The wide variability of perospirone metabolism and the effect of perospirone on prolactin in psychiatric patients.
BACKGROUND
Perospirone was developed in Japan and is used for the treatment of schizophrenia and related illnesses. The authors investigated the relationship between the dosage of perospirone and the plasma levels of perospirone and its active metabolite, ID15036, and also evaluated the impact of the plasma concentrations of perospirone and ID15036 on the plasma prolactin level to examine whether perospirone or ID15036 affected the dopamine D(2) blockade, in psychiatric patients treated with perospirone.


METHODS
The subjects consisted of 21 adults treated with perospirone (4-60 mg/day). The plasma perospirone and ID15036 levels were measured in 21 patients and serum prolactin levels were investigated in 10 male patients with schizophrenia.


RESULTS
The plasma ID15036 level was higher than the plasma perospirone, and a positive correlation was observed between the dosage of perospirone and the ID15036 levels (p=0.032). The 10 male patients showed a positive correlation between the plasma perospirone levels and plasma prolactin levels (r=0.688, p=0.028) and between the plasma ID15036 levels and prolactin levels (r=0.775, p=0.009).


CONCLUSIONS
The plasma levels of ID15036 may have a greater impact on the dopamine D(2) blockade than perospirone in patients treated with perospirone.
Suzuki
Yutaro
Y
Department of Psychiatry, Niigata University Graduate School of Medical and Dental Sciences, Niigata, Japan.
Sawamura
Kazushi
K
Ono
Shin
S
Fukui
Naoki
N
Sugai
Takuro
T
Watanabe
Junzo
J
Tsuneyama
Nobuto
N
Inoue
Yoshimasa
Y
Someya
Toshiyuki
T
D000328:Adult; D000368:Aged; D014150:Antipsychotic Agents / Q000097:blood / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006801:Humans; D007124:Immunoenzyme Techniques; D007206:Individuality; D007211:Indoles / Q000097:blood; D054833:Isoindoles / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D008875:Middle Aged; D011388:Prolactin / Q000097:blood*; D012559:Schizophrenia / Q000188:drug therapy*; D013844:Thiazoles / Q000097:blood / Q000493:pharmacokinetics*
D014150:Antipsychotic Agents; D007211:Indoles; D054833:Isoindoles; D013844:Thiazoles; C494108:hydroxyperospirone; D011388:Prolactin; C065533:perospirone