Absorption, metabolism and excretion of 14C-sultopride in the rat.
Rats received (14C)-Sultopride (St) in doses of 20 mg/kg by ip. and oral route. After ip.-administration, urinary elimination was 62% of administered dose in 72 hours, fecal excretion, 25% in 96 hours. Conversely, at 120 hours after oral administration, renal elimination was 46% and fecal elimination 34%. From these data 75% absorption of St in rat intestine may be deduced. From total excreted radioactivity (feces plus urine; ip. route) 35% is due to unchanged St. Seven metabolites were isolated from the urine. By comparison of isolated compounds with chemically synthesized putative metabolites using spectrophotometric and radiometric TLC scanning procedures 5 metabolites were identified: O-desmethylated St (DMSt; 20% of total radioactivity excreted), sulfon-desethylated St (SDESt; 13%), 5-pyrrolidine-oxo St (OSt; 3%), the product of hydrolysis of the central amide bond (MESS; 4%) and the secondary metabolite O-desmethyl-oxo St (ODMST; less than 1%). Two metabolites both minor (1% or less), remained unidentified. In guinea-pigs, metabolism of St leads almost exclusively to OSt while in mice, to DMSt.
D000042:Absorption; D000284:Administration, Oral; D000077582:Amisulpride; D000818:Animals; D005243:Feces / Q000032:analysis; D005260:Female; D006168:Guinea Pigs; D007274:Injections, Intraperitoneal; D007408:Intestinal Absorption; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains; D013045:Species Specificity; D013469:Sulpiride / Q000031:analogs & derivatives* / Q000378:metabolism / Q000652:urine
D013469:Sulpiride; D000077582:Amisulpride