英文药名：ACTOS OD Tablets（Pioglitazone hydrochloride）

中文药名：盐酸吡格列酮口腔崩解片

生产厂家：武田制药

アクトスOD錠15／アクトスOD錠30

治疗类别名称
胰岛素抵抗性改善剂
-2型糖尿病治疗药物-
商標名
ACTOS OD Tablets
化学構造式

一般名
ピオグリタゾン塩酸塩（Pioglitazone Hydrochloride）〔JAN〕
化学名
（5RS）-5-｛4-［2-（5-Ethylpyridin-2-yl）ethoxy］benzyl｝thiazolidine-2, 4-dione monohydrochloride
分子式
C19H20N2O3S・HCl
分子量
392.90
融点
193℃（分解点）
性状
吡格列酮盐酸盐是一种白色结晶性或结晶性粉末。 N，易溶略N-二甲基甲酰胺或甲醇，微溶于乙醇（99.5），并且几乎不溶于水。易溶于0.1mol/L的盐酸测试解决方案。 N，N-二甲基甲酰胺溶液（1→20）示出了没有旋光性。
适应病症
2型糖尿病
（1）仅当不能在任何以下的处理而得到的胰岛素抵抗性充分的效果估计。
1）饮食疗法，运动疗法
2）饮食，使用磺酰脲剂除了运动疗法
3）用节食，除了运动疗法α-葡萄糖苷酶抑制剂
4）饮食，除了运动疗法使用双胍类药物
（2）饮食，使用胰岛素制剂，除了运动疗法
用法与用量
1.饮食，在唯一的运动疗法和饮食的情况下，除了使用磺酰脲类或α-葡萄糖苷酶抑制剂或双胍类药物运动疗法。
成人：每天一次，每次口服15-30毫克。此外，性别，年龄，将根据症状进行调整，到最大为45mg的。
2.饮食，如果要使用的胰岛素制剂中除运动疗法
成人：每天一次，每次口服15毫克。此外，性别，年龄，将根据症状进行调整，到最大为30mg。
药效药理
本剂作用于胰岛素的胰岛素受体结合后部分，以降低胰岛素抵抗，抑制葡萄糖产生于肝脏，在周边组织降低血糖升高葡萄糖的利用。这种效应被认为是由于正常化胞内胰岛素信号转导机制，是胰岛素抵抗的主要病因。
(1) 糖代謝改善作用
1) 饮食，在30毫克的双盲对照研究，因为一旦在2型糖尿病患者每天吡格列酮被12周的唯一运动疗法的施用，空腹血糖，糖化血红蛋白降低，1,5-AG的上升被确认。
2) 饮食，在12周的联合给药30毫克的双盲对照研究为每天一次，吡格列酮的患者2型糖尿病患者中，除了使用锻炼治疗磺脲类药物，空腹血糖，中，糖化血红蛋白1降，5-AG，血胰岛素的降低的上升已观察。
3) 饮食，患者的2型糖尿病患者中用于联合16周每天给药30毫克的双盲对照研究中，除了使用伏格列波单个吡格列酮以运动疗法，和空腹血糖，观察到糖化血红蛋白的降低那里。
4) 饮食，12周15毫克作为一次除运动疗法的患者的2型糖尿病中使用二甲双胍，在接着进行16周30毫克，每天吡格列酮联合给药的双盲对照研究，空腹血糖，糖化血红蛋白血统已被观察到。
5) 饮食，在组合16周施用30毫克的双盲对照研究如每天一次吡格列酮在治疗2型糖尿病，同时使用胰岛素制剂除了运动疗法，空腹血糖，糖化血红蛋白的降低观察。
6) 具有胰岛素抵抗的肥胖2型糖尿病的动物模型（KKAy小鼠，Wistar肥鼠），以降低高血糖和高胰岛素血症。另一方面，胰岛素缺乏I型糖尿病动物模型的高血糖（链脲霉素糖尿病大鼠），正常大鼠的正常血糖（Sprague-Dawley大鼠）显示没有影响。
(2) 耐糖能改善作用
有胰岛素抵抗，吡格列酮在Wistar肥鼠和Zucker肥胖大鼠表明葡萄糖耐量受损是为10-12天施用，禁食20小时，血浆葡萄糖增加葡萄糖给药后抑制后口服给予葡萄糖减少胰岛素分泌过多的已被观察到。
(3) 胰岛素抵抗改善作用
1) 节食，只有运动疗法或饮食疗法，在临床药理学研究认为30毫克为12周的患者2型糖尿病患者在使用给药每天一次，吡格列酮与类型除了锻炼治疗磺脲类剂（葡萄糖钳夹技术），外周血增加的组织的葡萄糖摄取和肝脏已经观察。
2) 有胰岛素抵抗，吡格列酮在Zucker肥胖大鼠是Wistar肥鼠和肥胖症是肥胖糖尿病14天施用，空腹20小时后施用胰岛素，观察到增强的降血糖的胰岛素给药后是的。
3) 在KKAy小鼠是肥胖的糖尿病和附睾脂肪组织的总脂肪级分的胰岛素刺激的隔膜的糖原分的时间增加的葡萄糖摄取。
4) 抑制从Wistar肥鼠的肝脏葡萄糖生产是肥胖糖尿病，增加外周组织糖的利用。
(4) 作用机序
1) 在外周组织中增强胰岛素作用
在Wistar肥鼠的后肢比目鱼肌，以增强胰岛素（糖原合成和糖酵解促进效果）（离体）的作用。此外，在从Wistar肥鼠的附睾脂肪组织，分离的脂肪细胞，以提高胰岛素（葡萄糖氧化和总脂质合成促进作用）（离体）的作用。
2) 提高在肝脏胰岛素作用
在Wistar肥鼠，增强在肝脏葡糖激酶的活性，它降低葡萄糖-6-磷酸酶的活性，并抑制葡萄糖产生（体内）。
3) 胰岛素受体作用增强
在Wistar肥鼠的骨骼肌，正常化降低胰岛素受体和胰岛素受体底物的磷酸化，以增强磷脂酰肌醇3-激酶（体内）的活性。
4) TNF-α生成抑制作用
抑制在Wistar肥鼠中发现的骨骼肌的TNF-α增强的产量，在平行与此来降低高血糖（体内）。
包装规格
口腔崩解片
15mg：100片（10片×10），420片（14片×30），500片（10片×50）
30mg：100片（10片×10），420片（14片×30），500片（10片×50）
制造厂商
武田化学工业有限公司

原处方资料附件：http://www.info.pmda.go.jp/go/pack/3969007F3027_2_01/
ACTOS OD Tablets（Pioglitazone hydrochloride）
Brand name : ACTOS OD Tablets 15
　Active ingredient: Pioglitazone hydrochloride
　Dosage form: yellowish white tablets, φ7.1 mm, thickness 2.8 mm
　Print on wrapping: (Face) 376, アクトスOD15, (Back) アクトスOD15
ACTOS OD Tablets 30（アクトスOD錠30）
Brand name : ACTOS OD Tablets 30
　Active ingredient: Pioglitazone hydrochloride
　Dosage form: yellowish white tablets, φ7.1 mm, thickness 2.8 mm
　Print on wrapping: (Face) 377, アクトスOD30, (Back) アクトスOD30
Effects of this medicine
This medicine improves hyperglycemia by enhancing the action of insulin.
Usually, used for treatment of type II diabetes mellitus.
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 a heart disease or a history of heart disease, ketosis, diabetic coma or precoma, insulin-dependent diabetes mellitus, hepatic disorder, renal disorder, or severe infection; are in a pre- or post-operative state; have an injury, pituitary abnormality, adrenal disorder, inadequate food intake, or debility; are doing strenuous physical exercise, or a heavy drinker; or have a bladder cancer or a history of bladder cancer, or diabetic retinopathy.
•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, take 0.5 to 1 tablets (15 to 30 mg of pioglitazone) at a time, once a day, before or after breakfast. The dosage should be adjusted according to your gender, age and symptoms, but 1.5 tablets (45 mg) a day is the upper limit of dosage.
When given concomitantly with an insulin preparation, for adults, take 0.5 tablets (15 mg of pioglitazone) at a time, once a day, before or after breakfast. The dosage should be adjusted according to your gender, age and symptoms, but 1 tablet (30 mg) a day is the upper limit of dosage.
Strictly follow the instructions of your doctor/pharmacist.
•This medicine may be moistened with saliva on the tongue, then lightly squashed with the tongue, and swallowed with saliva. It may also be taken with water like usual drugs.
•If you missed a dose, take the missed dose as soon as possible if prior to noon. As hypoglycemia may occur, do not take the medicine after severe exercise or on an empty stomach. DO NOT take double doses to make up for the missed dose.
•If you took too much of the medicine (more than ordered), check with your doctor/pharmacist.
•Do not stop taking the medicine without the instructions of your doctor.
Precautions while taking this medicine
•Strictly adhere to dietary instructions given and to kinesitherapy prescribed.
•Much caution should be exercised as hypoglycemia may occur.
•When hypoglycemia symptoms occur, take an adequate amount of sugar (e.g., sugar, glucose, soft drinks). If you are taking the medicine concomitantly with an α-glucosidase inhibitor (drugs which delay absorption of sugar such as voglibose and acarbose), ingest glucose in case of any hypoglycemic symptoms.
•Although this drug has not been concluded to cause bladder cancer, there has been a report overseas stating that a potential risk for bladder cancer increases with increasing duration of this drug medication. Therefore, patients receiving this drug are followed by periodic urinary tests, etc. If hematuria, frequent urination, painful micturition, etc. appear, check with your doctor.
Possible adverse reactions to this medicine
Common side effects are reported as below. If any of them occurs, check with your doctor/pharmacist: anemia, increased blood pressure, palpitation, pressurized feeling in the chest, hot flush, rash, itching, nausea, vomiting, abdominal discomfort, heart burn, abdominal pain, enlarged feeling of abdomen, diarrhea, constipation, excessive appetite, loss of appetite, dizziness, light-headedness, headache, sleepiness, malaise, lassitude, numbness, weight increase, aggravation of diabetic retinopathy, shortness of breath, 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.
•swelling, rapid weight increase, shortness of breath, palpitation [heart failure]
•swelling, rapid weight increase [edema]
•loss of appetite, yellowing of the skin or whites of the eyes [liver disorder, jaundice]
•cold sweat, feeling hungry, trembling of hands/feet [hypoglycemia]
•lassitude, muscle pain, brown urine [rhabdomyolysis]
•pain in the pit of stomach, nausea, black stool [relapse of gastric ulcer]
•fever, cough, breathing difficulty [interstitial pneumonia]
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 the reach of children. Store away from direct sunlight, heat and humidity.
•Discard the remainder. Do not store them.
Takeda Chemical Industries, Ltd.Internal
Revised: 7/2011
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.