Positron Emission Tomographic Analysis of Central D1 and D2 Dopamine Receptor Occupancy in Patients Treated with Classical Neuroleptics and Clozapine: Relation to Extrapyramidal Side Effects

Archives of General Psychiatry

Volumn 49, Issue 7, 1992, Pages 538-544

  Farde, Lars ^a   Nordström, Anna Lena ^a   Wiesel, Frits Axel ^b   Pauli, Stefan ^a   Halldin, Christer ^a   Sedvall, Göran ^a  

^a KAROLINSKA INSTITUTE   (Sweden)

^b Ulleraker Hospital   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

CHLORPROMAZINE; CLOZAPINE; DOPAMINE 1 RECEPTOR; DOPAMINE 2 RECEPTOR; DOPAMINE RECEPTOR; FLUPENTIXOL; FLUPENTIXOL DECANOATE; HALOPERIDOL; HALOPERIDOL DECANOATE; MELPERONE; NEUROLEPTIC AGENT; PERPHENAZINE; PERPHENAZINE ENANTHATE; PIMOZIDE; REMOXIPRIDE; SULPIRIDE; THIORIDAZINE; TRIFLUOPERAZINE; ZUCLOPENTHIXOL DECANOATE;

ADULT; AKATHISIA; ARTICLE; BASAL GANGLION; CLINICAL ARTICLE; CONTROLLED STUDY; DRUG EFFECT; EXTRAPYRAMIDAL SYNDROME; FEMALE; HUMAN; MALE; ORAL DRUG ADMINISTRATION; PARKINSONISM; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RADIOACTIVITY; RECEPTOR BLOCKING; RECEPTOR OCCUPANCY; SCHIZOPHRENIA;

ADOLESCENT; ADULT; ANTIPSYCHOTIC AGENTS; BASAL GANGLIA; BASAL GANGLIA DISEASES; CLOZAPINE; DOPAMINE ANTAGONISTS; FEMALE; HUMAN; IODINE RADIOISOTOPES; MALE; PUTAMEN; RACLOPRIDE; RECEPTORS, DOPAMINE; SALICYLAMIDES; SCH-23390; SCHIZOPHRENIA; SUPPORT, NON-U.S. GOV'T; SUPPORT, U.S. GOV'T, P.H.S.; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 0026718710     PISSN: 0003990X     EISSN: 15383636     Source Type: Journal    
DOI: 10.1001/archpsyc.1992.01820070032005     Document Type: Article

References (60)

1. Carlsson A, Lindqvist M. Effect of chlorpromazine or haloperidol on formation of 3-methoxytyramine and normetanephrine in mouse brain. Acta Pharmacol Toxicol. 1963;20: 140–144.
2. Van Rossum JM. The significance of dopamine-receptor blockade for the mechanism of action of neuroleptic drugs. Arch Int Pharmacodyn Ther. 1966;160: 492–494.
3. Andén NE, Bucher SG, Corrodi H, Fuxe K, Ungerstedt U. Receptor activity and turnover of dopamine and noradrenaline after neuroleptics. Eur J Pharmacol. 1970;11: 303–314.
4. Seeman P, Lee T, Chau-Wong M, Wong K. Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature. 1976;261: 717–719.
5. Creese I, Burt DR, Snyder SH. Dopamine receptor binding clinical and pharmacological potencies of antischizophrenic drugs. Science. 1976;192: 481–483.
6. Peroutka SJ, Snyder SH. Relationship of neuroleptic drug effects at brain dopamine, serotonin, adrenergic and histamine receptors to clinical potency. Am J Psychiatry. 1980;137: 1518–1522.
7. Farde L, Wiesel F-A, Halldin C, Sedvall G. Central D2-dopamine receptor occupancy in schizophrenic patients treated with antipsychotic drugs. Arch Gen Psychiatry. 1988;45: 71–78.
8. Baron JC, Marinot JL, Cambon H, Boulenger JP, Poirier MF, Caillard V, Blin J, Huret JD, Loch C, Maziére B. Striatal dopamine receptor occupancy during and following withdrawal from neuroleptic treatment: correlative evaluation by positron emission tomography and plasma prolactine levels. Psychopharmacology. 1989;99: 463–472.
9. Smith M, Wolf AP, Brodie JD, Arnett CD, Barouche F, Shiue CY, Fowler JS, Russell JAG, MacGregor RR, Wolkin A, Angrist B, Rotrosen J, Peselow E. Serial [18F]N-methylspiperone PET studies to measure changes in antipsychotic drug D2 receptor occupancy in schizophrenic patients. Biol Psychiatry. 1988;23: 653–663.
10. Kebabian JW, Petzold GL, Greengard P. Dopamine sensitive adenylate cyclase in the caudate nucleus of rat brain, and its similarity to the ‘dopamine receptor.’ Proc Natl Acad Sci USA. 1972;69: 2145–2149.
11. Waddington JL, O'Boyle KM. Drugs acting on brain dopamine receptors: a conceptual re-evaluation five years after the first selective D-1 antagonist. Pharmacol Ther. 1989;43: 1–527.
12. Farde L, Halldin C, Stone-Elander S, Sedvall G. PET-analysis of human dopamine receptor subtypes using [11C]-SCH23390 and [11C]-raclopride. Psychopharmacology. 1987;92: 278–284.
13. Farde L, Wiesel FA, Nordström AL, Sedvall G. D1- and D2dopamine receptor occupancy during treatment with conventional and atypical neuroleptics. Psychopharmacology. 1989;99:S28–31.
14. Hyttel J. SCH23390—the first selective dopamine-D, antagonist. Eur J Pharmacol. 1983;9: 153–154.
15. Delay J, Deniker O. Caractéristiques psycho-physiologiques des médicamentes neuroleptiques. In: Garattini S, Ghetti V, eds. The Psychotropic Drugs. Amsterdam, the Netherlands: Elsevier Publishing Co; 1957: 557–564.
16. Stille G, Hippius H. Kritische Stellungsnahme zum Begriff der Neuroleptika (anhand von pharmakologischen und klinischen Befunden mit Clozapin). Pharmacopsychiatry. 1971;4: 182–191.
17. Meltzer HY, Fang VS. The effects of neuroleptics on serum prolactin in schizophrenic patients. Arch Gen Psychiatry. 1976;33: 279–286.
18. Angst J, Jaenicke U, Padrutt A, Scharfetter C. Ergebnisse eines Doppelblinsversuches von HF 1854 (8-chlor-11-(4-methyl-1-piperazinyl)-5H-dibenzo (b,e) 1,4)diazepin) im Vergleich zu Levomepromazine. Pharmacopsychiatry. 1971;4: 192–200.
19. Casey DE. Clozapine: neuroleptic-induced EPS and tardive dyskinesia. Psychopharmacology. 1989;99:S47-S53.
20. Meltzer HY, Goode DJ, Schyve PM, Young M, Fang VS. Effect of clozapine on human serum prolactin levels. Am J Psychiatry. 1979; 136: 1551–1555.
21. Kane JM, Cooper TB, Sachar EJ, Halpern FS, Bailine S. Clozapine plasma levels and prolactin response. Psychopharmacology. 1981; 73: 181–187.
22. Kane J, Honigfeld G, Singer J, Meltzer H. Clozapine for the treatmentresistent schizophrenic. Arch Gen Psychiatry. 1988;45: 789–796.
23. Farde L, Hall H, Ehrin E, Sedvall G. Quantitative analysis of dopamine-D2 receptor binding in the living human brain by positron emission tomography. Science. 1986;231: 258–261.
24. Wong DF, Gjedde A, Wagner HN Jr. Quantification of neuroreceptors in the living human brain, I: irreversible binding of ligands. J Cereb Blood Flow Metab. 1986;6: 137–146.
25. Farde L, Wiesel F-A, Halldin C, Stone-Elander S, Nordström A-L, Hall H, Sedvall G. D2-dopamine receptor characteristics in neurolepticnaive patients with schizophrenia: a PET-study with [11C]raclopride. Arch Gen Psychiatry. 1990;47: 213–219.
26. ECDEU Manual—Assessment Manual for Psychopharmacology. US Dept of Health, Education, and Welfare; 1976.
27. Simpson GM, Angus JWS. A rating scale for extrapyramidal side effects. Acta Psychiatr Scand. 1970;45(suppl 212): 11–19.
28. Barnes TRE. A rating scale for drug-induced akathisia. Br J Psychiatry. 1989;154: 672–676.
29. Farde L, Ehrin E, Eriksson L, Greitz T, Hall H, Hedström C-G, Litton J-E, Sedvall G. Substituted benzamides as ligands for visualization of dopamine-D2 receptor binding in the human brain by positron emission tomography. Proc Natl Acad Sci USA. 1985;82: 3863–3867.
30. Halldin C, Stone-Elander S, Farde L, Ehrin E, Fasth KJ, Langström B, Sedvall G. Preparation of [11C]-labelled SCH 23390 for the in vivo study of dopamine D-1 receptors using positron emission tomography. Appl Radiat lsot. 1986;37: 1039–1043.
31. Halldin C, Farde L, Högberg T, Hall H, Stöm P, Ohlberger A, Solin O. A comparative PET-study of five carbon-11 or fluorine-18 labelled salicylamides: preparation and in vitro dopamine D-2 receptor binding. Nucl Med Biol. 1991;8: 871–881.
32. Litton J, Bergström L, Eriksson L, Bohm C, Blomqvist G, Kesselberg M. Performance study of the PC-384 positron camera system for emission tomography of the brain. J Comput Assit Tomogr. 1984;8: 74–87.
33. Berströ M. Boethius J, Eriksson L, Greitz T, Ribbe T, Widen L. Head fixation device for reproducible positron alignment in transmission CT and positron emission tomography. I Comput Assist Tomogr. 1981;8: 74–87.
34. Cortés R, Camps M, Gueye B, Probst A, Palacios J. Dopamine receptors in human brain: autoradiographic distribution of D, and D2 sites in Parkinson syndrome of different etiology. Brain Res. 1989;483: 30–38.
35. Shapiro SS, Wilk MB. An analysis of variance test for normality (complete samples). Biometrika. 1972;52: 591–601.
36. Ryan F, Joiner L, Ryan A Jr. The Minitab Handbook. 2nd ed. Boston, Mass: Duxbury Press; 1985: 185–190.
37. Wong DF, Wagner HN, Dannals RF, Links JM, Frost J, Ravert HT, Wilson A, Rosenbaum AE, Gjedde A, Douglass KH, Petronis JD, Folstein MF, Toung TR, Burns D, Kuhar M. Effects of age on dopamine and serotonin receptors measured by positron emission tomography in the living human brain. Science. 1984;226: 1393–1396.
38. Baron J, Maziére B, Loch C, Cambon H, Sgouropoulos P, Bonnet A, Agid Y. Loss of striatal [76Br]Bromospiperone binding sites demonstrated by positron tomography in progressive supranuclear palsy. J Cereb Blood Flow Metab. 1986;6: 131–136.
39. Nordström AL, Farde L, Halldin C. PET-analysis of [11C]raclopride binding in the basal ganglia: reliability and age effects. Hum Psychopharmacol. In press.
40. Burt DR, Creese I, Snyder SH. Antischizophrenic drugs: chronic treatment elevated dopamine receptor binding in brain. Science. 1977;196: 326–328.
41. Clow A, Theodorou A, Jenner P. Changes in rat striatal dopamine turnover and receptor activity during one year's neuroleptic administration. Eur J Pharmacol. 1980;63: 135–144.
42. Owen F, Cross AJ, Waddington JL. Dopamine-mediated behaviour and 3H-spiperone binding to striatal membranes in rats after nine months' haloperidol administration. Life Sci. 1980;26: 55–59.
43. Mackay AVP, Iversen LL, Rossor M, Spokes E, Bird E, Arregui A, Creese I, Snyder SH. Increased brain dopamine and dopamine receptors in schizophrenia. Arch Gen Psychiatry. 1982;39: 991–997.
44. Kornhuber J, Riederer P, Reynolds GP, Beckmann H, Jellinger K, Gabriel E. 3H-spiperone binding in post-mortem brains from schizophrenic patients: relationship to neuroleptic drug treatment, abnormal movements, and positive symptoms. J Neural Transm. 1989;75: 1–10.
45. Seeman P. Elevation of dopamine D2 receptors in schizophrenia is underestimated by radioactive raclopride. Arch Gen Psychiatry. 1990;47: 1170–1172.
46. Zetterstöm T, Sharp T, Ungerstedt U. Effect of neuroleptic drugs on striatal dopamine release and metabolism in the awake rat stud by intracerebral dialysis. Eur J Pharmacol. 1984;106: 27–37.
47. Zhang W, Tilson H, Stachowiak MK, Hong JS. Repeated haloperidol administration changes basal release of striatal dopamine and subsequent response to haloperidol challenge. Brain Res. 1989;484: 389–392.
48. Kuczenski R, Segal D. Concomitant characterization of behavioral and striatal neurotransmitter response to amphetamine using in vivo dialysis. J Neurosci. 1989;9: 2051–2065.
49. Davis JM. Dose equivalence of the antipsychotic drugs. J Psychiatr Res. 1974;11: 65–69.
50. Alfredsson G, Bjerkenstedt L, Edman G, Härnryd C, Oxenstierna G, Sedvall G, Wiesel FA. Relationships between drug concentrations in serum and CSF, clinical effects and monoaminergic variables in schizophrenic patients treated with sulpiride or chlorpromazine. Acta Psychiart Scand. 1984;69(suppl 311): 49–74.
51. Lewander T, Westerbergh SE, Morrison D. Clinical profile of remoxipride: a combined analysis of a comparative double-blind multicenter trial programme. Acta Psychiatr Scand. 1990;82(suppl 358): 92–98.
52. Schmauss M, Wolff R, Erfurth A, Rüther E. Tolerability of longterm clozapine treatment. Psychopharmacology. 1989;99: S105–108.
53. Bondesson U, Lindström LH. Determination of clozapine and its N-methylated metabolite in plasma by use of gas chromatography— mass spectrometry with single ion detection. Psychopharmacology. 1988;95: 472–475.
54. Ackenheil M. Clozapine: pharmacokinetic investigations and biochemical effects in man. Psychopharmacology. 1989;99:S32-S37.
55. Michaelis L, Menten ML. Die Kinetik der Invertinwirkung. Biochem Z. 1913;49: 333–369.
56. Hall H, Farde L, Sedvall G. Human dopamine receptor subtypes: in vitro binding analysis using 3H-SCH23390 and 3H-raclopride. I Neural Transm. 1988;73: 7–21.
57. Andersen P. Comparison of the pharmacological characteristics of [3H]raclopride and [3H]SCH23390 binding to dopamine receptors in vivo in mouse brain. Eur J Pharmacol. 1988;146: 113–120.
58. Sokoloff P, Giros B, Martres MP, Bouthenet ML, Schwartz JC. Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature. 1990;347: 146–151.
59. Andén NE, Stock G. Effect of clozapine on the turnover of dopamine in the corpus striatum and the limbic system. J Pharmacol. 1973;25: 346–351.
60. Van Tol H, Bunzow J, Guan H, Sunahara R, Seeman P, Niznik H, Civelli O. Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. Nature. 1991;350;610–614.