RADIOIMMUNOASSAYS FOR THE SULFOXIDE, 7 -HYDROXY AND N41 -OXIDE METABOLITES OF TRIFLUOPERAZINE: DEVELOPMENT AND APPLICATIONS
Date
1985
Authors
Journal Title
Journal ISSN
Volume Title
Publisher
ORCID
Type
Degree Level
Doctoral
Abstract
Trifluoperazine is a piperazine type phenothiazine anti-psychotic agent which is-extensively metabolised to numerous metabo-lites. It is generally considered that the major metabolites of the
phenothiazine antipsychotic agents are involved in the therapeutic response and/or adverse effects of these drugs. Therefore, in order to investigate plasma level—clinical outcome correlations of piperazine type phenothiazine drugs, it would be desirable to develop analytical methods for such metabolites. In particular, the 7-hydroxy and N4'-oxide metabolites of the piperazine type phenothiazine compounds are considered to be active while the sulfoxide has been associated with
clinical deterioration. Since these metabolites are present in low plasma concentrations and are reputed to be unstable at all stages of sample preparation for analysis, sensitive methods of analysis which could be applied directly to plasma samples were desired. Radioimmuno -
assay fits these needs and in view of the simplicity and sample turn-around-time, it is especially suitable for large clinical studies. In this work,radioimmunoassay methods were developed which allowed for the first time the plasma measurement of the sulfoxide, 7 -hydroxy and N4' -
oxide metabolites of trifluoperazine. The applicability of these methods was demonstrated in pilot studies involving the plasma analysis of these metabolites and trifluoperazine after single dose administra—tion to healthy volunteers and dogs.
Description
Keywords
RADIOIMMUNOASSAYS, TRIFLUOPERAZINE
Citation
Degree
Doctor of Philosophy (Ph.D.)
Department
Pharmacy and Nutrition