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Pathway Description
Esmolol Action Pathway
Homo sapiens
Drug Action Pathway
Esmolol, sold as Brevibloc, is a cardioselective beta-1 receptor blocker drug. As a beta-blocker, esmolol blocks the agonistic effect of the sympathetic neurotransmitters by competing for receptor binding sites, and as it is cardioselective, it binds primarily to those in the heart. Esmolol is injected intravenously, and when it enters the heart, it binds to the beta-1 adrenergic receptor, preventing signalling. Normally, epinephrine and norepinephrine bind to the beta-1 adrenergic receptor with equal affinity and trigger a G-protein signalling cascade that result in the heart muscle contracting. When esmolol binds, it causes the rate and force of these heart contractions to be decreased, in order to help treat supraventricular tachycardia. Esmolol is rapidly metabolized in red blood cells, and once metabolized it is inactivated, giving it a short time of activity within the body.
References
Esmolol Pathway References
Borchard, U. Pharmacological properties of beta-adrenoceptor blocking drugs. Journal of Clinical and Basic Cardiology. 1998;1(1):5-9.
DiPiro, J.T., Talbert, R.L., Yee, G.C., Matzke, G.R., Wells, B.G, & Posey, M.L. Pharmacotherapy: A pathologic approach. (6th ed) (2005) p.207-208. New York: McGraw-Hill Medical Publishing Division.
Jahn P, Eckrich B, Schneidrowski B, Volz-Zang C, Schulte B, Mutschler E, Palm D: Beta 1-adrenoceptor subtype selective antagonism of esmolol and its major metabolite in vitro and in man. Investigations using tricresylphosphate as red blood cell carboxylesterase inhibitor. Arzneimittelforschung. 1995 May;45(5):536-41.
Pubmed: 7612051
Volz-Zang C, Eckrich B, Jahn P, Schneidrowski B, Schulte B, Palm D: Esmolol, an ultrashort-acting, selective beta 1-adrenoceptor antagonist: pharmacodynamic and pharmacokinetic properties. Eur J Clin Pharmacol. 1994;46(5):399-404.
Pubmed: 7957532
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
Striated Muscle Contraction References
Cooke R: The sliding filament model: 1972-2004. J Gen Physiol. 2004 Jun;123(6):643-56. doi: 10.1085/jgp.200409089.
Pubmed: 15173218
Szent-Gyorgyi A: The mechanism of muscle contraction. Proc Natl Acad Sci U S A. 1974 Sep;71(9):3343-4.
Pubmed: 4610574
Kuo IY, Ehrlich BE: Signaling in muscle contraction. Cold Spring Harb Perspect Biol. 2015 Feb 2;7(2):a006023. doi: 10.1101/cshperspect.a006023.
Pubmed: 25646377
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