Excretion and metabolism of intramuscularly administered [14C]-haloperidol decanoate in rats.
Arzneimittelforschung
; 36(3): 453-6, 1986 Mar.
Article
em En
| MEDLINE
| ID: mdl-3707664
ABSTRACT
Urinary, fecal and biliary excretion, together with enterohepatic circulation, of radioactivity were studied after intravenous (50 mg eq/kg) and intramuscular (5 and 50 mg eq/kg) administration of [14C]-haloperidol decanoate in rats. The composition of urinary and biliary metabolites was also examined. The rate of excretion after intravenous administration lowered rapidly with the half-life of about 1.5 days and about 95% of dose was excreted in excreta within 10 days. Shortly after intramuscular administration, the rate of excretion lowered rapidly but then more gradually later (half-lives after administration of 5 and 50 mg eq/kg were 16.4 and 11.2 days, respectively). About 90% of dose was excreted within 42 days after intramuscular administration. About 1.6% of dose/day was excreted in the bile during 15-17 days after intramuscular administration, of which about 30% was reabsorbed within 24 h (enterohepatic circulation). The major urinary metabolite was p-fluorophenylaceturic acid and the biliary metabolite, glucuronide and sulfate of haloperidol. No unchanged decanoate was detected in the excreta.
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Base de dados:
MEDLINE
Assunto principal:
Haloperidol
Limite:
Animals
Idioma:
En
Revista:
Arzneimittelforschung
Ano de publicação:
1986
Tipo de documento:
Article