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COMPARISON OF THE MEAN ANTI-D2 ACTIVITY,
THE MEAN ANTI-5-HT2A ACTIVITY AND THE
MEAN ANTI-5-HT2A ACTIVITY / ANTI-D2
ACTIVITY (S/D) RATIO IN PLASMA OF BETWEEN TYPICAL ANTIPSYCHOTIC
AGENTS AND ATYPICAL ANTIPSYCHOTIC AGENTS
DEPT. OF PSYCHIATRY ST. MARIANNA UNIVERSITY SCHOOL OF MEDICINE,
KAWASAKI, JAPAN
H. SUZUKI, Y. MOROKAWA, K. GEN, M. KAMIMURA, H. TAKAGI,
N. YAMAGUCHI, AND A. AOBA
Ever since the introduction of atypical antipsychotic agents
for the treatment of schizophrenia, the pharmacological characteristics
and efficacy of typical antipsychotic agents and atypical antipsychotic
agents have been repeatedly compared. In this study, we measured
the plasma anti-D2 activity and the anti-5-HT2A
activity in schizophrenic patients undergoing treatment with
risperidone, zotepine, olanzapine, chlorpromazine, bromperidol,
or haloperidol in order to clarify the pharmacological characteristics
and efficacy of typical antipsychotic agents and atypical antipsychotic
agents in vivo. Of the 223 patients who were enrolled in the
study, 67 were in the risperidone-administered group, 86 in
the zotepine-administered group, 10 in the olanzapine-administered
group, 26 in the chlorpromazine-administered group,14 in the
bromperidol-administered group, and 20 in the haloperidol -administered
group. All these patients were diagnosed as having schizophrenia
based on the DSM-IV criteria. Blood samples were collected from
these subjects after administration of a fixed dose of the respective
drugs for 14 days. The anti-D2 and the
anti-5-HT2A activities in plasma were
measured by the radioreceptor assay method using ［3H］-spiperone
and ［3H］-ketanserin. The anti-5-HT2A
activity was divided by the anti-D2 activity
in plasma to obtain the S/D ratio. The relationship between
the mean anti-D2 activity and the mean
anti-5-HT2A activity in plasma is evaluated
using the risperidone standard curve. There was a significant
correlation between the mean anti-D2 activity
and the mean anti-5-HT2A activity in plasma
for the risperidone-administered group(p<0.01, r=0.40). There
was no significant correlation between the mean anti-D2
activity and the mean anti-5-HT2A activity
in plasma for the other groups. Below is the mean anti-D2
activity, the mean anti-5-HT2A activity
and the mean S/D ratio in vivo.
| (mean±sd) *p<0.001
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anti-D2
activity(nmol) |
anti-5-HT2A
activity（nmol） |
S/D ratio |
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| risperidone |
26.6±25.0 |
21.6±19.2 |
1.2±1.1 |
| zotepine |
18.1±21.1 |
1.8±9.3 |
1.2±1.2 |
| olanzapine |
43.9±34.5 |
33.1±31.1 |
1.0±1.2 |
|
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| chlorpromazine |
6.7±7.6 |
1.0±0.2 |
0.2±0.2 |
| bromperidol |
2.3±1.5 |
0.0±0.0 |
0.0±0.0 |
| haloperidol |
0.19±0.1 |
0 |
0 |
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The mean S/D ratio for the three typical antipsychotic agents
(chlorpromazine, bromperidol, and haloperidol) was 0.5 and the
mean S/D ratio for the three atypical antipsychotic agents (risperidone,
zotepine, olanzapine) was 1.2. Therefore the mean S/D ratio
for typical antipsychotic agents (chlorpromazine, bromperidol,
and haloperidol) was significantly lower than atypical antipsychotic
agents (risperidone, zotepine, olanzapine).
From these results, it was suggested that the value of S/D ratio
in vivo is important to classify the antipsychotic agents to
typical antipsychotic agents and atypical antipsychotic agents
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