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钙通道阻滞剂(Calcium channel blocker)
钙通道阻滞剂(Calcium channel blocker)
Ca2+ is the key component of the contraction coupling between the myocardium and the vascular smooth muscle. The increase of intracellular Ca2+ concentration strengthens the muscle contraction and leads to the elevation of blood pressure and the acceleration of heart rate. Calcium antagonists and calcium channel blockers, calcium channel effects on contraction of muscle cell membrane, blocking calcium ions into the cell, so that the decreased myocardial contractility decreased heart rate, oxygen consumption decreased; at the same time, the peripheral vasodilation, reduce vascular resistance, reduce the burden on the heart. Therefore, calcium antagonists have the effects of anti - angina, anti - arrhythmia, anti - hypertension and so on.
Ca2+ channels have many subtypes, among which type L is the most important and the main route of Ca2+ influx during cellular excitation. The calcium antagonist according to the structure can be divided into 1 4-, two hydrogen pyridine, thiadipone, aryl alkyl amine and two phenyl piperazine and prenylamine class. Calcium antagonists and ion channels can be divided into selective calcium antagonists and non selective calcium antagonists. The first three types are selective for L channels, and the latter two belong to non selective calcium antagonists.
1, 4- two dihydropyridine
1, 4, two dihydropyridine calcium antagonist in specificity is high, a kind of powerful, these drugs can selectively act on vascular smooth muscle, dilate coronary artery, increase blood flow, anti angina and good anti hypertensive drug, and on the whole, under the condition of no inhibition of the heart, the side effect is small.
The clinical use of 1 4-, two dihydropyridine calcium antagonists are mainly nifedipine (nifedipine, 9-29), nicardipine (nicardipine, 9-30) and nimodipine (nimodipine, 9-31) and nitrendipine (nitrendipine, 9-32), nisoldipine (nisodipine, 9-33), amlodipine (nmlodipine 9-34), elnadipine (isradipine, 9-35).
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