| 简介：
英文药名：Diacomit（Stiripentol drysyrup）
中文名称：司替戊醇干糖浆
生产厂家：日本明治制药
药物分类名称
抗癫痫药
批准日期：2012年11月
欧文商標名
DIACOMIT CAPSULES 250mg
DIACOMIT DRYSYRUP 250mg
DIACOMIT DRYSYRUP 500mg
一般名
スチリペントール Stiripentol
化学名
（1E,3RS）-1-（Benzo［d］［1,3］dioxol-5-yl）-4,4-dimethylpent-1-en-3-ol
分子式
C14H18O3
分子量
234.29
構造式
性 状
Stilipentol是一种白色至微黄色的结晶粉末。
该产品微溶于乙醇（96％），微溶于氯仿，几乎不溶于水。
熔点
约75°C
分配系数（LogP）
2.94（辛醇/水系统）
处理注意事项
由于使用的颜料，干糖浆制剂可能具有红棕色颗粒。
批准条件
由于日本的临床试验数量非常有限，通过对所有病例进行使用结果调查，直到制造和销售后累积了一定数量的病例数据，书籍 除了掌握使用药物的患者的背景信息外，在早期阶段收集有关该药物安全性和有效性的数据，并采取必要措施正确使用该药物。
药用药理学
1.抗惊厥作用
据报道，在各种癫痫动物模型中，它显示出抗惊厥作用。
（1）抑制由戊四唑诱导的小鼠和大鼠的惊厥。
（2）抑制小鼠和大鼠的最大电击惊厥。
（3）抑制荷包牡丹碱和士的宁诱发小鼠惊厥。
（4）
通过脑内给予氢氧化铝抑制猴子诱发的自发性惊厥性癫痫发作。
（5）抑制遗传性癫痫的动物模型的癫痫样发作（惊厥听源性小鼠，菌株引起小发作状缺勤大鼠）。
2.作用机制
（1）药物是，GABA摄取的抑制活性，GABA转氨酶活性通过促进对脑组织中的浓度GABA增加作用和GABA A受体变构调节效果降低作用，提高GABA神经传递。该产物对具有α3或δ亚基的GABAA受体显示出更强的活性。
（2）本药物，药物代谢基于抑制CYP抑制作用，增加组合抗癫痫药物的血液水平，以提高其抗惊厥作用。[参见“药代动力学”部分]
适应症
联合用clobazam和丙戊酸钠治疗阵发性癫痫或强直 - 阵挛性癫痫发作的Dravet综合征患者对clobazam和丙戊酸钠没有足够的疗效。
用法与用量
通常，1岁及以上的患者口服给药为每天50 mg / kg，每日2至3剂，在用餐期间或饭后立即服用stipantntol。 给药开始于每天20mg / kg，并且以1周或更长的间隔以1mg / kg或更多的间隔增加。 然而，对于体重为50千克或以上的患者，开始以每天1000毫克的剂量作为镇咳药，每隔一周或更长时间增加500毫克。
最大日剂量不得超过50毫克/千克或2500毫克，以较低者为准。
包装
干糖浆
250毫克：60包
500毫克：60包
胶囊：250毫克（瓶装）60粒
制造商销售代理（进口）
明治精华制药有限公司
完整资料附件：http://www.info.pmda.go.jp/go/pack/1139011M1028_1_04/
DIACOMIT DRYSYRUP 250mg（ディアコミットドライシロップ分包250mg）
Brand name : DIACOMIT DRYSYRUP 250mg
Active ingredient: Stiripentol
Dosage form: very light reddish white granules
Print on wrapping: ディアコミットドライシロップ分包250mg, 1包（846mg）中 スチリペントール250mg
Effects of this medicine
This medicine reduces excessive excitation of the nerves in the brain to help control epileptic seizures.
It is usually used together with other medicines to treat clonic seizures or tonic-clonic seizures in Dravet syndrome.
Before using this medicine, be sure to tell your doctor and pharmacist
•If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines.
If you have liver dysfunction, renal dysfunction, blood disorder, respiratory disease, or QT prolongation (abnormal electrocardiogram).
•If you are pregnant or breastfeeding.
•If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.)
Dosing schedule (How to take this medicine)
•Your dosing schedule prescribed by your doctor is <<to be written by a healthcare professional>>
•For patients aged 1 year or older (weighing less than 50 kg): In general, take 50 mg/kg of the active ingredient a day in 2 or 3 divided doses at or just after a meal, by mixing well with water. When taking this medicine for the first time, start with 20 mg/kg a day and then the dosage will be increased by 10 mg/kg at every intervals of 1 week or longer up to 50 mg/kg a day. The maximum daily dose is 50 mg/kg.
For patients aged 1 year or older (weighing 50 kg or more): In general, take 1,000 mg/kg of the active ingredient a day in 2 or 3 divided doses at or just after a meal, by mixing well with water. The dosage will be increased by 500 mg/kg at every intervals of 1 week or longer. The maximum daily dose is 2,500 mg/kg.
This medicine is used concomitantly with other antiepileptic medicine. This preparation contains 250 mg of the active ingredient in a packet. In any case, strictly follow the instructions.
•Do not open the packet before use.
•Mix the medicine well with water and drink the mixture immediately.
•For adjusting the dose, mix well 1 packet (250 mg of active ingredient) with about 10 mL of water, measure your prescribed dose using a measuring cup or dropper, and drink the dose immediately.
•Do not prepare the mixture beforehand and leave it alone. Discard remaining mixture with water.
•If you miss a dose, take the missed dose with a snack as soon as possible; however, do not take with any caffeine-containing food such as chocolate. Let at least 4 hours pass between doses. You should never take two doses at one time.
•If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist.
•Do not stop taking this medicine unless your doctor instructs you to do so.
Precautions while taking this medicine
•This medicine may cause decreased appetite and weight decrease. If any such sign appears, please consult with your doctor or pharmacist.
•This medicine may cause sleepiness and depression of your attentiveness, concentration and reflexive motor function. Avoid driving a car or operating dangerous machinery.
•Take care in taking this medicine with caffeine-containing food (e.g., chocolate, coffee, tea, green tea, or coke) since it may intensify the effects of caffeine.
•Be moderate in drinking alcohol since it affects the effects of this medicine.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include somnolence, decreased appetite, ataxia (light headedness) and tremor (trembling). If any of these symptoms occur, consult with your doctor or pharmacist.
The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately.
•fever, sore throat, nose bleeding, gum bleeding, subcutaneous bleeding [neutropenia, thrombocytopenia]
The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above.
Storage conditions and other information
•Keep out of reach of children. Store away from direct sunlight, heat and moisture.
•Discard the remainder. Do not store them. Seek advice of your pharmacy or medical institution about proper disposal of the unused medicines.
Meiji Seika Pharma Co., Ltd.Internal
Published: 11/2012
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment. |
