Taylor David
Pharmacy Department, Maudsley Hospital, Denmark Hill, London SE5 8AZ, UK.
Br J Psychiatry Suppl. 2009 Nov;52:S13-9. doi: 10.1192/bjp.195.52.s13.
Depot antipsychotics are widely used in clinical practice. Long-acting formulations of second-generation antipsychotics are now being developed and introduced.
To review the pharmacology, pharmacokinetics and adverse effect profiles of currently available antipsychotic long-acting injections (LAIs).
The psychopharmacological properties of first- and second-generation antipsychotic LAIs are reviewed using data available up to October 2008.
First-generation antipsychotic (FGA) LAIs are associated with a high rate of acute and chronic movement disorders. Risperidone LAI is better tolerated in this respect, but is associated with hyperprolactinaemia and weight gain. Olanzapine LAI causes weight gain and other metabolic effects but appears not to be associated with an important incidence of movement disorders.
Dosing of LAIs is complicated by delayed release of drug, changes in plasma levels without change in dose, and by the lack of data establishing clear dose requirements. All LAIs offer the prospect of assured adherence (although patients may still default on treatment) but their use is complicated by adverse effects, complex pharmacokinetics and confusion over dose-response relationships.
长效抗精神病药物在临床实践中广泛应用。目前正在研发和引入第二代抗精神病药物的长效制剂。
综述目前可用的抗精神病长效注射剂（LAIs）的药理学、药代动力学和不良反应情况。
利用截至2008年10月的现有数据，对第一代和第二代抗精神病LAIs的精神药理学特性进行综述。
第一代抗精神病（FGA）LAIs与急性和慢性运动障碍的高发生率相关。在这方面，利培酮长效注射剂耐受性较好，但与高催乳素血症和体重增加有关。奥氮平长效注射剂会导致体重增加和其他代谢影响，但似乎与运动障碍的重要发生率无关。
LAIs的给药因药物的延迟释放、剂量不变时血浆水平的变化以及缺乏确定明确剂量要求的数据而变得复杂。所有LAIs都提供了确保依从性的前景（尽管患者仍可能不遵守治疗），但其使用因不良反应、复杂的药代动力学和剂量反应关系的混乱而变得复杂。
