Development of radioimmunoassays for trifluoperazine and their application to metabolic studies of the drug

Antisera to trifluoperazine have been raised in New Zealand white rabbits to several different types of immunogens, where there was variation in the length and nature of the side chain attached to the phenothiazine nucleus, as well as in the number of hapten residues coupled to bovine serum albumin. A radioimmunoassay for trifluoperazine has been developed which is capable of quantitating 0.3125 ng ml-1 in a 200 microliter plasma sample, with cross-reactivities to the sulfoxide, 7-hydroxy, and N-desmethyl metabolites of trifluoperazine of the order of less than 1, 11, and 12%, respectively. Some of the investigated antisera were applied to metabolic studies involving trifluoperazine, where it was demonstrated that N-desmethyltrifluoperazine, rather than 7-hydroxytrifluoperazine, was a major metabolite of trifluoperazine in plasma of a volunteer following administration of a single 5 mg oral dose.