新しい向〓神薬Butyrophenone系化合物について

Some of butyrophenone derivatives, the third category of excellent psychotropic agents, were examined from the clinical view-point. The specific properties of these drugs consisted in stronger neuroleptic action than that of phenothiazine derivatives or of reserpine, also in poor involvement of autonomic nervous system and as well in prominent neurodysleptic action (Divry). This neurodysleptic action is divided into two types: major paro ysmal syndrome and minor subacute manifestation (restlessness syndrome). The latter syndrome is said very important and unique, as it is sometimes effectively utilized to crack “the shell of autism” of schizophrenic patients.<BR>In our experiments, benperidol, haloperidol, dipiperon and trifluperidol (and spiroperidol shortly after this report) were given per os chiefly to schizophrenic patients, and the results and comparison among them were described hereafter.<BR>Dipiperon and benperidol tended to ameliorate disturbance of sleep, while haloperidol and trifluperidol seemed often to bring disturbance of sleep in agitated state due to neurodysleptic action. Intravenous application of haloperidol and trifluperidol, however, brought sleepiness clinically as well as in EEG findings. Major dystonic syndrome was often observed in case of haloperidol and benperidol, while minor syndrome was more frequently observed in case of trifluperidol. The neurodysleptic action of dipiperon was milder than the others, but it seemed to possess thymoleptic action at the same time.<BR>These butyrophenone derivatives, except dipiperon, were quite effective on paranoidhallucinatory state and psychomotor excitation of both acute and chronic psychoses. Main application of these drugs was, in our opinion, as follows: haloperidol was quite effective for mania, acute psychoses (implying schizophrenia), trifluperidol for confusion and both acute and chronic schizophrenia, benperidol for acute psychoses and dipiperon for atypical psychoses and for the beginning stage of schizophrenia. At the same time, effectiveness of these drugs was recognized in epileptic patients.<BR>As to the side effect, extrapyramidal manifestations, neurodysleptic action, certain symptoms of autonomic nervous system were observed. But these side effects were easily removed by antagonistic agents.<BR>Finally, it is always necessary to consider dosage, kind, side effects, etc. quite cautiously when usage of these of these drugs is enterprised, as the personal susceptibility to these drugs differs to pretty high extent.<BR>Appendix: Clinical effect of spiroperdol is said to situate between that of holoperidol and trifluperdol.