Antifungal Pharm
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| most important antifungal drug for severe infections ? | * Amp-B
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| Are the mainstays of standard treatment ? | * -Azoles (itra and flu)
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| Amphotericin B spectrum ? | * treats just about everything.... DOC for most severe fungal infections
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| When to use ? | * Systemic use reserved for severe, life-threatening infections
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| MOA of Amp-B ? | * preferentially binds to ergosterol in fungal membranes to punch holes in it
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| Amp B Lipid Formulations ? | * less toxicity and nephrotoxicity, but expensive
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| Amp-B SE's ? | * Nephrotoxicity (constricts afferent arterioles)so monitor kidneys, Hypokalemia , cytokine storm - n/v/f,
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| Flucytosine Spectrum ? | * Narrow spectrum antimycotic - Cryptococcals
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| Flucytosine use ? | * Systemic candidiasis & cryptococcal infections
---Cryptococcal meningitis
.... * never used alone, usu w/Amp-B
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| Flucytosine MOA ? | * blocks dUMP/nucleic acid synthesis to make RNA/DNA
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| Flucytosine Side Effects ? | * Bone Marrow Depression, n/v/d, GI mucositis - sores in mouth
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| Antifungal azoles advantages ? | * treatment of systemic fungal infections bc low toxicity
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| Azole disadvantages ? | * Inhibit P450 drug-metabolizing enzymes and can increase the levels of many other drugs
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| Azole MOA ? | * Inhibits fungal cytochrome P450-dependent lanosterol 14-alpha-demethylase, which decreases ergosterol, which disrupts fungal cell membrane
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| Fluconazole usu uses ? | * Coccidioidomycosis, meningitis, cryptococcosis, candidiasis.... * Not aspergillosis
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| Fluconazole bioavailability and drug/drug interactions ? | * Absorption not affected by food or gastric pH.... * Fewer drug interactions than itraconazole.... * Eliminated by kidneys so can be used for UTIs
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| Itraconazole activity ? | * Invasive aspergillosis , Blastomycosis, Cryptococcosis, Histoplasmosis ,
Suspected fungal infection w/ neutropenic fever
, Coccidioidomycosis
, Sporotrichosis
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| Itraconazole bioavailability ? | * Requires food and acidic gastric pH for drug solubilization, acid lowering drugs can lower this drugs effectiveness
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| Itraconazole Oral Solution? | * doesnt need an acidic environment.... but causes GI upset....excreted via hepatic system
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| Itraconazole Side Effects ? | * drug/drug interactions, CYP3A4 inhibitor.... * has Negative Ionotropic Effects - Can cause hypertension, hypokalemia, and peripheral edema
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| Voriconazole use ? | * invasive aspergillosis (DOC)
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| Voriconazole basics ? | * not affected by pH or food.... * hepatically eliminated
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| Voriconazole Side Effects ? | * Inhibits CYP3A4, Visual Changes, Neurotoxic, photosensitive rash, arrhytmias/QT prolongation
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| Caspofungin MOA ? | * Impairs cell wall production
inhibits beta-(1,3)-D-glucan synthesis (cell wall component) weaken cell wall
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| Active against ? | * Active against Candida and aspergillus
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| When to use ? | * salvage therapy when Amp B or voriconazole has failed (or drug intolerance)
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