Disposition of /sup 14/C-acetohydroxamic acid and /sup 14/C-acetamide in the rat
Acetohydroxamic acid (AHA) has been identified as a potential agent for the treatment of infection-induced staghorn renal calculi in patients. The pharmacokinetics and disposition of /sup 14/C-acetamide have been evaluated in rats following iv and oral administration. The results of these experiments suggest that, following oral administration to rats, AHA is absorbed very rapidly from the gastrointestinal tract and is metabolized to acetamide and CO/sub 2/. Approximately 50-56% of the iv dose and 40-49% of the oral dose of /sup 14/C-AHA is excreted in the urine, suggesting a significant nonrenal elimination pathway for AHA and metabolite(s). Administration of /sup 14/C-acetamide to rats revealed that the compound is predominantly eliminated via the renal route, accounting for 68% of the administered radioactive dose. However, approximately 30% of the dose in the case of both AHA and acetamide could not be recovered, either in the urine or in the breath, during the 72-hr period of the experiment. This suggests that acetamide, may undergo further metabolism to get incorporated into the acetate pool. This would result in very slow elimination of the remaining activity as /sup 14/CO/sub 2/ or as another unknown metabolite.
- Research Organization:
- Univ. of Houston, TX
- OSTI ID:
- 5765777
- Journal Information:
- Drug Metab. Dispos.; (United States), Vol. 12:4
- Country of Publication:
- United States
- Language:
- English
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ACETAMIDE
PHARMACOLOGY
CARBON 14 COMPOUNDS
INTESTINAL ABSORPTION
HYDROXAMIC ACIDS
CALCULI
CARBON DIOXIDE
INTRAVENOUS INJECTION
KIDNEYS
ORAL ADMINISTRATION
RATS
ABSORPTION
AMIDES
AMINES
ANIMALS
BODY
CARBON COMPOUNDS
CARBON OXIDES
CHALCOGENIDES
HYDROXY COMPOUNDS
INJECTION
INTAKE
LABELLED COMPOUNDS
MAMMALS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
OXIDES
OXYGEN COMPOUNDS
RODENTS
UPTAKE
VERTEBRATES
550501* - Metabolism- Tracer Techniques