Antipsychotic efficacy: relationship to optimal D2-receptor occupancy.

作者: Luca Pani , Luigi Pira , Giorgio Marchese

DOI: 10.1016/J.EURPSY.2007.02.005

关键词: Extrapyramidal symptomsDrugAntipsychoticPharmacodynamicsSchizophreniaBioinformaticsPsychologyPsychiatryDopamine receptor D2DopamineTolerability

摘要: Clinically important differences exist between antipsychotic agents and formulations in terms of safety tolerability. Features the biochemical interaction D2-receptor may underlie these differences. This article reviews current information on relationship receptor occupancy clinical response. A literature search was performed using keywords ‘antipsychotic or neuroleptic’, ‘receptor’ ‘occupancy’ ‘dopamine’ ‘D2’ supplemented by authors’ knowledge literature. Imaging data have generally supported hypotheses that optimal striatum lies a ‘therapeutic window’ ∼65 ∼80%, however, pharmacokinetic pharmacodynamic properties drug should also be taken into account to fully evaluate its therapeutic effects. Additional research, perhaps preclinical models, is needed establish various regions brain duration blockade order maximise efficacy tolerability profiles atypical antipsychotics thereby improve treatment outcomes for patients with schizophrenia.

参考文章(77)
Larry Ereshefsky, Cynthia A Mascarenas, Comparison of the Effects of Different Routes of Antipsychotic Administration on Pharmacokinetics and Pharmacodynamics The Journal of Clinical Psychiatry. ,vol. 64, pp. 18- 23 ,(2003)
Philip Seeman, Atypical Antipsychotics: Mechanism of Action: The Canadian Journal of Psychiatry. ,vol. 47, pp. 27- 38 ,(2002) , 10.1177/070674370204700106
Joseph M Pierre, Extrapyramidal Symptoms with Atypical Antipsychotics Drug Safety. ,vol. 28, pp. 191- 208 ,(2005) , 10.2165/00002018-200528030-00002
Andrew H Miller, Michael T Compton, Antipsychotic-induced hyperprolactinemia and sexual dysfunction. Psychopharmacology Bulletin. ,vol. 36, pp. 143- 164 ,(2002)
Daniel E. Casey, Pathophysiology of antipsychotic drug-induced movement disorders. The Journal of Clinical Psychiatry. ,vol. 65, pp. 25- 28 ,(2004)
Nina R Schooler, Relapse and rehospitalization: comparing oral and depot antipsychotics. The Journal of Clinical Psychiatry. ,vol. 64, pp. 14- 17 ,(2003)
S Kapur, P Seeman, Antipsychotic agents differ in how fast they come off the dopamine D2 receptors. Implications for atypical antipsychotic action. Journal of Psychiatry & Neuroscience. ,vol. 25, pp. 161- 166 ,(2000)
Gary D Tollefson, Charles M Beasley Jr, Pierre V Tran, Jamie S Street, John A Krueger, Roy N Tamura, Karin A Graffeo, Martha E Thieme, Olanzapine versus haloperidol in the treatment of schizophrenia and schizoaffective and schizophreniform disorders: results of an international collaborative trial. American Journal of Psychiatry. ,vol. 154, pp. 457- 465 ,(1997) , 10.1176/AJP.154.4.457
C. M. Davis, Stephen R Saklad, L. Ereshefsky, G. Toney, T. Tran-Johnson, R. C. Lyman, Kinetics and clinical evaluation of haloperidol decanoate loading dose regimen. Psychopharmacology Bulletin. ,vol. 26, pp. 108- 114 ,(1990)