部份中文磷酸西他列汀处方资料（仅供参考）
英文名：Sitagliptin Phosphate Hydrate 
商標名：JANUVIA Tablets
中文名：磷酸西他列汀片
生产商：默克制药
产品简介
Januvia是DPP-4抑制剂类药物中首种获批准的药物。磷酸西他列汀作用特点是在刺激胰岛素分泌的同时，能减轻饥饿感，而且不会使体重增加，也不会发生低血糖和水肿现象，适合血糖控制不好且经常发生低血糖的糖尿病患者使用。
ジャヌビア錠12.5mg／ジャヌビア錠25mg／ジャヌビア錠50mg／ジャヌビア錠100mg
药效分类名称
选择性DPP-4抑制剂
◎糖尿病药物◎
批准日期：2013年 11月
商品名
JANUVIA Tablets
一般的名称
シタグリプチンリン酸塩水和物（Sitagliptin Phosphate Hydrate）
化学名
(3R)-3-Amino-1-[3-(trifluoromethyl)-5,6-dihydro[1, 2, 4] triazolo [4, 3-α]pyrazin-7(8H)-yl]-4-(2, 4, 5-trifluorophenyl)butan-1-one monophosphate monohydrate
分子式
C16H15F6N5O・H3PO4・H2O
分子量
523.32
化学構造式
性状
本产品为白色粉末。 该产品微溶于水，微溶于甲醇，微溶于乙腈或乙醇（99.5）。
药效药理
作用机理
肠降血糖素胰高血糖素样肽1（GLP-1）和葡萄糖依赖性促胰岛素多肽（GIP）是参与维持葡萄糖稳态的激素。西他列汀抑制DPP-4酶并抑制DPP-4对肠降血糖素的降解。通过增加活性肠降血糖素浓度，以血糖水平依赖性方式增强胰岛素促促促分泌素作用和降低胰高血糖素浓度的作用，以改善血糖控制。
人类DPP-4抑制作用
它选择性地抑制人DPP-4（重组，血清来源，CACO-2细胞来源）的活性（体外）。
葡萄糖耐量和改善葡萄糖代谢的作用
在2型糖尿病患者中，该药物抑制DPP-4活性，使活性GLP-1和GIP的血浆水平提高约2倍，使血清中的胰岛素和C肽水平升高，并升高胰高血糖素水平，从而导致血糖​​降低，降低空腹血糖水平以及抑制口服葡萄糖负荷后餐后或餐后高血糖。
在使用正常小鼠进行的葡萄糖耐量试验中，该药物抑制了血糖水平的升高。此时，观察到血浆中DPP-4的抑制和血浆中GLP-1浓度的增加。
在高负荷饮食导致肥胖，高血糖和高胰岛素血症并显示葡萄糖耐量降低的饮食负荷型肥胖小鼠（DIO小鼠）中，该药物以与正常水平相同的程度抑制了由于葡萄糖负荷引起的血糖水平升高老鼠.
在以胰岛素抵抗和高血糖为特征的2型糖尿病模型的db/db小鼠中，该药物将血糖水平正常化至与正常小鼠相同的水平。
适应症
2型糖尿病
用法用量：
成人通常的剂量是每天口服一次口服西他列汀50mg。 如果效果不佳，可以每天一次剂量增加至100mg，同时仔细观察病程。
包装规格
片
12.5毫克：
PTP 100片（10片×10）140片（14粒×10）500片（10片×50）瓶100粒
25mg：
PTP 100片（10片×10）140片（14粒×10）500片（10片×50）瓶100粒
50毫克：
PTP 100片（10片×10）140片（14粒×10）500片（10片×50）700片（14粒×50）瓶500粒
100毫克：
PTP 100片（10片×10）140片（14粒×10）500片（10片×50）瓶500粒
制造厂商
MSD有限公司
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/3969010F1034_2_31/?view=frame&style=XML&lang=ja
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JANUVIA Tablets(Sitagliptin Phosphate Hydrate ジャヌビア錠25mg)
JANUVIA Tablets 25mg（ジャヌビア錠25mg）
Brand name : JANUVIA Tablets 25mg
　Active ingredient: Sitagliptin phosphate hydrate
　Dosage form: pale reddish yellow tablet, major axis: 9.1 mm, minor axis:3.8 mm, thickness: 2.5 mm
　Print on wrapping: JANUVIA 25mg, ジャヌビア25mg, MSD 221 
Effects of this medicine
This medicine inhibits enzyme that degrades incretin, blood glucose stabilizing substance. It consequently enhances insulinotropic action and effect of lowering glucagon level in state of hyperglycemia to improve blood glucose control.
It is usually used to treat type 2 diabetes.
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 stage, type 1 diabetes, infection, injury, renal dysfunction, pituitary gland disorder, adrenal gland disorder, insufficient diet, a history of abdominal surgery or intestinal obstruction.
If you are in pre/postoperative period or debilitated.
If you exercise intensely or drink a lot of alcohol.
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 patients with normal renal function or mild renal dysfunction : In general, for adults, take 50 mg of sitagliptin at a time, once a day. If the dose seems to be insufficient, it may be increased up to 1 tablet (100 mg) at a time, once a day, adequately monitoring the condition.
For patients with moderate renal dysfunction : In general, for adults, take 25 mg of sitagliptin at a time, once a day. If the dose seems to be insufficient, it may be increased up to 50 mg at a time, once a day, adequately monitoring the condition.
For patients with severe or end stage renal dysfunction : In general, for adults, take 12.5 mg of sitagliptin at a time, once a day. If the dose seems to be insufficient, it may be increased up to 25 mg at a time, once a day, adequately monitoring the condition.
This medicine contains 100 mg of sitagliptin per a tablet. In either case, strictly follow the instructions.
If you miss a dose, take the missed 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
Strictly follow diet and exercise therapy instructed by your doctor.
The medicine may cause hypoglycemic symptoms. Pay attention when you work at heights, drive a car or operate dangerous machinery.
?In case hypoglycemic symptoms occurs, take food or drink that contains enough amount of sugar (sugar, glucose, refreshing drink, etc.).If you are taking the medicine concomitantly with an α-glucosidase inhibitor (medicines which delay absorption of sugar), ingest glucose in case of any hypoglycemic symptoms occur.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include hypoglycemia and constipation. 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.
?breathing difficulty, hives, swelling around eyes and lips [anaphylactic reaction]
fever, erythema, bloodshot eyes [Stevens-Johnson syndrome, dermatitis exfoliativa]
chills, craving for food, tremor in limbs [hypoglycemia]
loss of appetite, general malaise, yellowness in skin or conjunctiva [hepatic dysfunction, jaundice]
decreased urine output, general edema, malaise [acute renal failure]
severe pain in the upper abdomen, back pain, nausea [acute pancreatitis]
fever, dry cough, breathing difficulty [interstitial pneumonia]
failure of passing stool, stomach ache, abdominal bloating [intestinal obstruction]
pain of the limb muscle, stiffness, numbness [rhabdomyolysis]
continuous bleeding, blue spot, subcutaneous bleeding [thrombopenia]
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.
MSD K.K.Internal
Revised: 3/2015
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.