Incremental dosage of the new antipsychotic mazapertine induces tolerance to cardiovascular and cognitive effects in healthy men

Clinical Pharmacology and Therapeutics

Volumn 59, Issue 6, 1996, Pages 675-685

  Kleinbloesem, Cornelis H ^a   Jaquet Müller, Françoise ^b   Al Hamdan, Yousif ^b   Baldauf, Cornelia ^b   Gisclon, Lee ^b   Wesnes, Keith ^b   Curtin, Christopher R ^b   Stubbs, R John ^b   Walker, Sally A ^b   Brunner Ferber, Françoise ^b  

^a Clin Pharma Research AG   (Switzerland)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

MAZAPERTINE; NEUROLEPTIC AGENT; PLACEBO; UNCLASSIFIED DRUG;

ADULT; ARTICLE; CARDIOVASCULAR EFFECT; CLINICAL TRIAL; COGNITION; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG EFFECT; DRUG TOLERANCE; HEADACHE; HEART OUTPUT; HUMAN; HUMAN EXPERIMENT; HYPOTENSION; MALE; NAUSEA; NERVOUSNESS; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; ORTHOSTATIC HYPOTENSION; PRIORITY JOURNAL; PROLACTIN BLOOD LEVEL; RANDOMIZED CONTROLLED TRIAL; SWEATING; VERTIGO; VOLUNTEER;

ADMINISTRATION, ORAL; ADULT; ANTIPSYCHOTIC AGENTS; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; COGNITION; DOPAMINE ANTAGONISTS; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; DRUG TOLERANCE; HALF-LIFE; HEMODYNAMIC PROCESSES; HUMANS; HYPOTENSION, ORTHOSTATIC; MALE; MIDDLE AGED; PIPERAZINES; PSYCHOMOTOR PERFORMANCE;

EID: 12644300660     PISSN: 00099236     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0009-9236(96)90008-9     Document Type: Article

References (18)

1. Black DW, Yates WR, Andreasen NC. Schizophrenia, schzophreniform disorder and delusional (paranoid) disorders. In: Talbott JA, Hales RE, Yudofsky SC, eds. The American Psychiatric Press textbook of psychiatry. 1st ed. Washington, DC: American Psychiatric Press, 1988:382-4.
2. Silverstone T. Clinically relevant differences between antipsychotic compounds. Acta Psychiatr Scand 1990; 82(suppl 358):88-91.
3. Reynolds GP. Developments in the drug treatment of schizophrenia. Trends Pharmacol Sci 1992;13:116-21.
4. Seeman P, Lee T, Chau-Wong M, Wong K. Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature 1976;261:717-9.
5. 11C]raclopride. psychopharmacology 1992;107:23-9.
6. Seeman P. Atypical neuroleptics: role of multiple receptors, endogenous dopamine, and receptor linkage. Acta Psychiatr Scand 1990;(suppl)358:14-20.
7. Chiodo LA, Bunney BS. Possible mechanisms by which repeated clozapine administration differentially affects the activity of two subpopulations of midbrain dopamine neurons. J Neurosci 1985;5:2539-44.
8. 1A-adrenergic affinity and a low potential for extrapyramidal effects. J Med Chem 1994;37:1060-2.
9. Spiegel R. Psychopharmacology: an introduction. 2nd ed. Chichester, New York: Wiley 1989:7-8.
10. Shapiro LA, Offord SJ, Ordway GA. The effect of chronic treatment with a novel aryl-piperazine antipsychotic on monoamine receptors in rat brain. Brain Res 1995;677:250-6.
11. 123]IBZM for SPECT determination of human brain dopamine receptor occupancy by the novel antipsychotic RWJ-37796. J Nucl Med [in press].
12. Buclin T, Stucki R, Jaquet-Müller F, et al. Tolerability and pharmacological profile of the novel antipsychotic RWJ-37796 mazapertine in healthy volunteers [abstract]. Clin Pharmacol Ther 1993;53:179.
13. Wesnes KA, Simpson PM, Christmas L. A microcomputerized system for evaluating the cognitive actions of drugs in the young, elderly and demented [abstract]. Eur J Clin Pharmacol 1989;36:A38.
14. Breithaupt K, Erb KA, Neumann B, Wolf GK, Belz GG. Comparison of four noninvasive techniques to measure stroke volume: dual-beam Doppler echoaortography, electrical impedance cardiography, mecanosphygmography and M mode echocardiography of the left ventricule. Am J Noninvas Cardiol 1990;4:203-9.
15. Simpson GR, Angus JWS. A rating scale for extrapyramidal side effects. Acta Psychiatr Scand 1970;212:11-9.
16. Barnes TRE. A rating scale for drug-induced akathisia. Br J Psychiatry 1989;154:672-6.
17. 2-receptors as a tool for selecting dose regimen of a new antipsychotic agent [abstract]. Pharm Res 1993; 10(10 suppl):S358.
18. 2-dopamine occupancy as a function of intravenous rising dose of RWJ-37796 in normal living human brain [abstract]. J Nucl Med 1993;34(5 suppl):109P.