Owens D G
Department of Psychiatry, University of Edinburgh, U.K.
J Clin Psychiatry. 1994 May;55 Suppl:29-35.
The effectiveness of conventional neuroleptics in schizophrenia is often limited by extrapyramidal side effects (EPS), which are known to contribute to poor compliance and relapse. However, there is now evidence that drugs that block 5-HT2 receptors as well as D2 receptors have better EPS profiles. Risperidone has these pharmacologic properties. In two large clinical trials, risperidone (2, 6, 10, 16 mg/day or 4, 8, 12, 16 mg/day) was compared with either placebo and haloperidol (20 mg/day) or risperidone (1 mg/day) and haloperidol (10 mg/day). Extrapyramidal side effects were assessed using the Extrapyramidal Symptom Rating Scale and by recording the use of anticholinergic medication. Other adverse effects were assessed using the UKU Side Effects Scale. In both studies, the severity of EPS in the risperidone groups was significantly less than in the haloperidol group. In the placebo-controlled study, doses of 2 and 6 mg/day of risperidone produced no worse EPS than placebo. Other side effects were minor, and included brief hypotension (mediated via alpha-blockade) and weight gain. Overall, risperidone at antipsychotic doses was better tolerated than haloperidol.
传统抗精神病药物治疗精神分裂症的疗效常受锥体外系副作用（EPS）的限制，已知这些副作用会导致依从性差和病情复发。然而，现在有证据表明，同时阻断5-HT2受体和D2受体的药物具有更好的EPS表现。利培酮具有这些药理特性。在两项大型临床试验中，将利培酮（2、6、10、16mg/天或4、8、12、16mg/天）与安慰剂和氟哌啶醇（20mg/天）或利培酮（1mg/天）和氟哌啶醇（10mg/天）进行了比较。使用锥体外系症状评定量表并记录抗胆碱能药物的使用情况来评估锥体外系副作用。使用UKU副作用量表评估其他不良反应。在两项研究中，利培酮组的EPS严重程度均显著低于氟哌啶醇组。在安慰剂对照研究中，利培酮2mg/天和6mg/天剂量产生的EPS不比安慰剂更严重。其他副作用较小，包括短暂性低血压（通过α受体阻断介导）和体重增加。总体而言，抗精神病剂量的利培酮比氟哌啶醇耐受性更好。
