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英文药名：Careload LA Tablets(Beraprost sodium)
中文药名：贝前列素钠LA片
日文药名：ケアロードLA錠
生产厂家：安斯泰来制药
ケアロードLA錠60μg
贝前列素是首个具有口服活性的前列环素类似物。空腹吸收迅速，30分钟后达峰浓度，清除半衰期为35～40分钟2。
治疗类别名称
口服前列环素（PGI2）衍生物缓释制剂
欧文名
Careload LA Tablets 60μg
一般名
ベラプロストナトリウム（JAN）beraprost（INN）
化学名
Monosodium（1RS,2RS,3aSR,8bSR）-2,3,3a,8b-tetrahydro-2-hydroxy-1-［（1E,3SR,4RS）-3-hydroxy-4-methyloct-1-en-6-yn-1-yl］-1H-cyclopenta［b］benzofuran-5-butanoate
Monosodium（1RS,2RS,3aSR,8bSR）-2,3,3a,8b-tetrahydro-2-hydroxy-1-［（1E,3SR,4SR）-3-hydroxy-4-methyloct-1-en-6-yn-1-yl］-1H-cyclopenta［b］benzofuran-5-butanoate
構造式
分子式
C24H29NaO5
分子量
420.47
性状
白色粉末。非常易溶于甲醇，不溶于水或乙醇（99.5）。它是吸湿性的。水溶液（1→200）示出了没有旋光性。
分配系数（正辛醇/水系统）
pH值为3460
pH为715
pH为90.41
操作注意事项
为了避免光和水分，避光，它被存储在一个密闭容器中。
药效药理
1. 药理作用
(1) 血小板聚集抑制作用
1）在口服给药至健康成人，其抑制血小板聚集。
2）聚集诱导物质通过，有一个人的血小板凝块分解动作（体外）来抑制人的血小板聚集。
(2) 血管扩张和血流增加作用
K+，这是通过PGF2α，肠系膜动脉等等，各种萃取动脉和血清素收缩，到由苯肾上腺素收缩狗的分离的肺动脉狗的股动脉，示出一个放松的效果（体外），狗各种器官容器的增加血流量。
(3) 血管平滑肌细胞增殖的抑制作用
抑制人肺动脉血管平滑肌细胞的血小板衍生的生长因子刺激的生长（体外）。
(4) 对疾病模型的作用
1） 肺动脉高压模型
在野百合碱诱导的大鼠肺动脉高压模型，右心室收缩压的升高，抑制肺血管的肌肉肥大在电影中的口服给药。
在血栓素激动剂诱导犬肺动脉高压模型，降低肺动脉压和肺血管阻力在静脉给药。
在栓塞引起的大鼠肺动脉高压模型，打压右心室收缩压上升。
2）血栓模型
给大鼠动脉血栓形成和大鼠静脉血栓等，认识到血栓形成的抑制效果。
2. 作用机序
以及前列环素，通过血小板及血管平滑肌的前列腺环素受体贝拉普罗斯特酸钠，激活腺苷酸环化酶，细胞内cAMP浓度上升，由Ca 2+内流抑制和血栓烷A2的产生抑制和类似物，血管扩展动作，显示了抗血小板作用和血管平滑肌细胞增殖的抑制效果。
适应证
肺动脉性肺高血压症
用法用量
口服给药：每天总量为120μg，分2-3次服用。
包装规格：
100片（10片×10）
生产商：安斯泰来制药
Careload LA Tablets（Beraprost sodium）
Brand name : Careload LA Tablets 60mcg
Active ingredient: Beraprost sodium
Dosage form: white to yellowish white tablet (φ: 7.0mm, thickness: 2.9mm)
Print on wrapping: (Face) ケアロードLA 60, house-mark, ケアロード, TR60, LA60μg, (Back) Careload LA 60μg, house-mark, ケアロードLA 60μg
http://www.info.pmda.go.jp/go/pack/2190027G1022_1_09/
The World First Oral Prostacyclin (PGI2) Derivative Prolonged Release
Japan-October 22, 2007-Toray Industries Inc. (“Toray”; Headquarters: Tokyo, President and CEO: Sadayuki Sakakibara) and Astellas Pharma Inc. (“Astellas ”; Headquarters: Tokyo; President and CEO: Masafumi Nogimori) today announced that Toray has obtained marketing approval for its oral PGI2 derivative prolonged release, Careload ® LA Tablets 60µg (generic name: beraprost sodium), to be indicated for pulmonary arterial hypertension (PAH) on October 19,2007. Careload will be listed in the NHI drug price list and launched in December 2007.
Beraprost sodium is a PGI2 derivative discovered by Toray. Toray has been developing many formulations of beraprost sodium for a long period and achieved to sustain its blood concentration and lower the maximum blood concentration (Cmax) of it.
Toray has submitted an application for beraprost sodium with indication for PAH based on the results of Japanese clinical trials subjecting primary pulmonary hypertension and pulmonary hypertension following collagenosis in September 2006. It has been designated for a priority review by Ministry of Health, Labour and Welfare in February 2007. Careload ® LA Tablets 60µg has been admitted its efficacy and safety and obtained marketing approval for treatment of PAH.
About PAH
PAH is that peripheral arteriole lumen of pulmonary artery where blood pumped from heart to lung gets narrow, and it makes difficult for blood to flow. This causes pulmonary artery high pressure. PAH is classified in two types, one is primary pulmonary hypertension (PPH), and the other is secondary pulmonary hypertension following specific diseases. Exertional dyspnea, fatigability and palpitation are commonly observed initial symptoms, and once it advances, heart failure may result.
About Careload ®
Careload ® is the world first oral PGI2 derivative prolonged release and expected to provide a new therapeutic choice, an oral agent which can be widely used, to patients suffering from PAH.
Toray had obtained marketing approval for beraprost sodium tablets to be indicated for improvement of ulcer, pain and feeling of coldness associated with chronic arterial occlusion
in January 1992, primary pulmonary hypertension in September 1999, and it has already been available in Japanese market as Dorner ® Tablets by Astellas since April 1992. Careload ® LA Tablets 60µg will be marketed by Astellas as well as Dorner ® tablets.
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