Lewander T, Westerberg S E, Ogren S O, Von Bahr C, Köhler C
C.N.S. Research & Development, Astra Research Centre, Södertälje, Sweden.
Encephale. 1990 Mar-Apr;16(2):153-7.
Remoxipride, a substituted benzamide, is a new antipsychotic agent which differs from classical neuroleptics in several ways. It has a selective action on the dopamine D2 receptors in the brain and little effect on a variety of other receptor types including serotonin, noradrenaline, acetylcholine and histamine receptors. This implies advantages over classical neuroleptics which have less selective modes of action and subsequently increased propensities to cause side effects. The pharmacokinetics of remoxipride are uncomplicated. The drug is rapidly absorbed, plasma levels increase with dose, and elimination is via urinary excretion. No clinically significant drug interactions have been found. Remoxipride has been shown to be as effective in the treatment of schizophrenic patients as haloperidol in both short and long term double-blind trials. Both positive and negative symptoms are improved. However, remoxipride shows advantages over haloperidol in that the incidences of extrapyramidal symptoms and increased plasma prolactin concentrations are lower in remoxipride recipients. There are no clinically relevant adverse effects on chemistry, haematology or cardiovascular variables.
瑞莫必利是一种取代苯甲酰胺类新型抗精神病药物,在多个方面与传统抗精神病药物不同。它对大脑中的多巴胺D2受体具有选择性作用,而对包括5-羟色胺、去甲肾上腺素、乙酰胆碱和组胺受体在内的多种其他受体类型影响很小。这意味着它比传统抗精神病药物具有优势,因为传统药物的作用模式选择性较低,因而更容易产生副作用。瑞莫必利的药代动力学情况并不复杂。该药吸收迅速,血浆浓度随剂量增加而升高,通过尿液排泄消除。尚未发现具有临床意义的药物相互作用。在短期和长期双盲试验中,瑞莫必利已被证明在治疗精神分裂症患者方面与氟哌啶醇同样有效。阳性和阴性症状均得到改善。然而,瑞莫必利比氟哌啶醇更具优势,因为接受瑞莫必利治疗的患者锥体外系症状和血浆催乳素浓度升高的发生率较低。对化学、血液学或心血管指标无临床相关不良反应。