Butaperazine dimaleate metabolism

Abstract

1. 2 - [1 - ¹⁴C]Butyryl - 10 - [3 - (4 - methylpiperazin - 1 - yl)propyl]phenothiazine (butaperazine) was synthesized and its metabolism, excretion and distribution studied in rats and dogs.

2. A specific fluorescent method for butaperazine is described, and blood levels have been determined in dogs and humans following oral dosing.

3. Two compounds, resulting from hydroxylation of the phenothiazine ring and N-demethylation, are the major metabolites. The sulphoxide, sulphone and a reduction product of the butyryl side chain carbonyl group are minor metabolites.

4. The drug appears to be rapidly absorbed, undergoes biliary excretion and is excreted primarily in the faeces of rats and dogs.