ABSTRACT

The polyenes are a family of several hundred naturally derived macrolide antibiotics. Those most well studied to date possess an internal cyclic ester, with 4-7 conjugated double bonds. They exhibit a broad spectrum of antifungal activity and have a common mechanism of action (1). The polyenes bind to sterols in all eukaryotic cells, but some have greater affinity for ergosterol found in fungal cell membranes, as opposed to cholesterol found in mammalian cell membranes. This difference in affinity between fungal and mammalian sterols has allowed for human use, a select few of the polyenes that have been studied. Amphotericin B, nystatin, and pimaricin are the most commonly used polyenes in clinical practice. This chapter will focus exclusively on amphotericin B and its lipid formulations.