02264nas a2200385 4500000000100000008004100001260001300042653002500055653001200080653001200092653003300104653003000137653001100167653002100178653002300199653001200222653000900234653002400243653001500267653002500282653001500307653001500322100001200337700001400349700001500363700001300378700001500391245023600406856005900642300001000701490000700711050003200718520111400750022001401864 1995 d c1995 Mar10aAdministration, Oral10aAnimals10aDapsone10aDrug Administration Schedule10aDrug Therapy, Combination10aFemale10aFluoroquinolones10aLeprostatic Agents10aleprosy10aMice10aMice, Inbred BALB C10aMice, Nude10aMycobacterium leprae10aQuinolones10aRifamycins1 aGidoh M1 aMatsuki G1 aTsutsumi S1 aHIDAKA T1 aNakamura S00aInhibition of the multiplication of Mycobacterium leprae in nude mice by intermittent administration of a new rifamycin derivative, 3'-hydroxy-5'-(4-isobutyl-1-piperazinyl)benzoxazinorifamycin (KRM-1648) combined with sparfloxacin. uhttp://leprev.ilsl.br/pdfs/1995/v66n1/pdf/v66n1a06.pdf a39-470 v66 aInfolep Library - available3 a

Inhibition of the multiplication of Mycobacterium leprae in the footpads of nude mice by the oral administration of sparfloxacin, a new quinolone, and 3'-hydroxy-5'-(4-isobutyl-1-piperazinyl)benzoxazinorifamycin (KRM-1648), selected from a series of newly synthesized benzoxazinorifamycins, was studied. When the 2 drugs were administered alternately at intervals of 3 or 4 days, (i.e., each drug was administered once weekly), or simultaneously once weekly, between 3 and 5 months after inoculation of nude mice with M. leprae, 10 mg sparfloxacin and 0.6 mg KRM-1648 per kg bodyweight were sufficient to prevent multiplication of the organisms. Only partial inhibition of multiplication was achieved by alternate administration of 5 mg sparfloxacin and 0.3 mg KRM-1648 per kg, as was the case for 20 mg sparfloxacin per kg or 1 mg KRM-1648, each drug administered alone once weekly. The addition to these 2 drugs of dapsone, administered in the diet in a concentration of 0.001 g per 100 g, enhanced their effect. The potential usefulness of multidrug regimens including these compounds is considered.

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