Important Metabolites to Measure in Pharmacodynamic Studies of Chlorpromazine

摘要

SummaryPlasma concentrations of chlorpromazine (CPZ) and six metabolites were measured in 12 chronic schizophrenic patients on a fixed dose of CPZ. All six metabolites were measured in significant concentrations, ranging from 12 to 57percnt; of the parent drug concentration. They are listed in order of decreasing mean concentration as follows: chlorpromazine-N-oxide chlorpromazine sulfoxide 7-OH chlorpromazine Nor2chlorpromazine sulfoxide Nor2chlorpromazine Nor1chlorpromazine. CPZ concentrations showed significant correlation with the 7-OH chlorpromazine metabolite concentration. Since these metabolites have been associated with in vitro activity and occur in significant concentrations, it is recommended that all six metabolites be measured in studies correlating drug levels with pharmacodynamic effects.