部份中文地诺单抗处方资料（仅供参考）
商品名：PRALIA
英文名：Denosumab(Genetical Recombination)
中文名：地诺单抗重组注射器
生产商：第一三共制药
药品介绍
2013年6月，第一三共推出PRALIA皮下注射60mg注射器（PRALIA，subcutaneous injection 60mg syringe）。
プラリア皮下注60mgシリンジ
药用类别名称
人抗RANKL单克隆抗体制剂
批准日期：2013年5月
商標名
PRALIA SUBCUTANEOUS INJECTION SYRINGE
一般名：
一般名
デノスマブ(遺伝子組換え)
Denosumab(Genetical Recombination)
本質
重组抗nf-b激活受体配体(抗 rankl)是一种人IgG2单克隆抗体, 由CHO细胞转染, 编码轻链和重链。它是由448氨基酸残基(γ-2链)和由215个氨基酸残基组成的轻链(链)2分子组成的糖蛋白。
分子量
約150,000
批准条件
制定药品风险管理计划并加以实施。
药用药理学
Denosumab是一种人型IgG2单克隆抗体, 与人RANKL结合具有奇异性和高亲和力。
1. 抑制骨吸收
当去花糖对天鹅单皮给药时, 尿i型胶原蛋白交联n-恐怖肽是骨吸收标志物降低。此外, 在给药期间, 反复皮下给药, 尿i型胶原蛋白交联n-恐怖肽持续减少。
2. 对骨密度的影响
每周一次在剂量的denosumab重组小鼠(人RANKL 敲定鼠标) 被表达嵌合RANKL denosumab结合到10mgg/公斤, 3周反复皮下给药, 血清TRAP5b浓度是骨吸收标志物显著降低, 骨密度增加。 此外, 每月一次在剂量的 denosumab 25或50mgkg 到卵巢切除的巨细胞, 当反复皮下注射 16个月, 骨密度和骨强度松质骨和皮质骨增加, 观察到骨质量和骨强度正相关。
3. 对骨折愈合的影响
人 RANKL 敲不入小鼠每周两次股闭合性骨折脱田膜, 剂量为10mgkg, 21或42天反复皮下注射, 临时骨的重塑延迟, 但骨折部位的骨强度没有降低。
4. 对关节炎的影响
大鼠关节炎模型动物, 骨蛋白是一个替代分子的去甲免疫球蛋白结晶片段(OPG-Fc)在2天内3mgkg在关节炎的发作后, 在服用5次, 它不影响脚踝的炎症, 观察到踝关节组织提取物中骨密度的增加以及破骨细胞的数量、血清和TRAP5b浓度的降低。
5. 作用机制
RANKL是作为膜结合或可溶性类型存在的, 通过RANK音符形成破骨细胞是一种受体表达在破骨细胞表面, 其祖细胞控制骨吸收, 功能和生存, 它是必要的蛋白质来调节。德诺苏马通过抑制破骨细胞的形成来抑制RANK/RANKL途径并抑制骨吸收。因此, 为了增加皮质骨和松质骨的骨量, 相信可以增强骨的强度。
注)RARK: 核工厂-b的受体激活剂
适应症
1. 骨质疏松症
2. 抑制类风湿性关节炎引起的骨侵蚀的进展
用法与用量
1. 骨质疏松症
通常情况下, 成人不相体(重组)60mg 一次, 6个月, 皮下注射。
2. 抑制类风湿性关节炎引起的骨侵蚀的进展
通常情况下, 成人不相体(重组)60mg 一次, 6个月, 皮下注射。此外, 在6个月一次的给药中, 当观察到骨侵蚀的进展时, 三个月一次, 就可以皮下注射。
包装
注射器
60毫克注射器 (1mL) 1瓶
制造和销售来源
第一三共
提携
AMGEN
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/3999435G1023_1_08/
PRALIA Subcutaneous Injection 60mg Syringe（プラリア皮下注60mgシリンジ）
Brand name : PRALIA Subcutaneous Injection 60mg Syringe
　Active ingredient: Denosumab (genetical recombination)
　Dosage form: injection
　Print on wrapping:
Effects of this medicine
This medicine is anti-RANKL antibody which inhibits bone loss and increases bone density to prevent bone fracture.
It is usually used to treat osteoporosis.
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 an allergy to natural rubber (latex), hypocalcemia, renal disorder or a potential to develop hypocalcemia.
•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, administer by subcutaneous injection once every 6 months. It may be administered over a long period according to your response to the treatment.
Precautions while taking this medicine
•Necrosis/osteomyelitis of the jaw bone may occur in the patients who are taking medicines for bone lesion including this medicine or similar drugs (Bisphosphonate). These adverse reactions often related to dental treatment such as tooth extraction. Receive adequate explanation about the following points from your doctor or pharmacist.
(1) Receive dental checkup as needed, and if possible, receive dental treatment such as tooth extraction prior to taking the medicine, after consultation with your doctor.
(2) Maintain your oral hygiene by brushing your teeth while taking this medicine.
(3) Receive dental checkup regularly while taking the medicine.
(4) Inform your dentist that you are taking the medicine when you see a dentist.
(5) Avoid any treatments such as tooth extraction while taking the medicine.
If abnormalities in teeth/jaw (jaw pain, loose teeth or swollen gums) occur, see a dentist/oral surgery specialist immediately.
•In order to prevent hypocalcemia, ingest calcium and vitamin D everyday under the instruction of your doctor. If you have difficulty in taking them orally, consult with your doctor.
•Since hypocalcemia may occur without any symptoms, frequent blood test is needed. Keep blood test schedule under the instruction of your doctor.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include hypocalcemia, back pain, hypertension, eczema or joint pain. 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.
•shaking limbs, muscular weakness, convulsion, numbness, arrhythmia [hypocalcemia]
•oral pain, swelling of mouth, redness, loose teeth, numbness of jaw, heavy feeling in jaw, fever, loss of appetite[necrosis of the jaw bone, osteomyelitis of the jaw]
•hoarse voice, swelling around eyes/lips, hives, impaired judgment, palpitation, shortness of breath, breathing difficulty, dullness, impaired mind, hot flush, decreased consciousness, lightheadedness[anaphylaxis]
•pain of thigh or inguinal region [atypical subtrochanteric and diaphyseal femoral fractures]
•chill, high fever, redness with local pain and fever [serious skin infection]
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.
DAIICHI SANKYO COMPANY, LIMITEDInjection
Revised: 1/2014
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.