英文药名：TOPINA Fine Granules（Topiramate）

中文药名：托吡酯颗粒

生产厂家：协和发酵麒麟

トピナ細粒10%

治疗类别名称
抗癫痫药
批准上市日期：2014年5月
欧文商標名
TOPINA Fine Granules
一般名
トピラマート　Topiramate
化学名
（-）-2, 3：4, 5-Di-O-isopropylidene-β-D-fructopyranose sulfamate
分子式
C12H21NO8S＝339.36
化学構造式

性状
为白色结晶，而不是臭，味微苦。
可溶性
易溶于甲醇或乙醇（99.5），微溶于水。
分配系数
logP'OCT= 0.59
（测量方法：摇瓶法正辛醇/ pH7的缓冲溶液）
药效药理
1.药理作用
(1) 抑制震动抽搐（大鼠，小鼠）。
(2) 抑制部分性癫痫模型（鼠）的火种抽搐。
(3) 强直性惊厥和缺乏遗传性癫痫模型（自发癫痫大鼠）神的攻击，抑制惊厥（DBA/ 2鼠标）。
(4) 短暂性Nokyo血液和出生后抑制低氧负荷诱发惊厥（鼠）。
2.作用机制
通过这种药物，它的出现抑制受到持久性去极化脉冲发射频率，抑制L型钙电流，抑制红藻氨酸诱发内向电流，通过GABAA受体推广和GABA氯离子涌入人类碳酸酐酶观察到酶（Ⅱ型和IV型）的抑制。从这些事实，这种药物的抗癫痫作用是电压依赖性钠通道抑制作用，电压依赖性L-型钙通道抑制作用，AMPA（α氨基-3-羟基-5-甲基异恶唑-4-丙酸）/红藻氨酸盐型谷氨酸盐受体功能抑制作用，估计是基于所述GABA A受体功能增强GABA的存在效果和碳酸酐抑制作用。
适应症
联合治疗抗癫痫药物对其它抗癫痫药物中充分的效果没有观察到癫痫患者的部分发作（有或没有继发性全身性发作）
用法与用量
成人：
开始与单一剂量为每日二次，每次50mg，之后，逐渐在一个星期或以上的时间间隔的增加，分割的日剂量为200-400毫克的口服给药两次作为维持剂量。此外，虽然根据症状，每天多达600毫克的最高剂量调整。
小児：
2岁以上的孩子开始与每日剂量为1mg/kg的吡口服给药，增加至每日剂量为2mg/ kg的具有两个以上周的间隔。此后，在两周的时间间隔或更逐渐增加少于为2mg/kg的作为单一的每日剂量的6毫克/千克口服给药维持剂量每日剂量。可以根据症状，每天和最多的为9mg/ kg或600mg的一个小小的剂量的最高剂量调整。此外，无论分为每日两次口服。
包装规格
颗粒10％：[瓶装]100克

制造厂商
协和发酵麒麟有限公司
完整资料附件：http://www.info.pmda.go.jp/go/pack/1139008C1020_1_04/
About the release of a new formulation "Topina ® fine granule 10%" of anti epileptic drug Topina®
On May 13, 2014, Kyowa Hakko Kirin Co., Ltd. (Head office: Tokyo, Representative Director: President: Chen Yu Hui, hereinafter "Kyowa Hakko Kirin") will release the anti epileptic drug "Topina® fine granule 10%" .
Topin ® tablets have been prescribed for many adult epilepsy patients as a concomitant medication against partial seizures of epilepsy which has not been adequately effective with other antiepileptic drugs since its release in September 2007, and in November 2013 Has been approved for partial change of dosage and dose for children aged 2 years and older for use with other medicines, and it is now possible to contribute to patients in children.
Topin ® fine grain 10% to be released this time was approved in January 2014 and was listed in the drug price standard in April of the same year. This product is easy to take even for epilepsy patients who are difficult to drink tablets such as some children and elderly people, and improvement of medication adherence * is expected.
The Kyowa Hakko Kirin Group pursues progress in life science and technology and contributes to the health and abundance of the people of the world by creating new value.
※ Medication Adherence
It means that the patient voluntarily takes medicine prescribed by a doctor to take doses and take doses.
Product outline of "Topina® fine grain 10%" Product name Topina ® fine grain 10%
Common name Topiramart
Indications/Combination therapy with antiepileptic drugs for partial seizures (including secondary generalized seizures) of epilepsy patients who are not adequately effective with other antiepileptic drugs
DOSAGE AND ADMINISTRATION Adults: In general, starting with oral administration once daily or twice daily as a topiramate for an adult in a single dose of 50mg. Thereafter, it gradually increases at intervals of 1 week or more, and the daily dose of 200 to 400 mg is administered orally as divided doses twice as maintenance dose.
Incidentally, depending on the symptoms, it will be increased or decreased appropriately, but the maximum daily dose should be 600 mg.
Children: For children aged 2 years and older, usually start with oral administration of 1mg/kg daily as Topiramate and increase to 2mg/kg daily at intervals of 2 weeks or more. After that, gradually increase by 2 mg/kg or less as a daily dose at intervals of 2 weeks or more, and daily dose of 6 mg/kg is orally administered as maintenance dose.
The dosage may be increased or decreased according to symptoms, but the maximum daily dose should be 9 mg/kg or 600 mg, whichever is lower. Both shall be administered orally in divided doses twice a day.
Packaging unit [rose]100 g
Approval acquisition date January 17, 2014