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Glossary of ANTIFUNGAL DRUGS

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What are the polyenes?
Polyenes (Amphotericin and Nystatin) are characterized by a conjugated double bond system w a macrolide ring
What makes the polyenes selctive?
Amphotericin B and Nystatin have a higher affinity for ERGOSTEROL than for cholesterol and are therefore selective for fungal membranes
Which polyene is more potent?
AMphotericin B is 6X more potent than Nystatin and is soluble enough to be administered IV.
Nephrotoxicity
How do the AZOLES work?
inhibition of 14-alfa-demethylase, a CYP450 involved in ergosterol synthesis.
What are the 3 things you NEED to know about the various AZOLES?
ITRACONAZOLE- oral tx of nail infection, DOC for dermatophytoses and onychomycosis
VORICONAZOLE- DOC invasive aspergillosis
FLUCONAZOLE- good CNS penetration, superior for tx of AIDS assoc Cryptococcal meningitis
What is he one allylamine we study?
TERBINAFINE
by inhibiting fungal squalene epoxidase the effect is two fold:
1)inhibit membrane synthesis
2)toxic buildup of squalene
What is the ONLY approved drug for the topical tx of dermatophyte infections of hair and nails?
Ciclopirox olamine!
a pyridone antifungal agent that inhibits the uptake of extracellular nutrients
Why is flucytosine used almost exclusively with Amphotericin B?
bc clinical resistance occurs frequently
What major pathogen is GRISEOFULVIN not effective against?
Candida infections

insoluble cmpd effective in tx of fungal infections of skin, hair and mails caused by Epidermophyton, Microsporum, and Trichophyton.
What is important to know about Griseofulvin?
it is virtually INSOLUBLE in H2O and is more readily absorbed if taken w a fatty meal
Absorption from gut is inhibited by barbituates

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