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苯磺酸氨氯地平

苯磺酸氨氯地平
CAS Number: 111470-99-6

苯磺酸氨氯地平

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
CEP
Japan
Korea
Taiwan
Russia
Indonesia
创新品牌(美国)
Norvasc

Mechanism of Action

Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Experimental data suggest that amlodipine binds to both dihydropyridine and nondihydropyridine binding sites. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specificion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Negative inotropic effects can be detected in vitro but such effects have not been seen in intact animals at therapeutic doses. Serum calcium concentration is not affected by amlodipine. Within the physiologic pH range, amlodipine is an ionized compound (pKa=8.6), and its kinetic interaction with the calcium channel receptor is characterized by a gradual rate of association and dissociation with the receptor binding site, resulting in a gradual onset of effect.

Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.

The precise mechanisms by which amlodipine relieves angina have not been fully delineated, but are thought to include the following:

Exertional Angina: In patients with exertional angina, NORVASC reduces the total peripheral resistance (afterload) against which the heart works and reduces the rate pressure product, and thus myocardial oxygen demand, at any given level of exercise.

Vasospastic Angina: NORVASC has been demonstrated to block constriction and restore blood flow in coronary arteries and arterioles in response to calcium, potassium epinephrine, serotonin, and thromboxane A2 analog in experimental animal models and in human coronary vessels in vitro. This inhibition of coronary spasm is responsible for the effectiveness of NORVASC in vasospastic (Prinzmetal’s or variant) angina.

Indication

NORVASC is a calcium channel blocker and may be used alone or in combination with other antihypertensive and antianginal agents for the treatment of:

  • Hypertension
  • NORVASC is indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.
  • Coronary Artery Disease
  • Chronic Stable Angina
  • Vasospastic Angina (Prinzmetal’s or Variant Angina)
  • Angiographically Documented Coronary Artery Disease in patients without heart failure or an ejection fraction < 40%

Dr. Reddy's的专长

Dr. Reddy's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's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。

Dr. Reddy's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。 Dr. Reddy's博士 苯磺酸氨氯地平 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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