Details

Autor(en) / Beteiligte

• Breyer, Ursula
• Gaertner, Hans Jörg
• Prox, Axel

Titel

Formation of identical metabolites from piperazine- and dimethylamino-substituted phenothiazine drugs in man, rat and dog

Ist Teil von

• Biochemical pharmacology, 1974-01, Vol.23 (2), p.313-322

Ort / Verlag

England: Elsevier Inc

Erscheinungsjahr

1974

Link zum Volltext

Quelle

Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)

Beschreibungen/Notizen

• Degradation of the piperazine ring in the phenothiazine drugs perazine, trifluoperazine, fluphenazine, prochlorperazine and perphenazine in vivo leads to the formation of γ-(phenothiazinyl-10)-propylamine (PPA) and of its ring-substituted analogues CF 3-PPA and Cl-PPA. The sulfoxides of these metabolites have been identified as urinary biotransformation products in patients ingesting perazine or fluphenazine, in rats treated chronically with perazine, trifluoperazine, prochlorperazine or perphenazine, and in a dog given fluphenazine. The structures of the compounds have been confirmed by mass spectrometry. The primary amines are also known metabolites of dimethylamino-substituted phenothiazines, since PPA results from didemethylation of promazine, and CF 3-PPA and Cl-PPA (= nor 2-chlorpromazine) are formed from triflupromazine and chlorpromazine, respectively.