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APTIOM®(eslicarbazepine acetate)-醋酸艾司利卡西平
Important Safety Information and Indication for Aptiom (eslicarbazepine acetate):
Do not take APTIOM if you are allergic to eslicarbazepine acetate, any of the other ingredients in APTIOM, or oxcarbazepine.
Suicidal behavior and ideation: APTIOM may cause suicidal thoughts or actions, depression, or mood problems. Call your doctor right away if you experience these or any other effects or reactions: thoughts about suicide or dying; attempting to commit suicide; new or worse depression, anxiety, or irritability; feeling agitated or restless; panic attacks; trouble sleeping (insomnia); acting aggressive; being angry or violent; acting on dangerous impulses; an extreme increase in activity and talking (mania); or other unusual changes in behavior or mood.
Allergic reactions: APTIOM may cause serious skin rash or other serious allergic reactions that may affect organs or other parts of your body like the liver or blood cells. You may or may not have a rash with these types of reactions. Call your doctor right away if you experience any of the following symptoms: swelling of the face, eyes, lips, or tongue; trouble swallowing or breathing; hives; fever, swollen glands, or sore throat that do not go away or come and go; painful sores in the mouth or around your eyes; yellowing of the skin or eyes; unusual bruising or bleeding; severe fatigue or weakness; severe muscle pain; or frequent infections or infections that do not go away.
Low salt (sodium) levels in the blood: APTIOM may cause the level of sodium in your blood to be low. Symptoms may include nausea, tiredness, lack of energy, irritability, confusion, muscle weakness or muscle spasms, or more frequent or more severe seizures.
Nervous system problems: APTIOM may cause problems that can affect your nervous system, including dizziness, sleepiness, vision problems, trouble concentrating, and difficulties with coordination and balance. APTIOM may slow your thinking or motor skills. Do not drive or operate heavy machinery until you know how APTIOM affects you.
Liver problems: APTIOM may cause problems that can affect your liver. Symptoms of liver problems include yellowing of your skin or the whites of your eyes, nausea or vomiting, loss of appetite, stomach pain, or dark urine.
Most common adverse reactions: The most common side effects in patients taking APTIOM include dizziness, sleepiness, nausea, headache, double vision, vomiting, feeling tired, problems with coordination, blurred vision, and shakiness.
Drug interactions: Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Taking APTIOM with certain other medicines may cause side effects or affect how well they work. Do not start or stop other medicines without talking to your healthcare provider. Especially tell your healthcare provider if you take oxcarbazepine, carbamazepine, phenobarbital, phenytoin, primidone, clobazam, omeprazole, simvastatin, rosuvastatin, or birth control medicine.
Discontinuation: Do not stop taking APTIOM without first talking to your healthcare provider. Stopping APTIOM suddenly can cause serious problems.
Pregnancy and lactation: APTIOM may cause your birth control medicine to be less effective. Talk to your healthcare provider about the best birth control method to use. APTIOM may harm your unborn baby. APTIOM passes into breast milk. Tell your healthcare provider if you are pregnant or plan to become pregnant, or are breastfeeding or plan to breastfeed. You and your healthcare provider will decide if you should take APTIOM. If you become pregnant while taking APTIOM, talk to your healthcare provider about registering with the North American Antiepileptic Drug (NAAED) Pregnancy Registry. The purpose of this registry is to collect information about the safety of antiepileptic medicine during pregnancy. You can enroll in this registry by calling 1-888-233-2334.
Get medical help right away if you have any of the symptoms listed above.
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch
醋酸艾司利卡西平片APTIOM(eslicarbazepine acetate)已被美国批准为癫痫口服使用
适应证和用途
APTIOM是适用于作为癫痫部分性发作的辅助治疗癫痫部分性发作.
剂量和给药方法
（1）开始治疗400 mg每天1次。一周后，剂量增加至800mg每天1次(推荐维持剂量)。最大推荐维持剂量是1200 mg每天1次(在800 mg每天1次最小一周后)。
（2）有中度至严重肾受损患者：在200 mg每天1次开始治疗，在两周后，剂量增加至400 mg每天1次。最大推荐维持剂量为600 mg每天1次。
剂型和规格
片：200mg，400mg，600mg，800mg。
APTIOM Rx
Pharmacological Class:
Dibenzazepine.
Active Ingredient(s):
Eslicarbazepine acetate 200mg+, 400mg, 600mg+, 800mg+; (+) scored tabs.
Company
Sunovion Pharmaceuticals Inc
Indication(s):
Adjunctive treatment of partial-onset seizures.
Pharmacology:
Aptiom is extensively converted to eslicarbazepine, which may be responsible for therapeutic effects in humans. The precise mechanism by which eslicarbazepine exerts anticonvulsant activity is unknown, but is thought to involve inhibition of voltage-gated sodium channels.
Clinical Trials:
The efficacy of Aptiom as adjunctive therapy was established in 3 randomized, double-blind, placebo-controlled trials in adults with epilepsy. Patients enrolled had partial-onset seizures with or without secondary generalization and were not adequately controlled with 1–3 concomitant AEDs.
Studies 1 and 2 compared Aptiom 400mg, 800mg, and 1200mg once daily with placebo. Study 3 compared Aptiom 800mg and 1200mg once daily with placebo. In all trials following an 8-week baseline phase, patients were randomized to a 2-week initial titration phase, and then a subsequent 12-week maintenance phase.
The primary efficacy endpoint was the standardized seizure frequency during the maintenance phase over 28 days. The Aptiom 400mg/day dose was studied in Studies 1 and 2 and did not show significant treatment effect. A statistically significant effect was observed with Aptiom 800mg/day in Studies 1 and 2, and with Aptiom 1200mg/day in all 3 trials. Results in Study 1 showed that the Aptiom 800mg arm had a seizure frequency value of 5.0 (P=0.047) and the Aptiom 1200mg arm had a value of 4.3 (P=0.001) vs. 6.6 with placebo. In Study 2, the Aptiom 800mg arm showed a value of 6.2 (P=0.006) and the Aptiom 1200mg arm had a value of 6.6 (P=0.042) vs. 8.6 with placebo. In Study 3, the Aptiom 1200mg arm had a value of 6.0 (P=0.004) vs. 7.9 with placebo.
Legal Classification:
Rx
Adults:
Initially 400mg once daily; increase to 800mg once daily after one week. Max maintenance dose: 1200mg once daily (initiate only after ≥1 week at 800mg once daily). May initiate at 800mg once daily if need additional seizure reduction and outweighs increased adverse reaction risk. Moderate-to-severe renal impairment (CrCl <50mL/min): initially 200mg once daily; increase to 400mg once daily after 2 weeks. Max maintenance dose of 600mg once daily may be beneficial.
Children:
<18 years: not established.
Warnings/Precautions:
Increased risk of suicidal thinking or behavior; monitor for clinical worsening or unusual changes. Discontinue if serious dermatologic reactions or DRESS/multi-organ hypersensitivity occurs. Measure serum sodium and chloride levels during therapy and esp. if hyponatremia symptoms develop. Monitor for neurological adverse reactions (esp. in elderly). Monitor LFTs at baseline; discontinue if jaundice or evidence of significant liver injury occurs. Severe hepatic impairment: not recommended. Avoid abrupt cessation. Pregnancy (Cat. C). Nursing mothers: not recommended.
Interaction(s)
Do not take as adjunctive therapy with oxcarbazepine. Antagonized by carbamazepine, phenobarbital, phenytoin, and primidone; monitor and adjust dose. May potentiate phenytoin, clobazam, omeprazole. May antagonize simvastatin, rosuvastatin. May decrease effectiveness of oral contraceptives; use additional non-hormonal forms. May affect thyroid function tests. Caution with other drugs known to decrease serum sodium. Monitor INR when given with warfarin.
Adverse Reaction(s)
Dizziness, somnolence, nausea, headache, diplopia, vomiting, fatigue, vertigo, ataxia, blurred vision, tremor; rare: serious skin reactions (eg, SJS, TEN), DRESS/multi-organ hypersensitivity, anaphylaxis, angioedema, liver injury.
Notes:
To enroll in the North American Antiepileptic Drug Pregnancy Registry call (888) 233-2334.
How Supplied:
Tabs 200mg, 400mg—30; 600mg—60, 90; 800mg—30, 90
LAST UPDATED:
4/24/2014
FDA批准Aptiom用于治疗成人患者的癫痫发作
11月8日，美国食品药品管理局（FDA）批准 Sunovion公司 Aptiom（醋酸艾司利卡西）作为一种辅助药物用于治疗癫痫有关的癫痫发作。癫痫是一种大脑神经细胞异常或过度活动引起的脑失调。美国每年大约会发生20万癫痫发作和癫痫新病例。
Aptiom被批准用于治疗部分性癫痫发作，这是癫痫患者中所发现的最常见癫痫发作形式。癫痫发作能引起多种症状，包括重复的肢体运动、不寻常的行为和丧失意识的全身性痉挛。“一些癫痫患者不能从现有的治疗中获得满意的癫痫发作控制，”FDA药品评价与研究中心神经病学产品部门代理主任、医学博士Eric Bastings说。“我们继续给患者提供一种新的治疗选择是非常重要的。”
在三项临床研究中，部分性癫痫发作受试者被随机配给Aptiom或安慰剂，临床研究的结果证实Aptiom在减少癫痫发作频次方面是有效的。临床试验中，Aptiom用药患者报道的最常见副作用包括头晕、嗜睡、恶心、头痛、眼花、呕吐、疲劳、运动协调性丧失。这些和其它副作用及建议监测的事项均在药物标签中有描述。
与其它抗癫痫药物一样，Aptiom可在为数不多的人群中引起自杀想法或行为。如果患者有自杀或死去的想法，出现新的或恶化的焦虑或抑郁、或在行为或情绪上出现其它不寻常的变化，他们应该立刻与医生联系。
Aptiom在获得批准时附带一用药指南，用药指南可以为患者提供有关该药品的重要信息，帮助患者避免严重不良事件。该指南在患者每次填充处方时分发给他们。Aptiom由位于Mass市马尔堡的Sunovion制药公司上市销售
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