Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:dateCreated
1997-7-31
pubmed:abstractText
Acute extrapyramidal syndromes (EPS) are frequently recorded during treatment with classical neuroleptic drugs. In patients with EPS a consistent finding is high central D2-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 D2 occupancy (20-67%). We have proposed that the PET demonstration of low D2 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 D2 occupancy and EPS liability reported for clozapine. Sertindole is a new antipsychotic drug which has shown a low incidence of acute EPS in clinical studies. In the present study PET was used to measure central D2-dopamine receptor binding in the basal ganglia at baseline and 6 h after oral administration of 4 mg sertindole to two healthy males. D2-dopamine receptor occupancy was 15% in one subject and 6% in the other. The low occupancy level demonstrated at 4 mg indicates the need for a PET study in patients at the suggested clinical dose level of 12-24 mg a day. In particular, it is important to determine whether sertindole induces antipsychotic effects at a D2 occupancy level which is lower that found in patients treated with classical antipsychotics.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0268-1315
pubmed:author
pubmed:issnType
Print
pubmed:volume
12 Suppl 1
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
S3-7
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1997
pubmed:articleTitle
D2 occupancy, extrapyramidal side effects and antipsychotic drug treatment: a pilot study with sertindole in healthy subjects.
pubmed:affiliation
Department of Clinical Neuroscience, Karolinska Institutet, Stockholm, Sweden.
pubmed:publicationType
Journal Article, Clinical Trial, Research Support, Non-U.S. Gov't