title: The wide variability of perospirone metabolism and the effect of perospirone on prolactin in psychiatric patients.
abstract: 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.
authors.affiliation: Department of Psychiatry, Niigata University Graduate School of Medical and Dental Sciences, Niigata, Japan.
authors.forename: Yutaro
authors.initials: Y
authors.lastname: Suzuki
authors.forename: Kazushi
authors.initials: K
authors.lastname: Sawamura
authors.forename: Shin
authors.initials: S
authors.lastname: Ono
authors.forename: Naoki
authors.initials: N
authors.lastname: Fukui
authors.forename: Takuro
authors.initials: T
authors.lastname: Sugai
authors.forename: Junzo
authors.initials: J
authors.lastname: Watanabe
authors.forename: Nobuto
authors.initials: N
authors.lastname: Tsuneyama
authors.forename: Yoshimasa
authors.initials: Y
authors.lastname: Inoue
authors.forename: Toshiyuki
authors.initials: T
authors.lastname: Someya
mesh_terms: 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*
chemical_list: D014150:Antipsychotic Agents; D007211:Indoles; D054833:Isoindoles; D013844:Thiazoles; C494108:hydroxyperospirone; D011388:Prolactin; C065533:perospirone