部份中文醋酸去氨加压素处方资料（仅供参考）
商品名：DESMOPRESSIN・Spray
英文名：Desmopressin Acetate Hydrate
中文名：醋酸去氨加压素水合物
生产商：协和发酵麒麟制药
デスモプレシン・スプレー10協和
药用类别名称
中枢性尿崩症用剤
批准日期：2003年6月
欧文商標名
DESMOPRESSIN・Spray 10 Kyowa
一般名
デスモプレシン酢酸塩水和物 Desmopressin Acetate Hydrate
化学名
1-Deamino-8-D-arginine-vasopressin acetate trihydrate
略名
DDAVP
分子式
C46H64N14O12S2・C2H4O2・3H2O＝1183.31
構造式
性状
它是一种白色粉末。
溶解度
溶于水、甲醇或醋酸(100), 难以溶于乙醇(99.5)。
组成
绝望喷雾10京华包含以下成分在一个瓶子5mL。
活性成分
醋酸盐水合物--500μg
添加剂
氯化苯并呋喃溶液、太阳站氯化钠、太阳站柠檬酸水合物、磷酸氢二钠
药用药理学
1. 抗利尿活性
在大鼠中施用蒸馏水25Ml/kg 后, 皮下给药剂量, 在剂量后5小时内测定尿量, 在 0.1 ng kg 或更多时增加剂量的尿量减少。
2. 作用机制
(1) 对加压素V2受体的影响
血管加压素V1在大鼠的目前的代理, 结合亲和力的V2受体和催产素受体(Ki)分别为1748, 1.04, 481nmol/L, 血管加压素 V2 受体表现出选择性结合亲和力(Ki-1.04 Nmole/l)。与麝香碱受体(M1、M2、M3)的结合亲和力几乎没有观察到 (Ki >1x105nmoll)。
(2) 提高水和尿素渗透性
在离体金仓鼠肾髓质内层组装管中, 水和尿素从流明膜侧到基膜侧的渗透性, 分别为0.01 nmol或更多, 浓度大于0.1nmol/L。
适应症
夜尿症
用法与用量
继泌尿系渗透压或尿底比重降低引起的疾病后
遗尿
通常, 睡前每天开始给鼻腔服用一次, 如去甲酯, 如果效果不足, 可增加至20μg(2次喷施), 即在睡前一天一次作为去甲酯醋酸盐。
此外, 1天的最大剂量为 20μg(2次喷雾) 作为酸性盐水合物的脱硫剂。
临床结果
夜间尿(平均尿渗透压力*800momsml 或平均尿距离重力*1.02) 的尿液在第二天早上醒来的夜间尿液, 在双盲比较测试与安慰剂作为控制药物, 年龄8.9±1.8岁 (平均±标准偏差), 年龄范围6至14岁儿童夜间尿液天数的减少是制剂平均±4.1天标准偏差为4.3±4.1天, 因为安慰剂为1.7±3.1天, 经确认, 与安慰剂相比, 该制剂可显著减少夜间尿液数量(p < 0.001)。该制剂的副作用发生率为10.5% (8/76 例), 安慰剂为15.8% (12/76 例), 两组间差异显著。(P=0.472)
包装
1瓶
製造和銷售來源
协和发酵麒麟制药
注：以上中文不够完整，使用者以原处方资料为准。
完整说明附件：http://www.info.pmda.go.jp/go/pack/2419700R2029_1_14/
DESMOPRESSIN Spray（Desmopressin acetate hydrate）
DESMOPRESSIN・Spray 10 Kyowa（デスモプレシン・スプレー10協和）
Brand name : DESMOPRESSIN・Spray 10 Kyowa
　Active ingredient: Desmopressin acetate hydrate
　Dosage form: nasal spray
Effects of this medicine
This medicine has the same action as "vasopressin", an antidiuretic hormone to control urine volume, secreted from pituitary gland in the brain. It is a nasal spray which promotes reabsorption of water in renal tubule of the kidney to concentrate urine and consequently prevents excessive urination.
It is usually used in the treatment of central diabetes insipidus.
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: hypertension, coronary artery thrombosis, angina pectoris, anterior pituitary dysfunction or nasal disease (including its history).
•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 children, use 1 to 2 sprays (2.5-5 mcg of the active ingredient); for adults, use 2 to 4 sprays (5-10 mcg) into nostril at a time, once to twice daily. The dosage may be adjusted according to the amount of water ingestion, urinary volume, specific gravity of urine and urine osmolality. Strictly follow the instructions.
•When the bottle of the medicine is used for the first time or it has not been used for more than a week, press the pump several times (approx. 4 times) and make sure that the medicine is sprayed in the form of a mist. Blow your nose before using to stabilize absorption of the medicine. In using, make sure that the end of the tube inside the bottle is placed in the liquid and spray at one push. According to the instruction in another sheet supplied with the medicine (the instruction is written only in Japanese), try to use the medicine faster and more accurately.
•If you missed a dose, use a dose as soon as possible. If you instructed to use the medicine twice daily, wait approx. 6 hours to use the next dose. You should never use two doses at one time.
•If you accidentally used more than your prescribed dose, consult with your doctor or pharmacist.
•Do not stop using this medicine unless your doctor instructs you to do so.
Precautions while taking this medicine
•Be aware of the amount of water ingestion to avoid excessive intake.
•Severe dehydration may occur in infants who cannot take water on their own. Make sure to let them drink a proper amount of water on a daily basis.
•If you have rhinitis or injury in nose, and it is difficult to use the medicine, consult with your doctor or pharmacist immediately.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include headache, loss of appetite, nausea, vomiting, facial edema, abdominal pain, nasal bleeding, fever, insomnia, somnolence and nasal discomfort. 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.
•malaise, headache, nausea [water intoxication]
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. Avoid freezing and store in a refrigerator, and keep the bottle at a standing position.
•When you carry the medicine with you, put the bottle in a package and keep the bottle at a standing position in a bag (if you put it in your pocket, the medicine may leak out due to warming by your body temperature).
•When you go on a tour and carry the medicine with you, avoid keeping it at a high temperature and keep it at a stable temperature.
•Discard the remainder. Do not store them. Ask the pharmacist how to discard them.
Kyowa Hakko Kirin Co.,LtdExternal
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.