Quetiapine in the treatment of schizophrenia and related disorders.
Quetiapine in the treatment of schizophrenia and related disorders.
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DOI：
10.2147/nedt.2007.3.2.219
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发表时间：
2007-04
影响因子：
3.2
通讯作者：
Möller HJ
中科院分区：
文献类型：
--
作者：
Riedel M;Müller N;Strassnig M;Spellmann I;Severus E;Möller HJ
奎硫平是1985年由阿斯利康制药公司的科学家开发的。它于1997年9月获得美国食品和药物管理局的正式批准，并于2000年在德国获得批准。从那时起，喹硫平在大约70个国家被用于治疗严重的精神疾病，包括加拿大、大多数西欧国家和日本。喹硫平是二苯并噻唑类衍生物，具有相对广泛的受体结合谱。对脑5 -羟色胺受体（5HT2A）、组胺受体（H1）、多巴胺能受体D1、D2受体有较强的亲和性，对α1-和α2-肾上腺素能受体有中等的亲和性，对肌肉素能M1受体有较弱的亲和性；它证明了边缘系统有很大的选择性。与D2受体相比，这种对5HT2A受体具有较高亲和力的受体占用谱是喹硫平抗精神病特性和低锥体外系副作用发生率的部分原因。喹硫平在减轻精神分裂症阳性和阴性症状方面的疗效已在若干安慰剂对照对照的临床试验中得到证实。奎硫平在治疗精神分裂症的认知、焦虑抑郁和侵袭性症状方面也显示出强大的疗效。长期试验显示对广泛的症状具有持续的耐受性。奎硫平在治疗中度至重度躁狂发作、治疗对立违抗性或行为障碍的青少年以及老年痴呆人群中也已被证明具有疗效和耐受性。最近的数据表明，喹硫平也可能有效治疗双相抑郁症状，而不会增加引发躁狂发作的风险，以及边缘型人格障碍。与其他抗精神病药物相比，喹硫平具有良好的副作用。在临床试验中，仅观察到QT间期轻微而不显著的延长。在新的抗精神病药物中，体重增加和新发作的代谢副作用占据了中间地带。由于其良好的疗效和耐受性，喹硫平已在精神分裂症和躁狂发作的治疗中得到了很好的确立。
Quetiapine was developed in 1985 by scientists at AstraZeneca (formerly Zeneca) Pharmaceuticals. It received official US Food and Drug Administration approval in September 1997 and approval in Germany in 2000. Since then, quetiapine has been used in the treatment of severe mental illness in approximately 70 countries including Canada, most Western European countries, and Japan. Quetiapine is a dibenzothiazepine derivative with a relatively broad receptor binding profile. It has major affinity to cerebral serotonergic (5HT2A), histaminergic (H1), and dopaminergic D1 and D2 receptors, moderate affinity to α1- und α2-adrenergic receptors, and minor affinity to muscarinergic M1 receptors; it demonstrates a substantial selectivity for the limbic system. This receptor occupancy profile with relatively higher affinity for the 5HT2A receptor compared with the D2 receptor is in part responsible for the antipsychotic characteristics and low incidence of extrapyramidal side-effects of quetiapine. The efficacy of quetiapine in reducing positive and negative symptoms of schizophrenia has been proven in several clinical trials with placebo-controlled comparators. Quetiapine has also demonstrated robust efficacy for treatment of cognitive, anxious-depressive, and aggressive symptoms in schizophrenia. Long-term trials show sustained tolerability for a broad spectrum of symptoms. Quetiapine has also proven efficacy and tolerability in the treatment of moderate to severe manic episodes, and in the treatment of juveniles with oppositional-defiant or conduct disorders, and in the geriatric dementia population. Recent data indicate that quetiapine may also be effective in the treatment of bipolar depressive symptoms without increasing the risk of triggering manic episodes, and in borderline personality disorder. In comparison with other antipsychotics, quetiapine has a favorable side-effect profile. In clinical trials only small insignificant prolongations of the QT interval were observed. Weight-gain liabilities and new-onset metabolic side-effects occupy a middle-ground among newer antipsychotics. As a result of its good efficacy and tolerability profile quetiapine has become well established in the treatment of schizophrenia and manic episodes.