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Chemical Compound Review

ESMOLOL     methyl 3-[4-[2-hydroxy-3-(propan-2...

Synonyms: CHEMBL768, SureCN3605, Esmolol (INN), CHEBI:4856, AG-H-26080, ...
 
 
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Disease relevance of ESMOLOL

 

Psychiatry related information on ESMOLOL

 

High impact information on ESMOLOL

  • METHODS AND RESULTS: We created a model of global LV dysfunction by esmolol and phenylephrine infusion in six dogs. initially with LV expansion limited by increasing pericardial restraint and then with the pericardium opened [8].
  • Thirty-two patients age 6 to 22 years with unexplained recurrent syncope or presyncope underwent tilt-testing involving two to four tilts (60 degrees) at baseline, during esmolol infusion (500 micrograms/kg load, 50 to 140 micrograms/kg per minute), after esmolol withdrawal, and during isoproterenol infusion if not contraindicated [9].
  • Esmolol is a new ultra short-acting (half-life [t1/2] beta 9 min) beta 1-adrenergic-receptor antagonist reported to have no intrinsic sympathomimetic activity [1].
  • BP slightly decreased during esmolol infusion, whereas heart rate, ionized calcium, phosphate, magnesium, and plasma and urine catecholamines remained unchanged [10].
  • Esmolol increased mean plasma PTH by 33 +/- 8% (P < 0.01), due to a preferential increase in the pulsatile PTH secretion component (+129 +/- 44%, P < 0.02) [10].
 

Chemical compound and disease context of ESMOLOL

 

Biological context of ESMOLOL

 

Anatomical context of ESMOLOL

  • The effect of esmolol (100 micrograms/kg per min) on the response of global cardiovascular and regional myocardial contractile function (sonomicrometry) to pacing-induced tachycardia and acute left ventricular afterloading was assessed in dogs with a critical stenosis of the left anterior descending coronary artery (LAD) [18].
  • Change in activation after the administration of esmolol was also assessed and compared to the shift documented with successful sinus node (SN) modification [19].
  • Data were acquired before and during esmolol infusion, thereby allowing assessment of hemodynamic responses with the sympathetic nervous system functionally intact as well as ablated [20].
  • The elimination of esmolol is independent of renal or hepatic function as it is metabolised by red blood cell cytosol esterases to an acid metabolite and methanol [21].
  • CONCLUSIONS: Esmolol infusion in sepsis improved oxygen utilization of myocardium and preserved myocardial function [22].
 

Associations of ESMOLOL with other chemical compounds

 

Gene context of ESMOLOL

  • However, fractional shortening failed to detect changes in contractility during atrial pacing and esmolol infusion and its percent change was <20% [27].
  • It is concluded that acute beta blockade with esmolol can be achieved in patients with COPD and cardiac disorders with little risk of bronchospasm [28].
  • Data were obtained at baseline, at dobutamine and esmolol infusion to alter contractile state, and at inferior vena cava and aortic occlusion to alter preload and afterload [29].
  • The blood esterase mediating the hydrolysis of esmolol was characterized in several different species including man [30].
  • Use of esmolol in a parturient with hypertrophic obstructive cardiomyopathy [31].
 

Analytical, diagnostic and therapeutic context of ESMOLOL

  • Esmolol, a new ultrashort-acting (9 minute half-life) beta-receptor blocking agent, was given by continuous intravenous infusion for up to 24 hours in 24 patients (21 with isolated coronary bypass surgery and 3 with valve replacement) 1 to 7 days after surgery [32].
  • Coronary blood flow velocities (using a 0.014-in. [0.035 cm] Doppler guide wire) were measured at rest, during atrial pacing and during intravenous administration of a short-acting beta-blocker (esmolol, 50 to 500 micrograms/kg body weight per min) with continuous atrial pacing [33].
  • Is esmolol cardioprotective? Tolerance of pacing tachycardia, acute afterloading and hemodilution in dogs with coronary stenosis [18].
  • We sought to evaluate the effectiveness of esmolol vs placebo in 40 patients emerging from general anesthesia for neurosurgery [34].
  • Multiple blood, urine, and dialysate samples were collected during a 72-hour period and assayed for esmolol and ASL-8123 by HPLC [35].

References

  1. Use of an ultra short-acting beta-blocker in patients with acute myocardial ischemia. Kirshenbaum, J.M., Kloner, R.A., Antman, E.M., Braunwald, E. Circulation (1985) [Pubmed]
  2. Esmolol tilt testing with esmolol withdrawal for the evaluation of syncope in the young. Ovadia, M., Thoele, D. Circulation (1994) [Pubmed]
  3. A new dosing regimen for esmolol to treat supraventricular tachyarrhythmia in Chinese patients. Ko, W.J., Chu, S.H. J. Am. Coll. Cardiol. (1994) [Pubmed]
  4. The effect of esmolol on cerebral blood flow, cerebral vasoreactivity, and cognitive performance: a functional magnetic resonance imaging study. Heinke, W., Zysset, S., Hund-Georgiadis, M., Olthoff, D., von Cramon, D.Y. Anesthesiology (2005) [Pubmed]
  5. Defining the dose range for esmolol used in electroconvulsive therapy hemodynamic attenuation. Howie, M.B., Hiestand, D.C., Zvara, D.A., Kim, P.Y., McSweeney, T.D., Coffman, J.A. Anesth. Analg. (1992) [Pubmed]
  6. Esmolol and the adrenergic response to perioperative stimuli. Murthy, V.S., Hwang, T.F., Sandage, B.W., Laddu, A.R. Journal of clinical pharmacology. (1986) [Pubmed]
  7. Experience with esmolol for the treatment of cocaine-associated cardiovascular complications. Sand, I.C., Brody, S.L., Wrenn, K.D., Slovis, C.M. The American journal of emergency medicine. (1991) [Pubmed]
  8. Insights from three-dimensional echocardiography into the mechanism of functional mitral regurgitation: direct in vivo demonstration of altered leaflet tethering geometry. Otsuji, Y., Handschumacher, M.D., Schwammenthal, E., Jiang, L., Song, J.K., Guerrero, J.L., Vlahakes, G.J., Levine, R.A. Circulation (1997) [Pubmed]
  9. Accelerometer systolic time intervals as fast-response sensors of upright posture in the young. Ovadia, M., Gear, K., Thoele, D., Marcus, F.I. Circulation (1995) [Pubmed]
  10. Beta1-adrenergic blockade augments pulsatile PTH secretion in humans. Schmitt, C.P., Obry, J., Feneberg, R., Veldhuis, J.D., Mehls, O., Ritz, E., Schaefer, F. J. Am. Soc. Nephrol. (2003) [Pubmed]
  11. Effects of beta-blockade and atropine on ischemic responses in left ventricular regions subtending coronary stenosis during dobutamine stress echocardiography. Chen, L., Ma, L., de Prada, V.A., Chen, M., Feng, Y.J., Waters, D., Gillam, L., Chen, C. J. Am. Coll. Cardiol. (1996) [Pubmed]
  12. A minimally invasive approach for efficient gene delivery to rodent hearts. Ding, Z., Fach, C., Sasse, A., Gödecke, A., Schrader, J. Gene Ther. (2004) [Pubmed]
  13. Esmolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy. Benfield, P., Sorkin, E.M. Drugs (1987) [Pubmed]
  14. Spinal cord perfusion pressure in dogs after control of proximal aortic hypertension during thoracic aortic cross-clamping with esmolol or sodium nitroprusside. Ryan, T., Mannion, D., O'Brien, W., Grace, P., Bouchier-Hayes, D., Cunningham, A.J. Anesthesiology (1993) [Pubmed]
  15. Beta-adrenergic blockade accelerates conversion of postoperative supraventricular tachyarrhythmias. Balser, J.R., Martinez, E.A., Winters, B.D., Perdue, P.W., Clarke, A.W., Huang, W., Tomaselli, G.F., Dorman, T., Campbell, K., Lipsett, P., Breslow, M.J., Rosenfeld, B.A. Anesthesiology (1998) [Pubmed]
  16. Use of an ultrashort-acting beta-receptor blocker (esmolol) in patients with acute myocardial ischemia and relative contraindications to beta-blockade therapy. Kirshenbaum, J.M., Kloner, R.F., McGowan, N., Antman, E.M. J. Am. Coll. Cardiol. (1988) [Pubmed]
  17. The class III antiarrhythmic effect of sotalol exerts a reverse use-dependent positive inotropic effect in the intact canine heart. Peralta, A.O., John, R.M., Gaasch, W.H., Taggart, P.I., Martin, D.T., Venditti, F.J. J. Am. Coll. Cardiol. (2000) [Pubmed]
  18. Is esmolol cardioprotective? Tolerance of pacing tachycardia, acute afterloading and hemodilution in dogs with coronary stenosis. Spahn, D.R., Frasco, P.E., White, W.D., Smith, L.R., McRae, R.L., Leone, B.J. J. Am. Coll. Cardiol. (1993) [Pubmed]
  19. Three-dimensional nonfluoroscopic mapping and ablation of inappropriate sinus tachycardia. Procedural strategies and long-term outcome. Marrouche, N.F., Beheiry, S., Tomassoni, G., Cole, C., Bash, D., Dresing, T., Saliba, W., Abdul-Karim, A., Tchou, P., Schweikert, R., Leonelli, F., Natale, A. J. Am. Coll. Cardiol. (2002) [Pubmed]
  20. Noninvasive assessment of the direct action of oral nifedipine and nicardipine on left ventricular contractile state in patients with systemic hypertension: importance of reflex sympathetic responses. Borow, K.M., Neumann, A., Lang, R.M., Ehler, D., Valentine-Bates, B., Wolff, A., Friday, K., Murphy, M. J. Am. Coll. Cardiol. (1993) [Pubmed]
  21. Esmolol. A review of its therapeutic efficacy and pharmacokinetic characteristics. Wiest, D. Clinical pharmacokinetics. (1995) [Pubmed]
  22. Infusion of the beta-adrenergic blocker esmolol attenuates myocardial dysfunction in septic rats. Suzuki, T., Morisaki, H., Serita, R., Yamamoto, M., Kotake, Y., Ishizaka, A., Takeda, J. Crit. Care Med. (2005) [Pubmed]
  23. ECT in a patient with aortic aneurysm. Devanand, D.P., Malitz, S., Sackeim, H.A. The Journal of clinical psychiatry. (1990) [Pubmed]
  24. Liquid-chromatographic analysis for esmolol and its major metabolite in urine. Achari, R., Drissel, D., Hulse, J.D. Clin. Chem. (1986) [Pubmed]
  25. Noninvasive, automated and continuous cardiac output monitoring by pulmonary capnodynamics: breath-by-breath comparison with ultrasonic flow probe. Peyton, P.J., Venkatesan, Y., Hood, S.G., Junor, P., May, C. Anesthesiology (2006) [Pubmed]
  26. Assessment of right ventricular diastolic suction in dogs with the use of wave intensity analysis. Sun, Y., Belenkie, I., Wang, J.J., Tyberg, J.V. Am. J. Physiol. Heart Circ. Physiol. (2006) [Pubmed]
  27. Effects of changes in left ventricular contractility on indexes of contractility in mice. Nemoto, S., DeFreitas, G., Mann, D.L., Carabello, B.A. Am. J. Physiol. Heart Circ. Physiol. (2002) [Pubmed]
  28. Esmolol and ventilatory function in cardiac patients with COPD. Gold, M.R., Dec, G.W., Cocca-Spofford, D., Thompson, B.T. Chest (1991) [Pubmed]
  29. Effects of modulation of left ventricular contractile state and loading conditions on tissue Doppler myocardial performance index. Cannesson, M., Jacques, D., Pinsky, M.R., Gorcsan, J. Am. J. Physiol. Heart Circ. Physiol. (2006) [Pubmed]
  30. Biochemical properties of blood esmolol esterase. Quon, C.Y., Stampfli, H.F. Drug Metab. Dispos. (1985) [Pubmed]
  31. Use of esmolol in a parturient with hypertrophic obstructive cardiomyopathy. Fairley, C.J., Clarke, J.T. British journal of anaesthesia. (1995) [Pubmed]
  32. Esmolol: a new ultrashort-acting beta-adrenergic blocking agent for rapid control of heart rate in postoperative supraventricular tachyarrhythmias. Gray, R.J., Bateman, T.M., Czer, L.S., Conklin, C.M., Matloff, J.M. J. Am. Coll. Cardiol. (1985) [Pubmed]
  33. Functional, angiographic and intracoronary Doppler flow characteristics in symptomatic patients with myocardial bridging: effect of short-term intravenous beta-blocker medication. Schwarz, E.R., Klues, H.G., vom Dahl, J., Klein, I., Krebs, W., Hanrath, P. J. Am. Coll. Cardiol. (1996) [Pubmed]
  34. Esmolol for the control of hypertension after neurologic surgery. Gibson, B.E., Black, S., Maass, L., Cucchiara, R.F. Clin. Pharmacol. Ther. (1988) [Pubmed]
  35. Pharmacokinetics of esmolol and ASL-8123 in renal failure. Flaherty, J.F., Wong, B., La Follette, G., Warnock, D.G., Hulse, J.D., Gambertoglio, J.G. Clin. Pharmacol. Ther. (1989) [Pubmed]
 
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