摘要
目的：评价奥氮平的抗精神病作用。方法：通过苯丙胺诱导的小鼠定向运动实验、５－ＨＴＰ诱导的小鼠头部抽动实验、大鼠僵住症试验，对奥氮平进行药效学观察，并与氯氮平及氟哌啶醇的药效进行比较。结果：奥氮平（ｉｇ，ＥＤ５０５．８８ｍｇ／ｋｇ）、氯氮平（ｉｇ，ＥＤ５０３７．１６ｍｇ／ｋｇ）、氟哌啶醇（ｉｇ，ＥＤ５００．７４ｍｇ／ｋｇ）能显著地拮抗苯丙胺诱导的小鼠定向运动，且有明显的量效关系。奥氮平（ｉｇ，ＥＤ５００．５４ｍｇ／ｋｇ）、氯氮平（ｉｇ，ＥＤ５０３．１０ｍｇ／ｋｇ）、氟哌啶醇（ｉｇ，ＥＤ５００．７１ｍｇ／ｋｇ）能明显地拮抗５－ＨＴＰ诱导的小鼠头部抽动。大鼠僵住症实验中，奥氮平、氯氮平、氟哌啶醇的ｉｇ，ＥＤ５０分别是２６，１４９，０．５４ｍｇ／ｋｇ。结论：奥氮平有拮抗多巴胺及５－ＨＴ的活性，且其拮抗５－ＨＴ的作用比拮抗多巴胺的作用强，奥氮平的锥体外系不良反应轻，是一较好的抗精神病药物，奥氮平与氟哌啶醇合用对一些患者可能是较好的治疗方案。
Objective: To evaluate the antipsychotic effects of olanzapine. Methods: The
effects of olanzapine on amphetamine induced forced action and 5hydroxytryptophan (5HTP)
induced head twitches were observed in mice. The experiments of catalepsy induced by
olanzapine were carried out in rats. The results were compared with those of clozapine and
haloperidol. Results: Olanzapine (2.4￣9.6 mg/kg, ig, ED50 5.88 mg/kg), clozapine (12￣48
mg/kg, ig, ED50 37.16 mg/kg), haloperidol (0.225￣0.900 mg/kg, ig, ED50 0.74 mg/kg) could
significantly antagonize amphetamineinduced forced action in mice in dosedependent manner.
Olanzapine (0.3￣1.2 mg/kg, ig, ED50 0.54 mg/kg), clozapine (1.5￣6.0 mg/kg, ig, ED50 3.10
mg/kg), haloperidol (0.225￣0.900 mg/kg, ig, ED50 0.71 mg/kg) could significantly antagonize
5HTP induced head twitches in mice. In rats catalepsy tests, the ig, ED50 of olanzapine,
clozapine, haloperidol were 26, 149, 0.54 mg/kg, respectively. Conclusion: Olanzapine
possesses dopamine and 5HT antagon and was a more potent 5HT antagonist than dopamine
antagonist. Olanzapine has a low property for producing extrapyramidal symptoms.
Olanzapine is expected to find a place as a valuable alternative in classical antipsychotics.
The combination of olanzapine and haloperidol may be a good recipe for some patients.
出处
《第二军医大学学报》
CAS
CSCD
北大核心
1999年第5期308-311,共4页
Academic Journal of Second Military Medical University
