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Titolo:
D-2 OCCUPANCY, EXTRAPYRAMIDAL SIDE-EFFECTS AND ANTIPSYCHOTIC DRUG-TREATMENT - A PILOT-STUDY WITH SERTINDOLE IN HEALTHY-SUBJECTS
Autore:
FARDE L; MACK RJ; NYBERG S; HALLDIN C;
Indirizzi:
KAROLINSKA HOSP,PSYCHIAT CLIN S-17176 STOCKHOLM SWEDEN KAROLINSKA INST,DEPT CLIN NEUROSCI,PSYCHIAT SECT STOCKHOLM SWEDEN ABBOTT LABS ABBOTT PK IL 60064
Titolo Testata:
International clinical psychopharmacology
, volume: 12, anno: 1997, supplemento:, 1
pagine: 3 - 7
SICI:
0268-1315(1997)12:<3:DOESAA>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
D2-DOPAMINE RECEPTOR OCCUPANCY; C-11 RACLOPRIDE BINDING; SCHIZOPHRENIC-PATIENTS; NEUROLEPTIC THRESHOLD; DOPAMINE-RECEPTORS; DOUBLE-BLIND; PET; RISPERIDONE; OLANZAPINE; CLOZAPINE;
Keywords:
D-2-DOPAMINE RECEPTORS; POSITRON EMISSION TOMOGRAPHY; EXTRAPYRAMIDAL SIDE EFFECTS; SERTINDOLE; ANTIPSYCHOTIC DRUGS; HUMANS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
43
Recensione:
Indirizzi per estratti:
Citazione:
L. Farde et al., "D-2 OCCUPANCY, EXTRAPYRAMIDAL SIDE-EFFECTS AND ANTIPSYCHOTIC DRUG-TREATMENT - A PILOT-STUDY WITH SERTINDOLE IN HEALTHY-SUBJECTS", International clinical psychopharmacology, 12, 1997, pp. 3-7

Abstract

Acute extrapyramidal syndromes (EPS) are frequently recorded during treatment with classical neuroleptic drugs. In patients with EPS a consistent finding is high central D-2-receptor occupancy (> 80%) as demonstrated with positron emission tomography (PET). The exception is clozapine, an atypical antipsychotic which has low EPS liability and also induces a low D-2 occupancy (20-67%). We have proposed that the PET demonstration of low D-2 occupancy at antipsychotic dose levels can be viewed as a strategy to confirm atypicality. There have been strong incentives in recent years to discover new drugs which do not induce EPS,but so far no drug has been shown unequivocally to have the low D-2 occupancy and EPS liability reported for clozapine. Sertindole is a newantipsychotic drug which has shown a low incidence of acute EPS in clinical studies. In the present study PET was used to measure central D-2-dopamine receptor binding in the basal ganglia at baseline and 6 h after oral administration of 4 mg sertindole to two healthy males. D-2-dopamine receptor occupancy was 15% in one subject and 6% in the other. The low occupancy level demonstrated at 4 mg indicates the need fora PET study in patients at the suggested clinical dose level of 12-24mg a day. In particular, it is important to determine whether sertindole induces antipsychotic effects at a D-2 occupancy level which is lower that found in patients treated with classical antipsychotics.

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Documento generato il 03/04/20 alle ore 20:26:43