近日，FDA已批准扩大Fycompa（perampanel）的适应症，作为一种辅助药物用于12岁及以上伴有原发性全面强直阵挛（PGTC）癫痫发作的癫痫患者。此前，FDA已于2012年10月批准Fycompa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）的辅助治疗。Fycompa具有日服一次的益处，有望减少潜在的服药负担，并改善患者的药物依从性。
批准日期：2012年10月23日 公司：卫材（Eisai）
FYCOMPA（吡仑帕奈 perampanel）片，口服使用，CIII
FYCOMPA（吡仑帕奈 perampanel）口服液 uspension，CIII
最初美国批准：2012
警告：
严重的精神和行为反应，请参阅完整的黑框警告的完整处方信息。
严重或危及生命的精神和行为的不良反应，包括侵略，敌视，烦躁，愤怒和杀人意念和威胁已经报道了服用FYCOMPA患者
监测患者对这些反应以及用于在情绪，行为，或个性不属于典型的患者，特别是在滴定期间的变化，并在较高的剂量。
如果出现这些症状FYCOMPA应该会减少，应停药立即如果症状严重或正在恶化
目前的主要变化
适应证和用途 06/2015
用法与用量 04/2016
作用机理
Perampanel是离子型α氨基-3-羟基-5-甲基-4-异唑丙酸（AMPA）谷氨酸受体上突触后神经元的非竞争性拮抗剂。谷氨酸是中枢神经系统中主要的兴奋性神经递质，并在若干引起的神经元过度兴奋神经病症的牵连。
通过该FYCOMPA施加在人体中它的抗癫痫作用的确切机制是未知的。
适应症和用法
FYCOMPA，非竞争性AMPA谷氨酸受体拮抗剂，被表示为用于治疗辅助疗法：
有或没有在12岁及以上的癫痫患者继发性全身性发作的部分性发作
原发性全身强直 - 阵挛性发作在12岁及以上的癫痫患者
用法用量
在没有酶诱导抗癫痫药物给药（抗癫痫药）
在睡前，每日一次2毫克口服：开始剂量
基于由2毫克的增量每天一次不超过经常每隔一周临床响应和耐受性可能增加剂量。
推荐维持剂量：部分性发作-8至12毫克，每天一次睡前服用;原发性全身强直 - 阵挛性发作-8毫克，每天一次睡前服用
个体剂量应调整基于临床响应和耐受性
使用提供的适配器和计量注射器测量口服混悬液
在加药伴随酶诱导抗癫痫药物的存在：见
特殊人群
轻度和中度肝受损：最大推荐剂量为每日6毫克（轻度）和4毫克（中度），每天一次在睡前
严重肝损伤：不推荐
严重肾功能损害或血液透析：不推荐
老人：增加剂量比每2周没有更频繁
剂型和规格
片剂：2毫克，4毫克，6毫克，8毫克，10毫克和12毫克
口服混悬液：0.5毫克/毫升
禁忌症
没有
警告和注意事项
自杀行为和意念：监视自杀想法或行为
神经系统的影响：监测头晕，步态不稳，嗜睡和疲劳。
驾驶或操作机械时，患者应谨慎使用
瀑布：监控跌倒和受伤
抗癫痫药停药：在癫痫患者可出现癫痫发作频率增加
不良反应
最常见的不良反应（高于安慰剂≥5％和≥1％），包括头晕，嗜睡，乏力，烦躁，下降，恶心，体重增加，眩晕，共济失调，头痛，呕吐，挫伤，腹部疼痛和焦虑
药物相互作用
避孕药：12毫克，每天一次可能会降低含左炔诺孕酮激素避孕药的有效性。
细胞色素P450诱导剂：卡马西平，奥卡西平，苯妥英和增加perampanel的间隙并降低perampanel血浆浓度，降低FYCOMPA的有效性。当这些或相关酶诱导抗癫痫药物被引入或撤回，患者应进行密切监测。 FYCOMPA的剂量调整可能是必要。
不推荐同时使用：强CYP3A诱导除抗癫痫药物（如利福平，圣约翰草）。
特殊人群中使用
妊娠：根据动物实验数据，可能会对胎儿造成伤害。
修订：2016年4月
包装规格
片剂

2mg,4mg,6mg,8mg,10mg,12mg
口服溶液

FYCOMPA® (perampanel) Oral Suspension Now Available as an Option for Patients with Epilepsy Who May Have Difficulty Swallowing Tablets or Prefer Liquids
New FDA-Approved Formulation Indicated as Adjunctive Therapy for the Treatment of Partial-Onset Seizures and Primary Generalized Tonic-Clonic Seizures
2016,Eisai Inc. announced today the availability of FYCOMPA® (perampanel) Oral Suspension, a new bioequivalent interchangeable alternative to the FYCOMPA tablet for patients who have difficulty swallowing tablets or prefer liquids. FYCOMPA CIII is indicated as adjunctive therapy for the treatment of partial-onset seizures (POS) with or without secondarily generalized seizures, and primary generalized tonic-clonic (PGTC) seizures in patients with epilepsy 12 years of age and older. This new option, which comes in a single bottle with an adapter and syringes to measure the right dose, was approved by the U.S. Food and Drug Administration (FDA) on April 29, 2016. Please see Important Safety Information, including Boxed WARNING for Serious Psychiatric and Behavioral Reactions, below.
"Swallowing tablets can be a real concern for some patients with epilepsy," said Lynn Kramer, M.D., Chief Clinical Officer and Chief Medical Officer, Neurology Business Group, Eisai. "We are proud to offer this new option, which reinforces Eisai's ongoing commitment to advancing epilepsy care and addressing the unmet medical needs of patients and their families."
About FYCOMPA
FYCOMPA (perampanel) is indicated as adjunctive therapy for the treatment of partial-onset seizures with or without secondarily generalized seizures and primary generalized tonic-clonic seizures in patients with epilepsy 12 years of age and older.
FYCOMPA is an oral medication and the first and only FDA-approved non-competitive AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor antagonist. The precise mechanism by which FYCOMPA exerts its antiepileptic effects in humans has not been fully elucidated.
FYCOMPA is supplied as 2 mg, 4 mg, 6 mg, 8 mg, 10 mg and 12 mg film-coated tablets, and now in an oral suspension formulation. FYCOMPA has been designated by the U.S. Drug Enforcement Administration as a federally-controlled substance (CIII).
FYCOMPA, approved in 47 countries, was discovered and developed by Eisai. Over 60,000 patients globally have been treated with FYCOMPA.
Important Safety Information
FYCOMPA may cause: new or worse aggressive behavior, homicidal thoughts or threats, hostility, anger, anxiety, irritability, being suspicious or distrustful (believing things that are not true), and other unusual or extreme changes in behavior or mood. Before taking FYCOMPA, patients should tell their healthcare provider if they have or had mental problems, aggression or hostile behavior.
Patients, their caregivers, and families should monitor for these changes and call their healthcare provider right away if they have any new or worsening mental problems while taking FYCOMPA. The combination of alcohol and FYCOMPA significantly worsened mood and increased anger. Patients taking FYCOMPA should avoid the use of alcohol.
Antiepileptic drugs, including FYCOMPA, may cause suicidal thoughts or actions in a very small number of people, about 1 in 500. Patients should call their healthcare providers right away if they have any of the following symptoms, especially if they are new, worse, or worrisome: thoughts about suicide or dying, thoughts of self-harm, attempt to commit suicide, new or worse depression, new or worse anxiety, feeling agitated or restless, panic attacks, trouble sleeping (insomnia), new or worse irritability, acting aggressive, being angry or violent, acting on dangerous impulses, an extreme increase in activity and talking (mania), and other unusual changes in behavior or mood.
Patients may have problems walking normally if they are unsteady because they feel dizzy. These symptoms may increase when their dose of FYCOMPA is increased. A patient's risk of feeling dizzy and having problems walking normally may be higher if they are elderly. FYCOMPA may make patients feel sleepy or tired. Patients should not drive, operate heavy machinery, or do other dangerous activities until they know how FYCOMPA affects them. A patient's risk of feeling sleepy and tired may be higher if they are elderly.
Taking FYCOMPA may increase a patient's chance of falling. These falls can cause serious injuries. A patient's risk of falling may be higher if they are elderly.
Patients must not stop FYCOMPA without first talking to their healthcare provider. Stopping FYCOMPA suddenly can cause serious problems and can cause patients to have seizures more often.
The most common side effects seen in patients receiving FYCOMPA were dizziness, sleepiness, headache, tiredness, irritability, falls, nausea, problems with muscle coordination, problems walking normally, vertigo, and weight gain. Tell your healthcare provider about any side effect that bothers you or does not go away.
Taking FYCOMPA with certain other medicines can cause side effects or reduce either drug's benefit. These other medicines include: birth control, carbamazepine, phenytoin, oxcarbazepine, rifampin, and St. John's wort.
Before taking FYCOMPA, patients should tell their healthcare provider if they drink alcohol. Patients should not drink alcohol or take other medicines that make them sleepy or dizzy while taking FYCOMPA until they talk to their healthcare provider. FYCOMPA taken with alcohol or medicines that cause sleepiness or dizziness may make their sleepiness or dizziness worse.
Before taking FYCOMPA, patients should tell their healthcare provider if they are pregnant or plan to become pregnant while taking FYCOMPA. It is not known if FYCOMPA will harm your unborn baby. If a patient becomes pregnant while taking FYCOMPA, they should talk to their healthcare provider about registering with the North American Antiepileptic Drug Pregnancy Registry (1-888-233-2334).
Before taking FYCOMPA, patients should tell their healthcare provider if they are breastfeeding or plan to breastfeed. Patients should talk to their healthcare provider about the best way to feed their baby if they take FYCOMPA. Patients should not take FYCOMPA if they breastfeed.
Before taking FYCOMPA, patients should tell their healthcare provider if they have liver or kidney problems. They should not take FYCOMPA if they have severe kidney or liver problems.
FYCOMPA is a controlled substance (CIII) because it can be abused or lead to drug dependence. Before taking FYCOMPA, patients should tell their healthcare provider if they have abused prescription medicines, street drugs, or alcohol in the past. Patients should keep their FYCOMPA in a safe place to protect it from theft and should never give it to anyone else because it may harm them. Selling or giving away FYCOMPA is against the law.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=71cf3309-e182-473c-8b0b-280cabd0e122