Prolactinemia is uncoupled from central D-2/D-3 dopamine receptor occupancy in amisulpride treated patients

Show simple item record Bressan, R. A. Erlandsson, K. Spencer, E. P. Ell, P. J. Pilowsky, L. S. 2016-01-24T12:37:20Z 2016-01-24T12:37:20Z 2004-09-01
dc.identifier.citation Psychopharmacology. New York: Springer, v. 175, n. 3, p. 367-373, 2004.
dc.identifier.issn 0033-3158
dc.description.abstract Atypical antipsychotic drugs are classically associated with lower propensity to extrapyramidal symptoms (EPS) and hyperprolactinemia than typical antipsychotic drugs. It has not been clarified why some atypical antipsychotic drugs, such as amisulpride, induce prolactin plasma concentration (PRL) elevation, but little EPS. Previous studies have found an association between striatal D-2/D-3 receptor occupancy and PRL in typical antipsychotic treated patients suggesting that PRL is a marker of central D-2/D-3 receptors blockade. Objective: We have evaluated the relationship between PRL and central (striatum, temporal cortex and thalamus) D-2/D-3 receptor occupancy in amisulpride treated schizophrenic patients. Methods: Single photon emission tomography (SPET) and [I-123]-epidepride were used to determine D-2/D-3 receptor occupancy in eight amisulpride treated patients. PRL was measured concurrently with the scans. Results: the mean PRL was 1166 (range 499-1892 mIU/1) for a mean amisulpride dose of 406 mg/day (range 150-600 mg/day). Amisulpride plasma concentration and central D-2/D-3 receptor occupancy were positively correlated (r=0.83-0.89, df=4, P<0.05). No significant correlations were observed between PRL and amisulpride (daily dose or plasma concentration, P>0.05), or between PRL and central D-2/D-3 receptor occupancy (P>0.05). Conclusions: Our findings show that amisulpride-induced hyperprolactinemia is uncoupled from central D-2/D-3 receptor occupancy. Amisulpride has poor blood-brain barrier penetration and reaches much higher concentration at the pituitary, which is outside the blood-brain barrier. Higher D-2/D-3 receptor occupancy at the pituitary gland than at central regions is a possible explanation for amisulpride PRL elevation with low EPS. Further studies evaluating pituitary D-2/D-3 receptor occupancy in vivo are necessary to confirm this hypothesis. en
dc.format.extent 367-373
dc.language.iso eng
dc.publisher Springer
dc.relation.ispartof Psychopharmacology
dc.rights Acesso restrito
dc.subject prolactin en
dc.subject antipsychotic agents en
dc.subject atypical antipsychotic en
dc.subject neuroleptic en
dc.subject dopamine receptor en
dc.subject D-2-dopamine en
dc.subject schizophrenia en
dc.subject SPECT en
dc.subject [I-123]-epidepride en
dc.subject amisulpride en
dc.subject photon emission tomography en
dc.title Prolactinemia is uncoupled from central D-2/D-3 dopamine receptor occupancy in amisulpride treated patients en
dc.type Artigo
dc.contributor.institution Universidade Federal de São Paulo (UNIFESP)
dc.contributor.institution Univ London Kings Coll
dc.contributor.institution UCL Med Sch
dc.contributor.institution Guys & St Thomas Hosp Trust
dc.description.affiliation Universidade Federal de São Paulo, Dept Psiquiatria, BR-04026001 São Paulo, Brazil
dc.description.affiliation Univ London Kings Coll, Inst Psychiat, Sect Neurochem Imaging, London SE5 8AF, England
dc.description.affiliation UCL Med Sch, Middlesex Hosp, Inst Nucl Med, London, England
dc.description.affiliation Guys & St Thomas Hosp Trust, Med Toxicol Unit, London, England
dc.description.affiliationUnifesp Universidade Federal de São Paulo, Dept Psiquiatria, BR-04026001 São Paulo, Brazil
dc.identifier.doi 10.1007/s00213-004-1826-6
dc.description.source Web of Science
dc.identifier.wos WOS:000224527000012


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