RESUMO
Amphotericin B deoxycholate use has increased during the past years in parallel with the increase in the number of immunosuppressed patients suffering invasive fungal infections. This drug is associated with a high rate of side effects, especially renal toxicity. Lipid formulations (liposomal, lipid complex, colloidal suspension and the Indian liposomal formulation) have been developed, which share the same antifungal spectrum but differ in efficacy and toxicity. A review of amphotericin lipid formulations is presented, focusing on differences in efficacy and, especially renal toxicity. The main problem for use of these formulations in Latin America is their highcost.
Dado el aumento en el número de pacientes inmunosuprimidos en los últimos años, el uso de anfotericina B desoxicolato también se incrementó debido a una mayor incidencia de las infecciones fúngicas invasoras en esta población. Este medicamento tiene una alta frecuencia de efectos adversos, especialmente nefrotoxicidad. Se han desarrollado modificaciones de la presentación de anfotericina B con el desarrollo de formas lipídicas (liposomal, complejo lipídico, suspensión coloidal y fórmula liposomal procedente de la India) que tienen el mismo espectro y con variaciones en su efectividad y toxicidad. Se presenta una revisión de las formas lipídicas de anfotericina, sus diferencias en efectividad y, especialmente, nefrotoxicidad. El principal problema para su implementación en América Latina es el alto costo de estas presentaciones.
Assuntos
Humanos , Anfotericina B/química , Lipídeos/química , Antifúngicos/química , Leishmaniose/tratamento farmacológico , Anfotericina B/efeitos adversos , Coloides , Excipientes , Lipossomos , Micoses/tratamento farmacológico , Antifúngicos/efeitos adversosRESUMO
Polyene antibiotics are known for their remarkable antifungal properties. The alkali metal and quaternary alkylammonium salts of amphotericin B, nystatin and aureofungin have been prepared by ion-exchange method. The physico-chemical and biological properties of these salts have been studied with a view to evaluate their therapeutic advantages over the parent compounds. While the majority of the salts reported herein showed more water solubility; triethylammonium salts, unlike the other alkali metal salts, possessed marginally improved or similar bioactivity in comparison to their parent antibiotic having reduced toxicity.