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32 Cards in this Set
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Amphotericin B special characteristics
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very toxic
resistance is uncommon- due to decreased sterol in membrane light sensitive, stored in body tissues, lipophilic |
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Amphotericin B MOA
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fungicidal
Binds ergosterol in fungal membrane, forms channel causing leaky cell |
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Amphotericin B SEs
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permanent renal damage (80% of patients)
myocardial toxicity hepatotoxicity CNS |
Oz and eliminators
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Amphotericin B Use
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systemic or rapidly progressing fungal infection
immunocompromised |
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Flucytosine special characteristic
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rapid resistance if given alone
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Flucytosine phonemic friends
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Fluconazole- antifungal triazole
Fluticasone- steroid for asthma |
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Flucytosine MOA
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Inhibit fungal DNA synthesis:
cytosine deaminase converts to 5-FU to 5-dFMP which inhibits thymidylate synthetase, decreases dTTP |
unique target within group
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Imidazoles Characteristics & drug prototype
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N containing ring
useful but serious SEs "Ketoconazole" |
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Ketoconazole MOA
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fungicidal
inhibits 14-alpha demethylase (that converts ianosterol to ergosterol) |
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Ketoconazole SEs
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inhibits steroid synth (aldosterone, cortisol, testosterone)
inhibits TXA synth (useful to prevent ARDS) |
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Triazoles Characteristics & prototype
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same action as Imidazoles but less effect on host
resistance is a problem (use in combination) broad antifungal spectrum "Fluconazole" |
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Fluconazole MOA
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fungicidal
inhibits 14-alpha demethylase (that converts ianosterol to ergosterol) |
NOT fluticasone (asthma steroid)
NOT Flucytosine (antifungal) |
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Fluconazole SEs
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NVD, HA, Vertigo, allergy, hepatotoxic, teratogenicity
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Echinocandins characteristics & prototype
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mild SEs, affect cell wall synthesis
Caspofungin |
echinoCANdin
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Caspofungin MOA
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fungicidal via cell wall
inhibits beta 1,3-D-glucan synthesis |
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Caspofungin Use
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combination with amph B or Fluconazole to reduce use of toxic drug
Candidiasis, Aspergillosis |
candy-ass
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Caspofungin SEs
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MILD
NVD, Fever, hypokalemia, anemia |
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5 Anitfungal Agents
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Amphotericin B
Flucytosine Ketoconazole Fluconazole Caspofungin |
AFKFC
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Antiparasitic Agents
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PROTAZOA:
Metronidazole ANTIMALARIA (sporozoa): Chloroquine Mefloquine Artemisinin HELMINTH: Mebendazole (nematodes, Trichurius) Thiabendazole (Strongyloides) Praziquantel (Taenia) Pyrantel (Ascarius) |
gen protozoa
malaria helminths |
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Antiparasitic Agents common characteristic
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Free Radical Generators
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Metronidazole MOA
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Only activated in anaerobic system
Reduced Nitro group acts as electron acceptor to deprive cells of reducing equivs |
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Metronidazole USE
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Trichomoniasis & Giardiasis
Anaerobic bacteria brain abcesses H Pylori (in combo) |
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Metronidazole SEs
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disulfarim like effect
CNS (ataxia, psychosis, convulsions) Immunosuppressive candida superinfection |
drinking & AIDS
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Antimalarial Agents
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Chloroquine
Mefloquine Artemisinin |
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Chloroquine special characteristics
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avidly binds DNA (not MOA) so wide distribution
widespread resistance by falciparum |
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Chloroquine MOA
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kills schizonte in blood stage
inhibits plasmodial heme polymerase which generates free radical |
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Chloroquine Resistance
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gp160/gp 330
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Chloroquine SEs
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allergy, CNS, GI
Prolonged use: ototox, retinotox, myopathy Quinidine like effect (class I antiarrhythmic) |
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Mefloquine characteristics
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side effects much worse than chloroquine, longer t 1/2
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Mefloquine MOA
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same as chloroquine- generates free radical by inhibiting heme polymerase
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like chloroquine
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Mefloquine SEs
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hepatotoxicity, BM suppression, psychiatric symptoms (insomnia, halucinations, psychosis)
quinidine like effects (class I antiarrhyt) |
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Artemisinin special characteristics
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from Chinese medicine (Wormwood)
antiparasitic & antineoplastic endoperoxide bridge |
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