Carrithers Brennan, El-Mallakh Rif S
Department of Psychiatry and Behavioral Sciences, University of Louisville School of Medicine, Louisville, Kentucky 40202, USA.
Patient Prefer Adherence. 2020 Aug 25;14:1541-1551. doi: 10.2147/PPA.S235104. eCollection 2020.
Asenapine is a novel antipsychotic that has demonstrated efficacy in controlling psychosis in schizophrenia and mania in bipolar illness. It must be administered as a sublingual formulation because it is nearly completely metabolized in the first pass through the liver. Recently, a transdermal formulation of asenapine has been approved for schizophrenia by the Food and Drug Administration.
A systematic review of transdermal asenapine was done utilizing the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) model.
There are several formulations of transdermal asenapine but only Secuado has been approved for clinical use. Total bioavailability is 35%. Peak plasma concentration (Cmax) is 4 ng/mL and occurs within 1 hr (Tmax); elimination half-life (t) is 24 hrs (range 13.4 to 39.2 h). Asenapine is highly bound (95%) to albumin and α-acid glycoprotein. It has a unique receptor profile in which it functions as an antagonist at multiple receptors with affinity that is higher than D (K = 1.3) including D, D, 5HT, 5HT, 5HT, 5HT, 5HT, H, and α2. This profile suggests that asenapine may be of particular value off label for bipolar depression, anxiety, and aggression. Transdermal asenapine was only tested in one randomized, placebo-controlled study of acute psychosis in schizophrenia. It was superior to placebo at week 6 with nearly one-third of patients experiencing >30% improvement in total PANSS score which translates in a number needed to treat (NNT) of 9.
阿塞那平是一种新型抗精神病药物，已证明其在控制精神分裂症的精神病症状和双相情感障碍的躁狂症状方面有效。由于它在首次通过肝脏时几乎完全代谢，因此必须以舌下制剂的形式给药。最近，阿塞那平的透皮制剂已获美国食品药品监督管理局批准用于治疗精神分裂症。
利用系统评价与Meta分析的首选报告项目（PRISMA）模型对阿塞那平透皮制剂进行了系统评价。
阿塞那平有几种透皮制剂，但只有Secuado已获批准用于临床。总生物利用度为35%。血浆峰浓度（Cmax）为4 ng/mL，在1小时内达到（达峰时间[Tmax]）；消除半衰期（t）为24小时（范围为13.4至39.2小时）。阿塞那平与白蛋白和α-酸性糖蛋白高度结合（95%）。它具有独特的受体谱，在多个受体上起拮抗剂作用，其亲和力高于D2（解离常数[Kd]=1.3），包括D1、D3、5HT1A、5HT2A、5HT2B、5HT2C、5HT7、H1和α2。这一受体谱表明，阿塞那平在双相抑郁、焦虑和攻击行为的标签外使用可能具有特殊价值。阿塞那平透皮制剂仅在一项精神分裂症急性精神病的随机、安慰剂对照研究中进行了测试。在第6周时，它优于安慰剂，近三分之一的患者阳性和阴性症状量表（PANSS）总分改善>30%，治疗所需人数（NNT）为9。
