Potkin Steven G, Preda Adrian
a Psychiatry and Human Behavior, Robert R. Sprague Chair in Brain Imaging , UC Irvine , Irvine , CA 92617 , USA.
b Heath Sciences Clinical Professor of Psychiatry , UC Irvine School of Medicine , Orange , CA 92868 , USA.
Expert Opin Pharmacother. 2016;17(3):395-407. doi: 10.1517/14656566.2015.1114100.
Patient non-adherence increases the risk for relapse and the long-term care of schizophrenia. Long-acting injectable (LAI) antipsychotics can decrease this risk by ensuring adherence. An extended formulation, aripiprazole 400 mg once-monthly (AOM 400) LAI (AOM LAI), received regulatory approval in the year 2013 for the treatment of schizophrenia. AOM LAI is the first dopamine D2 partial agonist available in a long-acting formulation for the treatment of schizophrenia.
This review covers data on the efficacy and tolerability/safety of AOM LAI. AOM LAI is a lyophilized powder of aripiprazole, with an elimination half-life of 29.9 - 46.5 days, allowing for a 4-week injection interval. Antipsychotic efficacy was documented in a 12-week double-blind trial (n = 340) and in two maintenance-of-effect trials: a 38-week trial (n = 662) and a 52-week trial (n = 403). The side effect profile is similar to that of oral aripiprazole. Adverse events (≥5% and at least twice that for placebo) were typically mild or moderate and did not lead to discontinuation: increased weight, akathisia, injection site pain and sedation. The 400 mg dose is tolerated by >90% of patients. Injection does not require additional training of health personnel or post-injection observation.
AOM LAI is an efficacious and well-tolerated antipsychotic treatment for schizophrenia.
患者不依从性会增加精神分裂症复发风险和长期护理需求。长效注射用抗精神病药物可通过确保依从性来降低这种风险。一种延长剂型，阿立哌唑400mg每月一次长效注射剂（AOM 400）于2013年获得监管批准用于治疗精神分裂症。AOM LAI是首个以长效剂型用于治疗精神分裂症的多巴胺D2部分激动剂。
本综述涵盖了AOM LAI的疗效及耐受性/安全性数据。AOM LAI是阿立哌唑冻干粉末，消除半衰期为29.9 - 46.5天，允许4周的注射间隔。在一项为期12周的双盲试验（n = 340）以及两项疗效维持试验中记录了抗精神病疗效：一项为期38周的试验（n = 662）和一项为期52周的试验（n = 403）。副作用谱与口服阿立哌唑相似。不良事件（≥5%且至少是安慰剂组的两倍）通常为轻度或中度，不会导致停药：体重增加、静坐不能、注射部位疼痛和镇静。超过90%的患者可耐受400mg剂量。注射无需对医护人员进行额外培训或注射后观察。
AOM LAI是一种治疗精神分裂症有效且耐受性良好的抗精神病药物。
