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Pharmacokinetic and Pharmacodynamic Factors Causing Variability in Response to Neuroleptic Drugs

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Clinical Pharmacology in Psychiatry

Part of the book series: Psychopharmacology Series ((PSYCHOPHARM,volume 3))

Abstract

When a new psychotropic drug is introduced on the market with claims that it acts more specifically than the previous ones this has to be proven - not just in in vitro receptor binding systems and animal experiments - but also in patients. That can only be done by properly designed clinical studies.

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References

  • Ahtee L, Mattila MJ, Vapaatalo HI (1967) The binding of some phenothiazines to human serum in vitro. Biochem Pharmacol 16: 2432–2435

    Article  PubMed  CAS  Google Scholar 

  • Alfredsson G, Lindberg M, Sedvall G (1982) The presence of 7-hydroxychlorpromazine in CSF of chlorpromazine-treated patients. Psychopharmacology (Berlin) 77: 376–378

    Article  CAS  Google Scholar 

  • Alfredsson G, Harnryd C, Wiesel F-A (1984) Effects of sulpiride and ehlorpromazine on depressive symptoms in schizophrenic patients - relationship to drug concentrations. Psychopharmacology (Berlin) 84: 237–241

    Article  CAS  Google Scholar 

  • Alfredsson G, Harnryd C, Wiesel FA (1985) Effects of sulpiride and ehlorpromazine on autistic and positive symptoms in schizophrenic patients - relationship to drug concentrations. Psychopharmacology (Berlin) 85: 8–13

    Article  CAS  Google Scholar 

  • Balant-Gorgia AE, Eisele R, Balant L, Garrone G (1984) Plasma haloperidol levels and therapeutic response in acute mania and schizophrenia. Eur Arch Psychiatr Neurol Sci 234: 1–4

    Article  CAS  Google Scholar 

  • Bigelow LB, Kirch DG, Braun T, Korpi ER, Wagner RL, Zalcman S, Wyatt RJ (1985) Absence of relationship of serum haloperidol concentration and clinical response in chronic schizophrenia: a fixed-dose study. Psychopharmacol Bull 21: 66–68

    PubMed  CAS  Google Scholar 

  • Bolvig Hansen L, Larsen N-E (1985) Therapeutic advantages of monitoring plasma concentrations of perphenazine in clinical practice. Psychopharmacology (Berlin) 87: 16–19

    Article  Google Scholar 

  • Bolvig Hansen L, Larsen NE, Gulmann N (1982) Dose-response relationships of perphenazine in the treatment of acute psychoses. Psychopharmacology (Berlin) 78: 112–115

    Article  Google Scholar 

  • Brown WA, Silver MA (1985) Serum neuroleptic levels and clinical outcome in schizophrenic patients treated with fluphenazine decanoate. J Clin Psychopharmacol 5: 143–147

    PubMed  CAS  Google Scholar 

  • Calil HM, Avery DH, Hollister LE, Creese I, Snyder SH (1979) Serum levels of neuroleptics measured by dopamine radio receptor assay and some clinical observations. Psychiatry Res 1:39— 44

    Google Scholar 

  • Cohen BM, Lipinski JF, Harris PQ, Pope HG, Friedman M (1980 a) Clinical use of the radioreceptor asssay for neuroleptics. Psychiatry Res 1: 173–178

    Google Scholar 

  • Cohen BM, Lipinski JF, Pope HG, Harris PQ, Altesman RI (1980 b) Neuroleptic blood levels and therapeutic effect. Psychopharmacology (Berlin) 70: 191–193

    Google Scholar 

  • Cross AJ, Crow TJ, Owen F (1981) 3H-Flupenthixol binding in post-mortem brains of schizophrenics: Evidence for a selective increase in dopamine D2 receptors. Psychopharmacology (Berlin) 74: 122–124

    Google Scholar 

  • Csernansky JG, Kaplan J, Holman CA, Hollister LE (1983) Serum neuroleptic activity, prolactin, and tardive dyskinesia in schizophrenic outpatients. Psychopharmacology (Berlin) 81: 115–118

    Article  CAS  Google Scholar 

  • Dahl SG (1976) Pharmacokinetics of methotrimeprazine after single and multiple doses. Clin Pharmacol Ther 19: 435–442

    PubMed  CAS  Google Scholar 

  • Dahl SG (1981) Pharmacokinetic aspects of new antipsychotic drugs. Neuropharmacology 20: 1299–1302

    PubMed  CAS  Google Scholar 

  • Dahl SG (1982) Active metabolites of neuroleptic drugs: possible contribution to therapeutic and toxic effects. Ther Drug Monit 4: 33–40

    Article  PubMed  CAS  Google Scholar 

  • Dahl SG (1986) Plasma level monitoring of antipsychotic drugs: clinical utility. Clin Pharmacokinet 11: 36–61

    Article  PubMed  CAS  Google Scholar 

  • Dahl SG, Hall H (1981) Binding affinity of levomepromazine and two of its major metabolites to central dopamine and adrenergic receptors in the rat. Psychopharmacology (Berlin) 74: 101–104

    Article  CAS  Google Scholar 

  • Dahl SG, Strandjord RE (1977) Pharmacokinetics of ehlorpromazine after single and chronic dosage. Clin Pharmacol Ther 21: 437–448

    PubMed  CAS  Google Scholar 

  • Davis JM, Ericksen SE, Hurt S, Chang SS, Javaid JI, Dekirmenjian H, Casper R (1985) Haloperidol plasma levels and clinical response: basic concepts and clinical data. Psychopharmacol Bull 21: 48–51

    PubMed  CAS  Google Scholar 

  • Dysken MW, Javaid JI, Chang SS, Schaffer C, Shahid A, Davis JM (1981) Fluphenazine pharmacokinetics and therapeutic response. Psychopharmacology (Berlin) 73: 205–210

    Article  CAS  Google Scholar 

  • Freedberg KA, Innis RB, Creese I, Snyder SH (1979) Antipsychotic drugs: differential plasma protein binding and therapeutic activity. Life Sci 24: 2467–2474

    Article  PubMed  CAS  Google Scholar 

  • Garver DL, Hirschowitz J, Glicksteen GA, Kanter DR, Mavroidis ML (1984) Haloperidol plasma and red blood cell levels and clinical antipsychotic response. J Clin Psychopharmacol 4: 133–137

    Article  PubMed  CAS  Google Scholar 

  • Hals PA, Hall H, Dahl SG (1986) Phenothiazine drug metabolites: Dopamine D2 receptor, α1 and α2-adrenoceptor binding. Eur J Pharmacol 125: 373–381

    Article  PubMed  CAS  Google Scholar 

  • Hulka BS, Cassel JC, Kupper LL (1976) Disparities between medications prescribed and consumed among chronic disease patients. In: Lasagna L (ed) Patient Compliance. Futura Mount Kisco, New York, pp 123–152

    Google Scholar 

  • Jorgensen A (1986) Metabolism and pharmacokinetics of antipsychotic drugs. In: Bridges JW, Chasseaud LF (eds) Progress in drug metabolism, vol 9. Taylor and Francis, London, pp 111–174

    Google Scholar 

  • Kirch DG, Bigelow LB, Wyatt RJ (1985) The interpretation of plasma haloperidol concentrations. Arch Gen Psychiatry 42: 838–836

    PubMed  CAS  Google Scholar 

  • Krieglstein J, Lier F, Michaelis J (1972) Albumin binding and hydrophobic character of promazine and chlorpromazine metabolites. Arch Pharmacol 272: 121–130

    Article  CAS  Google Scholar 

  • Kucharski LT, Alexander P, Tune L, Coyle J (1984) Serum neuroleptic concentrations and clinical response: a radioreceptor assay investigation of acutely psychotic patients. Psychopharmacology (Berlin) 82: 194–198

    Article  CAS  Google Scholar 

  • Larsson M, Axelsson R, Forsman A (1984) On the pharmacokinetics of perphenazine: a clinical study of perphenazine enanthate and decanoate. Curr Therapeutic Res 36: 1071–1088

    Google Scholar 

  • Lindenmayer JP, Smith D, Katz I (1984) Radioreceptor assay of neuroleptics in refractory chronic schizophrenic patients. J Clin Psychiatry 45: 117–119

    PubMed  CAS  Google Scholar 

  • Linkowski P, Houbain P, Von Frenckell R, Mendlewicz J (1984) Haloperidol plasma levels and clinical response in paranoid schizophrenics. Eur Arch Psychiatr Neurol Sci 234: 231–236

    Article  CAS  Google Scholar 

  • Mavroidis ML, Kanter DR, Hirschowitz J, Garver DL (1983) Clinical response and plasma haloperidol levels in schizophrenia. Psychopharmacology (Berlin) 81: 354–356

    Article  CAS  Google Scholar 

  • Mavroidis ML, Kanter DR, Hirschowitz J, Garver DL (1984 a) Therapeutic blood levels of fluphenazine: Plasma or RBC determinations? Psychopharmacol Bull 20: 168–170

    Google Scholar 

  • Mavroidis ML, Kanter DR, Hirschowitz J, Garver DL (1984 b) Fluphenazine plasma levels and clinical response. J Clin Psychiatry 45: 370–373

    Google Scholar 

  • Mavroidis ML, Kanter DR, Hirschowitz J, Garver DL (1984 c) Clinical relevance of thiothixene plasma levels. J Clin Psychopharmacol 4: 155–157

    Google Scholar 

  • Mavroidis ML; Garver DL, Kanter DR, Hirschowitz J (1985) Plasma haloperidol levels and clinical response: confounding variables. Psychopharmacol Bull 21: 62–65

    PubMed  CAS  Google Scholar 

  • Meitzer HY, Busch DA, Fang VS (1983) Serum neuroleptic and prolactin levels in schizophrenic patients and clinical response. Psychiatry Res 9: 271–283

    Article  Google Scholar 

  • Newman DC, Epperly M, Sangarasivam S, Maruta T, Homburger HA (1984) Neuroleptic levels in serum: clinical usefulness in schizophrenic patients. Clin Res 32:741 A

    Google Scholar 

  • Richelson E, Nelson A (1984) Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro. Eur J Pharmacol 103: 197–204

    Article  PubMed  CAS  Google Scholar 

  • Potkin SG, Shen Y, Zhou D, Pardes H, Shu L, Phelps B, Poland R (1985) Does a therapeutic window for plasma haloperidol exist? Preliminary Chinese data. Psychopharmacol Bull 21: 59–61

    PubMed  CAS  Google Scholar 

  • Silverstone T, Cookson J, Ball R, Chin CN, Jacobs D, Lader S, Gould S (1984) The relationship of dopamine receptor blockade to clinical response in schizophrenic patients treated with pimozide or haloperidol. J Psychiatry Res 18: 255–268

    Article  CAS  Google Scholar 

  • Smith RC, Vroulis G, Misra CH, Schoolar J, De John C, Korivi P, Leelavahti DE, Arzu D (1980) Receptor techniques in the study of plasma levels of neuroleptics and antidepressant drugs. Commun Psychopharmacol 4: 451–465

    PubMed  CAS  Google Scholar 

  • Smith RC, Baumgartner R, Misra CH, Mauldin M, Shvartsburd A, Ho BT, De John C (1984 a) Haloperidol. Plasma levels and prolactin response as predictors of clinical improvement in schizophrenia: chemical v radioreceptor plasma level assays. Arch Gen Psychiatry 41: 1044–1049

    Google Scholar 

  • Smith RC, Baumgartner R, Ravichandran GK, Shvartsburd A, Schoolar JC, Allen P, Johnson R (1984 b) Plasma and red cell levels of thioridazine and clinical response in schizophrenia. Psychiatry Res 12: 287–296

    Google Scholar 

  • Smith RC, Baumgartner R, Burd A, Ravichandran GK, Mauldin M (1985) Haloperidol and thioridazine drug levels and clinical response in schizophrenia: comparison of gas-liquid chromatography and radioreceptor drug level assays. Psychopharmacol Bull 21: 52–58

    PubMed  CAS  Google Scholar 

  • Tang SW, Glaister J, Davidson L, Toth R, Jeffries JJ, Seeman P (1984) Total and free plasma neuroleptic levels in schizophrenic patients. Psychiatry Res 13: 285–293

    Article  PubMed  CAS  Google Scholar 

  • Tune LE, Creese I, De Paulo JR, Slavney PR, Coyle JT, Snyder SH (1980) Clinical state and serum neuroleptic levels measured by radioreceptor assay in schizophrenia. Am J Psychiatry 137: 187–190

    PubMed  CAS  Google Scholar 

  • Tune LE, Creese I, De Paulo JR, Slavney PR, Snyder SH (1981) Neuroleptic serum levels measured by radioreceptor assay and clinical response in schizophrenia. J Nerv Ment Dis 169: 60–63

    Article  PubMed  CAS  Google Scholar 

  • Van Putten T, May PRA, Jenden DJ (1981) Does a plasma level of chlorpromazine help? Psychol Med 11: 729–734

    Article  PubMed  Google Scholar 

  • Van Putten T, May PRA, Marder SR, Wilkins JN, Rosenberg BJ (1983) Plasma levels of thiothixene by radioreceptor assay: clinical usefulness. Psychopharmacology (Berlin) 79: 40–44

    Article  Google Scholar 

  • Van Putten T, Marder SR, May PRA, Poland RE, O’Brien RP (1985 a) Plasma levels, haloperidol and clinical response. Psychopharmacol Bull 21: 69–72

    Google Scholar 

  • Van Putten T, Marder SR, Mintz (1985 b) Plasma haloperidol levels: clinical response and fancy mathematics. Arch Gen Psychiatry 42: 835

    Google Scholar 

  • 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 (Berlin) 73: 55–62

    Article  CAS  Google Scholar 

  • Wode-Helgodt B, Borg S, Fyrö B, Sedvall G (1978) Clinical effects and drug concentrations in plasma and cerebrospinal fluid in psychotic patients treated with fixed doses of chlorpromazine. Acta Psychiatr Scand 58: 149–173

    Article  PubMed  CAS  Google Scholar 

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© 1987 Springer-Verlag Berlin Heidelberg

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Dahl, S.G., Hals, PA. (1987). Pharmacokinetic and Pharmacodynamic Factors Causing Variability in Response to Neuroleptic Drugs. In: Dahl, S.G., Gram, L.F., Paul, S.M., Potter, W.Z. (eds) Clinical Pharmacology in Psychiatry. Psychopharmacology Series, vol 3. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-71288-3_31

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  • DOI: https://doi.org/10.1007/978-3-642-71288-3_31

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-71290-6

  • Online ISBN: 978-3-642-71288-3

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