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Selara 依普利酮片

通用名称依普利酮片 Eplerenone
品牌名称Selara
产地|公司日本(Japan) | 辉瑞(Pfizer)
技术状态原研产品
成分|含量25mg
包装|存储100片/盒 室温
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通用中文 依普利酮片 通用外文 Eplerenone
品牌中文 品牌外文 Selara
其他名称
公司 辉瑞(Pfizer) 产地 日本(Japan)
含量 25mg 包装 100片/盒
剂型给药 片剂口服 储存 室温
适用范围 高血压, 慢性心力衰竭
通用中文 依普利酮片
通用外文 Eplerenone
品牌中文
品牌外文 Selara
其他名称
公司 辉瑞(Pfizer)
产地 日本(Japan)
含量 25mg
包装 100片/盒
剂型给药 片剂口服
储存 室温
适用范围 高血压, 慢性心力衰竭

使用说明书

(免责声明:本说明书仅供参考,不作为治疗的依据,不可取代任何医生、药剂师等专业性的指导。本站不提供治疗建议,药物是否适合您,请专业医生(或药剂师)决定。)
等待内容更新

中文说明

(免责声明:本说明书仅供参考,不作为治疗的依据,不可取代任何医生、药剂师等专业性的指导。本站不提供治疗建议,药物是否适合您,请专业医生(或药剂师)决定。)

 

英文药名:Selara Tablets(Eplerenone)

中文药名:依普利酮片

日文药名:セララ錠25mg/セララ錠50mg/セララ錠100mg

生产厂家:辉瑞公司
药物分类名称
选择性醛固酮阻滞剂
批准日期:2007年11月
商標名
Selara Tablets 25mg
Selara Tablets 50mg
Selara Tablets 100mg
一般名エプレレノン(Eplerenone)
化学名9,11α-Epoxy-7α-(methoxycarbonyl)-3-oxo-17α-pregn-4-ene-21,17-carbolactone
分子式C24H30O6
分子量414.49
構造式
性状
它是一种白色的结晶性粉末。
易溶于乙腈,微溶于甲醇,非常不溶于水或乙醇(99.5)。
批准条件
* Serara片剂25毫克·50毫克
制定药品风险管理计划,适当实施。
药效药理
1. 作用机序
依普通酮与盐皮质激素受体结合并抑制醛固酮(肾素 - 血管紧张素 - 醛固酮系统激素(RAAS))的结合。 醛固酮在上皮组织如肾脏和非上皮组织如心脏,血管和脑中结合盐皮质激素受体,并通过钠再吸收和其他机制增加血压。 Eplerenone被认为通过抑制这些醛固酮的作用发挥降压作用。 由于依普力酮抑制醛固酮对肾素分泌的负反馈,其不断增加血浆肾素活性和血浆醛固酮浓度,但这些增加不能减轻依普利酮的作用。
2. 受体结合的选择性
依普通酮选择性结合大鼠和人类盐皮质激素受体。 其他类固醇激素受体如糖皮质激素受体,雄激素受体,孕激素受体等的亲和力与盐皮质激素受体的亲和力相比小于1/20。 在使用大鼠的研究中,依普利酮的临床剂量没有显示归因于类固醇激素受体作用的副作用,而不是盐皮质激素受体。
3.对高血压的作用
(1) 依普利酮对醛固酮持续给药/盐负荷的单侧肾切除高血压大鼠的收缩压显示出持续的降压作用。
(2) Eplerenone在中风易发自发性高血压大鼠(SHRSP)中显示持续的降压作用在2周给药期间的收缩压。 与赖诺普利联合使用ACE抑制剂,抗高血压作用显着增强。
(3) 在Dahl盐敏感性大鼠中,盐敏感型低肾素型高血压动物模型依普利酮对持续给药4周后,对收缩压显示剂量依赖性降压作用。
适应病症
高血压:25 mg·50 mg·100 mg
慢性心力衰竭:25mg·50mg
在以下条件下进行基础治疗的患者如血管紧张素转换酶抑制剂或血管紧张素II受体拮抗剂,β受体阻滞剂,利尿剂等。
用法与用量
高血圧症
成人;每天应从50mg开始服用依普利酮,如果无效,可以增加至100mg。
慢性心不全
成人;每天应从25mg开始服用依普利酮,并以每日一次的方式每日一次,以每日一次的方式开始给药,取决于服药开始4周后的血清钾水平和患者状况。
然而,在中度肾功能不全的患者中,每天服用一次25mg,每天一次,最大剂量为25mg,每天一次。
此外,根据血清钾水平和患者状况,应适当减少或停止。
包装规格
片剂
25mg:100片(PTP)
50mg:100片(PTP),700片(PTP),500片(瓶)
100mg:100片(PTP)
制造销售
辉瑞公司
完整说明书附件:http://www.info.pmda.go.jp/go/pack/2149045F1029_2_06/

 

外文说明

(免责声明:本说明书仅供参考,不作为治疗的依据,不可取代任何医生、药剂师等专业性的指导。本站不提供治疗建议,药物是否适合您,请专业医生(或药剂师)决定。)

Description

This medicine inhibits to the binding of aldosterone to receptors which is involved in hypertensive effects, heart and vascular fibrosis, heart hypertrophy or ventricular arrhythmia. It consequently shows antihypertensive effects and anti-heart failure effects.
It is usually used to treat hypertension and chronic heart failure (for the case of receiving base treatment such as ACE inhibitors, angiotensin II receptor antagonist, beta-blocker or diuretic).

Presentation


Feature


Active Ingredients

Eplerenone

Effect/Efficacy

This medicine inhibits to the binding of aldosterone to receptors which is involved in hypertensive effects, heart and vascular fibrosis, heart hypertrophy or ventricular arrhythmia. It consequently shows antihypertensive effects and anti-heart failure effects.
It is usually used to treat hypertension and chronic heart failure (for the case of receiving base treatment such as ACE inhibitors, angiotensin II receptor antagonist, beta-blocker or diuretic).

Usage/Dosage

For treatment of hypertension: In general, for adults, start with 2 tablets (50 mg of the active ingredient) at a time, once a day. If it is not effective enough, the dosage may be increased up to 4 tablets (100 mg) per day. However, if you take the medicine in combination with other medicinal products that suppress its metabolism, the daily dosage may not be exceeded 1 tablet (25 mg) at a time, once a day.
For treatment of chronic heart failure: In general, for adults, start with 1 tablet (25 mg of the active ingredient) at a time, once a day. After 4 weeks from the start of taking as a guide, the dosage may be increased up to 2 tablets (50 mg) at a time, once a day according to the serum potassium level or conditions. However, if you have moderate renal dysfunction, start with 1 tablet (25 mg) at a time, once a day alternately. The maximum daily dose is up to 1 tablet (25 mg) at a time, once a day, the dosage may be decreased or discontinue according to the serum potassium level or conditions. If you take the medicine in combination with other medicinal products that suppress its metabolism, the daily dosage may not be exceeded 1 tablet (25 mg) at a time, once a day.
In any case, strictly follow the instructions.
If you miss a dose and remember it within one day, take the missed dose as soon as possible. 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.

Cautions

Precautions while taking this medicine :
Since this medicine may cause dizziness by declining blood pressure, pay close attention to performing dangerous operations machinery such as driving a car or working at heights.
Avoid taking health supplements containing St. John's wort (a kind of herb) with the medicine, since it may diminish medicinal effects with its enhanced metabolism.

Contraindication

The most commonly reported adverse reactions include headache, dizziness, nausea, fatigue, hypotension, renal dysfunction, indigestion and muscle cramp. 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.
numbness of limbs or lips, muscle weakness, paralysis of limbs [hyperkalemia]
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.