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IC Part II > Antiviral and Antifungal Review > Flashcards

Antiviral and Antifungal Review Flashcards

1
Q
  • 5’ monophosphate formed by a CMV viral kinase
  • guanosine analog
  • triphosphate formed by cellular kinases
  • preferentially inhibits DNA polymerase
A

ganciclovir

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2
Q
  • guanosine analogs, monophosphorylated by HSV/VZV thymidine kinase and not in uninfected cells –> few adverse effects
  • preferentially inhibit DNA polymerase by chain termination
A

acyclovir, valacyclovir, famciclovir

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3
Q
  • preferentially inhibits viral DNA polymerase, does not require phosphorylation by viral kinase
  • treats CMV retinitis in immunocompromised patients, acyclovir resistant HSV, long half life
  • nephrotoxicity
A

cidofovir

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4
Q
  • viral DNA/RNA polymerase inhibitor and HIV reverse transcriptase inhibitor
  • binds to pyrophosphate binding site of enzyme
  • treats CMV retinitis when ganciclovir fails, acyclovir resistant HSV
  • nephrotoxic, electrolyte abnormalities, seizures
A

foscarnet

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5
Q

-for primary keratoconjunctivitis and recurrent epithelial keratitis caused by herpes simplex I and II

A

trifluridine

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6
Q

for herpes simplex of face or lips, OTC

A

docosanol

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7
Q
  • thymidine analog, substrate/inhibitor for HIV reverse transcriptase
  • inhibits stable infection of new cells
  • well absorbed, CNS, rapidly metabolized
  • use in 3 or 4 drug cocktail for HIV, resistant due to mutations in reverse transcriptase
  • adverse: bone marrow depression, CNS, toxicity in drugs competing for glucoronidation
A

zidovudine

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8
Q 
zidovudine
zalcitabine
lamivudine
abacavir
tenofovir (nucleotide) 
emtricitabine
A

nucleoside reverse transcriptase inhibitors

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9
Q
  • first gen oral NNRTI
  • non competitive, binds near but not in active site
  • rapid resistance
  • can be active against AZT resistant HIV
  • life threatening skin rash
  • CPY3A4 substrate
A

non-nucleoside reverse transcriptase inhibitors (NNRTI)

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10
Q 
nevirapine
efavirenz
delavirdine
etravirine
rilpivirine
A

NNRTIs

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11
Q
  • prevent viral particle production, prevent maturation of new viruses, pol gene cleaves polypeptide products of mRNA
  • adverse: hyperglycemia, altered fat distribution, hyperlipidemia, insulin resistance
A

HIV protease inhibitors

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12
Q
  • first HIV protease inhibitor
  • well tolerated
  • low oral bioavailability
  • extensive 1st pass
  • DDIs
  • use in combo with RT inhibitors
A

saquinavir

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13
Q

coformulated with protease inhibitors to “boost” levels, inhibitor of CYP3A4

A

ritonavir

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14
Q
  • CCR5 antagonist
  • binds CCR5 on human CD4 cells
  • inhibits gp120 conformational change required for HIV fusion with CD4 cell
A

maraviroc

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15
Q

interferes with entry of HIV-1 into host cells by inhibiting the fusion of virus and cell membranes, binds gp41

A

enfuvirtide

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16
Q

-inhibit catalytic activity of integrase

A

dolutegravir, elvitegravir, raltegravir

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17
Q
  • antimetabolite, blocks GMP formation
  • aerosol for RSV
  • known teratogen, dose dependent myelosuppression
  • treatment of hepatitis
A

ribavirin

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18
Q
  • oral agent effective against all common influenza viruses
  • pro drug
  • NA inhibitor
A

oseltamivir

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19
Q
  • oral inhalation
  • influenza A and B
  • effective in early infection
  • bronchospasm in asthmatics
A

zanamivir

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20
Q
  • treatment of acute, uncomplicated influenza in adults who’ve been symptomatic <2 days
  • 600 mg single dose
A

peramivir

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21
Q
  • block viral uncoating by blocking M2 proton channel
  • given in first 48 hours of contact
  • admin orally, protects only influenza A
A

amantadine, rimantadine

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22
Q

standard of care for treatment of HCV?

A

peginterferon alfa + ribavirin

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23
Q
  • nucleotide analog, inhibits HCV RNA dependent RNA polymerase
  • given in combo with peg interferon and ribavirin
A

sofosbuvir

24
Q

______ have ergosterol in membrane instead of cholesterol

25
- IV drug that inhibits synthesis of glucan, a major fungal cell wall component - use for invase aspergillosis in patients who fail ampho B therapy
caspofungin
26
amphotericin B binds ______ in fungal membranes, producing a pore causing leaking of contents
ergosterol
27
amphotericin B must be given _____ or ______, widely distributed except CNS, excretion 2 weeks
IV, intrathecal
28
-reservoir of amphotericin, has lower affinity for drug than fungal membrane but higher affinity for drug than patient's membranes
liposomal
29
amphotericin B often combined with ________ to delay resistance and use lower doses due to synergism
flucytosine
30
infusion related reactions, fever, chills, muscle spasms, vomiting, headache, hypotension - pretreat w/ antipyretics, antihistamines, aanalgesics, coticosteroids - nephrotoxicity
amphotericin B
31
flucytosine activated by fungal ________ and converted to 5-flurouracil, blocks DNA and RNA synthesis
cytosine deaminase
32
- CNS, excreted in urine - low toxicity to patient - narrow spectrum, rapid resistance so only use with ampho B
flucytosine
33
- inhibit ergosterol synthesis - oral antifungal for systemic - inhibit CYPs, extensive DDI - severe hepatotoxicity, gynecomastia, interactions w/ cyclosporines and antihistamines
ketoconazole
34
broader spectrum, less adverse than ketoconazole
itraconazole
35
-effective against aspergillosis, fluconazole susceptible and resistant candida, and cryptococcus neoformans
voriconazole
36
- water soluble azole - good CSF delivery - more selective for fungal P450s
fluconazole
37
newer and broad spectrum member of azole family, good for candida and aspergillus -oral only
posaconazole
38
- inhibits synthesis of B(1,3)D-glucan, an essential component of fungal cell wall - treats invase aspergillus - candida: intra abdominal abscess, esophagitis, peritonitis, febrile neutropenic patients - hypotension, tachycardia, fever, chills, rash, anemia, hypokalemia
caspofungin
39
-topical antifungal, too toxic for systemic use
nystatin
40
griseofulvin concentrates in _______ tissue, treats ringworm athlete's foot, disrupts mitotic spindle in fungal cells, hepatitis and DDIs with warfarin and phenobarbital
keratinized
41
- topic or systemic - concentrates in keratinized tissue - inhibits squalene epoxidase
terbinafine
42
only ______ affects tissue schizonts
primaquine
43
- alters metabolism of hemoglobin by parasite, blocks nucleic acid synthesis - highly effective blood schizonticide - clears parasite from all 4 plasmodia (used w/ primaquine for vivax and ovale) - prophylactic, preferred when resistance not a problem
chloroquine
44
- visual impairment with long term therapy - widespread resistance - p glycoprotein efflux mechanism (block with verapamil)
chloroquine
45
- destruction of asexual bloods forms of malarial pathogens falciparum and vivax - oral only, metabolized in liver - CNS psychotropic effects - use for chloroquine resistant malaria
mefloquine
46
- anti folate drug combo effects on protozoa - effective blood schizonticide for p falciparum, slow acting - multi drug resistance common
fansidar (pyrimethamine-sulfadoxine)
47
- selectively inhibits parasite mitochondrial electron transport - inhibits DHFR - prevent or treat acute uncomplicated p falciparum malaria - increased transaminase, headaches, dizziness
atovaquone plus proguanil
48
- treat chloroquine resistant p falciparum - interferes with oxygen uptake and carb metabolism, intercalates into DNA - cinchonisms: flushed, tinnitus, blurred vision, confusion
quinine, quinidine
49
- chinese herbal medicine - activated by oxidative metabolism - rapidly acting blood schizonticide, useful for MDR p falciparum
artemesinin
50
standard prophlactic drug for SE Asia with high rates of resistance to mefloquine
doxycycline
51
-derived from artemesinin, treats MDR p falciparum
artemether, lumefantrine
52
- tissue shizonticide - metabolites are intracellular oxidants - use in combo with chloroquine for prophylaxis/cure of p vivax, p ovale - withheld until G6PD status is known - hemolytic anemia, GI distress
primaquine
53
- tissue amebicide activated by electron donation - used for urogenital trichomonas, giardia, aspiration pneumonia, anaerobics - disulfiram effect
metronidazole and nitazoxanide
54
- concentrates in liver, spleen, kidney - doesn't enter CNS - pneumocystic prophylaxis in sulfonamide intolerant pts - resp stimulation then depression
pentamidine
55
diloxanide furoate, iodoquinol, paromomycin treat?
aymptomatic amebiasis intestinal infections
56
- depolarizing neuromuscular blocking agent on nicotinic receptor - increases release of acetylcholine and inhibits cholinesterase in the worm - use: ascariasis, pinworm, hookworm, whipworm - n/v/d/anorexia
pyrantel pamoate
57
- increases chloride permeability, polarizing cells leading to paralysis - use for strongyloidiasis, onchocerciasis
ivermectin

IC Part II (29 decks)

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