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Abstract
1. The metabolism of the bronchodilator, 5-(1-bydroxy-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 [14C]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 desisopropyl-procaterol, 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.