近日，美国默克安定药Sycrest已在欧洲获准上市，该药是规格为5mg/片的舌下片剂。Sycrest批准了用于治疗成人精神分裂症急性发作与1型双极症的急性狂躁发作或混合性发作。Sycrest可供精神分裂症治疗药物一线疗法使用，也是首个同时获得这两项适应症的精神药物。在美国该药商品名定为Saphris。
Sycrest在美国名为Saphris
Sycrest这种非典型性的安定药Sycrest（马来酸盐，Saphris；先灵葆雅，现在与默克合并）是一种双向复合胺，既是5-羟色胺2受体拮抗剂，也是多巴胺D1/D2受体拮抗剂，在美国获得两类相关适应症的批文。用于成人精神分裂症的急性治疗，以及狂躁或混合双向情感障碍的治疗。
其实早在今年6月份，Sycrest就得到了欧洲药监局人用医疗产品委员会的认可。因此Sycrest该次能顺利在欧洲上市是意料之事。
Sycrest获准在欧洲上市依据
参加Sycrest该次临床实验项目的双相情感障碍躁狂症患者多达1300名。有精神病学专家表示，Sycrest是治疗躁狂症的有效药物，它为这类患者提供了又一种可选的治疗方案，并且在副作用（如导致体重增加）方面小于其他几种同类药。
老年痴呆症患者使用Sycrest存在治疗风险，因此在使用前需咨询临床医生。同时Saphris再治疗精神分裂症的临床试验常见不良反应为燥动、口腔鼓味觉减退和嗜睡。在治疗双相性精神障碍的临床试验常见不良反应为燥动、体重增加、嗜睡、眩晕和运动失调。因此在使用Sycrest进行治疗时，需注意是否发生相关不良反应。
Sycrest: sublingual treatment for acute mania
Sycrest (asenapine) is a new atypical antipsychotic licensed for the treatment of acute manic or mixed episodes in bipolar disorder.
PHARMACOLOGY
Asenapine is an atypical antipsychotic that acts as an antagonist at dopaminergic, serotonergic and alpha-adrenergic receptors. Although the exact mechanism of action is not understood, its activity at D2 and 5-HT2A receptors is thought to be important in treating bipolar disorder. Actions at 5-HT1A, 5-HT1B, 5-HT2C, 5-HT6, 5-HT7, D3 and alpha2-adrenergic receptors may also contribute to the therapeutic effect. Unlike many other antipsychotics, asenapine has a low affinity for muscarinic receptors, which may be beneficial in patients where antimuscarinic effects are undesirable.1
The bioavailability of asenapine administered orally is low (2%), owing to extensive first-pass metabolism. When formulated as a sublingual tablet, asenapine is rapidly absorbed and achieves peak plasma concentrations within 90 minutes. To ensure optimal absorption, the manufacturer recommends avoiding eating or drinking for 10 minutes after the tablet has completely dissolved.1
CLINICAL STUDIES
The short-term efficacy of asenapine in the treatment of acute manic or mixed episodes in bipolar I disorder was evaluated in two 3-week randomised, double-blind phase 3 trials of similar design, which included placebo and olanzapine as controls. Patients with rapid cycling were excluded from both studies.1–3
Following a placebo run-in period, participants were randomised to receive flexible-dose sublingual asenapine (10mg twice daily on day 1, then 5mg or 10mg twice daily), oral olanzapine (15mg once daily on day 1, then 5–20mg once daily) or placebo. Young Mania Rating Scale (YMRS) was assessed at baseline and at day 21 as the primary efficacy measure.2,3
In the first study (n=488), patients receiving asenapine showed a significantly greater reduction in YMRS score as early as day 2 compared with patients on placebo (-3.0 vs -1.5; p<0.01), and this difference was maintained at day 21 (-10.8 vs -5.5; p≤0.0001).2 Similar results were observed in the second study (n=489), with a significantly greater reduction in YMRS score for asenapine than placebo after 2 days (-3.2 vs -1.7; p=0.022) and at 21 days (-11.5 vs -7.8; p<0.007).3
Olanzapine was also significantly more effective than placebo at days 2 and 21 in both studies. The studies were not designed to directly compare asenapine and olanzapine.2,3
Patients who completed either short-term study were eligible to join a double-blind 9-week extension study investigating the longer term safety and efficacy of asenapine. A total of 504 patients were enrolled and continued their assigned treatment with asenapine or olanzapine; those originally assigned to receive placebo were switched to asenapine. The treatment effect was maintained, with asenapine displaying non-inferiority to olanzapine in terms of reduction in YMRS score after 12 weeks (-24.4 vs -23.9).4
Asenapine was generally well tolerated in the trials, with the most common adverse events being somnolence, dizziness and sedation. Extrapyramidal symptoms were observed more frequently in patients receiving asenapine than in those receiving olanzapine.
剂型与包装规格：
20片x5mg
60片x5mg
20片x10mg
60片x10mg