| 简介：
部份中文托格列净处方资料（仅供参考）
英文名：Tofogliflozin Hydrate
商標名：DEBERZA Tablets
中文名：托格列净片
生产商：興和制药
产品简介
托格列净（Tofogliflozin）于2014年3月24日由日本PMDA批准上市的2型糖尿病药物。该药由中外制药、赛诺菲和兴和共同研发，赛诺菲、兴和分别以商品名Deberza®，Apleway®销售。Deberza®被批准用于治疗2型糖尿病，口服片剂，规格为20mg，推荐使用剂量为每天一次，每次一片。
デベルザ錠20mg
治疗类别名称
-2型糖尿病剂-
选择性SGLT2抑制剂
批准日期：2014年5月
商品名
DEBERZA Tablets 20mg
一般的名称
トホグリフロジン水和物（Tofogliflozin Hydrate）（JAN）
化学名
（1S,3́R,4́S,5́S,6́R）-6-［（4-Ethylphenyl）methyl］-6́-（hydroxymethyl）-3́,4́,5́,6́-tetrahydro-3H-spiro［2-benzofuran-1,2́-pyran］-3́,4́,5́-triol monohydrate
分子式
C22H26O6・H2O
分子量
404.45
性状
它是白色粉末，不吸湿。极易溶于N，N-二甲基乙酰胺，甲醇或乙醇（99.5），微溶于水。
化学構造式
融点
71～92℃
药效药理
1. 作用机序
Tofogliflozin选择性地抑制葡萄糖共转运钠转运-2（钠葡萄糖共转运体2，SGLT2）负责通过肾小球葡萄糖排泄在尿中葡萄糖过滤重吸收通过促进降低血液葡萄糖
2. 药理作用
(1) 在体外抑制活性（Ki值：0.0029μmol/L）针对tofogliflozin的抑制活性人SGLT2（Ki值：6.0μmol/L）对人SGLT1在强2100倍。在另一方面，SGLT2抑制活性的：羧酸是一种主要代谢物tofogliflozin（IC 50值：0.0039μmol/L）的（IC 50值2.7μmol/ L）弱，故1/700。
(2) 在ZDF大鼠tofogliflozin的II型糖尿病模型动物产生为葡萄糖肾排泄清除率值的单次口服给药为每四个小时的每个周期长达12小时相比，溶剂给药组给药是显著更高之后。
(3) 2型糖尿病的动物模型的结果tofogliflozin到GK大鼠单次口服剂量，通过饮食负荷的增加的血糖水平，抑制显著相比，溶剂给药组作为。
(4) 2型糖尿病模型动物的db/db小鼠4周重复口服给药作为tofogliflozin糖化血红蛋白值显著下降相比，溶剂给药组的结果。
(5) 每日一次给药tofogliflozin2.5,5,10,20,40mg2型糖尿病日（国际合作第二阶段），结果12周，最后给药日的第一天，累计尿糖排泄从上届政府的变化量几乎达到20毫克的剂量。另外，HbA1c和空腹血糖的剂量依赖性方式降低。
注）批准了单剂量本剂为20mg（见“用法与用量”）。
适应症：
2型糖尿病。
用法用量：
推荐剂量20mg/天，效果不理想时可以加至40mg/天，早上服用，餐前餐后均可。
包装规格
片
20毫克：PTP：100片、140片（14片×10）、500片、700片（14片×50）[塑料瓶]500片
制造厂商
興和株式会社
注：以中文处方资料不够完整，使用者以原处方资料为准。
完整资料附件：
https://www.info.pmda.go.jp/go/pack/3969021F1032_1_11/
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DEBERZA Tablets 20mg（Tofogliflozin hydrate デベルザ 20mg）
Brand name :DEBERZA Tablets 20mg
Active ingredient:Tofogliflozin hydrate
Dosage form:light yellow tablet with split line (round and scored), diameter: approx. 6.1 mm, thickness: approx. 3.3 mm
Print on wrapping:
デベルザ 20mg, DEBERZA 20 mg, 122, 糖尿病用薬
Effects of this medicine
This medicine lowers blood glucose levels by acting on kidney and promoting the excretion of glucose into urine.
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: ketosis, diabetic coma or precoma, infection or injury.
If you are in the pre-/post-operative period.
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))
In general, for adults, take 20 mg of tofogliflozin once a day, before or after breakfast. Strictly follow the instructions.
If you miss a dose, you should never take two doses at one time. Take the missed dose (one day's worth) as soon as possible. If it is almost time for the next dose, continue your regular dosing schedule.
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
Pay attention especially when you are engaged in dangerous activities such as working at heights and driving a car because development of hypoglycemia during such activities may lead to an accident. Carry a card stating that you are a diabetic patient. Carry sugar or glucose with you in preparation for hypoglycemia. If hypoglycemic symptoms occur while you are taking this medicine concomitantly with an alpha-glucosidase inhibitor (acarbose, voglibose, etc.), take the glucose.
This medicine may cause urinary-tract infection or genital infection. Pay attention and consult with your doctor in the event of onset.
This medicine may cause polyuria or frequent urination, leading to decrease in body fluid volume and dehydration. Try to drink an adequate amount of fluid. Pay attention to excessive decrease in body weight, as body weight may decrease.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include dry mouth and frequent urination. 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.
light-headedness, lassitude, cold sweats, dizziness, headache, palpitation, hunger, shaking of hands and feet [hypoglycemia]
chills, fever, side ache, back pain[pyelonephritis]
redness, pain, swelling, fever and edema in the genital area[necrotizing fasciitis of vulva and perineal area (Fournier's gangrene)]
chills, sudden high fever with the shiver, arthralgia, muscular pain[sepsis]
change in urine volume, malaise, thirst, lassitude, dizziness, dry skin [dehydration]
nausea, vomiting, loss of appetite, abdominal pain, severe dry mouth, malaise, breathing difficulty, lowering of consciousness[ketoacidosis]
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 moisture.
Discard the remainder. Do not store them.
Internal
Revised: 8/2019
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. |
