Musselman Meghan, Faden Justin, Citrome Leslie
Lewis Katz School of Medicine, Temple University, 100 E. Lehigh Avenue, Suite 305B, Philadelphia, PA 19125, USA.
Lewis Katz School of Medicine, Temple University, Philadelphia, PA, USA.
Ther Adv Psychopharmacol. 2021 Sep 11;11:20451253211035269. doi: 10.1177/20451253211035269. eCollection 2021.
Asenapine is a second-generation (atypical) antipsychotic medication not available in a pill that can be swallowed; rather, it is commercialized in sublingual and transdermal formulations. This is a consequence of extensive first-pass metabolism if ingested. The sublingual formulation is approved in many jurisdictions for the treatment of schizophrenia and manic or mixed episodes associated with bipolar I disorder and is available generically. The efficacy profile is well characterized in a number of clinical trials, including an off-label use for the management of agitation. Obstacles to its use include food and drink restrictions, twice-daily dosing and adverse effects such as dysgeusia (distorted, altered, or unpleasant taste) and oral hypoesthesia (numbness). Transdermal asenapine was approved by the US Food and Drug Administration in 2019 for the treatment of schizophrenia in adults. Efficacy was established in a registrational study examining acutely ill inpatients with schizophrenia. The patch needs to changed once daily. Obstacles to its use include the potential for skin reactions such as erythema and pruritis, and being a branded product, it is more costly than other options. This is a narrative review of the chemistry and pharmacokinetics/pharmacodynamics of asenapine, as well as summarizing the efficacy and tolerability of both sublingual and transdermal asenapine, and its possible place in treatment.
阿塞那平是一种第二代（非典型）抗精神病药物，没有可吞咽的片剂剂型；相反，它有舌下和透皮两种剂型上市。这是因为口服时会发生广泛的首过代谢。舌下剂型在许多司法管辖区被批准用于治疗精神分裂症以及与双相I型障碍相关的躁狂或混合发作，且有通用名药物。其疗效在多项临床试验中得到了充分表征，包括用于激越管理的非标签用途。其使用的障碍包括对食物和饮料的限制、每日两次给药以及诸如味觉障碍（味觉扭曲、改变或不适）和口腔感觉减退（麻木）等不良反应。透皮阿塞那平于2019年被美国食品药品监督管理局批准用于治疗成人精神分裂症。在一项针对急性精神分裂症住院患者的注册研究中确定了其疗效。该贴片需要每天更换一次。其使用的障碍包括可能出现皮肤反应，如红斑和瘙痒，而且作为品牌产品，它比其他选择更昂贵。本文是对阿塞那平的化学、药代动力学/药效学的叙述性综述，同时总结了舌下和透皮阿塞那平的疗效和耐受性，以及它在治疗中可能的地位。
