The prolactin response to an antipsychotic drug, bromperidol was studi
ed in 24 schizophrenic in-patients (13 males, 11 females). Eight patie
nts were given 6 mg/day, 8 were given 12 mg/day and 8 were given 18 mg
/day. Duration of treatment was 3 weeks. Plasma concentrations of brom
peridol and reduced bromperidol were measured by high-performance liqu
id chromatography, and that of prolactin was measured by radioimmunoas
say. Bromperidol treatment significantly (P<0.01) increased plasma con
centration of prolactin each week. The mean+/-S.D. of the Delta-prolac
tin (the mean concentration during treatment minus the pretreatment co
ncentration) was 13.3+/-12.4 ng/ml. Multiple regression analysis showe
d that the Delta-prolactin concentration was significantly greater in
females than in males (P<0.05) and correlated to plasma concentrations
of bromperidol (P<0.001) and reduced bromperidol (P<0.0001). These re
sults suggest that the prolactin response to bromperidol treatment dep
end on plasma concentrations of both bromperidol and reduced bromperid
ol and gender, and that reduced bromperidol is involved in the pharmac
ological effects during bromperidol treatment.