Plasma concentrations of timiperone and its reduced metabolite in the patients on timiperone

Psychiatry and Clinical Neurosciences

Volumn 52, Issue 5, 1998, Pages 535-540

  Shimoda, Kazutaka ^a   Someya, Toshiyuki ^b   Morita, Sachiyo ^a   Hirokane, Genta ^a   Yokono, Aya ^a   Shibasaki, Morikazu ^c   Takahashi, Saburo ^d  

^a SHIGA UNIVERSITY OF MEDICAL SCIENCE   (Japan)

^b NIIGATA UNIVERSITY   (Japan)

^c Shiga Pref Mental Health Center   (Japan)

^d National Hospital Organization   (Japan)

Author keywords

Haloperidol; Ketone reductase; Reduced haloperidol; Reduced timiperone; Reduction; Timiperone

Indexed keywords

HALOPERIDOL; KETONE REDUCTASE; OXIDOREDUCTASE; TIMIPERONE; UNCLASSIFIED DRUG;

ADULT; ARTICLE; BODY WEIGHT; CLINICAL ARTICLE; DRUG BLOOD LEVEL; DRUG MECHANISM; DRUG METABOLISM; ENZYME ACTIVITY; ENZYME KINETICS; FEMALE; HUMAN; HUMAN CELL; HUMAN TISSUE; MALE; ORAL DRUG ADMINISTRATION; PREDICTION; SCHIZOPHRENIA;

ADOLESCENT; ADULT; ANTIPSYCHOTIC AGENTS; BUTYROPHENONES; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; HUMANS; MALE; MIDDLE AGED; OXIDATION-REDUCTION; SCHIZOPHRENIA; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0031736173     PISSN: 13231316     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1440-1819.1998.00421.x     Document Type: Article

References (19)

1. Yamasaki T, Kojima H, Sakurai T et al. Pharmacological studies on timiperone, a new neuroleptic drug, part I. Arzneim-Forsch. Drug Res. 1981; 31: 701-707.
2. 3H-spiroperidol binding to rat striatal dopamine receptors. Eur. J. Pharmacol. 1979; 59: 245-251.
3. Kariya T, Shimozono Y, Itoh H et al. A comparison of the clinical effects of timiperone, a new butyrophenone derivative, and a haloperidol on schizophrenia using double-blind technique. J. Int. Med. Res. 1983; 11: 66-77.
4. Nakazawa T, Ohara K, Sawa Y et al. Comparison of efficacy of timiperone, a new butyrophenone derivative, and clocapramine in schizophrenia: A multicenter double-blind study. J. Int. Med. Res. 1983; 11: 247-258.
5. Tachizawa H, Sudo K, Sasano H, Sano M. Disposition and metabolism of timiperone in the rat, dog, and monkey. Drug Metab. Dispos. 1981; 9: 442-8.
6. Korpi ER, Costakos DT, Wyatt RJ. Rapid formation of reduced haloperidol in guinea pigs following haloperidol administration. Acta Pharmacol. Toxicol. 1985; 56: 94-98.
7. Inaba T, Kovacs J. Haloperidol reductase in human and guinea pig livers. Drug Metab. Dispos. 1989; 17: 330-333.
8. Inaba T, Kalow W, Someya T, Takahaski S, Cheung SW, Tang SW. Haloperidol reduction can be assayed in human red blood cells. Can. J. Physiol. Pharmacol. 1989; 67: 1468-1469.
9. Ereshefsky L, Davis CM, Harrington CA et al. Haloperidol and reduced haloperidol plasma levels in selected schizophrenic patients. J. Clin. Psychopharmacol. 1984; 4: 138-142.
10. Shostak M, Perel JM, Stiller RL, Wyman W, Curran S. Plasma haloperidol and clinical response: A role for reduced haloperidol in antipsychotic activity. J. Clin. Psychopharmacol. 1987; 7: 394-400.
11. Ko GN, Korpi ER, Kirsh DG. Haloperidol and reduced haloperidol concentrations in plasma and red blood cells from chronic schizophrenic patients. J. Clin. Psychopharmacol. 1989; 9: 186-190.
12. Shimoda K, Shibasaki M, Inaba T, Someya T, Cheung SW, Takahashi S. Carbonyl reduction of timiperone in human liver cytosol. Pharmacol. Toxicol. 1998 (in press).
13. American Psychiatric Association. Diagnostic and Statistical Manual of Mental Disorders (3rd edn, revised). The American Psychiatric Association, Washington DC, 1987.
14. Someya T, Takahashi S, Shibasaki M, Inaba T, Cheung SW, Tang SW. Reduced haloperidol/haloperidol ratios in plasma: Polymorphism in Japanese psychiatric patients. Psychiatry Res. 1990; 31: 111-120.
15. Someya T, Shibasaki M, Kato T, Noguchi T, Ishida N, Takahashi S. Haloperidol reductase activity in red blood cells from oriental patients on haloperidol. Prog. Neuropsychopharmacol. Biol. Psychiatry 1991; 15: 275-278.
16. Young D, Midha KK, Fossler MJ et al. Effect of quinidine on the interconversion kinetics between haloperidol and reduced haloperidol in humans: Implication for the involvement of cytochrome P450IID6. Eur. J. Clin. Pharmacol. 1993; 44: 433-438.
17. Perry PJ, Miller DD, Arndt SV, Smith DA, Holman TL. Haloperidol dosing requirements: The contribution of smoking and nonlinear pharmacokinetics. J. Clin. Psychopharmacol. 1993; 13: 46-51.
18. Someya T, Inaba T, Tyndale RF, Tang SW, Takahashi S. Conversion of bromperidol to reduced bromperidol in human liver. Neuropsychopharmacology 1991; 5: 177-182.
19. Wong JMY, Mahon WA, Kalow W, Inaba T. Carbonyl (phenone) reductase in human liver: Structure activity relationship among substrate. Drug Metab. Dispos. 1992; 20: 465-466.