| 简介：
部分中文吡格列酮盐酸盐/格列美脲处方资料（仅供参考）
英文名：Pioglitazone Hydrochloride/Glimepiride
商品名：SONIAS Combination Tablets
中文名：吡格列酮盐酸盐/格列美脲配合錠
生产商：武田制药
ソニアス配合錠LD／ソニアス配合錠HD
药用类别名称
噻唑烷基异丙基药物制剂
—2型糖尿病治疗—
批准日期：2011年3月
商標名
SONIAS Combination Tablets LD
SONIAS Combination Tablets HD
盐酸吡格列酮
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
盐酸吡格列酮是一种白色结晶或结晶性粉末。N, 易溶于n-二甲基甲酰胺或甲醇, 几乎不溶于乙醇 (99.5), 不易溶于水。 它融化成0.1 moll盐酸检测溶液。N, n-二甲基甲酰胺溶液(1→20) 不具有光转特性。
格列美脲
化学構造式
一般名
グリメピリド（Glimepiride）〔JAN〕
化学名
1-(4-｛2-［（3-Ethyl-4-methyl-2-oxo-3-pyrroline-1-carbonyl）amino］ethyl｝phenylsulfonyl)-3-（trans-4-methylcyclohexyl）urea
分子式
C24H34N4O5S
分子量
490.62
融点
約202℃（分解）
性状
格列美脲是一种白色结晶性粉末。 几乎不溶于二氯甲烷, 很难溶于甲醇或乙醇 (99.5), 几乎不溶于水。
药用药理学
吡格列酮
(1) 行动机制
吡格列酮通过作用后, 胰岛素结合部分的胰岛素受体, 抑制糖的生产在肝脏, 以减少糖在外周组织中的使用, 以增加血糖, 减少胰岛素抵抗。这种作用被认为是由于细胞内胰岛素信号转导机制正常化, 是胰岛素抵抗的一个主要原因。
(2) 改善胰岛素抵抗的效果
1) 有胰岛素抵抗, 给予吡格列酮对扎克脂肪大鼠是Wistar脂肪大鼠和肥胖型糖尿病14天, 经空腹20小时后给予胰岛素, 观察胰岛素给药后血糖减少的增加。
2) 为了增加胰岛素刺激过程中的糖分, 对KKAy小鼠横隔膜脂肪组织的总脂肪分数和睾丸下脂肪组织的糖的吸收是肥胖型糖尿病。
3) 抑制 Wistar 脂肪大鼠肝脏产生糖分, 这是一种肥胖糖尿病, 以增加糖在周围组织中的使用。
(3) 提高外周组织中的胰岛素活性
在宽星脂肪大鼠后单侧肌肉中, 胰岛素 (糖原合成和糖酵解增强作用) 的作用增强 (体外)。此外, 在脂肪组织Wistar脂肪大鼠周围的离体脂肪细胞中, 胰岛素(葡萄糖氧化和总脂合成增强作用) 的作用得到增强 (体外)。
(4) 增加肝脏中的胰岛素活性
在 Wistar脂肪大鼠中, 为提高肝脏中葡萄糖激酶的活性, 降低葡萄糖-6-磷酸酶的活性, 抑制了糖的产生(体内)。
(5) 增强胰岛素受体的作用
在宽星脂肪大鼠骨骼肌中, 为使减少的胰岛素受体和胰岛素受体底物的磷酸化正常化, 增强了磷脂酰丝琳-3激酶(体内) 的活性。
(6) tnf-Α生产的抑制作用
为了抑制Wistar脂肪大鼠骨骼肌TNF-α的产量增加, 同时降低高血糖(体内)。
(7) 糖代谢改善作用
1) 饮食, 除了运动治疗中的双盲比较试验中进行30毫克12周, 结合2型糖尿病患者使用磺酰脲剂1天吡格列酮, 空腹血糖, 降低HbA1c, 增加1, 5-AG, 观察到血液胰岛素的降低。
2) 在肥胖的2型糖尿病模型动物与胰岛素抵抗 (KKAy 小鼠, Wistar脂肪大鼠), 以减少高血糖和高胰岛素血症。另一方面, 1型糖尿病模型动物 (链霉素糖尿病大鼠) 胰岛素缺乏、正常大鼠 (Sprague-Dawley大鼠) 正常血糖没有表现出这种作用。
(8) 提高糖分耐受性的措施
在 Wistar脂肪大鼠和糖耐量的Zucker脂肪大鼠中给予10~12天的胰岛素抵抗, 经20分钟禁食后口服葡萄糖, 观察葡萄糖给药后血糖升高的抑制和胰岛素分泌的减少。
格列美脲
(1) 作用机制
Grimepido 主要通过刺激胰腺β细胞 (胰腺作用) 促进内源性胰岛素分泌, 被认为表达了降血糖作用。 此外, 在体外试验中还显示了糖转运载体的活化参与。
(2) 降血糖作用与胰岛素分泌
1) 在早餐前给9例健康成年男性服用单剂甘美皮多1mg 时, 与安慰剂给药时间相比, 早餐后血糖浓度显著降低。 此时cmax血清胰岛素浓度, 但在Grimepido给药时与安慰剂给药时没有明显差异, 与安慰剂给药时间相比, 早餐后4小时的 AUC 显著增加。
2) 家兔, 大鼠, 在口服给药试验使用狗, 观察格里梅皮多的血糖作用从1小时后给药。与Griben酰De相比, 显示出相同或更多的降血糖效果。
(3) 增强胰岛素作用
在使用人工胰岛的犬正常血糖胰岛素夹紧试验中, 观察到Grimepido给药促进外周组织糖的吸收, 肝糖治疗能力增加。 此外, 格里美比通过长期口服胰岛素抵抗KKAy小鼠, 以改善高血糖和高胰岛素血症。
已报告了利用肌肉和脂肪组织进行的体外研究、胰腺外部活动通过增加激活和糖转运载体的糖转运等机制的参与。
适应症
2型糖尿病
然而, 只有当治疗的吡格列酮盐酸和石丙二胺酮的组合被认为是适当的。
用法与用量
通常, 成人一片片每天一次(15mgsg或 30mgmg作为pioglitoneone/grimepido) 在早餐后或早餐后口服。
临床结果
对于2型糖尿病患者使用Grimepido, 15mgmg复合片(31例)或30mgmg 混合片(31例) 作为一天一次吡格列酮而不是Grimepido, 因为口服8周前或早餐后, 与HbA1c和空腹血糖水平前相比, 两组均有显著差异。
包装
LD: 100 片 (10 片 x10), 140 片 (14 片 x10)
HD: 100 片 (10 片 x10), 140 片 (14 片 x10)
制造商和分销商
武田特瓦制药有限公司
注：以上中文处方资料不够完整，使用者以原处方资料为准。
完整说明书附件：http://www.info.pmda.go.jp/go/pack/3969101F1025_2_02/
SONIAS Combination Tablets HD(Pioglitazone Hydrochloride/Glimepiride)
Brand name :
SONIAS Combination Tablets HD
Active ingredient:
Pioglitazone hydrochloride
Glimepiride
Dosage form:
white to yellowish white and reddish white, double-layered tablets, diameter: 8.1 mm, thickness: 3.3 mm
Print on wrapping:
(Face) ソニアスHD, (Back) ソニアスHD 324
Effects of this medicine
This medicine improves hyperglycemia by stimulating insulin secretion in the pancreas and by enhancing the systemic action of insulin.
It is usually used to treat type 2 diabetes mellitus.
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 a heart disease or a history of heart disease, ketosis, diabetic coma or precoma, type 1 diabetes mellitus, liver disorder, renal disorder or severe infection; are in a pre- or post-operative state; have an injury, gastrointestinal disorders such as diarrhea/vomiting, pituitary abnormality, adrenal disorder, inadequate food intake or debility; are doing strenuous physical exercise or a heavy drinker; have a bladder cancer/a history of bladder cancer or diabetic retinopathy.
If you are pregnant, possibly 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))
In general, for adults, take 1 tablet at a time, once a day, before or after breakfast. Strictly follow the instructions.
If you miss a dose, skip the missed dose and follow 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
Strictly follow the instructions on dietary/exercise therapy.
This medicine may cause hypoglycemia. Pay close attention when working at heights or operating dangerous machinery such as driving a car. Make sure to tell your family and persons around you that you are taking this medicine.
When hypoglycemia symptoms occur, take an adequate amount of sugar (e.g., sugar, glucose, soft drinks). If you are taking this medicine concomitantly with an α-glucosidase inhibitor (medicines which delay absorption of sugar such as voglibose and acarbose), ingest glucose in case of any hypoglycemic symptoms.
Increase in the potential risk of developing bladder cancer in patients taking this medicine cannot be completely denied. Therefore, patients taking this medicine are followed by periodic urinary tests, etc. If bloody urine, frequent urination, painful urination, etc. appear, consult with your doctor.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include hypoglycaemia, hypoglycaemia-like symptoms, anemia, blood pressure rising, palpitation, pressure in chest, facial flush, rash, itching, nausea, vomiting, epigastralgia, gastric distress, heartburn, abdominal pain, abdominal enlarged feeling, diarrhea, constipation, bulimia, loss of appetite, dizziness, light headedness, headache, sleepiness, malaise, lassitude, numbness, increased body weight, aggravation of diabetic retinopathy, shortness of breath, solar sensitiveness, depilation, vision disturbance and taste abnormality. 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.
edema, rapid increase in body weight, shortness of breath, palpitation [heart or cardiac failure]
consciousness disorder, lassitude, cold sweat, a sense of hunger, shivering of limbs [hypoglycaemia]
edema, rapid increase in body weight [edema]
loss of appetite, yellowing of the skin and the white of eyes [liver disorder/jaundice]
fever, general malaise, sore throat, red-brown urine [hemolytic anemia, agranulocytosis, pancytopenia]
lassitude, muscle pain, brown urine [rhabdomyolysis]
pain in the pit of the stomach, nausea, black stool [relapse of gastric ulcer]
fever, cough, respiratory distress [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 reach of children. Store away from direct sunlight, heat and moisture.
Discard the remainder. Do not store them.
Internal
Revised: 6/2017
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. |
