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14 Cards in this Set
- Front
- Back
Amphotericin B
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polyene related to nystatin - usually given IV as nonlipid colloid suspension; widely distributed except to CNS; bind to ergosterol and cause formation of artificial pores; most important drug for systemic mycoses; widest antifungal spectrum and remains DOC for apergillus, blastomyces, candida albicans, cryptococcus, histoplasma, and Mucor; fast infusions may cause fever, chills, muscle spasms; it decreases FGR and causes acidosis w/ loss of Mag and Potass; intrathecal dose may cause seizures and neurologic damage
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Flucytosine (5-FC)
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pyrmidine antimetabolite related to anticancer drugs -orally effective and widely distributed; accumulates in fungal cells by membrane permease and converted to 5-FU which blocks thymidylate synthase - resistance is due to fungal activity of permeases or deaminase; limited spectrum; limited to treament in combo w/ amphoB or fluconazole in Cryptococcus neoformans and possiby systemic candidal; prolonged use can cause reversible bone marrow suprresion, alopecia, and LiverD
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the Azoles
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Keto, Fluco, Itra, Voricon - Fluco and Vori are more reliably absorbed via oral; inducers of enzymes (rifampin) decrease bioavailabilty; they interfere w/ fungal cell permeabily by inhibiting synthesis of ergosterol;
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Ketoconazole
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rarely used for systemic; good use for chronic mucocutatneous candidasis and also in dermatophytes
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Fluconazole
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DOC in esophageal and Oropharnygeal candidiases and for most infections by Coccidioides; single oral dose erradicates yeast infections; DOC for initail and secondary proph against cryptococcal meningitss
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Itraconazole
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DOC for systemic infections by Blastomyces and Sporothrix and for subcutaneous chromoblastomycosis; alternative tx for asper, coccidio, cryptococcus, and histo; also used in onychomycosis
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Voriconazole
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newer azole w/ wider specturm than itra, coDOC for invansive apergillosis, and alternative in candidemia in AIDS
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Toxicity of Azoles
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vomitting, diarrhea, rahs and sometimes hepatoxicity; Keto is notorious inhibitor of P450 and may increase levles of many drugs; it also interfeeres w/ synthesis of adrenal and gonaldl steroids leading to gynecomastia, ammenorrhea, and infertility; Voriconazle causes transiet visual distubrances in more than 30%
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Drugs metabolized by enzymes inhibited by Keto?
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cisapride, chlordiazeopoxide, cyclosporine, didanosine, fluoxetine, loratidine, lovastatin, methadone, nifedipine, phenytoin, quinidine, tacrolimus, theophylline, verapamil, warfarin, zidovudine, and zolpidem
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Drugs that inhibit P450?
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chloramphenicaol, cimetidine, clarithromycin, disulfiram, erythromycin, ethanol, grapefruit joice, estradiol, fluconazole, isoniazide, itraconazole, MAOs, phenylbutazone, and secobarbital
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Capsofungin
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used IV, distributes widely, inhibits synthesis of B-glycan; a critical component of cell walls; currently used only in management of invasive aspergillosis; non-toxic (headache)
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Griseofulvin
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superficial fungal infections; distributed to stratum korneum where it binds keratin; exrected biliary; interferes w/ microtubule function in dermatophytes and may inhibit synthesis and polymerization of nucleic acids; resistance can occur when transport is decreased; DONT USE IN PATIENTS W/ PORPHYRIA, decreases bioavaliabilyt of warfarin and also causes disulfiram reactions w/ ethanol
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Terbinafine
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inhibits fungal ezyme squalene epoxidase which leads to toxic accumulation of squalene; fungicidal; accumulates in kerratin but much more effective than griseofulvin in onychomycosis; does not inhibit p450; dont use in liver disease
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Nystatin
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polyene disrupts by binding ergosterol, used topically to suprrese candidal and orally to eradicate GI fungi in pateints w/ immunosuprresion; miconazole, clotrimazole, haloprogin, tolnaftate, and undecylceni acid are others
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