Abstract
A program has been initiated to study the distribution of lincosaminides and their biologically active metabolites in the whole animal. Using bioautographic tic analysis, profiles of orally administered clindamycin and its metabolic products in the gastrointestinal tract, liver, blood, kidney and carcass of Sprague-Dawley rats have been constructed. The results of these experiments reveal the significant contribution of the N-demethyl metabolite to observed clindamycin antibacterial activity. From kinetic data it is evident that N-demethylclindamycin persists in the body longer than does clindamycin, further adding to its contribution toin vivo activity. The sulfoxide metabolites of clindamycin contribute little to the antibacterial activity of this drug. Over the time period studied, clindamycin and its sulfoxide displayed biphasic concentration-time curves, while N-demethylclindamycin and its sulfoxide were continuously increasing in concentration in the gastrointestinal tract indicating reabsorption or return through the biliary system. A material balance revealed that 50% of the administered dose of clindamycin was rapidly metabolized to antibacterially inactive metabolites.
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