近日，FDA批准新型的舌下含片剂SAPHRIS(asenapine)上市,该药可作为紧急用药治疗精神分裂症、狂躁症或伴有/不伴有精神病特征的I型双向情感障碍。SAPHRIS可用作一线药物治疗那些之前从未使用过任何药物的上述患者。
批准日期：公司：ACTAVIS PHARMA INC
SAPHRIS（阿塞那平[asenapine]）舌下含片，供口服使用
美国最初批准：2009年
警告：老年患者的死亡率增加与痴呆相关的精神病
查看完整的盒装警告的完整处方信息。
患有痴呆相关精神病的老年患者用抗精神病药治疗的风险增加。 SAPHRIS未被批准用于治疗痴呆相关性精神病患者。
最近的重大变化
适应症和用法：01/2017
剂量和用药：2017年1月
禁忌症（4）01/2017
警告和注意事项：01/2017
警告和注意事项：02/2017
作用机制
阿塞那平在精神分裂症和I型双相情感障碍中的作用机制尚不清楚。已经表明，阿塞那平在精神分裂症中的功效可以通过D2和5-HT2A受体的拮抗剂活性的组合来介导。
适应症和用法
SAPHRIS是一种非典型抗精神病药，用于：
•成人精神分裂症
•双极I障碍
o急性单药治疗躁狂或混合发作，成人和10至17岁的儿科患者
o成人对锂或丙戊酸钠的辅助治疗
o成人维持单药治疗
剂量和给药
                     开始剂量             推荐剂量           最大值剂量
成人精神分裂   每天5毫克，每天两次    每天舌下含药5毫克   舌下含服10毫克，每日两次
症-急性治疗
精神分裂症-    每天5毫克，每天两次    5-10岁，每天两次   舌下含服10毫克，每日两次
成人维持治疗
双极躁狂症-成  每天5-10毫克，每天两次 5-10岁，每天两次   舌下含服10毫克，每日两次
人：急性和维
持性单一疗法
双相躁狂症儿    2.5毫克，每天两次     每天2.5-10毫克     舌下含服10毫克，每日两次
科患者（10至
17岁）：单药
治疗
双极性躁狂症-  每天5毫克，每天两次   5-10岁，每天两次    舌下含服10毫克，每日两次
成人：作为锂
或丙戊酸钠的抗体
•不要吞服平板电脑。 SAPHRIS舌下片应放在舌下并完全溶解。片剂将在几秒钟内溶解在唾液中。给药后应饮食和饮水10分钟。
剂量形式和强度
舌下片，黑樱桃味：2.5mg，5mg和10mg
禁忌症
•严重肝功能损害（Child-Pugh C）。
•已知对SAPHRIS（阿塞那平）或制剂中的任何组分过敏。
警告和注意事项
•老年痴呆相关精神病患者的脑血管不良反应：脑血管不良反应发生率增加（如中风，短暂性脑缺血发作）。
•神经感觉恶性综合症：通过立即停止和密切监测进行管理。
•迟发性运动障碍：如果临床适当，则停用。
•代谢变化：监测高血糖/糖尿病，血脂异常和体重增加。
•直立性低血压：监测心率和血压，并警告患有已知心血管或脑血管疾病的患者，以及脱水或晕厥的风险。
•白细胞减少症，中性粒细胞减少症和粒细胞缺乏症：对已有低白细胞计数（WBC）或白细胞减少或中性粒细胞减少症史的患者进行完全血液计数（CBC）。如果WBC的临床显着下降在没有其他致病因素的情况下发生，则考虑继续使用SAPHRIS。
•QT延长：QT间期增加;避免使用也会增加QT间期的药物以及患有QT间期延长的危险因素的患者。
•癫痫发作：对有癫痫病史或有降低癫痫发作阈值的病人慎用。
•认知和运动损伤的可能性：操作机器时要小心。
不良反应
最常见的不良反应（发生率为安慰剂的5％和至少两倍）为：
•精神分裂症成人：静坐不能，口腔感觉减退，嗜睡。
•双相I障碍成人（单药治疗）：嗜睡，口腔感觉异常，头晕，锥体外系症状（排除性症状）和静坐不能。
•双相I障碍儿科患者（单药治疗）：嗜睡，头晕，味觉障碍，口腔感觉异常，恶心，食欲增加，疲劳，体重增加。
•Bipolar I Disorder Adults（Adjunctive）：嗜睡，口腔感觉异常。
要报告疑似不良反应，请致电1-800-FDA-1088或www.fda.gov/medwatch联系Allerganat 1-800-433-8871或FDA。
药物相互作用
•抗高血压药物：SAPHRIS可能引起低血压。
•帕罗西汀（CYP2D6底物和抑制剂）：与SAPHRIS联合使用时，可逐半减少帕罗西汀。
用于特定人群
•怀孕：在妊娠晚期暴露的新生儿可能引起锥体外系和/或戒断症状。
•儿科用途：未评估10岁以下患者的双相Idisorder治疗的安全性和有效性，以及年龄小于12岁的精神分裂症患者的评估。
包装提供/存储和处理
SAPHRIS（阿塞那平）舌下片剂提供如下：
2.5mg片剂，黑樱桃味
圆形，白色至灰白色舌下片，一侧有六边形。
防儿童包装
盒装60个6个水泡，10片NDC 0456-2402-60
医院单位剂量
盒装100个10个水泡，10片NDC 0456-2402-63
5mg片剂，黑樱桃味
圆形，白色至灰白色舌下片，圆圈内一侧有“5”。
防儿童包装
盒装60个6水泡，10片NDC 0456-2405-60
医院单位剂量
盒装100个10个水泡，10片NDC 0456-2405-63
10毫克片，黑樱桃味
圆形，白色至灰白色的舌下片，圆圈内一侧有“10”。
防儿童包装
盒装60个6水泡，10片NDC 0456-2410-60
医院单位剂量
盒装100个10个水泡，10片NDC 0456-2410-63
存储
储存在20°C至25°C（68°F至77°F）;在15°C和30°C（59°F和86°F）之间允许的偏移[见USP受控室温]。
完整说明资料附件：
https://www.allergan.com/assets/pdf/saphris_pi
SAPHRIS(asenapine)sublingual tablets
IMPORTANT RISK INFORMATION
What is the most important information I should know about SAPHRIS?
Elderly people with dementia-related psychosis (having lost touch with reality due to confusion and memory loss) taking antipsychotic drugs are at an increased risk for death. SAPHRIS is not approved for treating people with dementia-related psychosis.
SAPHRIS may cause serious side effects, including:
Stroke (which can be fatal) in elderly people with dementia
Neuroleptic malignant syndrome (NMS): Call your healthcare provider right away if you have high fever; stiff muscles; confusion; changes in pulse, heart rate, or blood pressure; or sweating. These can be symptoms of a rare but potentially fatal side effect called NMS. SAPHRIS should be stopped if you have NMS
Tardive dyskinesia (TD): Tell your healthcare provider if you cannot control the movements of your face, tongue, or other body parts. These could be signs of a serious and sometimes permanent side effect called TD. Risk of developing TD and the chance that it will become permanent are thought to increase the longer a person takes the medicine and the more medicine a person takes over time. TD can develop even after a person has been taking the medicine for a short time at low doses. TD may not go away, even if you stop taking SAPHRIS. TD may also start after you stop taking SAPHRIS
Problems with your metabolism, such as:
High blood sugar and diabetes: If you have diabetes or risk factors for diabetes (eg, being overweight or family history of diabetes), your blood sugar should be tested before you start SAPHRIS and regularly during treatment. Complications of diabetes can be serious and even life threatening. Tell your healthcare provider if you have symptoms such as feeling very thirsty or very hungry, urinating more than usual, or feeling weak
Increased blood cholesterol or triglycerides: Your healthcare provider may decide to check your cholesterol and triglyceride levels during treatment
Weight gain: Weight gain has been reported with SAPHRIS. Your healthcare provider should check your weight before and regularly during treatment
Decreased blood pressure: You may feel lightheaded or faint when you rise too quickly from a sitting or lying position. Ask your healthcare provider about ways to reduce feeling dizzy or lightheaded upon standing, such as sitting on the edge of the bed for several minutes before getting up in the morning or slowly rising after sitting
Falls: SAPHRIS may increase risk of falls, which could cause fractures or other injuries
Low white blood cell count: Low white blood cell counts have been reported with antipsychotic drugs, including SAPHRIS. This may increase your risk of infection. Very low white blood cell counts, which can be fatal, have been reported with other antipsychotics
Increases in prolactin levels: Tell your healthcare provider if you experience a lack of menstrual periods, leaking or enlarged breasts, or impotence, because SAPHRIS may raise the levels of prolactin. The levels may continue to be high when SAPHRIS is used over time
Seizures
Impaired judgment, thinking, and motor skills: Do NOT drive or use dangerous machinery until you know how SAPHRIS affects you. SAPHRIS may make you drowsy
Increased body temperature: SAPHRIS may make you more sensitive to heat. You may have trouble cooling off. Be careful when exercising or when doing things likely to cause dehydration or make you warm
Difficulty swallowing: SAPHRIS and medicines like it have been associated with difficulty swallowing
Who should not take SAPHRIS?
Do not take SAPHRIS if you have certain liver problems, or if you are allergic to any of its ingredients. Get emergency medical help if you are having an allergic reaction (eg, difficulty breathing; itching; swelling of the face, tongue, or throat; or light-headedness).
What should I tell my healthcare provider before taking SAPHRIS?
Tell your healthcare provider about any medical conditions and if you have or have had:
Diabetes or high blood sugar in you or your family
High levels of total cholesterol, triglycerides, or LDL-cholesterol; or low levels of HDL-cholesterol
Seizures or conditions that increase your risk for seizures
Low or high blood pressure
Low white blood cell count
Certain heart problems such as irregular heartbeats or are at risk for these problems, or if you take medicines that can cause irregular heartbeats, because SAPHRIS should be avoided in these circumstances。