Esmolol is an ultra-short-acting, cardioselective, intravenous beta-blocker with an elimination half-life of about nine minutes. After administration of a loading dose, its full therapeutic effect is evident within five minutes. Its efficacy in treating supraventricular arrhythmias is equal to that of propranolol, but unlike propranolol, the action of esmolol is titratable and is largely reversed within 10 to 30 minutes after stopping its administration. Esmolol is also effective in attenuating life-threatening perioperative tachycardia and hypertension caused by adrenergic stimulation in high-risk patients.
SumCY, YacobiA, KartzinelR, StampfliH, DavisCS, LaiC-M. Kinetics of esmolol, an ultra-short-acting beta blocker, and of its major metabolite.Clin Pharmacol Ther1983; 34: 427–34.
2.
GrayR, BatemanT, CzerL, ConklinC, MatloffJ. Esmolol—a new ultra short acting beta blocking agent for rapid control of heart rate in postoperative supraventricular tachyarrhythmias.J Am Coll Cardiol1985; 6: 1451–6.
3.
RevesJG, FlezzaniP. Perioperative use of esmolol.Am J Cardiol1985; 56: 57F–60F.
4.
MurthyVS, HwangT-F, SandageBW, LadduAR. Esmolol and the adrenergic responses to perioperative stimuli.J Clin Pharmacol1986; 26(suppl A): A27–A35.
5.
ShulmanB, ThysDM, GirardD. Hemodynamic effects of esmolol during anesthesia for myocardial revascularization (abstract).Anesthesiology1985; 63(3A): A64.
6.
LowenthalDJ, PorterRS, SarisSD. Clinical pharmacology, pharmacodynamics and interactions with esmolol.Am J Cardiol1985; 56: 14F–17F.
7.
ErhardtPW, WooCM, GorczynskiRJ, AndersonWG. Ultra-short-acting beta-adrenergic receptor blocking agents. 1. (Aryloxy) Propanolamines containing esters in the nitrogen substituent.J Med Chem1982; 25: 1402–7.
8.
ErhardtPW, WooCM, AndersonWG, GorczynskiRJ. Ultra-short acting beta-adrenergic receptor blocking agents. 2. (Aryloxy) Propanolamines containing esters on the aryl function.J Med Chem1982; 25: 1408–12.
9.
GreenspanAM, SeniorS, WebbCR, RaeAP, SokoloffNM, SpielmanSR. Electrophysiologic effects of esmolol: an ultra-short acting beta blocker (abstract).Circulation1984; 70: 441.
10.
GreenspanA, MorganrothJ, HorowitzL, SpielmanS, ZinsserS, SeniorS. Comparative electropharmacologic effects of esmolol, an ultra-short acting beta, blocking agent and propranolol in the therapy of atrial fibrillation.European Congress of Cardiology, Dusseldorf, Germany, July 8–12, 1984.
11.
ZarolinskiJ, BorgmanRJ, O'DONNELLJP. Ultra-short acting beta-blockers: a proposal for the treatment of the critically ill patient.Life Sci1982; 31: 899–907.
12.
KlonerRA, KirshenbaumJ, LangeR, AntmanEM, BraunwaldE. Experimental and clinical observations of the efficacy of esmolol in myocardial ischemia.Am J Cardiol1985; 56: 40F–48F.
13.
AndersonS, BlanskiL, ByrdRC. The Esmolol vs Placebo Multicenter Study Group. Comparison of the efficacy and safety of esmolol, a short-acting beta blocker, with placebo in the treatment of supraventricular tachyarrhythmias.Am Heart J1986; 111: 42–48.
14.
SheppardD, DistefonosS, ByrdRC. Effects of esmolol on airway function in patients with asthma.J Clin Pharmacol1986; 26: 169–74.
15.
RobertsonRM, WoodAJ, VaughnWK, RobertsonD. Exacerbation of vasomotonic angina pectoris by propranolol.Circulation1982; 65: 281–5.
16.
Norwegian Multicenter Study Group.Timolol-induced reduction in mortality and reinfarction in patients surviving acute myocardial infarction.N Engl J Med1981; 304: 801–7.
17.
Beta-Blocker Heart Attack Trial Research Group.A randomized trial of propranolol in patients with acute myocardial infarction: I. mortality results.JAMA1982; 247: 1707–14.
18.
HjalmarsonA, HerlitzJ, HolmbergS. The Goteborg metoprolol trial: effects on mortality and morbidity in acute myocardial infarction.Circulation1983; 67(suppl 1): 126–132.
19.
CranefieldPF. Action potentials, afterpotentials and arrhythmias.Circ Res1977; 41: 415–23.
20.
RosenMR, RederRF. Does triggered activity have a role in the genesis of cardiac arrhythmias?Ann Intern Med1981; 94: 794–801.
GibsonD, SowtonE. The use of beta-adrenergic receptor blocking drugs in dysrhythmias.Prog Cardiovas Dis1969; 12: 16–39.
23.
GettesLS, YoshonisKF. Rapid recurring supraventricular tachycardia: a manifestation of reciprocating tachycardia and an indication for propranolol therapy.Circulation1970; 41: 689–700.
24.
WellensHJJ, BarFWHM, LieKI. Effects of procainamide, propranolol and verapamil on mechanism of tachycardia in patients with chronic recurrent ventricular tachycardias.Am J Cardiol1977; 405: 579–85.
25.
GangES, BiggerJT, UhlEW. Effects of timolol and propranolol on inducible ventricular tachyarrhythmia in dogs with subacute myocardial infarction.Am J Cardiol1984; 53: 275–81.
26.
MenkhausPG, RevesJG, Kissini. Cardiovascular effects of esmolol in anesthetized humans.Anesth Analg1985; 64: 327–34.
27.
SafwatAM, ReitanJA, MisleGR. Use of propranolol to control rate-pressure product during cardiac anesthesia.Anesth Analg1981; 60: 732–5.
28.
BuhlerFR, BurkartF, LutoldF. Antihypertensive beta-blocking action as related to renin and age: a pharmacologic tool to identify pathogenic mechanisms in essential hypertension.Am J Cardiol1975; 36: 653–9.
29.
Medical Research Council Working Party.MRC trial of treatment of mild hypertension: principal results.Br Med J1985; 291: 97–104.
30.
GreenblattDJ, Koch-WeserJ. Adverse reactions to propranolol in hospitalized medical patients: a report from the Boston Collaborative Drug Surveillance Program.Am Heart J1973; 86: 478–84.
31.
BrandfonbrenerM, LandowneM, ShockNW. Changes in cardiac output with age.Circulation1975; 12: 557–66.
32.
MannDL, DenenbergBS, GashAK, MaklerPT, BoveAA. Effects of age on ventricular performance during graded supine exercise.Am Heart J1986; 111: 108–15.
33.
NixonJV, HallmarkH, PageK, RavenPR, MitchellJH. Ventricular performance in human hearts aged 61 to 73 years.Am J Cardiol1985; 56: 932–7.
34.
KendallMJ, WoodKL, WilkinsMR, WorthingtonDJ. Responiveness to beta-adrenergic receptor stimulation: the effects of age are cardioselective.Br J Clin Pharmacol1982; 14: 821–2.
35.
VestalRE, WoodAJJ, WoodMB. Reduced beta-adrenoreceptor sensitivity in the elderly.Clin Pharmacol Ther1979; 26: 181–6.
36.
FleischJH, MalingHM, BrodieBB. Beta receptor activity in aorta. Variations with age and species.Circulation Res1970; 26: 151–62.
37.
McgarryK, LaherM, FitzgeraldD, HoganJ., O'BRIENE, O'MALLEYK. Baroreceptor function in elderly hypertensives.Hypertension1983; 5: 763–6.
38.
RigbyJW, ScottAK, HawksworthGM, PetrieJC. A comparison of the pharmacokinetics of atenolol, metoprolol, oxprenolol and propranolol in elderly hypertensive and young healthy subjects.Br J Clin Pharmacol1985; 20: 327–31.
39.
CastledenCM, KayeCM, ParsonsRL. The effects of age on plasma levels of propranolol and practolol in man.Br J Clin Pharmacol1975; 2: 303–6.
40.
PieperJA. Serum protein binding interactions between propranolol and calcium channel blockers (abstract).Drug Intell Clin Pharm1984; 18: 492.
41.
O'MALLEYK, CrooksJ, DukeE, StevensonIH. Effects Of age and sex on drug metabolism.Br Med J1971; 3: 607–9.
42.
AbramsJ, AllenJ, AllinD. The Esmolol Multicenter Study Research Group. Efficacy and safety of esmolol vs. propranolol in the treatment of supraventricular tachyarrhythmias: a multicenter double blind clinical trial.Am Heart J1985; 110: 913–22.
43.
MorganrothJ, HorowitzLN, AndersonJ, TurlapatyP. The Esmolol Research Group. Comparative efficacy and tolerance of esmolol to propranolol for control of supraventricular tachyarrhythmias.Am J Cardiol1985; 56: 33F–39F.
44.
MurthyVS, HwangT-F, ZagarME. Cardiovascular pharmacology of ASL-8052, an ultra-short acting beta blocker.Eur J Pharmacol1983; 94: 43–51.
45.
MichelsonEL, PorterfieldJK, DasG. A comparison of esmolol and verapamil in the treatment of atrial fibrillation/flutter (abstract).J Am Coll Cardiol1986; 7: 157A.
46.
LangeR, KlonerR, BraunwaldE. First ultra-short-acting beta adrenergic blocking agent: its effect on size and segmental wall dynamics of reperfused myocardial infarcts in dogs.Am J Cardiol1983; 51: 1759–67.
47.
SungRJ, BlanskiL, KirshenbaumJ. Clinical experience with esmolol, a short-acting beta adrenergic blocker in cardiac arrhythmias and myocardial ischemia.J Clin Pharmacol1986; 26(suppl A): A15–A26.
48.
ReidLC, BraceDE. Irritation of respiratory tract and its reflex effect on heart.Surg Gynecol Obstet1940; 70: 157–62.
49.
BurstenCL, Lo PintoFJ, NewmanW. Electrocardiographic studies during endotracheal intubation: I. effects during usual routine techniques.Anesthesiology1950; 11: 224–37.
50.
TomoriZ, WiddicombeJG. Muscular, bronchomotor and cardiovascular reflexes elicited by mechanical stimulation of the respiratory tract.J Physiol1969; 200: 25–49.
51.
KingBD, HarrisLC, GreifensteinFE. Reflex circulatory responses to direct laryngoscopy and tracheal intubation performed during general anesthesia.Anesthesiology1951; 12: 556–66.
52.
RussellWJ, MorrisRG, FrewinDB. Changes in plasma catecholamine concentrations during endotracheal intubation.Br J Anaesth1981; 53: 837–9.
53.
CorkRC, WeissJL, HameroffSR. Fentanyl preloading for rapid-sequence induction of anesthesia.Anesth Analg1984; 63: 60–4.
54.
HoarPF, NelsonNT, ManganoDT. Adrenergic response to morphine-diazepam anesthesia for myocardial revascularization.Anesth Analg1981; 60: 406–11.
55.
FoexP., Prys-RobertsC. Anesthesia and the hypertensive patient.Br J Anaesth1974; 46: 575–88.
56.
FoxEJ, SklarGS, HillCH. Complications related to the pressor response to endotracheal intubation.Anesthesiology1977; 47: 524–5.
57.
SlogoffS, KeatsA. Does perioperative myocardial ischemia lead to postoperative myocardial infarction?Anesthesiology1985; 62: 107–14.
58.
MenkhausPG, RevesJG, KissinI. Cardiovascular effects of esmolol in anesthetized humans.Anesth Analg1985; 64: 327–34.
59.
KorenagaGM, KirkpatrickA, LordJC. Effect of esmolol on tachycardia induced by endotracheal intubation (abstract).Anesth Analg1985; 64: 238.
60.
NewsomeLR, RothJ, HugCJr, NagleD. Esmolol attenuates hemodynamic responses to intubation and surgical stimulation during open heart surgery (abstract).Anesthesiology1985; 63: A62.
61.
GaryRJ, BatemanTM, CzerLSC, ConklinC, MatloffJM. Use of esmolol in hypertension after cardiac surgery.Am J Cardiol1985; 56: 49F–56F.
