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Psychopharmacol Bull. 2020 Sep 14;50(4):60-82.
This is a comprehensive review of the literature regarding the use of asenapine for the treatment of schizophrenia (SZ) in adults. It covers an introduction, epidemiology, risk factors, pathophysiology, and current treatment modalities regarding SZ, provides a background on the mechanism of action of asenapine, and then reviews the existing evidence for use of asenapine in both its sublingual and transdermal formulation in the treatment of SZ.
SZ is a complex and multifactorial mental disorder which is thought to combine several genetic, epigenetic, and environmental factors causing abnormalities in the dopaminergic system. Symptoms are categorized in delusions, hallucinations, disorganization, and negative presentations like affective flattening and apathy. Current treatment focuses on antipsychotic medications by means of oral administration or long-acting injection. Asenapine is a second-generation antipsychotic with 5HT-2A antagonist and 5HT-1A/1B partial agonist properties, which provides a favorable profile in targeting schizophrenic symptoms, while reducing motor side effects and improving mood and cognition. Asenapine in its sublingual formulation was FDA approved for treatment of SZ and bipolar I disorder in adults in August of 2009 and has been proven to be both effective and safe. Transdermal patch of asenapine (Secuado) was FDA approved in October of 2019, the first and only FDA approved patch for SZ in adults, which offers another strategy for treatment to improve compliance and ease of administration.
SZ is a chronic and debilitating disease which is still not well understood and comes at great cost with regards to the quality of life for patients. Medication side-effects and compliance are enormous issues which take a toll on health care systems in industrialized nations and keep patients from achieving stability with their disease. Transdermal asenapine is a new first-in-class dosage form and provides a novel modality of administration. It has been shown to be effective in reducing positive, as well as negative symptoms, while still maintaining a favorable side-effect profile.
本文是一篇关于阿塞那平治疗成人精神分裂症（SZ）的文献综述，涵盖了 SZ 的引言、流行病学、风险因素、病理生理学和当前治疗方法，介绍了阿塞那平的作用机制背景，然后回顾了其舌下和透皮制剂在治疗 SZ 中的现有证据。
SZ 是一种复杂的多因素精神障碍，据认为它结合了几种遗传、表观遗传和环境因素，导致多巴胺能系统异常。症状可分为妄想、幻觉、思维紊乱和情感迟钝、淡漠等阴性表现。目前的治疗重点是通过口服或长效注射给予抗精神病药物。阿塞那平是一种具有 5HT-2A 拮抗剂和 5HT-1A/1B 部分激动剂特性的第二代抗精神病药物，它提供了一种针对精神分裂症症状的有利特征，同时减少运动副作用，改善情绪和认知。阿塞那平舌下制剂于 2009 年 8 月获得 FDA 批准用于治疗成人 SZ 和双相 I 障碍，已被证明既有效又安全。阿塞那平透皮贴片（Secuado）于 2019 年 10 月获得 FDA 批准，是 FDA 批准用于成人 SZ 的首个也是唯一一个贴片，为改善依从性和简化给药提供了另一种治疗策略。
SZ 是一种慢性和使人衰弱的疾病，目前还没有很好的理解，并且给患者的生活质量带来了巨大的代价。药物副作用和依从性是一个巨大的问题，这给工业化国家的医疗保健系统带来了沉重的负担，使患者无法稳定控制疾病。透皮阿塞那平是一种新的首创剂型，提供了一种新的给药方式。它已被证明能有效减轻阳性和阴性症状，同时仍保持有利的副作用特征。
