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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
Nystatin | Mechanism of Action?
same as amphotericin
26
Nystatin | Pharmacokinetics?
topical only | not absorbed orally
27
Nystatin | Adverse Reaction?
well tolerated given topically | mild GI upset (if swallowed)
28
Caspofungin | Mechanism of Action?
inhibits synthesis of cell wall component, disrupting assembly
29
Caspofungin | Pharmacokinetics?
IV infusion only | level decrease by P450 inducers
30
Caspofungin | Adverse Reaction?
infusion related symptoms (via histamine --> rash, pruritus, n/v)
31
Triazoles | Mechanism of Action?
like imidazoles, but more selective inhibition of fungal P450
32
Fluconazole [62] | Pharmacokinetics?
IV/po, renal excretion | enters CNS
33
Imidazoles | Mechanism of Action?
inhibit P450 ergosterol synthesis, | altering membrane permeability
34
Ketoconazole | Pharmacokinetics?
IV / po / topical | hepatic metabolism
35
Ketoconazole | Adverser Reaction?
anorexia, n/v, hepatotoxicity inhibits CYP450 drug metabolism andandrogen-GCbiosynthesis
36
Clotrimazole | Pharmacokinetics?
topical only
37
Terbinafine | Mechanism of Action?
inhibits squalene oxidase reducing ergosterol synthesis
38
Terbinafine | Pharmacokinetics?
po and topical | metabolized by hepatic P450
39
Terbinafine | Adverse Reaction?
headache, diarrhea, rash | inhibition of CYP450
40
Flucytosine | Mechanism of Action?
Converted to 5FU in fungi --> inhibits thymidylate synthetase and DNA synthesis
41
Flucytosine | Pharmacokinetics?
Well-absorbed and distributed renally elminated (decrease dose if renal impairment)
42
Flucytosine | Adverser Reaction?
n/v, skin rashes (prolonged use --> bone marrow depression)
43
Griseofulvin | Mechanism of Action?
binds to fungal microtubules | inhibiting mitosis
44
Griseofulvin | Pharmacokinetics?
poor po absorption, improved by microsizing particle, fatty meal
45
Griseofulvin | Adverser Reaction?
hypersensitivity reactions, GI distress, headache, confusion.
46
Fluconazole [62] | Adverser Reaction?
``` well tolerated (GI upset) lesser effect on CYP450 metabolism ```
47
Amantadine Rimantadine | Spectrum / Uses?
prophylaxis/treatment of influenza A [emergence of resistance has been high]
48
Oseltamivir, Zanamivir, Peramivir | Spectrum / Uses?
prophylaxis/treatment of influenza A, B, C
49
Acyclovir[155] , Valacyclovir [113], Penciclovir, [Famciclovir] Spectrum / Uses?
HSV-1/HSV-2 (mucosal, genital, encephalitis), also varicella-zoster (higher doses)
50
Docosanol (OTC) | Spectrum / Uses?
HSV-1 labialis
51
Ganciclovir [Valganciclovir valyl ester prodrug] | Spectrum / Uses?
HSV, VZV, CMV (more active, but more toxic than acyclovir) sight-threatening CMV retinitis
52
Ganciclovir [Valganciclovir valyl ester prodrug] | Mechanism of Action
phosphorylated by viral thymidine kinase to active form that inhibits viral DNA polymerase
53
Ganciclovir [Valganciclovir valyl ester prodrug] | Pharmacokinetics
poor oral absorption (good w/valganciclovir) distributes to CNS renal excretion
54
Ganciclovir [Valganciclovir valyl ester prodrug] | Adverse Reactions
bone marrow depression | bone marrow depression
55
Cidofovir | Spectrum / Uses?
``` active against many DNA viruses CMV infections (if resistant to ganciclovir / foscarnet) ```
56
Foscarnet | Spectrum / Uses?
CMV infections ([GAN] resistant) acyclovir resistant herpes infections HIV (2nd line)
57
Ribavirin | Spectrum / Uses?
``` respiratory syncitial virus (RSV) (inh) hepatitis C (oral) (w/interferon) ```
58
Nystatin | Spectrum / Uses?
superficial Candidal infections
59
Caspofungin | Spectrum / Uses?
aspergillosis (if refractory to ampho B)
60
Triazoles | Spectrum / Uses?
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61
Fluconazole [62] | Spectrum / Uses?
oropharyngeal/esophageal candidiasis vulvovaginal candidiasis (single dose) cryptococcal meningitis
62
Imidazoles | Spectrum / Uses?
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63
Ketoconazole | Spectrum / Uses?
systemic infections (e.g., candidiasis) (declining systemic use due to toxicity) wide use in dermatologic indications
64
Clotrimazole/ | Spectrum / Uses?
oral and vaginal candidiasis
65
Terbinafine | Spectrum / Uses?
onychomycosis of finger/toe nails (po) | athlete’s foot (topical)
66
Flucytosine | Spectrum / Uses?
serious infections of cryptococcosis, and candidiasis
67
Griseofulvin | Spectrum / Uses?
severe dermatophytosis of skin, hair, finger / toenails
68
Amphotericin | Spectrum / Uses?
broad spectrum, choice for life threatening systemic infections

Final D&D (16 decks)

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