Marchese Giorgio, Casu Gianluca, Casti Paola, Spada Gabriele Pinna, Pani Luca
CNR, Institute of Biomedical Technology, Sect Cagliari, Technological Park of Sardinia Sardegna Ricerche, Pula, Cagliari, Italy.
Eur J Pharmacol. 2009 Oct 12;620(1-3):36-41. doi: 10.1016/j.ejphar.2009.07.024. Epub 2009 Aug 5.
It has been proposed that long-acting risperidone could provide a constant antipsychotic efficacy associated with a reduced liability to induce extra-pyramidal symptoms. To ascertain this hypothesis, antagonism of amphetamine-induced hyperlocomotion and catalepsy were analyzed in rats for a period of 1-6 weeks following long-acting risperidone (20-60 mg/kg) injection. Long-acting risperidone reduced amphetamine-induced hyperlocomotion after 2-5 weeks from drug injection, without producing significant extra-pyramidal symptoms. Following the administration of long-acting risperidone a constant ability to antagonize amphetamine-induced hyperlocomotion was observed during the day, but not when the antipsychotic was chronically administered using a short-acting formulation. The pre-clinical results confirmed that long-acting risperidone may represent an advance in antipsychotic therapy.
有人提出,长效利培酮可提供持续的抗精神病疗效,且诱发锥体外系症状的可能性降低。为了验证这一假设,在大鼠注射长效利培酮(20 - 60 mg/kg)后的1 - 6周内,分析了其对苯丙胺诱导的运动亢进和僵住症的拮抗作用。注射长效利培酮2 - 5周后,其可降低苯丙胺诱导的运动亢进,且未产生明显的锥体外系症状。给予长效利培酮后,白天观察到其对苯丙胺诱导的运动亢进具有持续的拮抗能力,但使用短效制剂长期给予抗精神病药物时则未观察到这种情况。临床前结果证实,长效利培酮可能代表了抗精神病治疗的一项进展。