Introduction
Amlodipine besylate has the IUPAC namebenzenesulfonic acid;3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate. It is a third-generation 1,4-dihydropyridine calcium ion antagonist developed by Pfizer in the 1980s, used for cardiovascular diseases such as hypertension, angina pectoris, and congestive heart failure. This drug is unanimously recommended by the US FDA Cardiovascular and Renal Advisory Committee for the treatment of hypertension.
Mechanism of Action
Amlodipine besylate belongs to the dihydropyridine class of calcium ion antagonists and can effectively inhibit calcium ion transmembrane influx in cardiac muscle and vascular smooth muscle. It lowers blood pressure by directly dilating vascular smooth muscle. It has a prominent effect on peripheral blood circulation with strong selectivity for blood vessels, and can relax coronary arteries and systemic blood vessels. It increases coronary blood flow and reduces blood pressure. In vivo, it has weak negative inotropic effects and has no impact on the human sinoatrial node or atrioventricular node.
Medication for Treating Hypertension and Angina
Amlodipine besylate, also known as Norvasc or amlodipine, is currently a common drug in clinical practice in China for treating hypertension and angina pectoris. It belongs to the calcium channel blocker class and works by blocking calcium ion transmembrane entry into cardiac muscle and vascular smooth muscle cells, directly relaxing vascular smooth muscle to achieve antihypertensive effects. Clinically, it is used alone or in combination with other antihypertensive drugs to treat essential hypertension.
The mechanism of action for treating chronic stable angina and variant angina has not been fully determined, but it can relieve angina by dilating peripheral small arteries and coronary arteries, reducing total peripheral vascular resistance, relieving coronary artery spasm, reducing cardiac afterload, and decreasing cardiac energy consumption and oxygen demand.
