Abstract
After the oral administration of 35Schlorpropamide (CPA) to male rats, radioactivity circulated in plasma largely as unchanged drug (95% of total 35S activity from 0 to 48 hr) and disappeared from plasma with an average half-life of 13.6 hr. Approximately 80% of dose was recovered from urine and 12% from feces in 264 hr. Chlorobenzenesulfonylurea (CBSU) accounted for 55% of urine 35S activity, whereas unchanged drug accounted for 25%. Two polar hydroxylated metabolites, 2-hydroxy-CPA and 3-hydroxy-CPA, each accounted for 10% of activity excreted with rat urine. After oral administration to beagle dogs, 35S activity also circulated in plasma largely as unchanged drug (92%) and dissapeared with a half-life of 15.7 ± 2.7 hr. Approximately 80% of dose was recovered from urine and 7% from feces. Approximately 85% of urinary radioactivity was excreted as unchanged CPA, whereas 13% was present as CBSU and less than 2% was recovered as 2-hydroxy-CPA and 3-hydroxy-CPA. Chlorobenzenesulfonamide was not isolated as a metabolite from either species but was recovered from urine and plasma under certain conditions as an apparent degradation product of CBSU.
Footnotes
- Received September 20, 1973.
- Copyright © 1974 by The American Society for Pharmacology and Experimental Therapeutics
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