Assay Procedures for Thioridazine, Trifluoperazine, and Their Sulfoxides and Determination of Urinary Excretion of These Compounds in Mental Patients

Autor: West, Norman R., Rosenblum, Marcus P., Sprince, Herbert, Gold, Simon, Boehme, Diethelm H., Vogel, Wolfgang H.
Zdroj: Journal of Pharmaceutical Sciences; March 1974, Vol. 63 Issue: 3 p417-420, 4p
Abstrakt: Assay procedures for thioridazine, trifluoperazine, and their sulfoxides are described which are rapid, simple, and relatively specific (about 0.5 μg of drug or sulfoxide/ml). Chlorpromazine interferes with the determination of these drugs whereas imipramine, desipramine, biperidin, and haloperidol do not. The urinary concentrations of these four compounds were determined in 24-hr samples and timed-interval collections obtained from patients with schizophrenic reactions. Thioridazine and trifluoperazine seem to be extensively metabolized, and less than 1% of the unchanged drugs and 2–6% of the corresponding sulfoxides were observed in 24-hr urine samples. The ratio between the parent drug and its respective sulfoxide was fairly constant. Urinary excretions of thioridazine and its sulfoxide were dose independent, whereas those of trifluoperazine and its sulfoxide showed a strong dose dependency. Timed-interval collections during an 8-hr period showed rather consistent excretions of unchanged trifluoperazine and thioridazine but wide intra and interpatient variations in the sulfoxide excretions.
Databáze: Supplemental Index