McKeage Kate, Plosker Greg L
Adis International Limited, Auckland, New Zealand.
CNS Drugs. 2004;18(13):933-56. doi: 10.2165/00023210-200418130-00007.
Amisulpride (Solian), a substituted benzamide derivative, is a second-generation antipsychotic that preferentially binds to dopamine D2/D3 receptors in limbic rather than striatal structures. High dosages preferentially antagonise postsynaptic D2/D3 receptors, resulting in reduced dopamine transmission, and low dosages preferentially block presynaptic D2/D3 receptors, resulting in enhanced dopamine transmission. Amisulpride (200-1200 mg/day) was at least as effective as haloperidol and as effective as risperidone or olanzapine, in studies of up to 1 year in patients with schizophrenia manifesting predominantly positive symptoms. Amisulpride (50-300 mg/day) was significantly more effective than placebo in studies of up to 6 months in patients manifesting predominantly negative symptoms. Quality of life was also improved significantly more in patients receiving amisulpride than in those receiving haloperidol in 4- and 12-month studies in patients with predominantly mixed symptoms. Amisulpride was generally well tolerated in clinical trials. In patients with predominantly positive symptoms, amisulpride appeared to be better tolerated than haloperidol and was tolerated as well as risperidone and olanzapine. The incidence of extrapyramidal adverse effects with amisulpride was lower than with haloperidol but was generally similar to risperidone or olanzapine. Weight gain with amisulpride was less than that with risperidone or olanzapine and, unlike these agents, amisulpride does not seem to be associated with diabetogenic effects. Plasma prolactin levels are increased during amisulpride therapy and amenorrhoea occurs in about 4% of women. The incidence of adverse events with low dosages of amisulpride (< or = 300 mg/day) in patients with predominantly negative symptoms was similar to that observed with placebo. In conclusion, oral amisulpride (200-1200 mg/day) is at least as effective as haloperidol, and as effective as risperidone or olanzapine, in the treatment of patients with schizophrenia manifesting predominantly positive symptoms. In the treatment of patients manifesting predominantly negative symptoms, low dosages of amisulpride (50-300 mg/day) are significantly more effective than placebo. Amisulpride appears to be better tolerated than haloperidol, causing a lower incidence of extrapyramidal adverse effects and an improved quality of life. Compared with risperidone or olanzapine, amisulpride is more likely to cause hyperprolactinaemia, but has a lower propensity to cause weight gain and does not seem to be associated with diabetogenic effects. Thus, amisulpride is an effective and well tolerated option for the first-line treatment of patients with acute schizophrenia as well as for those requiring long-term maintenance therapy.
氨磺必利(索里昂)是一种取代苯甲酰胺衍生物,是第二代抗精神病药物,它优先与边缘系统而非纹状体结构中的多巴胺D2/D3受体结合。高剂量时优先拮抗突触后D2/D3受体,导致多巴胺传递减少;低剂量时优先阻断突触前D2/D3受体,导致多巴胺传递增强。在对以阳性症状为主的精神分裂症患者进行的长达1年的研究中,氨磺必利(200 - 1200毫克/天)至少与氟哌啶醇一样有效,且与利培酮或奥氮平效果相当。在对以阴性症状为主的患者进行的长达6个月的研究中,氨磺必利(50 - 300毫克/天)比安慰剂显著更有效。在对以混合症状为主的患者进行的4个月和12个月的研究中,接受氨磺必利治疗的患者的生活质量改善也明显优于接受氟哌啶醇治疗的患者。氨磺必利在临床试验中总体耐受性良好。在以阳性症状为主的患者中,氨磺必利的耐受性似乎优于氟哌啶醇,且与利培酮和奥氮平的耐受性相当。氨磺必利引起锥体外系不良反应的发生率低于氟哌啶醇,但总体上与利培酮或奥氮平相似。氨磺必利导致的体重增加少于利培酮或奥氮平,而且与这些药物不同,氨磺必利似乎与致糖尿病作用无关。氨磺必利治疗期间血浆催乳素水平会升高,约4%的女性会出现闭经。在以阴性症状为主的患者中,低剂量氨磺必利(≤300毫克/天)的不良事件发生率与安慰剂观察到的相似。总之,口服氨磺必利(200 - 1200毫克/天)在治疗以阳性症状为主的精神分裂症患者时至少与氟哌啶醇一样有效,且与利培酮或奥氮平效果相当。在治疗以阴性症状为主的患者时,低剂量氨磺必利(50 - 300毫克/天)比安慰剂显著更有效。氨磺必利的耐受性似乎优于氟哌啶醇,锥体外系不良反应发生率较低,生活质量得到改善。与利培酮或奥氮平相比,氨磺必利更易引起高催乳素血症,但导致体重增加的倾向较低,且似乎与致糖尿病作用无关。因此,氨磺必利是急性精神分裂症患者一线治疗以及需要长期维持治疗患者的一种有效且耐受性良好的选择。