / Uses?

A 
active against many DNA viruses
CMV infections (if resistant to ganciclovir / foscarnet)
56
Q

Foscarnet

Spectrum / Uses?

A

CMV infections ([GAN] resistant)
acyclovir resistant herpes infections
HIV (2nd line)

57
Q

Ribavirin

Spectrum / Uses?

A 
respiratory syncitial virus (RSV) (inh)
hepatitis C (oral) (w/interferon)
58
Q

Nystatin

Spectrum / Uses?

A

superficial Candidal infections

59
Q

Caspofungin

Spectrum / Uses?

A

aspergillosis (if refractory to ampho B)

60
Q

Triazoles

Spectrum / Uses?

61
Q

Fluconazole [62]

Spectrum / Uses?

A

oropharyngeal/esophageal candidiasis
vulvovaginal candidiasis (single dose)
cryptococcal meningitis

62
Q

Imidazoles

Spectrum / Uses?

63
Q

Ketoconazole

Spectrum / Uses?

A

systemic infections (e.g., candidiasis)
(declining systemic use due to toxicity)
wide use in dermatologic indications

64
Q

Clotrimazole/

Spectrum / Uses?

A

oral and vaginal candidiasis

65
Q

Terbinafine

Spectrum / Uses?

A

onychomycosis of finger/toe nails (po)

athlete’s foot (topical)

66
Q

Flucytosine

Spectrum / Uses?

A

serious infections of cryptococcosis, and candidiasis

67
Q

Griseofulvin

Spectrum / Uses?

A

severe dermatophytosis of skin, hair, finger / toenails

68
Q

Amphotericin

Spectrum / Uses?

A

broad spectrum, choice for life threatening systemic infections

Final D&D (16 decks)

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