Abstract
The clinical benefit of the atypical antipsychotic drug clozapine may be related to a combined effect on D2 and 5-HT2 receptors. To examine the basis for this hypothesis, positron emission tomography (PET) and the radioligand [11C]N-methylspiperone were used to determine cortical 5-HT2 receptor occupancy in three psychotic patients treated with 125 mg, 175mg and 200mg clozapine daily. The uptake of [11C]N-methylspiperone in the frontal cortex was very low compared to that in neuroleptic naive schizophrenic patients. 5-HT2 receptor occupancy calculated in the clozapine treated patients was 84%, 87% and 90%. The results show that clinical treatment with clozapine induces a high 5-HT2 receptor occupancy in psychotic patients at a low dose level.
Publication types
-
Clinical Trial
-
Research Support, Non-U.S. Gov't
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Adult
-
Antipsychotic Agents / pharmacokinetics
-
Clozapine / pharmacokinetics*
-
Clozapine / therapeutic use
-
Dopamine Agonists / pharmacokinetics
-
Female
-
Humans
-
Male
-
Middle Aged
-
Prefrontal Cortex / anatomy & histology
-
Prefrontal Cortex / metabolism
-
Psychotic Disorders / drug therapy
-
Psychotic Disorders / metabolism
-
Raclopride
-
Receptors, Serotonin / metabolism*
-
Salicylamides / pharmacokinetics
-
Schizophrenia / drug therapy
-
Schizophrenia / metabolism
-
Spiperone / analogs & derivatives
-
Spiperone / pharmacokinetics
-
Tomography, Emission-Computed
Substances
-
Antipsychotic Agents
-
Dopamine Agonists
-
Receptors, Serotonin
-
Salicylamides
-
Raclopride
-
Spiperone
-
3-N-methylspiperone
-
Clozapine