RESUMEN
The antibacterial effect of brodimoprim alone and in combination with dapsone has been studied in vitro in cell-free systems and in whole mycobacterial cells as well as in vivo in mice and humans. The obtained inhibitory effects in vitro and in vivo against model mycobacterial strains and M. leprae, the pharmacokinetic properties in human and its synergistic effect with the most used drug in the chemotherapy of leprosy, dapsone, make brodimoprim a promising candidate in the therapy of leprosy.
Asunto(s)
Dapsona/farmacología , Leprostáticos , Mycobacterium leprae/efectos de los fármacos , Trimetoprim/análogos & derivados , Adenosina Trifosfato/metabolismo , Animales , Cromatografía Líquida de Alta Presión , Interacciones Farmacológicas , Lepra/tratamiento farmacológico , Lepra/microbiología , Ratones , Ratones Endogámicos BALB C , Pruebas de Sensibilidad Microbiana , Mycobacterium leprae/genética , Mycobacterium leprae/metabolismo , Receptores Fc/efectos de los fármacos , Timidina/metabolismo , Trimetoprim/farmacologíaRESUMEN
Resistant strains of M. leprae have been reported to the various antileprosy drugs. There is currently no accepted test to identify the susceptibility pattern of M. leprae to the drugs in a short period. The only accepted test is the mouse foot method which takes a long period to yield results. The Fc receptor assay using the ability of viable M. leprae to alter the membrane of the macrophage is well established. It takes only ten days and is inexpensive. In 6 cases of leprosy patients the susceptibility pattern was worked out both with the in vitro Fc receptor assay and the vivo in mouse foot method The results correlated very well leading to the fact that the assay system is reliable. Hence it can be used not only to study the status of a patient, but also to shortlist the number of compounds to be tested on the mouse foot pad as anti-leprosy drug candidates.