Quiroz Jorge A, Rusch Sarah, Thyssen An, Palumbo Joseph M, Kushner Stuart
Central Nervous System, Pain and Translational Medicine Therapeutic Area at Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Raritan, New Jersey, USA.
Innov Clin Neurosci. 2011 Jun;8(6):20-8.
Risperidone long-acting injectable was previously approved for treatment of schizophrenia as biweekly injections in the gluteal muscle only. We present data on local injection-site tolerability and safety of risperidone long-acting injectable and comparability of systemic exposure of deltoid versus gluteal injections.
Risperidone long-acting injectable was administered in an open-label, single-dose, two-way crossover study, with patients randomized to receive either 25mg gluteal/37.5mg deltoid crossover in two treatment periods or 50mg gluteal/50mg deltoid injections crossover; each treatment period was separated by an 85-day observation period (Study 1) and an open-label, multiple-dose study (4 sequential 37.5mg or 50mg deltoid injections every 2 weeks) (Study 2). The pharmacokinetic results from both the studies have already been published.
In Study 1 (n=170), the majority of patients had no local injection-site findings, based on investigator and patient-rated evaluations. In Study 2 (n=53), seven of the 51 patients who received at least two deltoid injections discontinued (primary endpoint). However, none of the discontinuations were due to injection-site related reasons. The 90-percent upper confidence limit of the true proportion of injection-site issue withdrawals was 5.7 percent. No moderate or severe injection-site reactions were reported.
Intramuscular injections via the deltoid and gluteal sites are equivalent routes of administration of risperidone long-acting injectable with respect to local injection-site tolerability. The overall safety and tolerability profile of risperidone long-acting injectable was comparable when administered as an intramuscular injection in the deltoid (37.5mg and 50mg) and gluteal (25mg and 50mg) sites.
利培酮长效注射剂先前仅被批准用于治疗精神分裂症，每两周在臀肌处注射一次。我们提供了利培酮长效注射剂局部注射部位耐受性和安全性的数据，以及三角肌注射与臀肌注射全身暴露的可比性数据。
利培酮长效注射剂在一项开放标签、单剂量、双向交叉研究中给药，患者被随机分配在两个治疗期接受25mg臀肌注射/37.5mg三角肌注射交叉或50mg臀肌注射/50mg三角肌注射交叉；每个治疗期之间有85天的观察期（研究1）和一项开放标签、多剂量研究（每2周连续进行4次37.5mg或50mg三角肌注射）（研究2）。两项研究的药代动力学结果已经发表。
在研究1（n = 170）中，根据研究者和患者评估，大多数患者没有局部注射部位异常。在研究2（n = 53）中，51名接受至少两次三角肌注射的患者中有7人停药（主要终点）。然而，没有一次停药是由于注射部位相关原因。注射部位问题停药真实比例的90%置信上限为5.7%。未报告中度或重度注射部位反应。
就局部注射部位耐受性而言，通过三角肌和臀肌部位进行肌肉注射是利培酮长效注射剂等效的给药途径。当在三角肌（37.5mg和50mg）和臀肌（25mg和50mg）部位进行肌肉注射时，利培酮长效注射剂的总体安全性和耐受性相当。
