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Side effects of these drugs may include but are not limited to: Constipation; Peripheral edema, which can occur in as much as 70% of people receiving calcium channel blocker, is caused by calcium channel blockers' preferential arteriolar or precapillary dilation without commensurate dilation in the venous or postcapillary circulation.
More than ten thousand cases of calcium channel blocker toxicity were reported in the United States in 2010. [2] Along with beta blockers and digoxin, calcium channel blockers have one of the highest rates of death in overdose. [2] These medications first became available in the 1970s and 1980s. [2]
While negative inotropism may precipitate or exacerbate heart failure in the short term, certain beta blockers (e.g. carvedilol, bisoprolol and metoprolol) have been believed to reduce long-term morbidity and mortality in congestive heart failure. [13] Examples of negative inotropic agents include: Beta blockers [14]
Itraconazole (Onmel/Sporanox) exhibits a negative inotropic effect on the heart and thus could spur an additive effect when used concomitantly with isradipine. Itraconazole also inhibits an important cytochrome liver enzyme ( CYP 450 3A4) which is needed to metabolize isradipine and other calcium channel blockers .
The two drugs have similar properties; however, tiapamil appears to treat arrhythmic conditions without many of the hypotensive, negative inotropic, and negative chronotropic side effects. Tiapamil is a calcium channel blocker that acts on the slow calcium channels.
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.
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]
Amlodipine is a long-acting calcium channel antagonist that selectively inhibits calcium ion influx across cell membranes. [42] It targets L-type calcium channels in muscle cells and N-type calcium channels in the central nervous system which are involved in nociceptive signalling and pain perception.
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