The metabolism of 2-chloro-11- (4-methyl-1-piperazinyl) dibenzo- (b,f) (1,4) -thiazepine (clotiapine) . 3. the metabolism and excretion in the human
Gauch, R.; Lehner, H.
Il Farmaco; Edizione Pratica 24(2): 100-109
1969
ISSN/ISBN: 0430-0912 PMID: 5780179 Document Number: 5883
The metabolism of the neuroleptic 2-chloro-11-(4-methyl-1-piperazinyl)dibenzo4b,f][1,4]-thiazepine (Clotiapine DCI) and its excretion in human urine is described. Clotiapine is metabolized intensively by humans. Ca. 35% of the orally administered dose is excreted in the form of free (ca. 25%) and conjugated (ca. 10%), polarographically determinable, bases in the urine. The unconjugated compounds could be identified as the following 9 metabolites: 0.1% Clotiapine (I), 2.3% N-desmethyl derivative (II), 2A% sulphoxide (III), 12.7% N-desmethylsulphoxide (IV), 0.01% sulphone (V), 0.05% N-oxide (VII), 6.9% N-oxidesulphoxide (VIII), 0.2% lactamsulphoxide (X), and 0.4% of an unknown compound C. The N-demethylation is very pronounced. N-Oxidation and S-oxidation also take place. The main metabolite is the N-desm. ethylsulphoxide (IV). 4 Phenolic bases were detected after hydrolysis of the conjugated compound fraction.
Document emailed within 1 workday
