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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]
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.
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]
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.
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.
Tetrodotoxin, an example of a channel block molecule. A channel blocker is the biological mechanism in which a particular molecule is used to prevent the opening of ion channels in order to produce a physiological response in a cell. Channel blocking is conducted by different types of molecules, such as cations, anions, amino acids, and other ...
Efonidipine is a dihydropyridine calcium channel blocker marketed by Shionogi & Co. of Japan. It was launched in 1995, under the brand name Landel (ランデル). The drug blocks both T-type and L-type calcium channels. [1] Drug Controller General of India (DCGI) has approved the use of efonidipine in India. [2]
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