英文药名: Inspra(Eplerenone)

中文药名: 依普利酮片

生产厂家: Pfizer

药品简介

依普利酮（Eplerenone）是一种新型选择性醛固酮受体阻滞剂，与雄激素和黄体酮受体相互作用极小，本品半衰期较长，每日口服1次就可有效的控制高血压，减轻心、脑和肾等靶器官的损害，改善Ⅱ型糖尿病患者微量蛋白尿，而且其副作用发生率与安慰剂相似，耐受良好。依普利酮的面市，对于高血压患者控制高血压、预防与靶器官损害相关的心血管疾病、改善高血压患者的预后等方面均具有重要意义。
 
商品名

Inspra

开发与上市厂商

依普利酮（eplerenone）由美国辉瑞（Pfizer）公司研发， 2004年，月在美国首次上市，目前已在德国、英国和美国上市。

适应证

用于原发性高血压及心肌梗死后的心力衰竭。

药理

依普利酮通过与醛固酮受体结合，阻断肾素-血管紧张素-醛固酮系统(RAAS)中的醛固酮，从而发挥降低血压的作用。

本品口服后平均达峰时间约为 1.5小时。峰浓度(Cmax)和曲线T面积 (AUC)在25～100mg剂量范围内与剂量呈比例增加，当剂量超过100mg 后AUC与剂量呈反比。

本品的血浆蛋白结合率约为 50%，主要与α1，酸性糖蛋白结合。在健康志愿者和高血压患者中，表观分布容积在稳态时为43～90L。
本品的代谢主要通过CYP3A4酶进行。在人的血清中未能检出活性代谢物，在尿和粪便中可检出约5% 未经代谢的本品。口服单剂量放射标记的本品后，约32%的药物随粪便排泄，约67％的药物随尿液排泄。本品的消除半衰期约为4～6小时。表观血浆清除率约为10L/h。

临床评价

在3091例高血压患者中进行了本品单用及与其他抗高血压药合用的安全性与有效性评价。受试者中 46%为女性，14%为黑人，22%为老年人。研究排除了基线血清钾升高（＞5mmol/L）和基线血清肌酐升高（男性＞1.5mg/dL，女性＞1.3mg/dL）的受试者。

在基线舒张压为95～114 mmHg 的受试患者中进行了两项固定剂量、安慰剂对照、为期8～12周的单药治疗研究，以评价本品的抗高血压疗效。在两项研究中，61，例患者随机分入本品组，140例患者随机分入安慰剂组。患者每日接受本pp 25～400mg,一日1次或2次服用。

接受本品一日50～200 mg治疗的患者，静坐收缩压和舒张压显著降低，与安慰剂组相比收缩压降低 6～13mmHg，舒张压降低3～ 7mmHg。

这些研究中，24小时ABPM数据的分析结果表明：本品一日1次或 2次，在整个服药周期中都可维持降压疗效，且本品一日2次，每次 50mg比一日1次降压效果更好。

本品降压作用可在服药2周显现。本品可与血管紧张素转换酶 (ACE)抑制剂、血管紧张素Ⅱ受体阻断剂、钙拮抗剂、α受体阻断剂和氢氯噻嗪联用。且联合用药者，平均心率未发生明显改变。也未见本品对心率、QRS间期、PR间期或QT 间期的影响。

不良反应

主要不良反应有：咳嗽、腹泻、腹痛、心绞痛、心肌梗死、蛋白尿、头痛、眩晕、疲乏、流感样症状等。

其他不良反应有：男性乳房发育、不正常阴道出血；血钾、甘油三酯、胆固醇、谷丙转氨酶、γ- 谷氨酰转移酶、肌酐、尿酸水平升高，血钠水平降低。

注意事项

本品不可与补钾剂、含钾的盐或禁忌药（保钾利尿剂、CYP450肝药酶强抑制剂）合用。

非甾体抗炎药、锂剂可影响本品血药浓度而影响疗效。

血钾过高者、有微量蛋白尿的2 型糖尿病患者、血清肌酐水平过高者、肌醉清除率＜50mL/min者不可服用本品。孕妇、儿童、肝功能不全、肾功能不全者慎用。

用法与用量

可单用或与其他抗高血压药合用。推荐剂量为一日50mg，4周后若降压效果不理想可调整剂量至一日100mg。

包装规格
·25mg 28 片
·50mg 28 片
·25mg 30 片
·50mg 30 片

Inspra (Eplerenone Tablets)
Inspra (eplerenone tablets) is normally prescribed in the hypertension treatment. At the same time, it is known to improve the survival rate in the patients who have been through heart attacks or strokes. Such cases occur when the patients suffer from ventricular systolic diseases. The main ingredient in this medication is the eplerenone. It inhibits the activity of aldosterone, which is known to narrow the blood vessels. While on this treatment, the blood vessels are widened, resulting in a smooth blood flow. The blood pressure is released then.

Inspra (eplerenone tablets) is also known to deal with the sodium and fluid retention in the organism. For all these reasons, it is highly indicated against cardiac and kidney diseases. It is often used in associated therapies, but also in monotherapy. The latest formula dates since 2008. You need a medical prescription to use this drug. Therefore, your blood must be evaluated first.

Administration
Always use this drug exactly like your doctor prescribes, even if the instructions are not identical with what you can find in the prescribing information leaflet in the package. The optimal dose is 50mg a day. However, the patients start with 25mg a day, to prevent the unfortunate side effects. Getting from 25mg to 50mg usually takes 4 weeks. The adjustments are minor and rarely made.

The most common situations when Inspra (eplerenone tablets) is used in associated therapies are in the patients who have been through a heart attack or a stroke. If you feel like the drug is too powerful or you can barely notice any effects, talk to your doctor. Never make dose adjustments just because you think so. If you have renal or hepatic dysfunctions, you might need your liver or kidneys verified on a regular basis.

Inspra (eplerenone tablets) is available on the market in 25mg and 50mg tablets. They should be swallowed whole, without chewing or crushing them. Use a glass of water. Food is not important in the treatment, so you might get them with or without it. The tablets are rarely divided and only at the doctor’s recommendation. Take the dose at the same time everyday, so you don’t forget about it.

Contraindications
Your doctor will prescribe a different drug if you present allergies or sensitivity to eplerenone or any other ingredient.

Secondary effects
Expect dizziness, diarrhea, abdominal pains, headaches and cough while on the Inspra (eplerenone tablets) treatment. If you experience chest pain, irregular heartbeat or any other conditions, call your doctor and seek help.