Cohen L J
College of Pharmacy, University of Oklahoma, Oklahoma City 73190.
Pharmacotherapy. 1994 May-Jun;14(3):253-65.
Risperidone, a benzisoxazole derivative, is a novel antipsychotic agent that has an extremely strong binding affinity for serotonin 5-HT2 receptors, a strong binding affinity for dopamine D2 receptors, and a high affinity for alpha 1- and alpha 2-adrenergic receptors and histamine H1 receptors. Its affinity for serotonin receptors is approximately 200 times greater than that of haloperidol, and its dopamine antagonistic potency is comparable to that of haloperidol. Its major metabolite, 9-hydroxyrisperidone, has similar pharmacologic activity, and thus the parent compound and metabolite form the active antipsychotic moiety. Clinical trials demonstrate that risperidone is an effective antipsychotic agent that improves negative as well as positive symptoms of schizophrenia. At recommended dosages, the frequency of extrapyramidal side effects is no greater than that seen with placebo. The drug appears to be an advance in the treatment of psychoses.
利培酮是一种苯并异恶唑衍生物，是一种新型抗精神病药物，对5-羟色胺5-HT2受体具有极强的结合亲和力，对多巴胺D2受体具有较强的结合亲和力，对α1和α2肾上腺素能受体以及组胺H1受体具有高亲和力。它对5-羟色胺受体的亲和力比氟哌啶醇约大200倍，其多巴胺拮抗效力与氟哌啶醇相当。其主要代谢物9-羟利培酮具有相似的药理活性，因此母体化合物和代谢物形成了活性抗精神病部分。临床试验表明，利培酮是一种有效的抗精神病药物，可改善精神分裂症的阴性和阳性症状。在推荐剂量下，锥体外系副作用的发生率不高于安慰剂。该药物似乎是精神病治疗方面的一项进展。
