英文药名：KETAS Capsules(Ibudilast)
中文药名：异丁司特胶囊
生产厂家：杏林药业
ケタスカプセル10mg
治疗类别名称
磷酸二酯酶抑制剂
脑血管疾病，支气管哮喘改善剤
欧文商標名
KETAS Capsules 10mg
一般名：イブジラスト (Ibudilast) [JAN]
化学名：1-[2-(1-Methylethyl)pyrazolo[1,5-a]pyridin-3-yl]-2-methylpropan-1-one
分子式：C14H18N2O
分子量：230.31
融点 ：54～58℃
性状：
本品是一种白色结晶粉末。它是在甲醇，乙醇（99.5）非常可溶的或可溶于乙酸酐，在极微溶于水。
分配系数：
化学结构式：
活性成分的物理化学知识的表
| 有機溶媒相 | 水相 | 分配係数 |
| 1-オクタノール | 水 | 2.57×l03 |
| クロロホルム | 水 | 2.40×104 |
药效药理
1. 对脑血管障碍的影响
1) 脑血流增加作用
在脑血管疾病的患者，增加脑血流（PET）。
2) 颈内动脉平均血流改善作用
在慢性脑循环不全的患者，它增加了在颈总动脉的平均血液流量减少的循环阻力。
3) 血小板活性化抑制作用
在脑血管疾病的患者，其抑制血小板的活化。
4) 血小板凝集抑制作用
在脑血管疾病的患者，其抑制血小板聚集。
5) 血管内皮保护作用
在中风患者，抑制血管内皮细胞黏附分子的表达。
(2) 基本的药理作用
它抑制心脏和人类通过抑制磷酸二酯酶RT-PCR方法克隆脑磷酸二酯酶的活性。
1) 血管扩张作用
它增强了孤立的犬基底动脉前列环素的血管舒张作用。
另外，它增加了脑梗塞模型大鼠的脑局部血流。相比正常大鼠增加率较高。
2) 抗炎症作用
它抑制了TNFα的产生和NO在小鼠的神经胶质细胞。
此外，视束，理解的慢性脑灌注不足的大鼠模型中，观察到白质病变的胼胝体的抑制作用。
3) 血栓形成阻止作用
在脑血栓模型沙鼠，17来抑制血栓形成），在脑血栓模型大鼠，它由大脑血管阻塞抑制脑电图的扁平化。
4) 神经保护作用
在大鼠海马神经引起的谷氨酸抑制神经元损伤。
此外，恢复神经元密度的减少缺血瞬态脑缺血大鼠模型。
适应病症
1.支气管哮喘
2.改善头晕因脑梗塞后遗症慢性脑供血障碍
用法用量
1.在支气管哮喘的情况下
成年口服2次，每次口服10毫克。
2.在脑血管障碍的情况下
成人每天口服3次，每次10mg。该剂量可根据症状来调节。
包装规格
胶囊：10毫克
PTP包装：100胶囊（10粒×10），500胶囊（10粒×50）1000粒胶囊（10粒×100）2100胶囊（21粒×100）
瓶包装：500粒
制造厂商
杏林药业有限公司
注：上面部份中文资料仅参考，使用以原处方为准：http://www.info.pmda.go.jp/go/pack/4490010N1021_1_20/
KETAS Capsules（Ibudilast）
KETAS Capsules 10mg（ケタスカプセル10mg）
Brand name : KETAS Capsules 10mg
Active ingredient: Ibudilast
Dosage form: capsules (white cap, white body)
Print on wrapping: face：ケタスカプセル 10mg, KP-305
reverse side：KETAS cap 10mg, ケタスカプセル 10mg
Effects of this medicine
Cerebrovascular disorder: This medicine improves cerebrovascular disorder and relieves the subjective symptom of dizziness.
It is usually used to treat dizziness of chronic cerebral circulatory disturbance induced by an after effect of cerebral infarction.
Bronchial asthma: This medicine suppresses inflammation of respiratory tract in order to ease airway hypersensitivity.
It is usually used to treat bronchial asthma.
Before using this medicine, be sure to tell your doctor and pharmacist
•If you ever experienced any allergic reaction (itch, rash etc.) to any medicine.
If you have had intracranial bleeding recently.
•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>>
•General dosage regimen: For adults under treatment of cerebrovascular disorder, take 1 capsule (10mg of the active ingredient) at a time, 3 times a day. Dosage may be adjusted according to your disease/age/symptoms. Strictly follow the instructions of your doctor/pharmacist.
•General dosage regimen: For adults under treatment of bronchial asthma, take 1 capsule (10mg of the active ingredient) at a time, 2 times a day. Strictly follow the instructions of your doctor/pharmacist.
•If you missed a dose, take a dose as soon as possible. If it is almost time for the next dose (within 4 hours), skip the missed dose and continue your regular dosing schedule. DO NOT take a double dose to make up for the missed dose.
•If you took too much of this medicine (more than ordered), check with your doctor/pharmacist.
•Do not stop taking this medicine without the instructions of your doctor.
Precautions while taking this medicine
• Possible adverse reactions to this medicine
Common side effects are reported as below. If any of them occurs, check with your doctor/pharmacist: loss of appetite, nausea, hypersensitivity (rash, itch) etc.
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.
•bleeding tendency, subcutaneous bleeding [thrombocytopenia]
•fatigue, loss of appetite, yellowing of the skin/eyes [liver dysfunction, jaundice]
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 the reach of children. Store away from direct sunlight, heat and moisture.
•Discard the remainder. Do not store them.
Kyorin Pharmacetical Co.,LtdInternal
Revised: 4/2006
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.