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A radioreceptor assay for neuroleptic drugs

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Clinical Pharmacology in Psychiatry

Abstract

The routine monitoring of blood levels of drugs such as digoxin, gentamicin, lithium and anticonvulsants has been recognized as a valuable and necessary aid to clinical management. A similar approach to the control of therapy with antipsychotic, neuroleptic drugs has been complicated by (1) the large number of drugs presently in use, (2) their even larger number of active and inactive metabolites, (3) the lack of satisfactory assay procedures, and (4) a general lack of recognition of the toxic effects which may result from high dose levels.

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References

  • Alfredsson, G., Wode-Helgodt, B. and Sedvall, G. (1976). A mass fragmento-graphic method for the determination of chlorpromazine and two of its active metabolites in human plasma and CSF. Psychopharmacology, 48,123–31

    Article  PubMed  CAS  Google Scholar 

  • Baldessarini, R. J. and Tarsy, D. (1979). Relationship of the actions of neuroleptic drugs to the pathophysiology of tardive dyskinesia. Int. Rev. Neurobiol., 21, 1–45

    Article  PubMed  CAS  Google Scholar 

  • Brunswick, D. J. and Mendels, J. (1977). Reduced levels of tricyclic antidepressants in plasma from vacutainers. Commun. Psychopharmac., 1, 131

    CAS  Google Scholar 

  • Burnett, G. B., Prange, A. J., Jr, Wilson, I. C., Jolliff, L. A., Creese, I. C. and Snyder, S. H. (1980). Adverse effects of anticholinergic antiparkinsonian drugs in tardive dyskinesia. Neuropsychobiology, 6, 109–20

    Article  PubMed  CAS  Google Scholar 

  • Calil, H. M., Avery, D. H., Hollister, L. E., Creese, I. and Snyder, S. H. (1979). Serum levels of neuroleptics measured by dopamine radioreceptor assay and some clinical observations. Psychiat. Res., 1, 39–44

    Article  CAS  Google Scholar 

  • Clemens, J. A., Smalstig, E. B. and Sawyer, B. D. (1974). Antipsychotic drugs stimulate prolactin release. Psychopharmacologia, 40, 123

    Article  PubMed  CAS  Google Scholar 

  • Cohen, B. M., Lipinski, J. F., Harris, P. Q., Pope, H. G., Jr and Friedman, M. (1980). Clinical use of the radioreceptor assay for neuroleptics. Psychiat. Res., 1, 173–8

    Article  Google Scholar 

  • Cooper, T. B. (1978). Plasma level monitoring of antipsychotic drugs. Clin. Pharmacokinet., 3, 14–38

    Article  PubMed  CAS  Google Scholar 

  • Cooper, T. B., Simpson, G. M. and Lee, J. H. (1976). Thymoleptic and neuroleptic drug plasma levels in psychiatry: current status. Int. Rev. Neurobiol., 19, 269–309

    Article  PubMed  CAS  Google Scholar 

  • Creese, I. and Sibley, D. (1979). Radioligand binding studies: evidence for multiple dopamine receptors. Commun. Psychopharmac., 3, 385–95

    CAS  Google Scholar 

  • Creese, I. and Snyder, S. H. (1977). A simple and sensitive radioreceptor assay for antischizophrenic drugs in blood. Nature, Lond., 270, 180–2

    Article  CAS  Google Scholar 

  • Creese, I., Burt, D. R. and Snyder, S. H. (1976). Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs. Science, N. Y., 192, 481–3

    Article  CAS  Google Scholar 

  • Creese, I., Burt, D. R. and Snyder, S. H. (1978a). Biochemical actions of neuroleptic drugs: focus on the dopamine receptor. In Handbook of Psychopharmacology, Vol. 10 (ed. L. L. Iversen, S. D. Iversen and S. H. Snyder), Plenum Press, New York, pp. 37–89

    Chapter  Google Scholar 

  • Creese, I., Manian, A. A., Prosser, T. D. and Snyder, S. H. (1978b). 3H-Haloperidol binding to dopamine receptors in rat corpus striatum: influence of chlorpromazine metabolites and derivatives. Eur. J. Pharmac., 47, 291–6

    Article  CAS  Google Scholar 

  • Curry, S. H. (1970). Plasma protein binding of chlorpromazine. J. Pharm. Pharmac, 22, 193–7

    Article  CAS  Google Scholar 

  • Curry, S. H., Whelpton, R., de Schepper, P. J., et al. (1978). Plasma fluphenazine concentrations after injection of long acting esters. Lancet, i, 1217–8

    Article  Google Scholar 

  • Feinberg, A. P. and Snyder, S. H. (1975). Phenothiazine drugs: structure activity relationships explained by a conformation that mimics dopamine. Proc. natn. Acad. Sci. U.S.A., 72, 1899–903

    Article  CAS  Google Scholar 

  • Forsman, A. and Ohman, R. (1977). Studies on serum protein binding of haloperidol. Curr. Ther. Res., 21, 245–55

    PubMed  CAS  Google Scholar 

  • Freedberg, K. A., Innis, R. B., Creese, I. and Snyder, S. H. (1979). Antischizophrenic drugs: differential plasma protein binding and therapeutic activity. Life Sci., 24, 2467–74

    Article  PubMed  CAS  Google Scholar 

  • Fremstad, D. and Bergerud, K. (1976). Plasma protein binding of drugs as influenced by blood collection methods. Acta pharmac. toxicol., 39, 570

    Article  CAS  Google Scholar 

  • Greengard, P. A. (1976). Possible role for cyclic nucleotides and phosphorylated membrane proteins in postsynaptic actions of neurotransmitters. Nature, Lond., 260,101–8

    Article  CAS  Google Scholar 

  • Iversen, L. L. (1975). Dopamine receptors in the brain. Science, N. Y., 188, 1084–9

    Article  CAS  Google Scholar 

  • Janssen, P. A. J. and Van Bever, W. F. M. (1978). Structure activity relationships of the butyrophenones and diphenylbutylpiperidines. In Handbook of Psychopharmacology, Vol. 10 (ed. L. L. Iversen, S. D. Iversen, and S. H. Snyder), Plenum Press, New York, pp. 1–36

    Chapter  Google Scholar 

  • Jeste, D. V., Rosenblatt, J. E., Wagner, R. L. and Wyatt, R. J. (1979). High serum neuroleptic levels in tardive dyskinesia? New Engl. J. Med., 1184

    Google Scholar 

  • Klawans, H. L. (1973). The pharmacology of tardive dyskinesias. Am. J. Psychiat., 130, 82–6

    Article  PubMed  Google Scholar 

  • Koch, M. H. J. (1974). The conformation of neuroleptic drugs. Molec. Pharmac., 10, 425–37

    CAS  Google Scholar 

  • Lader, M. (1976). Monitoring plasma concentrations of neuroleptics. Pharmakopsychiatrie, 9, 170–7

    Article  CAS  Google Scholar 

  • Lader, S. (1980). A radioreceptor assay for neuroleptic drugs in plasma. Immunoassay, 1, 57

    Article  CAS  Google Scholar 

  • MacKay, A. V. P., Healey, A. F. and Baxter, J. (1974). The relationship of plasma chlorpromazine to its 7-hydroxy and sulphoxide metabolites in a large population of chronic schizophrenics. Br. J. clin. Pharmac., 1, 425–30

    Article  CAS  Google Scholar 

  • McDevitt, D. G., Frisk-Holmberg, M., Hollifield, J. W. and Shand, D. G. (1976). Plasma binding and the affinity of propanolol for a beta receptor in man. Clin. Pharmac. Ther., 20, 152–7

    CAS  Google Scholar 

  • Meltzer, H. Y., Fang, V. S., Simonovich, M. and Paul, S. M. (1977). Effect of metabolites of chlorpromazine on plasma prolactin levels in male rats. Eur. J. Pharmac., 41, 431

    Article  CAS  Google Scholar 

  • Nyberg, G., Axelsson, R. and Martensson, E. (1978). Binding of thioridazine and thioridazine metabolites to serum proteins in psychiatric patients. Eur. J. clin. Pharmac, 14, 341–50

    Article  CAS  Google Scholar 

  • Patzke, J., Lai, A., Glueck, B. L., Shaskan, E. G. and Rosenby, B. J. (1980). A radioreceptor assay for the measurement of neuroleptic drugs. Clin. Chem., 26, 799

    Google Scholar 

  • Phillipson, O. T., McKeown, J. M., Baker, J. and Healey, A. F. (1977). Correlation between plasma chlorpromazine and its metabolites and clinical ratings in patients with acute relapse of schizophrenic and paranoid psychosis. Br. J. Psychiat., 131, 172–84

    Article  CAS  Google Scholar 

  • Rosenblatt, J. E., Pary, R. J., Bigelow, L. B., DeLisi, L. E., Wagner, R. L., Kleinman, J. E., Weinberger, D. R., Potkin, S. G., Schiling, D., Jeste, D. V., Alexander, P. and Wyatt, R. J. (1980). Measurement of serum neuroleptic concentrations by radioreceptor assay: concurrent assessment of clinical response and toxicity. Psychopharmac.Bull., in press.

    Google Scholar 

  • Sakalis, G., Chan, T. L., Sathananthan, G., Schooler, N., Goldberg, S. and Gershon, S. (1977). Relationships among clinical response, extrapyramidal syndrome and plasma chlorpromazine and metabolite ratios. Commun. Psychopharmac., 1, 157–66

    CAS  Google Scholar 

  • Sakalis, G., Chan, T. L., Gershon, S. and Park, S. (1973). The possible role of metabolites in therapeutic response to chlorpromazine treatment. Psychopharmacologia, 32, 279

    Article  PubMed  CAS  Google Scholar 

  • Seeman, P., Lee, T., Chau-Wong, M. and Wong, K. (1976). Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature, Lond., 261, 717–9

    Article  CAS  Google Scholar 

  • Snyder, S. H., Banerjee, S. P., Yamamura, H. I. and Greenberg, D. (1974). Drugs, neurotransmitters and schizophrenia. Science, N. Y., 184, 1243–53

    Article  CAS  Google Scholar 

  • Snyder, S. H., Creese, I. and Burt, D. R. (1975). The brain’s dopamine receptor: labeling with [3H]dopamine and [3H]haloperidol. Psychopharmac Commun., 1, 663–73

    CAS  Google Scholar 

  • Tune, L. E., Creese, I., DePaulo, J. R., Slavney, P. R., Coyle, J. T. and Snyder, S. H. (1980a). Clinical state and serum neuroleptic levels measured by radioreceptor assay in schizophrenia. Am. J. Psychiat., 137, 187–90

    Article  PubMed  CAS  Google Scholar 

  • Tune, L. E., Creese, I., Coyle, J. T., Pearlson, G. and Snyder, S. H. (1980b). Low neuroleptic serum levels in patients receiving fluphenazine decanoate. Am. J. Psychiat., 137, 80–2

    Article  PubMed  CAS  Google Scholar 

  • Usdin, E. (1971). The assay of chlorpromazine and metabolites in blood, urine, and other tissues. CRC crit. Rev. clin. Lab. Sci., 2, 347–91

    Article  PubMed  CAS  Google Scholar 

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Author information

Authors and Affiliations

  1. University of California, San Diego, USA

    Ian Creese

  2. Department of Neurosciences, School of Medicine, La Jolla, California, 92093, USA

    Ian Creese

  3. Wellcome Reagents Limited, Beckenham, Kent, UK

    Susan Lader

  4. Burroughs Wellcome Company, Research Triangle Park, North Carolina, USA

    Burton Rosenberg

Authors
  1. Ian Creese
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  2. Susan Lader
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  3. Burton Rosenberg
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Editor information

Editors and Affiliations

  1. National Institute of Mental Health, Parklawn Building, Room 9C-09, 5600 Fishers Lane, Rockville, Maryland, 20857, USA

    Earl Usdin

  2. Department of Pharmacology, Institute of Medical Biology, University of Tromsø, N-9000, Tromsø, Norway

    Svein G. Dahl

  3. Department of Pharmacology, Odense University, J. B. Winslöwsvej 19, DK-5000, Odense C, Denmark

    Lars F. Gram

  4. Department of Clinical Psychiatry, Institute of Community Medicine, University of Tromsø, N-9000, Tromsø, Norway

    Odd Lingjærde

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© 1981 The contributors

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Creese, I., Lader, S., Rosenberg, B. (1981). A radioreceptor assay for neuroleptic drugs. In: Usdin, E., Dahl, S.G., Gram, L.F., Lingjærde, O. (eds) Clinical Pharmacology in Psychiatry. Palgrave Macmillan, London. https://doi.org/10.1007/978-1-349-05929-4_7

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