Antifungals Pharmacology

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OPPORTUNISTIC MYCOSES SYSTEMIC CANDIDIASIS (CANDIDAEMIA) (Candida albicans)  May cause septicaemia (candidemia), endocarditis, peritonitis, Classified depending on route of administrati... on  Systemic antifungals: oral and/or parenteral administration  Topical antifungals: direct (topical) application NB:  some antifungal classes (azoles, polyenes) cut across this classification  many superficial mycoses are treated either systemically or topically. AMPHOTERICIN B  a heptaene macrolide.  amphipathic (both hydrophobic and hydrophilic properties)  insoluble in water but formulated for IV infusion as:  colloidal preparations (AmphB-deoxycholate complex, AmphB- cholesteryl sulfate complex, AmphB-(phospho)lipid complex)  liposomal/vesicular formulations (AmBisome®) AMPHOTERICIN B Mechanism of Action. binds to sterols, primarily ergosterol (high-affinity) in the fungal membrane  forms pores or channels that increase the permeability of the membrane  leakage of small molecules and disruption of cell function AMPHOTERICIN B Selective toxicity.  Higher affinity for ergosterol than cholesterol of mammalian cells  Ergosterol is not present in mammalian membranes Resistance  rare;  usually intrinsic  either a lower membrane concentration, or a change in the structure of ergosterol [Show More]

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