Budget Amount *help |
¥2,400,000 (Direct Cost: ¥2,400,000)
Fiscal Year 1987: ¥1,000,000 (Direct Cost: ¥1,000,000)
Fiscal Year 1986: ¥1,400,000 (Direct Cost: ¥1,400,000)
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Research Abstract |
Most of antipsychotics have not only anti-dopamine 2 (D2) activities, but also anti-noradrenaline (NA) and anti-serotonin (5HT) activities. We measured anti-D2, anti-NA and anti-5HT activities in the plasma of schizophrenic patients receiving antipsychotics medication using radio receptor assay (RRA). We used in the RRA the following ^3H-ligand, displacer and receptor preparation, respectively : in D2 RRA, 1 nM ^3H-(-)-sulpiride, 100 nM haloperidol and rat striatum preparation,in NA RRA, 0.2 nM ^3H-prazosin, 200 nM prazosin and rat frontal cortex preparation, in 5HT RRA, 1 nM ^3H-ketanserine, 500 nM pipamperone and rat frontal cortex preparation. Anti-D2 activities were based on haloperidol equivalent (HPD-E) ng/ml and chlorpromazine equivalent (CPZ-E) ng/ml. Anti-NA and anti-5HT activities were based on CPZ-E ng/ml. Patients were divided into two groups : group 1 ; on the maintenance therapy of 42 stable outpatients, group 2 ; on the acute therapy of 18 hospitalized patients at the fir
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st onset or with acute exacerbation. Their clinical symptoms were rated by physicians using BPRS. Most of the cases were treated with monodrug, 81 % in group 1, and all in group 2, respectively. Furthermore, we investigated relationship between the plasma monoamine receptor binding activities, plasma drug concentration, clinical effect and patients' profiles. Results were summarized as follows. In the group 1, anti-D2 activities of many patients (69.1 %) were less than 10 HPD-E ng/ml and 100 CPZ-E ng/ml. The longer the illness duration was, the higher were the anti-D2, anti-NA and anti-5HT activities. And also, the daily doses and the negative symptom points increased along with the illness duration. In the group 2, 15 cases (80 %) showed good response to haloperidol (HPD), other 3 cases did not, but improved with other antipsychotics. There were positive correlation between anti-D2 activities, plasma HPD concentration and daily HPD dose. Anti-D2 activities of most patients (80 %) were less than 15 HPD-E ng/ml and 150 CPZ-E ng/ml. There was positive correlation between clinical improvement and anti-NA activities, but not anti-D2 activities in the patients with HPD monotherapy. Less
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