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30 Cards in this Set
- Front
- Back
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There are properties which make the drug therapy of _____ infections difficult
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Fungal
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Fungi have relatively simple cellular structure with ________ to animal cells
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Increasing similarity
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Fungi and a ______, and infections often occur in poorly ____ tissues
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Slow growth rate; vascularized
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Fungi have a different _____ than bacteria
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Cell wall and membrane structure
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Infections of internal organs
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Systemic mycoses
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Involve the outer layers of the skin, nails, or mucous membranes
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Superficial mycoses
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Slightly deeper infections of the skin, hair or nails by dermatophytes
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Dermatomycoses
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People with _______ are more susceptible to life threatening fungal infections
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Suppressed immune systems
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For therapy of severe systemic infections
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Amphotericin B (fungizone)
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Amphotericin B contains a large ______ with numerous conjugated double bonds
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Lactone ring
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Amphotericin B has an ______ character
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Amphiphilic
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Binds to ergosterol (membrane lipid) and forms pores - leading to cel leakage
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Amphotericin
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Broad spectrum - works on many different types of fungal infections (not gm +/-)
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Amphotericin
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Highly toxic as it binds to membrane cholesterol, administered only in the hospital
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Amphotericin
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Reduced binding affinity to ergosterol
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Mechanism of resistance to Amphotericin
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Alterations in fungal membrane steroids
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Mechanism of resistance to Amphotericin
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Amphotericin has a higher affinity for _____ in membranes than mammalian cholesterol
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Ergosterol
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Similar in structure and MOA to amphotericin
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Nystatin
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Too toxic for systemic use
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Nystatin
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Used primarily to tx candidal infections of the mucosa, skin, intestinal tract, and vagina
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Nystatin
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Slow renal elimination in unchanged form, decrease dose in renal insufficiency
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Nystatin
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Nystatin has a _______ that translates to poor oral absorption, poor CNS penetration. IV only; intrathecal required for fungal meningitis
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Nystatin
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Inhibit growth of fungi by blocking synthesis of ergosterol
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Azoles (ketoconazole)
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Relatively nontoxic, occasional hepatotoxicity. Interferes with drug metabolism.
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Azoles
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Increased drug efflux as they are recognized as poisons and pumped out of the body as a protective mechanism.
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Mechanisms of resistance to Azoles
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Alterations in membrane sterols
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Mechanisms of resistance to Azoles
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Reduced drug affinity for enzyme responsible for ergosterol synthesis
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Mechanisms of resistance to Azoles
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Members of imidazole class of antifungals that are too toxic for systemic use
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Clotrimazole and miconazole
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Azole that is broad spectrum, for systemic infections, relatively nontoxic, and interferes with drug metabolism
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Ketoconazole
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More reliable oral absorption and is also disturbed to CNS
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Fluconazole
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