Disposition and biotransformation of the antipsychotic agent olanzapine in humans

Drug Metabolism and Disposition

Volumn 25, Issue 1, 1997, Pages 81-93

  Kassahun, Kelem ^a   Mattiuz, Edward ^b   Nyhart Jr , Eldon ^b   Obermeyer, Boyd ^b   Gillespie, Todd ^b   Murphy, Anthony ^b   Goodwin, R Michael ^b   Tupper, David ^b   Callaghan, J Thomas ^b   Lemberger, Louis ^b  

^a ELI LILLY AND COMPANY   (United States)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

OLANZAPINE;

ADULT; ARTICLE; DRUG DISPOSITION; DRUG GLUCURONIDATION; DRUG HYDROXYLATION; DRUG TRANSFORMATION; HUMAN; MALE; NORMAL HUMAN; PRIORITY JOURNAL; PSYCHOSIS;

ADULT; ANTIPSYCHOTIC AGENTS; BENZODIAZEPINES; BIOTRANSFORMATION; CARBON RADIOISOTOPES; FECES; HUMANS; MALE; PIRENZEPINE; URINE;

EID: 0031030609     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (17)

1. N. A. Moore, N. C. Tye, M. S. Axton, and F. C. Risius: The behavioral pharmacology of olanzapine, a novel "atypical" antipsychotic agent. J. Pharmacol. Exp. Ther. 262, 545-551 (1992).
2. N. A. Moore, D. O. Calligaro, D. T. Wong, F. Bymaster, and N. C. Tye: The pharmacology of olanzapine, and other new antipsychotic agents. Curr. Opin. Invest. Drugs 2, 281-293 (1993).
3. R. J. Miller and C. R. Hiley: Antimuscarinic properties of neuroleptics and drug-induced parkinsonism. Nature 248, 596-597, (1974).
4. D. Coulemans, Y. Gelders, M. Hoppenbrouwers, and A. Reyntijene: Proceedings of the 14th CINP Congress, Florence, Italy, 1984.
5. H. Y. Meltzer and J. F. Nash: Effects of antipsychotic drugs on serotonin receptors. Pharmacol. Rev. 43, 587-604 (1991).
6. C. M. Beasley, G. Tollefson, P. Tran, W. Satterlee, T. Sanger, and S. Hamilton: Olanzapine versus placebo and haliperidol. Acute phase results of the North American double-blind olanzapine trial. Neuropsychopharmacology 14, 111-123 (1996).
7. C. M. Beasley, T. Sanger, W. Satterlee, G. Tollefson, P. Tran, and S. Hamilton: Olanzapine versus placebo: results of a double-blind, fixed-dose olanzapine trial. Psychopharmacology 124, 159-167 (1996).
8. D. S. Baldwin and S. A. Montgomery: First clinical experience with olanzapine (LY170053): results of an open-label safety and dose-ranging study in patients with schizophrenia. Int. Clin Psychopharmacol 10, 239-244 (1995).
9. D. O. Calligaro, J. Fairhurst, T. M. Hotten, N. A. Moore, and D. E. Tupper: The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053). Bioorg. Med. Chem. Lett. in press.
10. K. Bowden, I. M. Heilbron, E. R. Jones, and B. C. L. Weedon: Researches on acetylenic compounds. Part 1. The preparation of acetylenic ketones by oxidation of acetylenic carbinols and glycols. J. Chem. Soc. 39-45 (1946).
11. J. T. Catlow, R. D. Barton, M. Clemens, T. A. Gillespie, M. Goodwin, and S. P. Swanson: Analysis of olanzapine in human plasma utilizing reversed-phase high performance liquid chromatography with electrochemical detection. J. Chromatogr. B 68, 85-90 (1995).
12. E. Mattiuz, R. Franklin, T. Gillespie, A. Murphy, J. Bernstein, A. Chiu, T. Hotten, and K. Kassahun: Disposition and metabolism of olanzapine in mice, dogs and rhesus monkeys. Drug Metab. Dispos. in press.
13. B. J. Ring, J. Catlow, T. J. Lindsay, T. Gillespie, L. K. Roskos, B. J. Cerimele, S. P. Swanson, M. A. Hamman, and S. A. Wrighton: Identification of the human cytochromes P450 responsible for the in vitro formation of the major oxidative metabolites of the antipsychotic agent olanzapine. J. Pharmacol. Exp. Ther. 276, 658-666 (1996).
14. J. A. Chiu and R. B. Franklin: Analysis and pharmacokinetics of olanzapine (LY170053) and two metabolites in rat plasma using reversed-phase HPLC with electrochemical detection. J. Pharmaceu. Biomed. Anal. 14, 609-615 (1996).
15. M. W. Jann, S. R. Grimsley, E. C. Gray, and W. H. Chang: Pharmacokinetics and pharmacodynamics of clozapine. Clin. Pharmacokinet. 24, 161-176 (1993).
16. R. Gauch and W. Michaelis: The metabolism of 8-chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine (clozapine) in mice, dogs and human subjects. Farm. Ed. Prat. 26, 667-681 (1971).
17. V. B. Stock, G. Spiteller, and R. Heipertz: Exchange of aromatically bound halogen for OH-and SCH3-groups in metabolizing clozapine in the human organism. Arzneim. Forsch. Drug Res. 27, 982-990 (1977).