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32 Cards in this Set

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Amphotericin B special characteristics
very toxic
resistance is uncommon- due to decreased sterol in membrane
light sensitive, stored in body tissues, lipophilic
Amphotericin B MOA
fungicidal
Binds ergosterol in fungal membrane, forms channel causing leaky cell
Amphotericin B SEs
permanent renal damage (80% of patients)
myocardial toxicity
hepatotoxicity
CNS
Oz and eliminators
Amphotericin B Use
systemic or rapidly progressing fungal infection
immunocompromised
Flucytosine special characteristic
rapid resistance if given alone
Flucytosine phonemic friends
Fluconazole- antifungal triazole
Fluticasone- steroid for asthma
Flucytosine MOA
Inhibit fungal DNA synthesis:
cytosine deaminase converts to 5-FU to 5-dFMP which inhibits thymidylate synthetase, decreases dTTP
unique target within group
Imidazoles Characteristics & drug prototype
N containing ring
useful but serious SEs
"Ketoconazole"
Ketoconazole MOA
fungicidal
inhibits 14-alpha demethylase (that converts ianosterol to ergosterol)
Ketoconazole SEs
inhibits steroid synth (aldosterone, cortisol, testosterone)
inhibits TXA synth (useful to prevent ARDS)
Triazoles Characteristics & prototype
same action as Imidazoles but less effect on host
resistance is a problem (use in combination)
broad antifungal spectrum
"Fluconazole"
Fluconazole MOA
fungicidal
inhibits 14-alpha demethylase (that converts ianosterol to ergosterol)
NOT fluticasone (asthma steroid)
NOT Flucytosine (antifungal)
Fluconazole SEs
NVD, HA, Vertigo, allergy, hepatotoxic, teratogenicity
Echinocandins characteristics & prototype
mild SEs, affect cell wall synthesis
Caspofungin
echinoCANdin
Caspofungin MOA
fungicidal via cell wall
inhibits beta 1,3-D-glucan synthesis
Caspofungin Use
combination with amph B or Fluconazole to reduce use of toxic drug
Candidiasis, Aspergillosis
candy-ass
Caspofungin SEs
MILD
NVD, Fever, hypokalemia, anemia
5 Anitfungal Agents
Amphotericin B
Flucytosine
Ketoconazole
Fluconazole
Caspofungin
AFKFC
Antiparasitic Agents
PROTAZOA:
Metronidazole

ANTIMALARIA (sporozoa):
Chloroquine
Mefloquine
Artemisinin

HELMINTH:
Mebendazole (nematodes, Trichurius)
Thiabendazole (Strongyloides)
Praziquantel (Taenia)
Pyrantel (Ascarius)
gen protozoa
malaria
helminths
Antiparasitic Agents common characteristic
Free Radical Generators
Metronidazole MOA
Only activated in anaerobic system
Reduced Nitro group acts as electron acceptor to deprive cells of reducing equivs
Metronidazole USE
Trichomoniasis & Giardiasis
Anaerobic bacteria
brain abcesses
H Pylori (in combo)
Metronidazole SEs
disulfarim like effect
CNS (ataxia, psychosis, convulsions)
Immunosuppressive
candida superinfection
drinking & AIDS
Antimalarial Agents
Chloroquine
Mefloquine
Artemisinin
Chloroquine special characteristics
avidly binds DNA (not MOA) so wide distribution
widespread resistance by falciparum
Chloroquine MOA
kills schizonte in blood stage
inhibits plasmodial heme polymerase which generates free radical
Chloroquine Resistance
gp160/gp 330
Chloroquine SEs
allergy, CNS, GI
Prolonged use: ototox, retinotox, myopathy
Quinidine like effect (class I antiarrhythmic)
Mefloquine characteristics
side effects much worse than chloroquine, longer t 1/2
Mefloquine MOA
same as chloroquine- generates free radical by inhibiting heme polymerase
like chloroquine
Mefloquine SEs
hepatotoxicity, BM suppression, psychiatric symptoms (insomnia, halucinations, psychosis)
quinidine like effects (class I antiarrhyt)
Artemisinin special characteristics
from Chinese medicine (Wormwood)
antiparasitic & antineoplastic
endoperoxide bridge