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氯沙坦钾

氯沙坦钾
CAS Number: 124750-99-8

氯沙坦钾

治疗类别
抗高血压
API技术
合成
剂型
口服固体制剂
瑞迪博士研发状态
可得到
注册备案情况
USA
Canada
Europe
New Zealand
Japan
Saudi Arabia
Taiwan
Brazil
创新品牌(美国)
COZAAR

Mechanism of Action

Angiotensin II [formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II)] is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system, and an important component in the pathophysiology of hypertension. It also stimulates aldosterone secretion by the adrenal cortex. Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues, (e.g., vascular smooth muscle, adrenal gland). There is also an AT2 receptor found in many tissues but it is not known to be associated with cardiovascular homeostasis. Neither losartan nor its principal active metabolite exhibits any partial agonist activity at the AT1 receptor, and both have much greater affinity (about 1000-fold) for the AT1 receptor than for the AT2 receptor. In vitro binding studies indicate that losartan is a reversible, competitive inhibitor of the AT1 receptor. The active metabolite is 10 to 40 times more potent by weight than losartan and appears to be a reversible, non-competitive inhibitor of the AT1 receptor.

Neither losartan nor its active metabolite inhibits ACE (kininase II, the enzyme that converts angiotensin I to angiotensin II and degrades bradykinin), nor do they bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.

Indication

COZAAR is an angiotensin II receptor blocker (ARB) indicated for:

  • Treatment of hypertension, to lower blood pressure in adults and children greater than 6 years old. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.
  • Reduction of the risk of stroke in patients with hypertension and left ventricular hypertrophy. There is evidence that this benefit does not apply to Black patients. (1.2)
  • Treatment of diabetic nephropathy with an elevated serum creatinine and proteinuria in patients with type 2 diabetes and a history of hypertension.

Dr. Reddy的专长

Dr. Reddy总部位于印度海得拉巴,是全球领先的活性药物成分(API)供应商之一。 Dr. Reddy的API业务是美国、欧洲、巴西、拉丁美洲、日本、中国、韩国和新兴市场的制药公司的首选合作伙伴。

Reddy博士的API业务在过去30多年来在开发和制造复杂API(如类固醇,多肽,复杂长链分子和高效API(HPAPI /肿瘤药物))方面所建立的深厚技术优势中茁壮成长。 我们在知识产权和法规事务方面的实力可以帮助我们始终如一地达到并超越监管标准,从而为这一专业知识提供补充。 Reddy博士 氯沙坦钾 API是研发,知识产权和监管方面广泛专业知识的结果。

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