Pharmacokinetics and time-course of D2 receptor occupancy induced by atypical antipsychotics in stabilized schizophrenic patients

Journal of Psychopharmacology

Volumn 22, Issue 8, 2008, Pages 882-894

  Catafau, A M ^a,b,c   Penengo, M M ^c   Nucci, G ^b   Bullich, S ^c   Corripio, I ^d   Parellada, E ^e   Garcia Ribera C ^c   Gomeni, R ^b   Merlo Pich, E ^a,b  

^a GLAXOSMITHKLINE   (Spain)

^b GSK   (Italy)

^c HOSPITAL DEL MAR   (Spain)

^d HOSPITAL DE LA SANTA CREU I SANT PAU   (Spain)

^e HOSPITAL CLÍNIC   (Spain)

Author keywords

Antipsychotics; Atypical; D2 receptor; PK PD model; Schizophrenia; SPECT

Indexed keywords

CLOZAPINE; DOPAMINE 2 RECEPTOR; IODINE 123; N [(1 ETHYL 2 PYRROLIDINYL)METHYL] 3 IODO 6 METHOXYSALICYLAMIDE; OLANZAPINE; QUETIAPINE; RISPERIDONE;

ADULT; ARTICLE; CHRONIC DRUG ADMINISTRATION; CLINICAL ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOSE TIME EFFECT RELATION; FEMALE; HUMAN; MALE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; RECEPTOR OCCUPANCY; SCHIZOPHRENIA; SINGLE PHOTON EMISSION COMPUTER TOMOGRAPHY;

ADULT; ANTIPSYCHOTIC AGENTS; BENZAMIDES; FEMALE; HUMANS; MALE; PYRROLIDINES; RECEPTORS, DOPAMINE D2; SCHIZOPHRENIA; TOMOGRAPHY, EMISSION-COMPUTED, SINGLE-PHOTON;

EID: 49349105633     PISSN: 02698811     EISSN: 14617285     Source Type: Journal    
DOI: 10.1177/0269881107083810     Document Type: Article

References (72)

1. Antonini A., Leenders K.L. (1993) Dopamine D2 receptors in normal human brain: effect of age measured by positron emission tomography (PET) and [11C]raclopride. Ann NY Acad Sci 695: 81-85
2. Bernardo M., Parellada E., Lomena F., Catafau A.M., Font M., Gomez J.C. Lopez-Carrero C., Gutierrez F., Pavia J., Salamero M. (2001) Double-blind olanzapine vs. haloperidol D2 dopamine receptor blockade in schizophrenic patients: a baseline-endpoint. Psychiatry Res 107: 87-97
3. Burns M.J. (2001) The pharmacology and toxicology of atypical antipsychotic agents. Clin Toxicol 39: 1-14
4. Busatto G.F., Pilowsky L.S., Costa D.C., Ell P.J., Verhoeff N P L G, Kerwin R.W. (1995) Dopamine D2 receptor blockade in vivo with the novel antipsychotics risperidone and remoxipride-an 123I-IBZM single photon emission tomography (SPET) study. Psychopharmacology (Berl) 117: 55-61
5. Byerly M.J., DeVane C.L., Lindsay C. (1996) Pharmacokinetics of clozapine and risperidone: A review of recent literature. J Clin Psychopharmacol 16: 177-187
6. Callaghan J.T., Bergstrom R.F., Ptak L.R., Beasley C.M. (1999) Olanzapine. Pharmacokinetic and pharmacodynamic profile. Clin Pharmacokinet 37: 177-193
7. Catafau A.M., Bullich S., Danús M., Penengo M.M., Cot A., Abanades S., Farré M., Pavía J., Ros D., n(2008) Test-retest variability and reliability of 123I-IBZM SPECT measurement of striatal dopamine D2 receptor availability in healthy volunteers and influence of iterative reconstruction algorithms. Synapse 62: 62-69
8. Cheer S.M., Wagstaff A.J. (2004) Quetiapine: A review of its use in the management of schizophrenia. CNS Drugs 18: 173-199
9. Chiu C.C., Lane H.Y., Huang M.C., Liu H.C., Jann M.W., Hon Y.Y., Chang W.H., Lu M.L. (2004) Dose-dependent alterations in the pharmacokinetics of olanzapine during coadministration of fluvoxamine in patients with schizophrenia. J Clin Pharmacol 44: 1385-1390
10. Chouinard G., Ross-Chouinard A., Annable L., Jones B.D. (1980) Extrapyramidal Symptom Rating Scale (ESRS). Can J Neurol Sci 7: 233
11. Darby J.K., Pasta D.J., Elfand L., Dabiri L., Clark L., Herbert J. (1997) Risperidone dose and blood level variability: Accumulation effects and interindividual and intraindividual variability in the non-responder patient in the clinical practice setting. J Clin Psychopharmacol 17: 478-484
12. Dear G.J., Fraser I.J., Patel D.K., Long J., Pleasance S. (1998) Use of liquid chromatography-tandem mass spectrometry for the quantitative and qualitative analysis of an antipsychotic agent and its metabolites in human plasma and urine. J Chromatogr A 794: 27-36
13. DeVane C.L., Nemeroff C.B. (2001) Clinical pharmacokinetics of quetiapine. An atypical antipsychotic. Clin Pharmacokinet 407: 509-522
14. Dresel S., Tatsch K., Dahne I., Mager T., Scherer J., Hahn K. (1998) Iodine-123-iodobenzamide SPECT assessment of dopamine D2 receptor occupancy in riperidone-treated schizophrenic patients. J Nucl Med 39: 1138-1142
15. Dresel S., Mager T., Rossmuller B., Meisenzahl E., Hahn K., Moller H.J., Tatsch K. (1999) In vivo effects of olanzapine on striatal dopamine D(2)/D(3) receptor binding in schizophrenic patients: an iodine-123 iodobenzamide single-photon emission tomography study. Eur J Nucl Med Mol Img 26: 862-868
16. Ette E.I., Williams P.J. (2004) Population pharmacokinetics I: background, concepts, and models. Ann Pharmacother 38: 1702-1706
17. Fellows L., Ahmad F., Castle D.J., Dusci L.J., Bulsara M.K., Ilett K.F. (2003) Investigation of target plasma concentration-effect relationships for olanzapine in schizophrenia. Ther Drug Monit 25: 682-689
18. Frankle W.G., Gil R., Hackett E., Mawlawi O., Zea-Ponce Y., Zhu Z., Kochan L.D., Cangiano C., Slifstein M., Gorman J.M., Laruelle M., Abi-Dargham A. (2004) Occupancy of dopamine D2 receptors by the atypical antipsychotic drugs risperidone and olanzapine: theoretical implications. Psychopharmacology (Berl) 175: 473-480
19. Gefvert O., Bergstrom M., Langstrom B., Lundberg T., Lindstrom L., Yates R. (1998) Time course of central nervous dopamine-D2 and 5-HT2 receptor blockade and plasma drug concentrations after discontinuation of quetiapine (Seroquel) in patients with schizophrenia. Psychopharmacology (Berl) 135: 119-126
20. Gefvert O., Lundberg T., Wieselgren I.M., Bergstrom M., Langstrom B., Wiesel F., Lindstrom L. (2001) D(2) and 5HT(2A) receptor occupancy of different doses of quetiapine in schizophrenia: a PET study. Eur Neuropsychopharmacol 11: 105-110
21. Guitton C., Abbar M., Kinowski J.M., Chabrand P., Bressolle F. (1998) Multiple-dose pharmacokinetics of clozapine in patients with chronic schizophrenia. J Clin Psychopharmacol 18: 470-476
22. Guy W. (1976) ECDEU Assessment Manual for Psychopharmacology: Publication ADM 76-338. Washington, DC: US Department of Health, Education, and Welfare
23. Harvey E.J., Taylor D.M., Flanagan R.J. (2001) D2 receptor occupancy under recommended and high doses of olanzapine. J Psychopharmacol 15: 213-214
24. Hiemke C., Dragicevic A., Gründer G., Hätter S., Sachse J., Vernaleken I., Müller M.J. (2004) Therapeutic monitoring of new antipsychotic drugs. Ther Drug Monit 26: 156-160
25. Huang M.L., Van Peer A., Woestenborghs R., De Coster R., Heykants J., Jansen A A I, Zylicz Z., Visscher H.W., Jonkman J H G (1993) Pharmacokinetics of the novel antipsychotic agent risperidone and the prolactin response in healthy subjects. Clin Pharmacol Ther 54: 257-268
26. Jann M.W. (2002) Clinical significance of drug binding, protein binding, and binding displacement drug interactions. Psychopharmacology Bull 36: 22-41
27. Jerling M., Merle Y., Mentre F., Mallet A. (1997) Population pharmacokinetics of clozapine evaluated with the nonparametric maximum likelihood method. Br J Clin Pharmacol 44: 447-453
28. Jones C., Kapur S., Remington G., Zipursky R.B. (2000) Transient D2 dopamine receptor occupancy in low EPS incidence drugs: PET evidence. Biol Psychiatry 47 (Suppl 1). S112
29. Kapur S., Seeman P. (2000) Antipsychotic agents differ in how fast they come off the dopamine D2 receptors. Implications for atypical antipsychotic action. J Psychiatry Neurosci 25: 161-166
30. Kapur S., Zipursky R.B., Remington G., Jones C., DaSilva J., Wilson A.A., Houle S. (1998) 5-HT2 and D2 receptor occupancy of olanzapine in schizophrenia: a PET investigation. Am J Psychiatry 155: 921-928
31. Kapur S., Zipursky R.B., Remington G. (1999) Clinical and theoretical implications of 5-HT2 and D2 receptor occupancy of clozapine, risperidone, and olanzapine in schizophrenia. Am J Psychiatry 156: 286-293
32. Kapur S., Zipursky R., Jones C., Remington G., Houle S. (2000) Relationship between dopamine D(2) occupancy, clinical response, and side effects: a double-blind PET study of first-episode schizophrenia. Am J Psychiatry 157: 514-520
33. Kapur S., Zipursky R., Jones C., Shammi C.S., Remington G., Seeman P. (2000 a) A positron emission tomography study of quetiapine in schizophrenia- a preliminary finding of anantipsychotic effect with only transiently high dopamine D2 receptor occupancy. Arch Gen Psychiatry 57: 553-559
34. Kapur S., Remington G. (2001) Dopamine D(2) receptors and their role in atypical antipsychotic action: still necessary and may even be sufficient. Biol Psychiatry 50: 873-883
35. Kay S.R., Fiszbein A., Opler L.A. (1987) The positive and negative syndrome scale (PANSS) for schizophrenia. Schizophr Bull 13: 261-276
36. Kimko H.C., Reele S.S., Holford N.H., Peck C.C. (2000) Prediction of the outcome of a phase 3 clinical trial of an antischizophrenic agent (quetiapine fumarate) by simulation with a population pharmacokinetic and pharmacodynamic model. Clin Pharmacol Ther 68: 568-577
37. Knable M.B., Heinz A., Raedler T., Weinberger D.R. (1997) Extrapyramidal side effects with risperidone and haloperidol at comparable D2 receptor occupancy levels. Psychiatry Res 75: 91-101
38. Küfferle B., Tauscher J., Asenbaum S., Vesely C., Podreka I., Brucke T., Kasper S. (1997) IBZM SPECT imaging of striatal dopamine-2 receptors in psychotic patients treated with the novel antipsychotic substance quetiapine in comparison to clozapine and haloperidol. Psychopharmacology 133: 323-328
39. Laruelle M. (2000) Imaging synaptic neurotransmission with in vivo binding competition techniques: A critical review. J Cereb Blood Flow Metab 20: 423-451
40. Lavalaye J., Linszen D.H., Booij J., Reneman L., Gersons B.P., van Royen E.A. (1999) Dopamine D2 receptor occupancy by olanzapine or risperidone in young patients with schizophrenia. Psychiatry Res 92: 33-44
41. Mauri M.C., Laini V., Boscati L., Rudelli R., Salvi V., Orlandi R., Papa P. (2001) Long-term treatment of chronic schizophrenia with risperidone: a study with plasma levels. Eur Psychiatry 16: 57-63
42. Meisenzahl E.M., Dresel S., Frodl T., Schmitt G.J., Preuss U.W., Rossmuller B., Tatsch K., Mager T., Hahn K., Moller H.J. (2000) D2 receptor occupancy under recommended and high doses of olanzapine: an iodine-123-iodobenzamide SPECT study. J Psychopharmacol 14: 364-370
43. Miller D.D., Fleming F., Holman T.L., Penny P.J. (1994) Plasma clozapine concentrations as a predictor of clinical response: a follow-up study. J Clin Psychiatry 55 (Suppl B). 117-121
44. Nordström A.L., Farde L., Wiesel F.A., Forslund K., Pauli S., Halldin C., Uppfeldt G. (1993) Central D2-dopamine receptor occupancy in relation to antipsychotic drug effects-a double-blind PET study of schizophrenic patients. Biol Psychiatry 33: 227-235
45. Nordström A.L., Farde L., Eriksson L., Halldin C. (1995) No elevated D-2 dopamine receptors in neuroleptic-naive schizophrenic patients revealed by positron emission tomography and [C-11]n-methylspiperone. Psychiatry Res 61: 67-83
46. Nyberg S., Nordström A-L., Halldin C., Farde L. (1995) Positron emission tomography studies on D2 dopamine receptor occupancy and plasma antipsychotic drug levels in man. Int Clin Psychopharmacol 10 (Suppl 3). 81-85
47. Nyberg S., Eriksson B., Oxenstierna G., Halldin C., Farde L. (1999) Suggested minimal effective dose of risperidone based on PET-measured D2 and 5-HT2A receptor occupancy in schizophrenic patients. Am J Psychiatry 156: 869-875
48. Nyberg S., Chou Y.H., Halldin C. (2002) Saturation of striatal D(2) dopamine receptors by clozapine. Int J Neuropsychopharmacol 5: 11-16
49. Olesen O.V., Linnet K. (1999) Olanzapine serum concentrations in psychiatric patients given standard doses: the influence of comedication. Ther Drug Monit 21: 87-90
50. Olesen O.V., Licht R.W., Thomsen E., Bruun T., Viftrup J.E., Linnet K. (1998) Serum concentrations and side effects in psychiatric patients during risperidone therapy. Ther Drug Monit 20: 380-384
51. Perry P.J., Miller D.D., Arndt S.V., Cadoret R.J. (1991) Clozapine and nor-clozapine plasma concentrations and clinical response of treatment refractory schizophrenic patients. Am J Psychiatry 148: 23l - 235
52. Perry P.J., Lund B.C., Sanger T., Beasley C. (2001) Olanzapine plasma concentrations and clinical response: acute phase results of the North American Olanzapine Trial. J Clin Psychopharmacol 21: 14-20
53. Pickar D., Su T.P., Weinberger D.R., Coppola R., Malhotra A.K., Knable M.B., Lee K.S., Gorey J., Bartko J.J., Breier A., Hsiao J. (1996) Individual variation in D2 dopamine receptor occupancy in clozapine-treated patients. Am J Psychiatry 153: 1571-1578
54. Pilowsky L.S., Costa D.C., Ell P.J., Murray R.M., Verhoeff N.P., Kerwin R.W. (1992) Clozapine, single photon emission tomography, and the D2 dopamine receptor blockade hypothesis of schizophrenia. Lancet 340: 199-202
55. Pilowsky L.S., Busatto G.F., Taylor M., Costa D.C., Sharma T., Sigmundsson T., Ell P.J., Nohria V., Kerwin R.W. (1996) Dopamine D2 receptor occupancy in vivo by the novel atypical antipsychotic olanzapine - a 123I-IBZM single photon emission tomography (SPET) study. Psychopharmacology (Berl) 124: 148-153
56. Raggi M.A., Mandrioli R., Sabbioni C., Pucci V. (2004) Atypical antipsychotics: pharmacokinetics, therapeutic drug monitoring and pharmacological interactions. Current Medicinal Chemistry 11: 279-296
57. Remington G., Kapur S., Zipursky R. (1998) The relationship between risperidone plasma levels and dopamine D2 occupancy: a positron emission tomographic study. J Clin Psychopharmacol 18: 82-83
58. Rinne J.O., Hietala J., Ruotsalainen U., Sako E., Laihinen A., Någren K., Lehikoinen P., Oikonen V., Syvälahti E. (1993) Decrease in human striatal dopamine D2 receptor density with age: a PET study with [11C]raclopride. J Cereb Blood Flow Metab 13: 310-314
59. Scherer J., Tatsch K., Schwarz J., Oertel W., Kirsch M.C., Albus M. (1994) Striatal D2-dopamine receptor occupancy during treatment with typical and atypical neuroleptics. Biol Psychiatry 36: 627-629
60. Schmitt G.J., Meisenzahl E.M., Dresel S., Tatsch K., Rossmuller B., Frodl T., Preuss U.W., Hahn K., Moller H.J. (2002) Striatal dopamine D2 receptor binding of risperidone in schizophrenic patients as assessed by 123I-iodobenzamide SPECT: a comparative study with olanzapine. J Psychopharmacol 16: 200-206
61. Schotte A., Janssen P F M, Gommeren W., Luyten W H M L, VanGompel P., Lesage A.S., DeLoore K., Leysen J.E. (1996) Risperidone compared with new and reference antipsychotic drugs In vitro and in vivo receptor binding. Psychopharmacology (Berl) 124: 57-73
62. Seeman P., Lee T., Chau-Wong M., Wong K. (1976) Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature 261: 717-719
63. Seeman P. (2005) An update of fast-off dopamine D2 atypical antipsychotics. Am J Psychiatry 162: 1984-1985
64. Sidhu J., Job S., Bullman J., Francis E., Abbott R., Ascher J., Theis J.G. (2006) Pharmacokinetics and tolerability of lamotrigine and olanzapine coadministered to healthy subjects. Br J Clin Pharmacol 61: 420-426
65. Talvik M., Nordstrom A.L., Nyberg S., Olsson H., Halldin C., Farde L. (2001) No support for regional selectivity in clozapine-treated patients: a PET study with [(11)C]raclopride and [(11)C]FLB 457. Am J Psychiatry 158: 926-930
66. Talvik M., Nordstrom A.L., Larsen N.E., Jucaite A., Cervenka S., Halldin C., Farde L. (2004) A cross-validation study on the relationship between central D2 receptor occupancy and serum perphenazine concentration. Psychopharmacology 175: 148-153
67. Tauscher J., Küfferle B., Barnas C., Asenbaum S., Brücke T., Kasper S. (1997) Dopamine-2 receptor imaging in psychotic patients treated with quetiapine, clozapine, risperidone and haloperidol. Biol Psychiatry 42: 15S
68. Tauscher J., Kufferle B., Asenbaum S., Fischer P., Pezawas L., Barnas C., Tauscher-Wisniewski S., Brucke T., Kasper S. (1999) In vivo 123I-IBZM SPECT imaging of striatal dopamine-2 receptor occupancy in schizophrenic patients treated with olanzapine in comparison to clozapine and haloperidol. Psychopharmacology (Berl) 141: 175-181
69. Tauscher J., Küfferle B., Asenbaum S., Tauscher-Wisniewski S., Kasper S. (2002) Striatal dopamine-2 receptor occupancy as measured with [123I]iodobenzamide and SPECT predicted the occurrence of EPS in patients treated with atypical antipsychotics and haloperidol. Psychopharmacology (Berl) 162: 42-49
70. Tauscher J., Jones C., Remington G., Zipursky R.B., Kapur S. (2002 a) Significant dissociation of brain and plasma kinetics with antipsychotics. Mol Psychiatry 7: 317-321
71. Tauscher-Wisniewski S., Kapur S., Tauscher J., Jones C., Daskalakis Z.J., Papatheodorou G. et al. (2002) Quetiapine: an effective antipsychotic in first-episode schizophrenia despite only transiently high dopamine-2 receptor blockade. J Clin Psychiatry 63: 992-997
72. Tort A B L, Souza D.O., Lara D.R. (2006) Theoretical insights into the mechanism of action of atypical antipscyhotics. Prog Neuropsychopharmacol Biol Psychiatry 30: 541-548