Owen R T
Crewe, Cheshire, UK.
Drugs Today (Barc). 2010 Mar;46(3):173-81. doi: 10.1358/dot.2010.46.3.1476499.
Olanzapine, an atypical antipsychotic was first introduced in 1996 as an oral formulation and is used in the treatment of schizophrenia and bipolar disorder. Recent developments have included parenteral formulations to improve compliance in the treatment of schizophrenia and to treat agitation in patients with schizophrenia and bipolar mania. Olanzapine pamoate long acting injection (depot) is a novel formulation of the atypical antipsychotic olanzapine, which is licensed for the maintenance treatment of schizophrenia. When administered as the pamoate salt, olanzapine has an elimination half-life of approximately 30 days, allowing it to be given at 2- or 4-weekly intervals. An 8-week, randomized, double-blind study in 404 patients acutely ill with schizophrenia demonstrated significant antipsychotic efficacy (versus placebo). A 24-week, randomized, double-blind, active-controlled study in 1,065 schizophrenia patients stabilized with oral olanzapine demonstrated the depot formulation could delay exacerbation of positive symptoms or hospitalization. Apart from local injection reactions and a postinjection delirium/sedation syndrome, no new adverse events additional to those seen with oral olanzapine have been notedto date. The pivotal clinical trials of olanzapine rapid-acting intramuscular injection are reviewed in addition to post-hoc analyses, controlled and naturalistic studies since its launch.
奥氮平是一种非典型抗精神病药物,于1996年首次作为口服制剂推出,用于治疗精神分裂症和双相情感障碍。最近的进展包括胃肠外给药制剂,以提高精神分裂症治疗的依从性,并治疗精神分裂症和双相躁狂症患者的激越症状。奥氮平帕莫酸盐长效注射剂(长效储库型)是一种新型的非典型抗精神病药物奥氮平制剂,已获许可用于精神分裂症的维持治疗。当以帕莫酸盐形式给药时,奥氮平的消除半衰期约为30天,允许每2周或4周给药一次。一项针对404名急性精神分裂症患者的为期8周的随机双盲研究表明,奥氮平具有显著的抗精神病疗效(与安慰剂相比)。一项针对1065名使用口服奥氮平病情稳定的精神分裂症患者的为期24周的随机双盲、活性药物对照研究表明,长效注射剂制剂可延迟阳性症状的加重或住院治疗。除局部注射反应和注射后谵妄/镇静综合征外,迄今为止,尚未发现除口服奥氮平所见不良事件之外的新的不良事件。除了自奥氮平快速起效肌内注射剂推出后的事后分析、对照研究和自然观察研究外,本文还对其关键临床试验进行了综述。