Metabolism of actisomide in the dog, monkey and man : a novel rearrangement of N-dealkylated metabolites

The metabolism of actisomide, a novel antiarrhythmic agent, was studied in the dog, monkey and man and was found to be more extensive in the monkey than in the dog or man. The major metabolites identified were a piperidinyl hydroxylated metabolite, the mono-N-dealkylated, cyclized and piperidine hyd...

Full description

Saved in:
Bibliographic Details
Published in:European journal of drug metabolism and pharmacokinetics 1992-04, Vol.17 (2), p.145-154
Main Authors: COOK, C. S, ROZEK, L. F, HRIBAR, J, SCHOENHARD, G. L, KARIM, A
Format: Article
Language:English
Subjects:
Adult
Animals
Anti-Arrhythmia Agents - metabolism
Antiarythmic agents
Biological and medical sciences
Carbon Radioisotopes
Cardiovascular system
Dealkylation
Dogs
Feces - chemistry
Humans
Macaca mulatta
Male
Medical sciences
Pharmacology. Drug treatments
Pyrimidinones - metabolism
Species Specificity
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The metabolism of actisomide, a novel antiarrhythmic agent, was studied in the dog, monkey and man and was found to be more extensive in the monkey than in the dog or man. The major metabolites identified were a piperidinyl hydroxylated metabolite, the mono-N-dealkylated, cyclized and piperidine hydroxylated metabolite, and the cyclized and mono-N-dealkylated metabolite. Excretion of the parent drug was higher in urine than in feces in the dog, but in the monkey and man, urinary and fecal excretion of actisomide was similar. In all species the metabolites were primarily excreted in feces.
ISSN:0378-7966
2107-0180
DOI:10.1007/BF03188783