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Ziprasidone: efficacy, tolerability, and emerging data on wide-ranging effectiveness.

机译：齐普拉西酮：疗效，耐受性和广泛有效性的新兴数据。

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摘要

Ziprasidone is the fifth atypical antipsychotic to become available in the US market. This compound is a serotonin-dopamine-receptor antagonist, with greater affinity for the 5-HT(2A) receptor than the dopamine D2 receptor. Similar to aripiprazole, this compound also has agonist activity at the serotonin 5-HT(1A) receptor. This affinity has the potential to have particularly beneficial effects on cognitive and affective abnormalities in schizophrenia. Oral and short-acting intramuscular formulations are available. This compound has recently been approved for the treatment of acute mania as well as for schizophrenia. Ziprasidone is associated with low weight gain and a low potential to change lipid and glucose levels. Long-term tolerability data have indicated that initial concerns regarding QTc (corrected cardiac output) prolongation are not a major issue. Recent data have indicated that this compound has short-term antipsychotic efficacy that is equivalent to other members of the class, also with evidence of cognitive enhancement. Finally, longer term data has indicated that ziprasidone is successful in the prevention of relapse and has sustained cognitive benefits. Several issues remain to be addressed, including the efficacy of once-daily dosing, the need to take the medication with food, and the correct dosing strategy.
机译：齐普拉西酮是在美国市场上上市的第五种非典型抗精神病药。该化合物是5-羟色胺-多巴胺受体拮抗剂，对5-HT（2A）受体的亲和力高于多巴胺D2受体。与阿立哌唑相似，该化合物对5-羟色胺5-HT（1A）受体也具有激动剂活性。这种亲和力可能对精神分裂症的认知和情感异常产生特别有益的影响。有口服和短效肌内制剂。该化合物最近已被批准用于治疗急性躁狂症和精神分裂症。 Ziprasidone与体重增加低和改变脂质和葡萄糖水平的可能性低有关。长期耐受性数据已表明，有关QTc（校正的心输出量）延长的最初担忧不是主要问题。最近的数据表明，该化合物具有与该类其他成员同等的短期抗精神病功效，并且具有认知增强的证据。最后，长期数据表明，齐拉西酮可成功预防复发并具有持续的认知益处。有几个问题有待解决，包括每天一次给药的有效性，与食物一起服用药物的需要以及正确的给药策略。

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