Department of Psychiatry, University of Alberta, Edmonton, AL, Canada.
Expert Rev Neurother. 2012 Dec;12(12):1383-97. doi: 10.1586/ern.12.137.
Risperidone long-acting injection (RLAI) was the first second-generation antipsychotic available as a long-acting injection. Paliperidone (9-hydroxyrisperidone) is the active metabolite of risperidone, introduced initially as an extended release oral (ORal Osmotic System, OROS®, Alza Corporation) formulation (Invega®, Janssen). Paliperidone long-acting injection (PLAI) has now been developed as a suspension of paliperidone palmitate nanocrystals in an aqueous formulation (Invega Sustenna®, Xeplion®), administered monthly by intramuscular injection (deltoid or gluteal). Doses of PLAI can be expressed either in milligram equivalents (mg eq) of paliperidone palmitate or in milligrams of the active fraction of paliperidone. The recommended initiation regimen of 150 mg eq (234 mg) on day 1 and 100 mg eq (156 mg) on day 8 (both administered in the deltoid) achieves therapeutic blood levels rapidly and without the necessity of oral supplementation. No refrigeration or reconstitution prior to administration is required. PLAI has been shown in to be effective in controlling the acute symptoms of schizophrenia as well as delaying time to relapse. Safety and tolerability are comparable to RLAI with no new safety signals. Thus, PLAI may represent the rational development of RLAI with greater ease of use.
利培酮长效注射剂（RLAI）是第一个可用作长效注射剂的第二代抗精神病药物。帕利哌酮（9-羟基利培酮）是利培酮的活性代谢物，最初作为一种延长释放口服（ORal Osmotic System，OROS®，Alza 公司）制剂（Invega®，Janssen）推出。帕利哌酮长效注射剂（PLAI）现已开发为棕榈酸帕利哌酮纳米晶体的混悬液，以水制剂形式给药（Invega Sustenna®，Xeplion®），每月通过肌肉注射（三角肌或臀肌）给药。PLAI 的剂量可以表示为棕榈酸帕利哌酮的毫克当量（mg eq）或帕利哌酮的活性部分的毫克数。推荐的起始方案为第 1 天 150 mg eq（234 mg）和第 8 天 100 mg eq（156 mg）（两者均在三角肌注射），可快速达到治疗血药水平，无需口服补充。给药前无需冷藏或复溶。PLAI 已被证明可有效控制精神分裂症的急性症状，并延迟复发时间。安全性和耐受性与 RLAI 相当，无新的安全性信号。因此，PLAI 可能代表 RLAI 的合理发展，使用更方便。
