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Except for flucytosine and griseofluvin, all currently available antifungals have what target?
Fungal cell membrane or cell wall
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Why do most anti-fungals target the membrane or cell wall?
Because funal cell wall/membrane contain ergosterol instead of cholesterol, a differentiated target
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What drugs are the Polyene’s?
Amphotericin B and Nystatin
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How is Amphotericin B mainly administered?
IV, systemically
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What pH is Amphotericin B most active at and why?
6-7.5 pH, at which it is in a neutral form and is most lipophilic
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How did Amphotericin B get its name?
It has a N and COOH group that make it amphoteric
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Can Amphotericin be used in pregnant women?
Yes
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Is Amphotericin B broad ort narrow spectrum?
Broad
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What is the MOA for Amphotericin B?
Binds to ergosterol in membrane and increases permeability to K and Mg to leak out ( creates pores)
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How would you administer Amphotericin B if you want to use it systemically and why?
IV, not absorbed by GI
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In what (rare) instance might you use Amphotericin B orally?
Infection of the lumen of the GI
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Does Amphotericin B penetrate the CSF?
No
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Would hepatic or renal impairment affect serum levels of Amphotericin B?
No
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Is Amphotericin B effective topically?
No
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How would you administer Amphotericin B for a meningeal infection?
Intrathecally (because does not penetrate the CSF systemically)
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Does Amphotericin B inhibit CYP450 enzymes?
No
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Would Amphotericin B be used for empiric therapy of a severe fungal infection?
Yes
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What fungi can be treated with Amphotericin B?
Most: Candidiasis, aspergillosis, cryptococcosis, mucormycosis (zygomycosis), blastomycosis, protozoa (Leishmania genus) causing leishmaniasis
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What is the pregnancy category for Amphotericin B?
B
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What types of formulations are available for Amphotericin B?
Conventional and lipid based formulation
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C-AMB (Amphotericin B deoxycholate) is what formulation of Amphotericin B?
Conventional
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What does AMCD stand for?
Amphotericin B colloidial dispersion, a lipid based formulation
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What does LAmB stand for?
Liposomal Amphotericin B
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What does ABLC stand for?
Amphotericin B lipid complex
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Why does Amphotericin B come in lipid based formulation?
To reduce nephrotoxicity associated with Amphotericin B’s lipophilic adherence to nephron cell membranes
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Is Amphotericin B used for moderate or severe systemic infections?
Severe
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What are the main side effect sof Amphotericin B?
Mammalian membrane interactions, infusion related Fever/chills/HA/N/phlebitis/spasms, allergies/anaphylaxis, , hypochromic cormocytic anemia, renal toxicity, hypokalemia and hypomagnesemia
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What is the primary side effect of Amphotericin B?
Nephrotoxicity
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