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Pathway Description
Amlodipine Smooth Muscle Relaxation Action Pathway
Homo sapiens
Drug Action Pathway
Amlodipine is a calcium channel blocker used to treat hypertension and angina. It can be found under the brand names Amlobenz, Azor, Caduet, Dafiro, Exforge, Exforge Hct, Katerzia, Lotrel, Norliqva, Norvasc, Prestalia, Tribenzor, Twynsta and Viacoram. Amlodipine, initially approved by the FDA in 1987, is a popular antihypertensive drug belonging to the group of drugs called dihydropyridine calcium channel blockers. Due to their selectivity for the peripheral blood vessels, dihydropyridine calcium channel blockers are associated with a lower incidence of myocardial depression and cardiac conduction abnormalities than other calcium channel blockers. Amlodipine is considered a peripheral arterial vasodilator that exerts its action directly on vascular smooth muscle to lead to a reduction in peripheral vascular resistance, causing a decrease in blood pressure. Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the influx of calcium ions into both vascular smooth muscle and cardiac muscle. Experimental studies imply that amlodipine binds to both dihydropyridine and nondihydropyridine binding sites, located on cell membranes. The contraction of cardiac muscle and vascular smooth muscle are dependent on the movement of extracellular calcium ions into these cells by specific ion channels. Amlodipine blocks calcium ion influx across cell membranes with selectivity. A stronger effect of amlodipine is exerted on vascular smooth muscle cells than on cardiac muscle cells. Direct actions of amlodipine on vascular smooth muscle result in reduced blood pressure. Some side effects of using amlodipine may include headaches, dizziness, flushing, and a pounding heart.
References
Amlodipine Smooth Muscle Relaxation Pathway References
Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M: DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. doi: 10.1093/nar/gkx1037.
Pubmed: 29126136
Sutherland JK, Hallam RF: Soldering technique for osseointegrated implant prostheses. J Prosthet Dent. 1990 Feb;63(2):242-4. doi: 10.1016/0022-3913(90)90112-p.
Pubmed: 1968100
Clusin WT, Anderson ME: Calcium channel blockers: current controversies and basic mechanisms of action. Adv Pharmacol. 1999;46:253-96. doi: 10.1016/s1054-3589(08)60473-1.
Pubmed: 10332505
Nazzaro P, Manzari M, Merlo M, Triggiani R, Scarano AM, Lasciarrea A, Pirrelli A: Antihypertensive treatment with verapamil and amlodipine. Their effect on the functional autonomic and cardiovascular stress responses. Eur Heart J. 1995 Sep;16(9):1277-84. doi: 10.1093/oxfordjournals.eurheartj.a061086.
Pubmed: 8582392
Meredith PA, Elliott HL: Clinical pharmacokinetics of amlodipine. Clin Pharmacokinet. 1992 Jan;22(1):22-31. doi: 10.2165/00003088-199222010-00003.
Pubmed: 1532771
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