美国食品药品监督管理局（FDA）批准先灵葆雅公司的Saphris（阿莫沙平）舌下片上市。阿莫沙平是一种非典型抗精神病药物，用于治疗成人精神分裂症、慢性重度脑功能障碍和I型双相性精神障碍。
FDA基于3项短期、安慰剂对照和阳性药物对照的临床试验证明Saphris治疗精神分裂症的有效性；基于2项短期、安慰剂和阳性药物对照的临床试验证明Saphris治疗双相性精神障碍的有效性。
作为精神疾病治疗药物，该药的说明书中有[黑框警示]信息，警示医生，
老年痴呆症患者用药存在治疗风险。Saphris的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。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。

制造商：
先灵，一div.of默克公司

药理分类：
非典型抗精神病药物（二苯oxepino吡咯）

活性成分（补）：
Asenapine 5毫克，10毫克;舌下（广义）的标签。
指示（补）：
对于急性治疗：1）精神分裂症，2）躁狂或混合型双极症相关的事件。

药理作用：
虽然对asenapine行动的精神病和双相情感障碍是不知道确切的治疗机制，它可能是由于在血清素多巴胺D2和5 - HT2A受体及相关受体结合位点的拮抗作用。

临床试验：
在治疗精神分裂症的疗效评价asenapine三安慰剂控制和主动控制的6个星期的研究，精神分裂症患者在成人中谁是有急性发作。其中两个研究表示为asenapine效果优于安慰剂。在这些试验之一，asenapine 5毫克，每天两次有统计学上优于阳性与阴性症状量表安慰剂。在第二次审判，两个固定的asenapine剂量（5毫克或10毫克，每天两次）进行比较安慰剂。 5毫克，每天两次的剂量被证明是对PANSS总分优于安慰剂，每天两次的10毫克剂量并没有显示出任何额外的好处，并没有显着优于安慰剂。

两个3周的安慰剂控制和主动控制进行了研究与双极余障碍伴急性躁狂或混合发作或无精神病患者。青年躁狂量表来评估躁狂症状，随着临床整体印象双极规模。 Asenapine最初是在10毫克剂量，每日两次，并可以减少到5毫克，每日两次，第2天开始。在这两个试验中，研究药物被证明是统计上都优于评定量表安慰剂。

法律分类：
接收

成人：
不要挤压，咀嚼，或吞咽，不要吃或喝给药后10分钟。允许对舌片完全溶解。精神分裂症：5毫克，每日两次。双相情感障碍：10毫克，每日两次，如果发生不利影响，可能会减少到5毫克，每日两次。定期重新评估。

儿童：
不推荐。

警告/注意事项：
避免在先天性长QT综合征，心律失常。严重肝功能不全：不推荐。如果停止抗精神病药物恶性症候群发生的;考虑停止，如果发生迟发性运动障碍。心或脑血管疾病。预现有的低白细胞或白血球低下/中性粒细胞的历史，在第一几个月的治疗监测CBCs;停止，如果白细胞下降。糖尿病的危险因素（获得基线空腹血糖）。高血糖监视器。癫痫发作史。暴露在高温下。吞咽困难。写实际金额最小的接收。老年人（老年痴呆症有关的精神病不）。妊娠（Cat.C）。哺乳母亲：不推荐。

互动（补）：
避免药物能延长QT间隔（例如，类1A或III类抗心律失常药，齐拉西酮，氯丙嗪，甲硫达嗪，莫西沙星，酒精）。 Potentiates抗高血压药。 Potentiated由氟伏沙明。注意与其他中枢神经系统药物，药物，是CYP2D6的底物/酶抑制剂，药物引起体位性低血压和抗胆碱活性的药物。

不良反应（补）：
静坐不能，口腔感觉减退，嗜睡，头晕，锥体外系反应，胃肠不适，体位性低血压，晕厥，QT间期延长，高血糖，体重增加，高泌乳素血症。

如何提供：
sl的标签- 60

U.S. Food and Drug Administration (FDA) approval of Schering-Plough's Saphris (A Mosha level) sublingual tablets market. A Mosha level is an atypical antipsychotic for the treatment of schizophrenia in adults with chronic severe brain dysfunction and type I bipolar disorder.
FDA based on three short-term, placebo-controlled, and positive control of clinical trials for the effectiveness of the treatment of schizophrenia Saphris; based on two short-term, placebo and positive controlled clinical trials of drug treatment of bipolar disorder Saphris effectiveness .
As treatment of mental illness, drug instructions are [boxed warning] information, warning doctors
Alzheimer's disease risk in patients with drug treatment exists. Saphris clinical trials in the treatment of schizophrenia common adverse events were restlessness, taste loss and lethargy oral drums. Treatment of bipolar disorder common adverse reactions in clinical trials for the agitation, weight gain, drowsiness, dizziness and ataxia.
Schering-Plough Co., Ltd. announced that the U.S. FDA approved SAPHRIS ® (ASENAPINE) for acute manic or mixed episodes of schizophrenia and bipolar disorder type Ⅰ and non-adult psychiatric treatment of adults with functional
First of all, psychotropic drugs, and get preliminary approval to two signs
SAPHRIS expected fourth quarter of 2009 in the United States.

Schizophrenia affects, including about 24 million Americans, the world 200, I and bipolar disorder affects about one percent of adults, including 10 million Americans.

"Schizophrenia and bipolar disorder is a complex medical conditions, I can make the challenge of the clinician, said:" Shidifenke Potkin, MD, professor, psychiatry and human behavior, University of California Irvine, University and schizophrenia University and lead author of an important department of journalism as a SAPHRIS clinical development plan.

"With a new FDA approved treatment, such as SAPHRIS serious in these important diseases, because doctors need to choose to help them manage the patient's symptoms," McIntyre said: Roger schools, doctors, psychiatry and pharmacology Science, Canada Associate Professor, University of Toronto led the clinical study of bipolar disorder as SAPHRIS part of the key development projects.

In SAPHRIS FDA approval is based on the new drug application (NDA), involving more than 3,000 procedures from schizophrenia and bipolar disorder the validity of test data, including the patient's clinical studies. SAPHRIS 4500 applications support the human security of data, some patients more than two years. The approval is based on acute schizophrenia trials SAPHRIS (5 mg twice daily) and placebo were anxious of the bipolar disorder of type I, which SAPHRIS (10 mg, twice daily) significantly reduced the double affective disorder compared with placebo patients showed symptoms.

About SAPHRIS (asenapine)
SAPHRIS is an acute treatment of schizophrenia and manic bipolar adults or mental disease or acute psychotic episode and I mixed signs, the characteristics of adult patients. Schering-Plough reported that in the long-term clinical studies SAPHRIS additional top-line results. And SAPHRIS undergoing further clinical study.

In Europe, the marketing authorization application (MAA) for the asenapine ® brand under the SYCREST currently the European Medicines Agency (EMEA), based on my mania, schizophrenia and bipolar treatment-related review. The application will focus on procedures. 

Important SAPHRIS on Information Security

Increase in dementia-related psychosis mortality rate:
Elderly with dementia-related psychosis in patients with antipsychotic treatment is an increased risk of death. 17 placebo-controlled trials (modal time of 10 weeks) analysis, mainly in patients treated with atypical antipsychotics, reveals a 1.6 to 1.7 times the drug-treated patients in the placebo-treated patients the risk of death. In a typical ten weeks during the controlled trials, the mortality rate of patients in drug treatment is about 4.5 percent than the 2.6 percent rate of the placebo group. Although the causes of death are many, most of the deaths seemed to be no cardiovascular disease (such as heart failure, sudden death) or infections (eg pneumonia). SAPHRIS does not approve of dementia-related psychosis treatment.

Cerebrovascular adverse events:

cerebral blood vessels (cerebral vascular accident and transient ischemic attack) of adverse events compared with placebo subjects, including a higher incidence of death. SAPHRIS does not approve of dementia-related psychosis treatment.

Neuroleptic Malignant Syndrome (NMS):

The network management system is a potentially fatal symptom complex, has been reported with antipsychotic drugs, including SAPHRIS management. NMS can cause high fever, muscle rigidity, altered mental status, irregular pulse and blood pressure, tachycardia, diaphoresis and cardiac dysrhythmia. Additional signs may include elevated creatine phosphokinase, myoglobinuria (rhabdomyolysis) and acute renal failure. Management should include treatment of antipsychotics and other drugs at the same time is not important, intensive symptomatic treatment and medical monitoring, the waiter immediately stop any serious treatment of medical problems.

Tardive dyskinesia (TD):

The risk of developing TD and the potential may increase and become irreversible and the total cumulative dose of treatment duration increased. However, this syndrome can develop, but more commonly, in the low-dose treatment period was relatively short. Prescription should be with the Transport Department to reduce the risk of the same needs. If signs and symptoms should be considered stopped.

High blood sugar and diabetes:

high blood sugar and ketoacidosis, hyperosmolar coma or death related cases have been reported in patients with atypical antipsychotics. Atypical antipsychotics in patients with diabetes who began treatment should start fasting blood glucose testing and risk factors. Atypical antipsychotics, should include monitoring any polydipsia, polyuria, polyphagia, weakness, blood sugar symptoms. Patients who develop symptoms of atypical antipsychotics with high blood sugar, fasting blood glucose should be tested. In some cases, hyperglycemia has resolved when the atypical antipsychotics, and stopped, but some patients need anti-diabetic drug treatment despite continued antipsychotic withdrawal.

Weight gain:

in the short-term schizophrenia and bipolar disorder trials, there SAPHRIS between treatment and placebo patients, the average weight gain differential treatment. In a 52-week study, patients greater than or equal to 7 percent increase in body weight compared to 14.7.

Orthostatic hypotension, syncope hemodynamics:

 SAPHRIS can cause orthostatic hypotension and syncope. SAPHRIS should be used in patients with known cardiovascular disease, cerebrovascular disease, and create an environment in which their blood pressure and the elderly caution. SAPHRIS should be used in patients who received treatment with other drugs, can induce hypotension, caution, bradycardia, respiratory or central nervous system depression. Monitoring of orthostatic vital signs should be considered in all such patients, dose reduction should be considered low blood pressure.

Leukopenia, neutropenia, and agranulocytosis:

clinical trials and postmarketing experience, leukopenia / neutropenia have been reported are of antipsychotics, including SAPHRIS events. Pre-existing low white blood cell count (WBC) or leukopenia / neutropenia should have a complete blood count (CBC) in the monitoring and treatment history should be stopped during the first few months of their regular SAPHRIS the first signs of the patients white blood cells decline, other risk factors of cases.

QT interval prolongation:

SAPHRIS 2 to 5 ms in the QTc interval compared to placebo increased. No patient's treatment and SAPHRIS 60 ms or greater increase in QT from the baseline measurement, no experience equal to or greater than 500 ms in the QT interval is one. SAPHRIS combination with other drugs should be avoided in patients with a history, with known QTc interval prolongation and congenital QT prolongation or arrhythmia in contact and in some cases, may increase the incidence of torsades de pointes and / or Association between drug use and sudden death QTc prolongation.

Hyperprolactinemia:

Like other drugs antagonize dopamine D2 receptors, SAPHRIS can increase prolactin levels, and can persist in a long-term management of the height. Galactorrhea, amenorrhea, breast, and impotence compounds reported an increase in patients receiving prolactin.

Attack:

SAPHRIS should be used with caution in patients with a history of seizures or epilepsy, a lower threshold conditions, such as Alzheimer's disease dementia.

Dysphagia:

Esophageal motility disorders and the desire to have the use of antipsychotic drugs. Aspiration pneumonia is a kind of morbidity and common cause in elderly patients, especially with advanced Alzheimer's disease-like dementia mortality. SAPHRIS no indication of dementia-related psychosis treated, or not at risk of aspiration pneumonia.

Cognitive and motor dysfunction of the potential:

It is reported that patients treated with SAPHRIS sleepiness. Patients should pay attention to the relevant provisions of the mental alertness performance, such as operating dangerous machinery or driving motor vehicles until they have reason to believe SAPHRIS treatment did not affect them adversely.

Suicide:

suicide attempts and the possibility of mental illness is inherent in bipolar disorder. Close supervision of high risk patients, drug therapy. Prescriptions should be written to SAPHRIS minimum number of tablets to reduce the risk of overdose.

SAPHRIS not recommended in the treatment of severe liver injury.

Cooperation and strong CYP1A2 inhibitors (fluvoxamine) or CYP2D6 substrate and (paroxetine) inhibitor compounds SAPHRIS government should be cautious.

Common adverse reactions (incidence equal to or greater than 5 percentage points, at least twice placebo) were: akathisia, oral sensation, lethargy: schizophrenia patients. Bipolar disorders: drowsiness, dizziness, akathisia, extrapyramidal symptoms increase in weight than the other.

About Schizophrenia
Schizophrenia is a chronic, often disabling brain disease, symptoms, such as the so-called positive symptoms (including hallucinations, delusions and thought disorder), characteristics and negative symptoms, cognitive impairment and other areas of general psychopathology symptoms, such as caused by a variety of anxiety (or depression). Heterogeneity of clinical disease, about 1 about 24 million people around the world, including more than two million people in the United States, more than four million people in Europe, the percentage of lifetime prevalence.

Bipolar disorder type I
Type I bipolar disorder (also known as manic depression) is a chronic disease, manic features (elevated mood, extreme irritability, spasticity, decreased sleep, increased energy), depression (overwhelming feelings of sadness , suicidal thoughts), or a combination of both. It is the sixth leading cause of disability in the world, affecting about one per cent of adults, including 10 million Americans.

SAPHRIS

【生产厂家中文参考译名】美国先灵葆雅公司
【生产厂家英文名】先灵葆雅公司。美国股份有限公司
【原产地英文商品名】SAPHRIS 5毫克舌下含服60粒统计表
【原产地英文药品名】马来酸ASENAPINE
【中文参考商品译名】SAPHRIS 5毫克/片60片/盒舌下片
【中文参考药品译名】阿莫沙平舌下片
【原产地国家批准上市年份】2009/08/13
【临床试验期】完成