A radioreceptor assay for neuroleptic drugs

  • Ian Creese
  • Susan Lader
  • Burton Rosenberg
Chapter

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.

Keywords

Tardive Dyskinesia Brief Psychiatric Rate Scale Neuroleptic Drug Radioreceptor Assay Fluphenazine Decanoate 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
This is a preview of subscription content, log in to check access.

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. 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, 48,123–31PubMedCrossRefGoogle Scholar
  2. Baldessarini, R. J. and Tarsy, D. (1979). Relationship of the actions of neuroleptic drugs to the pathophysiology of tardive dyskinesia. Int. Rev. Neurobiol., 21, 1–45PubMedCrossRefGoogle Scholar
  3. Brunswick, D. J. and Mendels, J. (1977). Reduced levels of tricyclic antidepressants in plasma from vacutainers. Commun. Psychopharmac., 1, 131Google Scholar
  4. 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, 109–20PubMedCrossRefGoogle Scholar
  5. 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, 39–44CrossRefGoogle Scholar
  6. Clemens, J. A., Smalstig, E. B. and Sawyer, B. D. (1974). Antipsychotic drugs stimulate prolactin release. Psychopharmacologia, 40, 123PubMedCrossRefGoogle Scholar
  7. 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, 173–8CrossRefGoogle Scholar
  8. Cooper, T. B. (1978). Plasma level monitoring of antipsychotic drugs. Clin. Pharmacokinet., 3, 14–38PubMedCrossRefGoogle Scholar
  9. 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, 269–309PubMedCrossRefGoogle Scholar
  10. Creese, I. and Sibley, D. (1979). Radioligand binding studies: evidence for multiple dopamine receptors. Commun. Psychopharmac., 3, 385–95Google Scholar
  11. Creese, I. and Snyder, S. H. (1977). A simple and sensitive radioreceptor assay for antischizophrenic drugs in blood. Nature, Lond., 270, 180–2CrossRefGoogle Scholar
  12. 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, 481–3CrossRefGoogle Scholar
  13. 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. 37–89CrossRefGoogle Scholar
  14. 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, 291–6CrossRefGoogle Scholar
  15. Curry, S. H. (1970). Plasma protein binding of chlorpromazine. J. Pharm. Pharmac, 22, 193–7CrossRefGoogle Scholar
  16. Curry, S. H., Whelpton, R., de Schepper, P. J., et al. (1978). Plasma fluphenazine concentrations after injection of long acting esters. Lancet, i, 1217–8CrossRefGoogle Scholar
  17. 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, 1899–903CrossRefGoogle Scholar
  18. Forsman, A. and Ohman, R. (1977). Studies on serum protein binding of haloperidol. Curr. Ther. Res., 21, 245–55PubMedGoogle Scholar
  19. 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, 2467–74PubMedCrossRefGoogle Scholar
  20. Fremstad, D. and Bergerud, K. (1976). Plasma protein binding of drugs as influenced by blood collection methods. Acta pharmac. toxicol., 39, 570CrossRefGoogle Scholar
  21. Greengard, P. A. (1976). Possible role for cyclic nucleotides and phosphorylated membrane proteins in postsynaptic actions of neurotransmitters. Nature, Lond., 260,101–8CrossRefGoogle Scholar
  22. Iversen, L. L. (1975). Dopamine receptors in the brain. Science, N. Y., 188, 1084–9CrossRefGoogle Scholar
  23. 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. 1–36CrossRefGoogle Scholar
  24. 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., 1184Google Scholar
  25. Klawans, H. L. (1973). The pharmacology of tardive dyskinesias. Am. J. Psychiat., 130, 82–6PubMedCrossRefGoogle Scholar
  26. Koch, M. H. J. (1974). The conformation of neuroleptic drugs. Molec. Pharmac., 10, 425–37Google Scholar
  27. Lader, M. (1976). Monitoring plasma concentrations of neuroleptics. Pharmakopsychiatrie, 9, 170–7CrossRefGoogle Scholar
  28. Lader, S. (1980). A radioreceptor assay for neuroleptic drugs in plasma. Immunoassay, 1, 57CrossRefGoogle Scholar
  29. 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, 425–30CrossRefGoogle Scholar
  30. 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, 152–7Google Scholar
  31. 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, 431CrossRefGoogle Scholar
  32. 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, 341–50CrossRefGoogle Scholar
  33. 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, 799Google Scholar
  34. 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, 172–84CrossRefGoogle Scholar
  35. 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
  36. 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, 157–66Google Scholar
  37. Sakalis, G., Chan, T. L., Gershon, S. and Park, S. (1973). The possible role of metabolites in therapeutic response to chlorpromazine treatment. Psychopharmacologia, 32, 279PubMedCrossRefGoogle Scholar
  38. Seeman, P., Lee, T., Chau-Wong, M. and Wong, K. (1976). Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature, Lond., 261, 717–9CrossRefGoogle Scholar
  39. Snyder, S. H., Banerjee, S. P., Yamamura, H. I. and Greenberg, D. (1974). Drugs, neurotransmitters and schizophrenia. Science, N. Y., 184, 1243–53CrossRefGoogle Scholar
  40. 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, 663–73Google Scholar
  41. 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, 187–90PubMedCrossRefGoogle Scholar
  42. 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, 80–2PubMedCrossRefGoogle Scholar
  43. Usdin, E. (1971). The assay of chlorpromazine and metabolites in blood, urine, and other tissues. CRC crit. Rev. clin. Lab. Sci., 2, 347–91PubMedCrossRefGoogle Scholar

Copyright information

© The contributors 1981

Authors and Affiliations

  • Ian Creese
    • 1
    • 2
  • Susan Lader
    • 3
  • Burton Rosenberg
    • 4
  1. 1.University of CaliforniaSan DiegoUSA
  2. 2.Department of NeurosciencesSchool of MedicineLa JollaUSA
  3. 3.Wellcome Reagents LimitedKentUK
  4. 4.Burroughs Wellcome CompanyResearch Triangle ParkUSA

Personalised recommendations