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Compared with certain other L-type calcium channel blockers (for example those of the phenylalkylamine class such as verapamil) that have significant action at the heart, the dihydropyridine calcium channel blockers lower blood pressure mainly by relaxing the smooth muscle of the blood vessel walls. [3]
Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists [2] are a group of medications that disrupt the movement of calcium (Ca 2+) through calcium channels. [3] Calcium channel blockers are used as antihypertensive drugs, i.e., as medications to decrease blood pressure in patients with hypertension.
1,4-Dihydropyridine (DHP) is an organic compound with the formula CH 2 (CH=CH) 2 NH. The parent compound is uncommon, [ 2 ] but derivatives of 1,4-dihydropyridine are important commercially and biologically.
An L-type calcium channel with its subunits labeled along with some drugs known to inhibit the channel. The L-type calcium channel (also known as the dihydropyridine channel, or DHP channel) is part of the high-voltage activated family of voltage-dependent calcium channel. [2] "L" stands for long-lasting referring to the length of activation.
Special attention should be given to the coadministration of non-DHP with beta-blockers or ivabradine due to the increased risk of bradycardia. [13] Since both DHP and non-DHP are metabolized through the CYP3A4 system, grapefruit juice containing furanocoumarins (the potent inhibitors of the CYP3A4 enzyme) should be avoided. [13]
Its mechanism of action and clinical effects closely resemble those of nifedipine and the other dihydropyridine calcium channel blockers (amlodipine, felodipine), except that nicardipine is more selective for cerebral and coronary blood vessels. It is primarily a peripheral arterial vasodilator, thus unlike the nitrovasodilators (nitroglycerin ...
Molecules that act as channel blockers are important in the field of pharmacology, as a large portion of drug design is the use of ion channel antagonists in regulating physiological response. The specificity of channel block molecules on certain channels makes it a valuable tool in the treatment of numerous disorders.
Chemically, it is based upon a 1,4-thiazepine ring, making it a benzothiazepine-type calcium channel blocker. It is a potent and mild vasodilator of coronary and peripheral vessels, respectively, [29] which reduces peripheral resistance and afterload, though not as potent as the dihydropyridine (DHP) calcium channel blockers