部份中文氟骨三醇处方资料（仅供参考）
英文名：falecalcitriol
商品名：Flustan Tablets
中文名：氟骨三醇
生产商：大日本住友制药
フルスタン錠0.15／フルスタン錠0.3
治疗类别名称
活性维生素D3制剂
批准日期：2001年6月
商標名
FULSTAN
一般名
ファレカルシトリオール（JAN）
falecalcitriol（JAN、INN）
化学名
(＋)-(5Z,7E)-26,26,26,27,27,27-hexafluoro-9,10-secocholesta-5,7,10(19)-triene-1α,3β,25-triol
構造式
分子式
C27H38F6O3
**分子量
524.58
性状
本品为白色结晶或结晶性粉末, 非常溶于四氢呋喃, 易溶于乙腈或乙醇 (99.5), 不易溶于水。
因热量或光线而异。
熔点
约143°c
药用药理学
该制剂是活性维生素D3的衍生物, 小肠通过与分配给甲状旁腺和骨骼等目标组织的受体结合, 发挥以下作用。
(1) 钙代谢的调节
1) 维生素D缺乏大鼠: 通过静脉注射法拉莱钙素三醇, 促进小肠钙吸收和骨吸收 (骨钙动员) 的作用。
2) 培养骨组织: 法拉尔钙调尿素三醇在小鼠顶骨器官培养系统中表现出促进骨吸收的促进作用。
(2) 慢性肾功能衰竭对继发性甲状旁腺功能亢进的影响
肾功能衰竭病理模型 ('6) 大鼠肾拔毛, 口服法拉莱钙调素三醇, 增加了 PTH 在血液甲状旁腺激素 (PTH) 升高和甲状旁腺中的信使 RNA 表达。此外, 还观察到同种异体骨的增加, 纤维化的骨炎和钙化异常等骨病变的改善。
(3) 对甲状腺功能减退的影响
甲状旁腺大鼠是甲状旁腺功能障碍的病理模型, 口服法莱钙调素三醇, 观察血钙的增加。
(4) 抗枯萎病效果
1) 维生素 D 缺乏磷虾鼠: 通过口服法拉莱钙调尿素三醇, 改善了维生素D缺乏症大鼠的骨灰减少, 抑制了其发病。
2) 低聚血症维生素D耐药小鼠: 在被认为是家族性低血症维生素D耐药枯萎病模型的低钙血症小鼠中, 通过皮下给药法拉莱钙调尿素三醇, 观察到磷浓度的增加。
适应病症
0 维持透析中的继发性甲状旁腺功能亢进
0 改善甲状旁腺功能障碍(不包括肾功能衰竭的人)的低钙血症及相关症状(TECNY、抽筋、麻木、感觉异常等)
0 改善与Kulu疾病和骨瘤病(不包括肾功能衰竭的症状) 相关的各种症状(骨病变、骨痛和肌肉无力)
用法用量
0 继发性甲状旁腺功能亢进维持性透析的病例
通常情况下, 成人口服0.3微克, 每天一次作为法拉尔卡氏素蛋白醇。
然而, 年龄, 要适当地减肥的症状。
0 甲状腺功能障碍、库鲁病和骨瘤的情况下
通常情况下, 成人口服0.3 ~ 0.9微克, 每天一次作为法拉尔钙素醇。
然而, 年龄, 症状, 并酌情增加或减少的疾病类型。
临床结果
在国内204个设施进行的双盲比较试验中, 481例临床试验的评价目标的有效性如下。
(见表 3)
临床结果表
表3。

包装规格
片
0.15:ptp100 片 (10x10)
0.3:ptp100 片 (10x10)
制造和销售来源
大日本住友制药株式会社
联盟
Kissei Yakuhin Kogyo Ltd。
持证商：Dainippon Sumitomo Pharma Co.Ltd.
上市国：Japan
注：以上中文处方资料不够完整，使用者以原处方为准。
完整处方资料附件：http://www.info.pmda.go.jp/go/pack/3112005F1029_2_08/
New release of the active vitamin D3 formulation "Flustan® Tablets"
Kisei Yakuhin Kogyo Co., Ltd. (Representative director and President: Rikuo Kamizawa) will announce the active vitamin D3 formulation "Fulstan tablets" (General name Farale Calcineurin triol) from August 1 (Wednesday).
Flustan tablets are medical pharmaceuticals with secondary parathyroid hyperthyroid dysfunction under maintenance dialysis, hypocalcemia associated with hypothyroid dysfunction, and the adaptation of Kulu disease and osteomalacia. With the increase in dialysis patients, the treatment of dialysis complications caused by long-term dialysis has become a very important issue.
Secondary parathyroid hyperhyperthyroidism is a major background disease of dialysis osteosis, one of the complications that significantly degrades the quality of life of dialysis patients. Secondary hyperthyroid dysfunction in patients undergoing dialysis to compensate for calcium in the blood that decreases due to vitamin D3 deficiency resulting from dysfunction of the kidney, It develops by enhancing the secretion of parathyroid hormone with the effect of mobilizing calcium from the bone into the blood. When this secondary parathyroid disease progresses, resulting in bone pain and joint pain due to bone metabolic disorders, also blood vessels and internal organs by the calcium and phosphorus in the blood is high, such as causing calcification in the surrounding joints, the patient's QOL,
In addition, it has a serious effect on the prognosis of life.
The number of patients with secondary parathyroid hyperhyperthyroidism is estimated to be one-third of about 210,000 people in dialysis patients. In the treatment of secondary parathyroid hyperthyroid, oral or injectable agents of vitamin D3 formulations also have the effect of suppressing the secretion of parathyroid hormone.
However, the existing oral agent is not able to administer the amount sufficient to suppress the parathyroid hormone because it is easy to increase the calcium, and it has been pointed out that the injection is a problem such as high incidence of hypercalcemia as a side effect.
Flustan tablets are dosages that keep serum calcium within the normal range, have the characteristics of suppressing parathyroid hormones, and have obtained the adaptation of "secondary parathyroid hyperthyroid dysfunction under maintenance dialysis" for the first time as an oral agent. This is a product that Sumitomo Pharmaceutical Co., Ltd. and Taisho Pharmaceutical Corporation have introduced and jointly developed from the United States WARF (Wisconsin Alumni Research Foundation) and acquired manufacturing approval. In March of this year, the company concluded a supply contract with Sumitomo Pharma and Fulstan tablets and acquired the right to sell this product.
It will be released on the same day as "Hornel tablets" from Taisho Pharmaceutical. In our medium-term management plan forward Plan 21, we are strengthening our area strategy for "expansion of scale" and "strengthening competitiveness". We have positioned the renal dialysis area as a marketing priority area, and have been selling the blood coagulation inhibitor "AMAMEMIN® Intravenous" used for hemodialysis, and the health care Division sells ingredient-adjusted foods such as protein for patients with kidney disease. With the release of this product, we will further promote the region strategy in the renal dialysis area.
Product Name
Flustan® Tablets (Fulstan®)
■ General name
Farale calcineurin triol (Falecalcitriol)
■ Efficacy and effects
・Improvement of hypocalcemia and associated symptoms (such as Tentani, cramps, numbness, sensory abnormalities, etc.) in secondary parathyroid hyperthyroid dysfunction and hypothyroid dysfunction (excluding those in renal failure) under maintenance dialysis
・Improvement of the symptoms (bone lesions, bone pain, decreased muscle strength) associated with Kulu's disease and Osteomacia (excluding those in renal failure)
■ Dosage In the case of secondary parathyroid hyperthyroid under maintenance dialysis usually, the adult is orally administered 0.3 μg once a day as Farere Calcineurin ol.
However, age, to lose weight as appropriate by the symptoms. -Parathyroid dysfunction, in the case of Kulu disease and Osteomacia Usually, the adult is orally administered 0.3 ~ 0.9 μg as a fere calcineurin triol once a day.
However, age, symptoms, and increase or decrease as appropriate by the disease type.
■ Characteristics 1.
It is an active vitamin D3 formulation of oral administration with the adaptation of secondary parathyroid hyperthyroid (2 ° HPT) under maintenance dialysis. 2
For 2 ° HPT under maintenance dialysis, the parathyroid hormone is lowered in the dose to keep serum calcium within the normal range. 3
In the 2 ° HPT model, bone lesions such as increased bone and fibrous tissue volume are improved (rats). 4 The incidence of adverse reactions was 11.9% (54/452 cases). (Upon approval) the main side effect is hypercalcemia (5.1%) and itching (2.4%).
As a serious side effect, hypercalcemia, kidney stones and ureter stones have been reported.
■ Regulation category
Pharmaceuticals, designated medicines
■ Dosage type
Tablets
Manufacturing
Sumitomo Pharma Corporation
■ Sales Kissei Yakuhin Kogyo Co., Ltd.