Effects of various factors including the CYP2D6 genotype and coadministration of flunitrazepam on the steady-state plasma concentrations of bromperidol and its reduced metabolite

Psychopharmacology

Volumn 135, Issue 4, 1998, Pages 333-337

  Suzuki, A ^a   Otani, K ^b   Mihara, K ^a   Yasui, N ^a   Kondo, T ^a   Tokinaga, N ^a   Furukori, H ^a   Kaneko, S ^a   Inoue, Y ^c   Hayashi, K ^d  

^a HIROSAKI UNIVERSITY   (Japan)

^b YAMAGATA UNIVERSITY   (Japan)

^c Yoshitomi Pharmaceutical Industries Ltd   (Japan)

^d GUNMA UNIVERSITY   (Japan)

Author keywords

Bromperidol; CYP2D6 genotype; Flunitrazepam; Metabolism; Plasma concentration; Reduced bromperidol

Indexed keywords

BROMPERIDOL; CYTOCHROME P450; DRUG METABOLIZING ENZYME; FLUNITRAZEPAM; HALOPERIDOL;

ADULT; AGED; ARTICLE; CLINICAL TRIAL; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG METABOLISM; DRUG OXIDATION; ENZYME STRUCTURE; FEMALE; HUMAN; HUMAN TISSUE; LIVER CLEARANCE; MAJOR CLINICAL STUDY; MALE; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; SCHIZOPHRENIA; SEX DIFFERENCE; SMOKING; STRUCTURE ACTIVITY RELATION;

ADOLESCENT; ADULT; AGED; AGING; ANTI-ANXIETY AGENTS; ANTIPSYCHOTIC AGENTS; BIOTRANSFORMATION; CYTOCHROME P-450 CYP2D6; FEMALE; FLUNITRAZEPAM; GENOTYPE; HALF-LIFE; HALOPERIDOL; HUMANS; MALE; MIDDLE AGED; OXIDATION-REDUCTION; SCHIZOPHRENIA; SEX CHARACTERISTICS; SMOKING;

EID: 15144355309     PISSN: 00333158     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002130050519     Document Type: Article

References (42)

1. Benfield P, Ward A, Clark BG, Jue SG (1988) Bromperidol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in psychoses. Drugs 35: 670 684
2. Bertilsson L, Dahl ML (1996) Polymorphic drug oxidation: relevance to the treatment of psychiatric disorders. CNS Drugs 5:200 223
3. Bock KW, Schrenk D, Forsler A, Griese EU, Morike K, Broekmeier D, Eichelhaum M (1994) The influence of environmental and genetic factors on CYP2D6. CYP1A2 and UDP-glucuronosyl transferases in man using sparteine, caffeine, and paracetamol as probes. Pharmacogenetics 4:209 218
4. Brinn R, Brosen K, Gram LF, Haghfelt T, Otton SV (1986) Sparteine oxidation is practically abolished in quinidine-treated patients. Br J Clin Pharmacol 22:194 197
5. Broly F, Gaedigk A, Heim M, Eichelbaum M, Morike K, Meyer UA (1991) Debrisoquine/sparteine hydroxylation genotype and phenotype: analysis of common mutations and alleles of CYP2D6 in a European population. DNA Cell Biol 10:545-558
6. Dahl ML, Johansson I, Palmertz MP, Ingelman-Sundberg M, Sjoqvist F (1992) Analysis of the CYP2D6 gene in relation to debrisoquin and desipramine hydroxylation in a Swedish population. Clin Pharmacol Ther 51:12 17
7. Dahl ML, Yue QY, Roh HK, Johansson I, Sawe J, Sjoqvist F, Bertilsson L (1995) Genetic analysis of the CYP2D locus in relation to debrisoquine hydroxylation capacity in Korean, Japanese and Chinese subjects. Pharmacogenetics 5:159 164
8. Daly AK, Brockmoller J. Broly F, Eichelbaum M, Evans WE, Gonzalez FJ, Huang JD, Idle JR, Ingelman-Sundberg M, Ishizaki T, Jacqz-Aigrain E, Meyer UA, Nebert DW, Steen VM, Wolf CR, Zanger UM (1996) Nomenclature for human CYP2D6 alleles. Pharmacogenetics 6:193-201
9. Ereshefsky L, Jann MW, Saklad SR, Davis CM, Richards AL, Burch NR (1985) Effects of smoking on fluphenazine clearance in psychiatric inpatients. Biol Psychiatry 20:329-352
10. Evert B, Griese EU, Eichelbaum M (1994) A missense mutation in exon 6 of the CYP2D6 gene leading to a histidine 324 to proline exchange is associated with the poor metabolizer phenotype of sparteine. Naunyn Schmiedeberg's Arch Pharmacol 350:434 439
11. Froemming JS, Lam YWK, Jann MW, Davis CM (1989) Pharmacokinetics of haloperidol. Clin Pharmacokinet 17:396-423
12. Gaedigk A, Blum M, Gaedigk R, Eichelbaum M, Meyer UA (1991) Deletion of the entire cytochrome P450 CYP2D6 gene as a cause of impaired drug metabolism in poor metabolizers of the debrisoquine/sparteine polymorphism. Am J Hum Genet 48:943 950
13. Haring C, Barnas C, Saria A, Humpel C, Fleischhacker WW (1989) Dose-related plasma levels of clozapine. J Clin Psychopharmacol 9:71-72
14. Heim M, Meyer UA (1990) Genotyping of poor metabolizers of debrisoquine by allele-specific PCR amplification. Lancet 336:529-532
15. Hikida K, Inoue Y, Miyazaki T, Kojima N, Ohkura Y (1989) Determination of bromperidol in serum by automated column-switching high-performance liquid chromatography. J Chromatogr 495:227-234
16. Johansson I, Lundqvist E, Bertilsson L, Dahl ML, Sjoqvist F, Ingelman-Sundberg M (1993) Inherited amplification of an active gene in the cytochrome P450 CYP2D locus as a cause of ullrarapid metabolism of debrisoquine. Proc Natl Acad Sci USA 90: 11825-11829
17. Johansson I, Oscarson M, Yue QY, Bertilsson L, Sjoqvist F, Ingelman-Sundberg M (1994) Genetic analysis of the Chinese cytochrome P450 locus: characterization of variant CYP2D6 genes present in subjects with diminished capacity for debrisoquine hydroxylation. Mol Pharmacol 46:452-459
18. Kallio J, Huuponen R, Seppala M, Sako E, IIsalo E (1990) The effects of β-adrenoceptor antagonists and levomepromazine on the metabolic ratio of debrisoquine. Br J Clin Pharmacol 30:638-643
19. Kondo T, Tanaka O, Otani K, Mihara K, Tokinaga N, Kaneko S, Chiba K, Ishizaki T (1996) Possible inhibitory effect of diazepam on the metabolism of zotepine, an antipsychotic drug. Psychopharmacology 127:311-314
20. Luurila H, Olkkola KT, Neuvonen PJ (1996) Interaction between erythromycin and the benzodiazepines diazepam and flunitrazepam. Pharmacol Toxicol 78:117-122
21. Mattila MAK, Larni HM (1980) Flunitrazepam: a review of its pharmacological and therapeutic use. Drugs 20:353-374
22. Mazure CM, Nelson JC, Jatlow PI, Kincare P, Bowers MB (1990) The relationship between blood perphenazine levels, and side effects. J Clin Psychiatry 51:330-334
23. Miller DD, Kelly MW, Perry PJ, Coryell WH (1990) The influence of cigarette smoking on haloperidol pharmacokinetics. Biol Psychiatry 28:529-531
24. Oida T, Terauchi Y, Yoshida K, Kagemoto A, Sekine Y (1989) Use of antisera in the isolation of human specific conjugates of haloperidol. Xenobiotica 7:781-793
25. Olkkola KT, Aranko K, Luurila H, Hiller A, Saarnivaara L, Himberg JJ, Neuvonen PJ (1993) A potentially hazardous interaction between erythromycin and midazolam. Clin Pharmacol Ther 53:298-305
26. Otani K, Kondo T, Kaneko S, Hirano T, Mihara K, Fukushima Y (1992) Steady-state serum kinetics of zotepine. Hum Psychopharmacol 7:331-336
27. Otani K, Ishida M, Yasui N, Kondo T, Mihara K, Suzuki A, Kaneko S, Inoue Y, Shibata M, Ikeda K (1997a) No effect of the anticholinergic drugs trihexyphenydil and biperiden on the plasma concentrations of bromperidol and its reduced metabolite. Ther Drug Monk 19:165-168
28. Otani K, Ishida M, Yasui N, Kondo Y, Mihara K, Suzuki A, Furukori H, Kaneko S, Inoue Y (1997b) Interaction between carbamazepine and bromperidol. Eur J Clin Pharmacol 52:219-222
29. Otton SV, Inaba T, Kalow W (1984) Competitive inhibition of sparteine oxidation in human liver by β-adrenoceptor antagonists and other cardiovascular drugs. Life Sci 18:254-262
30. Rasmussen BB, Brosen K (1996) Determination of urinary metabolites of caffeine for the assessment of cylochrome P4501A2. xanthine oxidase, and N-acetyltransferase activity in humans. Ther Drug Monk 18:254-262
31. Roh HK, Dahl ML, Johansson I, Ingelman-Sundberg M, Cha YN, Bertilsson L (1996) Debrisoquine and S-mephenytoin hydroxylation phenotypes and genotypes in a Korean population. Pharmacogenetics 6:441-447
32. Saxena R, Shaw GL, Relling MV, Frame JN, Moir DT, Evans WE, Caporaso N, Weiffenbach B (1994) Identification of a new variant CYP2D6 allele with a single base deletion in exon 3 and its association with the poor metabolizer phenotype. Hum Mol Genet 3:923-926
33. Shvartsburd A, Dekirmenjian H, Smith RC (1983) Blood levels of haloperidol in schizophrenic patients. J Clin Psychopharmacol 3:7-12
34. Someya T, Inaba T, Tyndale RF, Tang SW, Takahashi S (1991) Conversion of bromperidol to reduced bromperidol in human liver. Neuropsychopharmacology 5:177-182
35. Spina E, Marlines C, Caputi AP, Cobaleda J, Pinas B, Carrillo JA, Benitez J (1991) Debrisoquine oxidation phenotype during neuroleptic monotherapy. Eur J Clin Pharmacol 41:467-470
36. Steen VM, Andreassen OA, Daly AK, Tefre T, Borresen AI, Idle JR, Gulbrandsen AK (1995) Detection of the poor metabolizer-associated CYP2D6 (D) gene deletion allele by long-PCR technology. Pharmacogenetics 5:215-223
37. Suzuki A, Otani K, Ishida M, Yasui N, Kondo T, Mihara K, Kaneko S, Inoue Y, Shibata M, Ikeda K (1997) Levomepromazine, but not thioridazine, increases plasma concentrations of bromperidol and its reduced metabolite. Ther Drug Monit 19:261-264
38. Watkins PB (1994) Noninvasive tests of CYP3A enzymes. Pharmacogenetics 4:171-184
39. Wode-Helgodt B, Alfredsson G (1981) Concentrations of chlorpromazine and two of its active metabolites in plasma and cerebrospinal fluid of psychotic patients treated with fixed drug doses. Psychopharmacology 73:55-62
40. Wong FA, Bateman CP, Shaw CJ, Patrick JE (1983) Biotransformation of bromperidol in rat, dog, and man. Drug Metab Dispos 11:301-307
41. Yue QY, Tomson T, Sawe J (1994) Carbamazepine and cigarette smoking induce differentially the metabolism of codeine in man. Pharmacogenetics 4:193-198
42. Zar H (1996) Biostatistical analysis, 3rd edn. Prentice Hall, Upper Saddele River, N.J.