Abstract
The relationship between plasma concentration and effect on arousal was studied in normal subjects after single oral and parenteral doses of melperone. A strong correlation between plasma concentration and effect was found when the effector compartment and central compartment were in equilibrium. The relationship was independent of the route of administration.
Similar content being viewed by others
References
Anden NE, Grabowska M (1976) Pharmacological evidence for a stimulation of dopamine neurons by noradrenaline neurons in the brain. Eur J Pharmacol 39:275–282
Bjerkenstedt L, Gullberg B, Härnryd C, Sedvall G (1977) Monoamine metabolite levels in cerebrospinal fluid of psychotic women treated with melperone or thiothixene. Arch Psychiatr Nervenkr 224:107–118
Bjerkenstedt L, Härnryd C, Grimm V, Gullberg B, Sedvall G (1978). A double-blind comparison of melperone and thiothixene in psychotic women using a new rating scale, the CPRS. Arch Psychiatr Nervenkr 226:157–172
Blumberg JB, Taylor RE, Sulser F (1975) Blockade by pimozide of a noradrenaline sensitive adenylate cyclase in the limbic forebrain: Possible role of limbic noradrenergic mechanisms in the mode of action of antipsychotics. J Pharm Pharmacol 27:125–128
Borgström L, Larsson H, Molander L (1982) Pharmacokinetics of parenterally and orally administered melperone in man. Eur J Clin Pharmacol 23:173–176
Christensson E, Björk A, Gustavsson B, Magee J, Nerme V, Olsson N-G (1981) FG 5606, a new antiaggressive compound with effects on different stress-induced disorders. Presented at the IIIrd World Congress of Biological Psychiatry, Stockholm, Sweden, June 28–July 3
Cohen BM, Herschel M, Aoba A (1979) Neuroleptic, antimuscarinic and antiadrenergic activity of chloropromazine, thioridazine and their metabolites. Psychiatr Res 1:199–208
Creese J, Snyder SH (1978) Behavioral and biochemical properties of the dopamine receptor. In: Lipton MA, DiMascio A, Killam KF (eds) Psychopharmacology — A generation of progress. Raven, New York, pp 377–388
Farley IJ, Price KS, McCullough E, Deck JHN, Hordynski W, Hornykiewicz O (1978) Norepinephrine in chronic paranoid schizophrenia: Above-normal levels in limbic forebrain. Science 200:456–458
Goldstein MJ, Judd LL, Rodnick EH, LaPolla A (1969) Psychophysiological and behavioral effects of phenothiazine administration in acute schizophrenics as a function of premorbid status. J Psychiatr Res 6:271–287
Kirkegaard A, Kirkegaard G, Geismar L, Christensen I (1981) Additional studies on side effects of melperone in long-term therapy for 1 to 15 years in psychiatric patients. Arzneim Forsch 31:737–740
Kornetsky C, Mirsky AF (1966) On certain psychopharmacological and physiological differences between schizophrenic and normal persons. Psychopharmacologia 8:309–318
Lake CR, Sternberg DE, van Kammen DP, Ballenger WE, Ziegler MG, Post RM, Kopin IJ, Bunney WE (1980) Schizophrenia: elevated cerebrospinal fluid norepinephrine. Science 207:331–333
Lee T, Seeman P, Tourtellotte WW, Farley IJ, Hornykiewicz O (1978) Binding of 3H-apomorphine in schizophrenic brains. Nature 274:897–900
Marwaha J, Hoffer BJ, Geller HM, Freedman R (1981) Electrophysiological interaction of antipsychotic drugs with central noradrenergic pathways. Psychopharmacology 73:126–133
Owen F, Crow TJ, Poulter M, Cross AJ, Longden A, Riley GJ (1978) Increased dopamine-receptor sensitivity in schizophrenia. Lancet I:223–225
Peroutka SJ, U'Prichard DC, Greenberg DA, Snyder SH (1977) Neuroleptic drug interactions with norepinephrine alpha receptor binding sites in rat brain. Neuropharmacology 16:549–556
Peroutka SJ, Snyder SH (1980) Relationship of neuroleptic drug effects at brain dopamine, serotonin, adrenergic and histamine receptors to clinical potency. Am J Psychiatry 137:1518–1522
Robinson SE, Berney S, Mishra R, Sulser F (1979) The relative role of dopamine and norepinephrine receptor blockade in the activation of antipsychotic drugs: metoclopramide, thiethylperazine, and molindone as pharmacological tools. Psychopharmacology 64:141–147
Sedvall G, Bjerkenstedt L, Lindström L, Wode-Helgodt B (1978) Clinical assessment of dopamine receptor blockade. Life Sci 23:425–430
Seeman P, Lee T, Chau-Wong M, Wong K (1976) Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature 261:717–719
Shagass C (1976) An electrophysiological view of schizophrenia. Biol Psychiatry 11:3–30
Silverman J (1972) Stimulus intensity modulation and psychological disease. Psychopharmacologia 24:42–80
Sovner R, DiMascio A (1978) Extrapyramidal syndromes and other neurological side effects of psychotropic drugs. In: Lipton MA, DiMascio A, Killam KF (eds) Psychopharmacology: A generation of progress. Raven, New York, pp 1012–1031
Spohn HE, Lacoursoiere RB, Thompson K, Coyne L (1977) Phenothiazine effects on psychological and psychophysiological dysfunction in chronic schizophrenics. Arch Gen Psychiatry 34:633–644
Sternberg DE, van Kammen DP, Lake CR, Ballenger JC, Marder SR, Bunney WE Jr (1981) The effect of pimozide on CSF norepinephrine in schizophrenia. Am J Psychiatry 138:1045–1051
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Molander, L., Borgström, L. Relationship between plasma concentration and arousal in normal subjects after single oral and parenteral doses of melperone, a butyrophenone neuroleptic. Psychopharmacology 79, 111–114 (1983). https://doi.org/10.1007/BF00427795
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00427795