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