英文药名：KIPRES Tablets(Montelukast Sodium)

中文药名：孟鲁司特钠片

生产厂家：杏林药业
治疗类别名称
白三烯受体拮抗剂，支气管哮喘，
过敏性鼻炎的治疗药物
欧文商標名
KIPRES Tablets 5mg
KIPRES Tablets 10mg
一般名：
モンテルカストナトリウム（Montelukast Sodium）[JAN]
化学名：
(+)-1-[[[(R)-3-[(E)-2-(7-Chloro-2-quinolyl)vinyl]-α-[2-(1-hydroxy-1-methylethyl)phenethyl]benzyl]thio]methyl] cyclopropaneacetic acid monosodium salt
分子式：
C35H35ClNNaO3S
分子量：
608.18
性状：
该产品是一种白色粉末，N，N-二甲基甲，甲醇，乙醇（95），或在吡啶非常易溶，易溶于水或乙二醇，并在乙醚中几乎不溶。
分配系数：1辛醇/磷酸盐缓冲液（pH值为7）分配系数是logKD=2.3±0.2。
化学構造式：

操作注意事项*
キプレス錠 5mg-10mg
储存：开封后，保存，避免受潮。
药效药理
作用机序
1.支气管哮喘
孟鲁司特是选择性地结合到半胱氨酰白三烯受体1（半胱氨酸LT1受体），LTD 4和LTE 4的病理生理作用是炎症介质引起（支气管收缩，增加血管通透性，和粘液分泌压制推广）。基于这种作用机理，孟鲁司特作为抗哮喘作用，改善哮喘炎症的各种因素。
2.过敏性鼻炎
在过敏性鼻炎，抗原激发后，半胱氨酰白三烯从鼻粘膜中任何立即相和Osohatsusho的释放。其释放与过敏性鼻炎的症状。此外，白三烯胱鼻内给药增加了鼻气流阻力，已经显示出恶化鼻闭症状。孟鲁司特通过阻断白三烯受体的作用，已经建议在缓解过敏性鼻炎的症状可发挥重要的作用。
LT受体拮抗剂（受体结合试验）
受容体結合試験（モルモット肺細胞膜、U937細胞膜及びTHP-1細胞膜）で、LTD4の受容体結合を強力に阻害し、その作用は血液成分による影響を受けなかった。LTC4及びLTB4に対する受容体拮抗作用は弱かった。
支气管收缩抑制作用（孤立的器官和动物研究）
LTD4在豚鼠离体气管收缩是竞争性抑制。此外，它表现出对豚鼠和松鼠猴LTD4引起的支气管收缩反应强烈和持久的抑制作用。另一方面，孟鲁司特没抑制LTC 4（即抑制LTC 4的代谢条件）的切除的组织的收缩。此外，使用豚鼠，花生四烯酸，支气管收缩羟色胺和乙酰胆碱诱导的组胺难以抑制。
由抗原诱导的支气管收缩的抑制动作
哮喘大鼠致敏，由抗原诱导的豚鼠和松鼠猴支气管收缩反应是由静脉注射和口服给药抑制。在临床试验中海外，75％直接与抗原施用和晚期的支气管收缩，分别为57％的抑制。
对速发型和迟发型反应的支气管收缩抑制作用
由抗原诱导致敏松鼠猴的直接和延迟的支气管收缩反应通过口服给药抑制。
针对过敏性休克的抑制作用
过敏性休克是由于致敏豚鼠卵白蛋白部分抑制。
鼻气流阻力增加（鼻塞）通过抗原诱导的抑制效果
使用致敏豚鼠，在鼻气流阻力的增加引起的卵清蛋白吸入（鼻塞），孟鲁司特1和3毫克/公斤（腹腔给药）为55％，分别表现出85％的抑制作用。
改善肺功能的作用
在慢性支气管哮喘患者轻至中度，并在1秒内提高音量和呼气峰流速。
嗜酸性粒细胞上的作用
在慢性支气管哮喘患者轻，中度，有人显著与痰安慰剂嗜酸性粒细胞比例相比减少。同样，成年人，外周血嗜酸细胞比例也显著在儿科患者减少了。
适应病症
支气管哮喘，过敏性鼻炎
用法用量
<支气管哮喘>
成人每天口服1次（睡前），每次10毫克。
<过敏性鼻炎>
成人每天口服1次（睡前），每次5毫克-10毫克。
包装规格
片：5mg
PTP包装：28片（14片×2），100片（10片×10），140片（14片×10）
片：10mg
PTP包装：28片（14片×2），100片（10片×10），140片（14片×10），420片（14片×30），500片（10片×50）

生产商
杏林药业
注：上面部份中文资料仅参考，使用以原处方为准：http://www.kegg.jp/medicus-bin/japic_med?japic_code=00065801
KIPRES Tablets(Montelukast Sodium)
KIPRES Tablets5mg（キプレス錠5mg）
Brand name : KIPRES Tablets5mg
　Active ingredient: Montelukast sodium
　Dosage form: bright grayish yellow tablet, major axis 7.6mm, minor axis 5.6mm, 2.9mm thick
　Print on wrapping:(face)キプレス錠5mg キプレス5 喘息・鼻炎（成人用）
(reverse side)KIPRES Tab.5, キプレス錠5mg, KP-374
KIPRES Tablets10mg（キプレス錠10mg）
Brand name : KIPRES Tablets10mg
　Active ingredient: Montelukast sodium
　Dosage form: bright grayish yellow tablet, diameter: 8.0mm, 4.1mm thick
　Print on wrapping:(face)キプレス錠10mg(reverse side)KIPRES Tab.10mg, キプレス錠10mg, KP-372
Brand name : KIPRES Tablets10mg
　Active ingredient: Montelukast sodium
　Dosage form: bright grayish yellow tablet, diameter: 8.0mm, 4.1mm thick
　Print on wrapping: (face)キプレス錠10mg (reverse side)KIPRES Tab.10mg, キプレス錠10mg, KP-372
Effects of this medicine
This medicine controls the contraction of bronchi by suppressing the leukotriene action. It helps prevent onset of coughs/wheezing/respiratory distress due to bronchial asthma. Also, it controls nasal ventilation resistance, etc. and improves symptoms of nasal obstruction/nasal discharge/sneezing due to allergic rhinitis.
It is usually used to treat bronchial asthma and allergic rhinitis in preventing purpose. For bronchial asthma, it cannot stop the asthma attack that is already taking place. Use other medicine to stop already occurring attacks.
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 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 bronchial asthma: In general, for adults, take 1 tablet (10 mg of montelukast) at a time, once a day at bedtime.
For allergic rhinitis: In general, for adults, take 5 to 10 mg of montelukast at a time, once a day at bedtime.
This medicine contains 10 mg of montelukast. In any cases, strictly follow the instructions of your doctor and pharmacist.
•If you miss a dose, take a dose as soon as possible. If it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. 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
• Possible adverse reactions to this medicine
The most commonly reported adverse reactions include diarrhea, stomachache, nausea, heartburn, headache, hepatic function abnormal, dry mouth, somnolence, gastric discomfort, fatigue, rash and pruritus. 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.
•cold sweat, pale face, respiratory distress [anaphylaxis]
•respiratory distress, swollen face/tongue/throat [angioedema]
•loss of appetite, general fatigue, yellowing of the skin/eyes [fulminant hepatitis, hepatitis, liver dysfunction, jaundice]
•fever, red-eye, rash/red-spots/fluid-filled blisters appear on skin/mucosa [toxic epidermal necrolysis, mucocutaneous ocular syndrome, erythema multiforme]
•bleeding from the nose/gums, bleeding under skin seen in limbs [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 the reach of children. Store away from light, heat and moisture.
•Discard the remainder. Do not store them.
Kyorin Pharmacetical Co.,LtdInternal
Revised: 2/2015
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.