近日，新一代癫痫药物Fycompa（perampanel）吡仑帕奈口服混悬液，作为一种辅助疗法，用于12岁及以上癫痫患者部分发作性癫痫（有或无继发性全身性癫痫发作）和原发性全面强直阵挛（PGTC）癫痫发作的治疗。
Fycompa口服混悬液剂型与Fycompa片剂剂型具有生物等效性和可互换性，将为吞咽片剂可能存在困难或更倾向液体制剂的癫痫患者提供一种新的选择。
在美国，Fycompa口服混悬液于今年4月底获FDA批准，该药的获批是基于一项生物等效性研究的数据。该研究在健康受试者中开展，证实了空腹条件下，单剂量Fycompa口服混悬液和单剂量Fycompa片剂具有生物等效性。
Fycompa是由卫材内部研发的一种首创（first-in-class）的抗癫痫药物（AEDs），该药是一种高度选择性、非竞争性的AMPA型谷氨酸受体拮抗剂。谷氨酸是介导癫痫发作的主要神经递质。作为AMPA受体拮抗剂，Fycompa能通过靶向突触后AMPA受体-谷氨酸的活动，减少与癫痫发作相关神经元的过度兴奋；这种作用机制与目前市售的抗癫痫药物（AEDs）不同。
目前，已上市Fycompa片剂规格包括2mg、4mg、6mg、8mg、10mg、12mg薄膜衣片，该药适应症为：作为一种辅助药物，用于12岁及以上癫痫患者部分性癫痫发作（有或无继发性全身性癫痫发作）和原发性全面强直阵挛（PGTC）癫痫发作的治疗。
批准日期：2012年10月24日 公司：卫材（Eisai）
FYCOMPA（吡仑帕奈[perampanel]）片剂，供口服使用
FYCOMPA（吡仑帕奈[perampanel]）口服悬浮液，供口服使用
美国初步批准：2012
警告：
严重的心理和行为反应有完整的BOXED警告的完整的规定信息。
已报告在采取FYCOMPA的患者中，严重或危及生命的精神和行为不良反应，包括侵略，敌意，烦躁，愤怒和杀人的想法和威胁
监测这些反应的患者以及患者情绪，行为或个性的变化，特别是在滴定期间和较高剂量时
如果发生这些症状，应减少FYCOMPA，如果症状严重或恶化，应立即停药
最近的主要变化
适应症和用法：7/2017
剂量和管理：7/2017
警告和注意事项：7/2017
作用机制
Per el是突触后神经元上离子型α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）谷氨酸受体的非竞争性拮抗剂。 谷氨酸是中枢神经系统中主要的兴奋性神经递质，并且涉及由神经元过度激发引起的许多神经障碍。
FYCOMPA在人体中发挥抗癫痫作用的确切机制是未知数。
适用范围及用途
FYCOMPA是非竞争性AMPA谷氨酸受体拮抗剂，适用于：
治疗12岁以上癫痫患者部分发作性癫痫发作或不伴有二次全身性癫痫发作
辅助治疗12岁及以上癫痫患者原发性全身性强直阵挛性发作
剂量和管理
在没有中度或强力CYP3A4诱导剂的情况下给药
起始剂量：2mg，每天一次，在睡前口服
可以根据临床反应和耐受性增加剂量，每次2毫克，每周一次，不得超过每周间隔
单药治疗或辅助治疗部分发作缉获量的推荐维持剂量：8mg至12mg，每天在睡前一次
•辅助治疗中推荐维持剂量为原发性全身性强直阵挛性癫痫发作：8mg，每天在睡前一次
•使用提供的适配器和剂量注射器测量口服悬浮液
在伴有中度或强力CYP3A4诱导剂的情况下给药：参见章节
具体人口
轻度和中度肝功能损害：最高推荐日剂量为6mg（轻度），4mg（中度），每天在睡前一次
严重肝功能不全：不推荐
严重肾损伤或血液透析：不推荐
老年人：每2周不要频繁增加剂量
剂量形式和强度
片剂：2mg，4mg，6mg，8mg，10mg和12mg
口服悬浮液：0.5mg/mL
禁忌症
没有
警告和注意事项
自杀行为与思想：监测自杀思想或行为。
神经功能：监测眩晕，步态障碍，嗜睡和疲劳
病人驾驶或操作机械时要小心谨慎。
瀑布：监测跌倒和受伤
与嗜酸性粒细胞增多症和系统性症状（DRESS）/多器官超敏反应的药物反应：如果不存在替代性病因，则停药。
抗癫痫药物的戒除：在癫痫患者中，癫痫发作频率可能会增加。
不良反应
最常见的不良反应（≥5％，高于安慰剂≥1％）包括头晕，嗜睡，疲劳，烦躁，跌倒，恶心，体重增加，眩晕，共济失调，头痛，呕吐，挫伤，腹痛和焦虑
要报告可疑的不良反应，请致电1-888-274-2378或FDA在1-800-FDA-1088或www.fda.gov/medwatch联系Eisai
药物相互作用
避孕药：12毫克每日一次可能会降低含有左炔诺孕酮的荷尔蒙避孕药的有效性
中度和强力的CYP3A4诱导剂（包括卡马西平，奥卡西平和苯妥英）：增加睫状increase素的清除率并降低ampampelel血浆浓度。当中度或强力的CYP3A4诱导物被引入或撤出时，密切监测患者。 FYCOMPA的剂量调整可能是必要的。
在特定人口中使用
怀孕：根据动物数据，可能会导致胎儿的伤害。
包装规格/存储和处理
提供
FYCOMPA片剂
2毫克是橙色，圆形，双面印刷，薄膜包衣片剂一侧用“2”凹陷，另一侧为“Є275”。它们提供如下：
瓶子30 NDC 62856-272-30
瓶90 NDC 62856-272-90
4毫克是红色，圆形，双面印刷，薄膜包裹的片剂一侧用“4”和另一边“Є277”。它们提供如下：
瓶子30 NDC 62856-274-30
瓶90 NDC 62856-274-90
6毫克是粉红色，圆形，双面印刷，薄膜包衣片在一侧为“6”，另一侧为“Є294”。它们提供如下：
瓶子30 NDC 62856-276-30
瓶装90 NDC 62856-276-90
8毫克是紫色，圆形，双面印刷，薄膜包衣片剂一侧用“8”凹下，另一侧为“Є295”。它们提供如下：
瓶子30 NDC 62856-278-30
瓶90 NDC 62856-278-90
10毫克为绿色，圆形，双面，薄膜包裹片一侧为“10”，另一侧为“Є296”。它们提供如下：
瓶子30 NDC 62856-280-30
瓶装90 NDC 62856-280-90
12毫克是蓝色，圆形，双面印刷，薄膜包衣片在一侧以“12”凹陷，另一侧为“Є297”。它们提供如下：
瓶子30 NDC 62856-282-30
瓶90 NDC 62856-282-90
FYCOMPA口服（暂停销售）
0.5mg/mL是白色至灰白色不透明液体。它提供在一个圆形琥珀色的PET瓶子与防儿童的封闭。它与一个分配器一起包装，提供两个20 mL刻度口服计量注射器和一个推入式瓶子适配器。
含有340毫升NDC的瓶子62856-290-38
存储
片剂：储存于20°C至25°C（68°F至77°F）;偏移允许为15°C至30°C（59°F至86°F）。 [见USP可控室温]额
口服悬浮液：不要超过30°C（86°F）。不要冻结在瓶子首次开启后的90天内使用。
完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=71cf3309-e182-473c-8b0b-280cabd0e122
FYCOMPA(perampanel) orals uspension, CIII
Important Safety Information
What is FYCOMPA(perampanel)？
FYCOMPA® is a prescription medicine used in people with epilepsy aged 12 and older alone or with other medicines to treat partial-onset seizures with or without secondarily generalized seizures and with other medicines to treat primary generalized tonic-clonic seizures
Important Safety Information
FYCOMPA may cause mental (psychiatric) problems, including: new or worse aggressive behavior (including homicidal behavior), hostility, anger, anxiety, or irritability; being suspicious or distrustful (believing things that are not true); seeing objects or hearing things that are not there; confusion; difficulty with memory; other unusual or extreme changes in behavior or mood. Tell your healthcare provider right away if you have any new or worsening mental problems while taking FYCOMPA.
Like other antiepileptic drugs, FYCOMPA may cause suicidal thoughts or actions in a very small number of people, about 1 in 500. Call your healthcare provider right away if you have any of these symptoms, especially if they are new, worse, or worry you: thoughts about suicide or dying; new or worse depression; feeling agitated or restless; trouble sleeping (insomnia); acting aggressive; being angry, or violent; an extreme increase in activity and talking (mania); attempt to commit suicide; new or worse anxiety; panic attacks; new or worse irritability; acting on dangerous impulses; other unusual changes in behavior or mood. Suicidal thoughts or actions can be caused by things other than medicines. If you have suicidal thoughts or actions, your healthcare provider may check for other causes.
Pay attention to any changes especially sudden changes in mood, behaviors, thoughts, or feelings and keep all follow-up visits with your healthcare provider as scheduled. Call your healthcare provider between visits as needed, especially if you are worried about symptoms.
Do not stop FYCOMPA without first talking with your healthcare provider. Stopping suddenly can cause serious problems and can cause you to have seizures more often.
Before taking FYCOMPA, tell your healthcare provider about all of your medical conditions, including if you: have or have had depression, mood problems, aggressive or hostile behavior (for example, homicidal behavior), suicidal thoughts or behavior, or other psychiatric problems; have liver or kidney problems; drink alcohol; have abused prescription medicines, street drugs, or alcohol in the past; are pregnant or plan to become pregnant. It is not known if FYCOMPA will harm your unborn baby. If you become pregnant while taking FYCOMPA, talk to your healthcare provider about registering with the North American Antiepileptic Drug Pregnancy Registry (1-888-233-2334); are breastfeeding or plan to breastfeed. Talk to your healthcare provider about the best way to feed your baby if you take FYCOMPA and to decide if you will take FYCOMPA or breastfeed. You should not do both.
Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Taking FYCOMPA with certain other medicines can cause side effects or reduce either drug’s benefit. These medicines include: birth control, carbamazepine, phenytoin, oxcarbazepine, rifampin, and St. John’s Wort.
What should I avoid while taking FYCOMPA?
Do not drive, operate heavy machinery, or do other dangerous activities until you know how FYCOMPA affects you. FYCOMPA may make you dizzy, sleepy, or tired. Do not drink alcohol or take other medicines that make you sleepy or dizzy until you talk to your healthcare provider. FYCOMPA taken with alcohol or medicines that cause sleepiness or dizziness may make your sleepiness or dizziness worse. FYCOMPA when taken with alcohol may also make your mood worse, increase anger, confusion, and depression.
FYCOMPA may cause other serious side effects, including: Dizziness, vertigo (sense of spinning), and problems walking normally. You may have problems walking normally if you are unsteady because you feel dizzy. These symptoms can increase when your dose of FYCOMPA is increased. Your risk of feeling dizzy and having problems walking normally may be higher if you are elderly; Sleepiness and tiredness; Increased risk of falls. Taking FYCOMPA can increase your chance of falling. These falls can cause serious injuries. Your risk of falling may be higher if you are elderly; A serious allergic reaction that may affect your skin or other parts of your body such as your liver, kidneys, heart, or blood cells. This allergic reaction can be life-threatening and can cause death. Call your healthcare provider right away if you have: a skin rash, hives; fever or swollen glands that do not go away; swelling of your face; shortness of breath; swelling of the legs; yellowing of the skin or whites of the eyes; or dark urine
The most common side effects of FYCOMPA include: dizziness; sleepiness; tiredness; irritability; falls; nausea and vomiting; weight gain; vertigo (sense of spinning); problems walking normally; problems with muscle coordination; headache; bruising; abdominal pain; anxiety
FYCOMPA is a controlled substance (CIII) because it can be abused or lead to drug dependence. Keep FYCOMPA in a safe place to protect it from theft and never give it to anyone else because it may harm them. Selling or giving away FYCOMPA is against the law.