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EDARBI tablet(azilsartan medoxomil阿齐沙坦酯衍生物片)

2011-04-10 16:37:36 作者：新特药房来源：中国新特药网天津分站浏览次数：632 文字大小：【大】【中】【小】

简介： 制造商：武田制药北美公司药理分类：血管紧张素Ⅱ受体阻滞剂（ARB）。活性成分（补）： Azilsartan沙坦酯40毫克，80毫克;标签。指示（补）：高血压。可单独使用或与其他抗高血压药物合用。 ...

关键字：EDARBI tablet(azilsartan medoxomil阿齐沙坦酯衍生物片)

制造商：
武田制药北美公司

药理分类：
血管紧张素Ⅱ受体阻滞剂（ARB）。

活性成分（补）：
Azilsartan沙坦酯40毫克，80毫克;标签。

指示（补）：
高血压。可单独使用或与其他抗高血压药物合用。

药理作用：
Azilsartan是一种选择性AT1受体亚型血管紧张素Ⅱ受体拮抗剂。它会阻止血管收缩和血管紧张素Ⅱ，一升压剂，醛固酮分泌的影响，如通过选择性阻断血管平滑肌和肾上腺的血管紧张素II结合的组织中AT1受体。它的行动，因此，对血管紧张素Ⅱ的合成途径无关。

实际的原料药是azilsartan沙坦酯钾盐，也azilsartan kamedoxomil而闻名。这是水解成活性代谢物，azilsartan在胃肠道，因为它被吸收。 Azilsartan是高度蛋白结合血浆白蛋白，它经历了由CYP2C9的酶代谢的影响。这是清除肾脏和肝脏都机制。稳态水平达到用药后5天。目前还没有观察到血清钾，钠临床意义的变化。

临床试验：
七双盲随机研究，包括安慰剂对照和比较主动控制的研究从6周至6个月的时间，结果，已经证明了azilsartan的降压效果。作者：5941轻度，中度或重度高血压患者参与了研究。 Azilsartan，每日剂量在80毫克，在统计学上优于安慰剂和活性比较，门诊（槽测量）和24小时平均血压测量，两个6周的研究（门诊）（奥美沙坦和缬沙坦）。在一比较，就超过24周azilsartan缬沙坦的研究，观察到类似的结果。大部分的降压效果明显的头2个星期的治疗。

在一项研究中，要继续azilsartan或安慰剂治疗26周后患者的随机，azilsartan已显示出在长期治疗的持续和一致的降压效果。有没有反弹的影响后，突然停止azilsartan治疗观察。虽然azilsartan是有效的，不分种族，作为单一治疗的效果，在黑色的病人对像在其他效果有很大的一半。这种效果差，已观察到其他ARB类药物和血管紧张素转换酶抑制剂，以及，这是归因于肾素在这个人口普遍较低的水平。

法律分类：
接收

成人：
≥18岁：单药治疗，而不是卷的枯竭：80毫克，每日一次。容积枯竭（例如，伴随高剂量利尿剂）：最初40毫克，每日一次。

儿童：
<18年：不推荐。

警告/注意事项：
正确盐/容衰竭治疗开始前，或减少初始剂量;低血压监视器。严重瑞士法郎。肾动脉狭窄。肾功能不全（血清肌酐显示器）。妊娠（部件C在第一三个月。猫第二D和第三孕期，避免）。哺乳母亲：不推荐。

互动（补）：
可能是拮抗，肾毒性的NSAIDs potentiated，包括选择性COX - 2抑制剂（监察老人和/或体积耗尽肾功能，定期）。

不良反应（补）：
腹泻;罕见：体位性低血压，头晕，恶心，无力，疲劳，肌肉痉挛，咳嗽。

如何提供：
制表- 30，90

最后更新：
2011年4月7日

Edarbi approved for treatment of hypertension

Edarbi (azilsartan medoxomil tablets; Takeda Pharmaceuticals North America) has been approved by the FDA for the treatment of hypertension in adults. This approval was based on data from Phase 3 clinical trials which showed that Edarbi successfully met the primary endpoint, change in 24-hour mean systolic blood pressure (SBP), with statistical significance of lowering blood pressure compared to placebo and head-to-head active comparators. Results from one study showed Edarbi at doses of 80 mg/day and 40 mg/day lowered 24-hour mean SBP by 14.3mmHg and 13.2mmHg from baseline, respectively. The blood pressure reductions of Edarbi (80 mg/day) were statistically superior to those of the active comparators valsartan 320mg/day (-10mmHg) and olmesartan medoxomil 40mg/day (-11.7mmHg). Similar results were observed in all three comparator studies.

EDARBI

Manufacturer:

Takeda Pharmaceuticals North America, Inc.

Pharmacological Class:

Angiotensin II receptor blocker (ARB).

Active Ingredient(s):

Azilsartan medoxomil 40mg, 80mg; tabs.

Indication(s):

Hypertension. May be used alone or in combination with other antihypertensive agents.

Pharmacology:

Azilsartan is a selective AT₁ subtype angiotensin II receptor antagonist. It blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II, a pressor agent, by selectively blocking the binding of angiotensin II to the AT₁ receptor in tissues such as vascular smooth muscle and the adrenal gland. Its action is, therefore, independent of the pathway for angiotensin II synthesis.

The actual drug substance is the potassium salt of azilsartan medoxomil, also known as azilsartan kamedoxomil. This is hydrolyzed to the active metabolite, azilsartan, in the gastrointestinal tract as it is absorbed. Azilsartan is highly protein-bound to plasma albumin, and it undergoes metabolism by the CYP2C9 enzyme. It is cleared by both renal and hepatic mechanisms. Steady-state levels are attained within 5 days of dosing. There were no observed clinically significant changes in serum potassium or sodium.

Clinical Trials:

The results of seven double-blind, randomized studies, including both placebo-controlled and active comparator-controlled studies ranging from 6 weeks to 6 months in duration, have demonstrated the antihypertensive effects of azilsartan. A total of 5941 patients with mild, moderate, or severe hypertension were involved in the studies. Azilsartan, dosed at 80mg daily, was statistically superior to placebo and active comparators (olmesartan and valsartan) in both clinic (trough measurements) and 24-hour mean blood pressure measurements (ambulatory) in two 6-week studies. In a study comparing azilsartan to valsartan over 24 weeks, similar results were observed. Most of the antihypertensive effect was evident within the first 2 weeks of treatment.

In a study that randomized patients to placebo or continued azilsartan therapy after 26 weeks, azilsartan has demonstrated a sustained and consistent antihypertensive effect during long-term treatment. There was no rebound effect observed after the abrupt cessation of azilsartan treatment. While azilsartan was effective regardless of race, the effect, as monotherapy, in black patients was about half as great as the effect in others. This difference in effectiveness has been observed in other ARBs and in ACE inhibitors as well, and it is attributed to the generally low levels of renin in this population.

Legal Classification:

Adults:

≥18 years: Monotherapy, not volume-depleted: 80mg once daily. Volume-depleted (eg, concomitant high-dose diuretics): initially 40mg once daily.

Children:

<18 years: not recommended.

Warnings/Precautions:

Correct salt/volume depletion before starting therapy, or reduce initial dose; monitor for hypotension. Severe CHF. Renal artery stenosis. Renal impairment (monitor serum creatinine). Pregnancy (Cat. C in 1^st trimester; Cat. D in 2^nd and 3^rd trimesters; avoid). Nursing mothers: not recommended.

Interaction(s):

May be antagonized by, and renal toxicity potentiated by NSAIDs, including selective COX-2 inhibitors (monitor renal function periodically in elderly and/or volume-depleted).