The metabolism of a bronchodilator procaterol HCL in the rat in vitro and in vivo.
1. The metabolism of the bronchodilator, 5-(1-hydroxy-2-isopropylamino-butyl)-8-hydroxycarbostyril hydrochloride hemihydrate (procaterol HCl), has been studied in vitro and in vivo after oral and intravenous administration to rats. 2. The recovery of [14 C] procaterol HCl and its metabolites in 72 h was about 42% each in urine and faeces for an oral dose (30 mg/kg) and about 53% in urine and 33% in faeces for an intravenous dose (30 mg/kg). 3. Six metabolites in rat excreta were identified as procaterol glucuronide, 5-(2-amino-1-hydroxybutyl)-8-hydroxycarbostyril (desisopropylprocaterol), 5-formyl-8-hydroxycarbostyril (5-formyl-8-HCS), 8-hydroxycarbostyril (8-HCS), procaterol sulphate and unchanged procaterol. 4. In experiments in vitro, procaterol HCl was metabolized into desisopropylprocaterol, 5-formyl-8-HCS, and their conjugates, by rat liver 9000 g supernatant fraction, but not by preparations of kidney, lung and small intestine. Conjugation of procaterol HCl with glucuronic acid occurred in liver and small intestine preparations.
D000605:Amino Alcohols / Q000378:metabolism*; D000818:Animals; D001993:Bronchodilator Agents / Q000378:metabolism*; D005243:Feces / Q000032:analysis; D005965:Glucuronates / Q000096:biosynthesis; D006868:Hydrolysis; D006912:Hydroxyquinolines / Q000378:metabolism; D066298:In Vitro Techniques; D007421:Intestine, Small / Q000378:metabolism; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D008168:Lung / Q000378:metabolism; D008297:Male; D051381:Rats
D000605:Amino Alcohols; D001993:Bronchodilator Agents; D005965:Glucuronates; D006912:Hydroxyquinolines