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Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Esmolol is a beta 1-selective adrenoceptor blocker that is rapidly metabolized by blood and liver esterases. The beta-receptor and hemodynamic effects of esmolol were determined in a group of 12 healthy men and were compared with those induced by both oral and intravenous propranolol. Esmolol was rapidly effective in inducing at least 90% of steady-state beta-blockade within 5 minutes of either initiating or changing the esmolol infusion rate. More importantly, when esmolol infusion was discontinued the beta-blockade had totally disappeared by 18 minutes after esmolol, 300 micrograms/kg/min, and had been reduced by 50% after 750 micrograms/kg/min. In contrast, 30 minutes after discontinuation of a propranolol infusion, there was no change in the level of beta-blockade. Propranolol was much more potent at blocking isoproterenol-induced tachycardia (dose ratio 33.5 +/- 2.5) than was even the highest dose (750 micrograms/kg/min) of esmolol (dose ratio 13.1 +/- 1.0). The same dose of intravenous propranolol was approximately equipotent to oral propranolol, 40 mg every 8 hours (dose ratio 33.5 +/- 2.5 and 34.5 +/- 3.6, respectively). In contrast, propranolol, 40 mg every 8 hours, and esmolol, 300 micrograms/kg/min, were equipotent in antagonizing exercise-induced tachycardia (40.1% +/- 2.3% and 42.7% +/- 3.2%, respectively). Esmolol had striking hypotensive effects. Systolic blood pressure fell by 20 mm Hg during esmolol infusions of 750 micrograms/kg/min. Esmolol appears to be a potent beta 1-selective adrenoceptor antagonist with a particularly strong hypotensive effect. It is likely to be very useful in the treatment of hemodynamically unstable patients and may be useful in the emergency treatment of hypertension.
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PMID:Ultra-short-acting beta-blockade: a comparison with conventional beta-blockade. 286 29

Sixteen subjects scheduled for surgical procedures under general anesthesia participated in an investigation of the effects of esmolol on the transient hypertension and tachycardia that was observed during endotracheal intubation and on the duration of succinylcholine-induced neuromuscular blockade. In eight subjects, infusion of esmolol was begun five minutes before induction of anesthesia and continued for 12 minutes after induction. In the remaining subjects, an equivalent volume of solvent (D5W) was infused for 12 minutes. Infusion of esmolol significantly attenuated the cardioacceleration observed during intubation without any significant effect on the pressor effects of the procedure. Esmolol delayed the recovery from succinylcholine-induced neuromuscular blockade by less than three minutes. The mechanism of this delay remains to be investigated, although such a delay does not have clinical significance. Esmolol-induced attenuation of the tachycardia seen during intubation may offer a protective effect on the myocardium, especially in elderly subjects and patients with coronary artery disease.
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PMID:Cardiovascular and neuromuscular effects of esmolol during induction of anesthesia. 287 Oct 54

The chemistry, pharmacology, pharmacokinetics, hemodynamic and electrophysiologic effects, clinical efficacy, adverse effects, drug interactions, compatibility and stability, dosage, and administration of esmolol hydrochloride are reviewed. Esmolol produces competitive blockade of beta receptors in both animals and humans. It does not possess membrane-stabilizing, intrinsic sympathomimetic, or alpha-adrenergic blocking activity. The relative cardioselectivity of esmolol is similar to that of metoprolol. Esterase metabolism accounts for the rapid total body clearance of 285 mL/kg/min and elimination half-life of 9.2 minutes. Its rapid metabolism following continuous intravenous infusion results in the rapid offset of pharmacologic effect after drug administration is discontinued. In patients with supraventricular tachyarrhythmias, esmolol produces rapid control of heart rate in an average effective dosage range from 97.2 to 115.0 micrograms/kg/min and effects that are similar to propranolol. Esmolol is effective and safe in managing tachycardia and hypertension during surgical stress and may be useful in postoperative hypertension or elevated heart rates during myocardial ischemia. Esmolol does not appear to interact with digoxin, morphine, warfarin, or succinylcholine to any clinically important extent. The most frequent adverse effects associated with esmolol infusion are hypotension and phlebitis. Hypotension can be avoided by careful titration, and if encountered, it can be rapidly resolved by dosage adjustment or discontinuation of the infusion. The ultrashort half-life and duration of action of esmolol may allow safer application of beta blockade in critically ill patients.
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PMID:Esmolol hydrochloride: an ultrashort-acting, beta-adrenergic blocking agent. 287 61

Because acute systemic hypertension early after cardiac surgery has been linked to catecholamine elevation, an open-label, randomized, crossover study was performed to compare the efficacy of esmolol, a new ultra-short-acting intravenous beta-blocking agent, to nitroprusside, the standard therapy. Controlled drug infusions to maximal dosage (esmolol, 300 micrograms/kg/min, and nitroprusside, 10 micrograms/kg/min) were titrated to achieve at least a 15% reduction in systolic pressure. The blood pressure (BP) endpoint was achieved with esmolol (within 29 +/- 14 minutes) in 18 of 20 patients (90%), compared with 19 of 20 (95%) with nitroprusside infusion (within 21 +/- 15 minutes, difference not significant [NS]). Systolic BP decreased from 170 +/- 13 to 136 +/- 12 mm Hg (mean +/- standard deviation) with esmolol and from 170 +/- 13 to 141 +/- 13 mm Hg with nitroprusside infusion (both p less than 0.05). Diastolic BP was reduced from 71 +/- 12 to 64 +/- 11 mm Hg with esmolol and from 71 +/- 12 to 52 +/- 13 mm Hg with nitroprusside infusion (both p less than 0.05). Esmolol infusion resulted in decreased heart rate, cardiac index and stroke volume index and increased right atrial pressure (all p less than 0.05), whereas nitroprusside infusion resulted in increased heart rate and cardiac index and decreased right atrial pressure, pulmonary arterial wedge pressure and systemic vascular resistance (p less than 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Comparison of esmolol and nitroprusside for acute post-cardiac surgical hypertension. 288 81

Esmolol is an ultrashort-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.
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PMID:Esmolol: a novel cardioselective, titratable, intravenous beta-blocker with ultrashort half-life. 288 93

Esmolol is a relatively cardioselective beta-adrenoceptor antagonist. Since esmolol is rapidly metabolised by blood-borne esterases, it has a very short half-life (about 9 mins) and a short duration of action. In this respect esmolol is unique amongst currently available beta-adrenoceptor antagonists, and it is anticipated that it will be particularly useful in critical care situations where administration by continuous intravenous infusion should permit a level of control over beta-adrenoceptor antagonism that has previously been unattainable. In perioperative settings, esmolol attenuates tachycardia induced by a variety of surgical stimuli such as endotracheal intubation, sternotomy and aortic dissection, suggesting a clinical use of the drug to prevent potentially serious complications in surgical patients with cardiovascular disease. Additionally, clinical studies have shown that titrated dosages of esmolol achieved therapeutic response rates of 66 to 79% in patients with supraventricular tachyarrhythmias, which favourably compared with response rates achieved with propranolol. In most of these patients esmolol produced a reduction in ventricular rate which was well maintained during infusion but disappeared within 30 minutes following esmolol withdrawal. Preliminary studies involving small numbers of patients have reported that esmolol exerts significant antihypertensive effects in patients with postoperative hypertension, and beneficial effects in patients with myocardial ischaemia and infarction, but support for these results is required from additional large, well-controlled studies. Esmolol has been generally well tolerated, and although hypotension has occurred in up to 44% of patients it resolved during or soon after the infusion of esmolol. Thus, esmolol is the first titratable beta-adrenoceptor antagonist able to be rapidly 'switched on' and 'off', a property that is expected to offer a major contribution to safety in critical care patients requiring beta-adrenoceptor antagonism for short durations.
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PMID:Esmolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy. 288 68

Esmolol (Brevibloc) is an intravenous, short-acting, titratable, cardioselective beta blocker with a very rapid onset and offset of action (t1/2 = 9.2 minutes). Esmolol-induced beta blockade can be maintained as long as infusion is continued. It exhibits neither intrinsic sympathomimetic activity nor significant membrane-stabilizing activity. It is rapidly metabolized by an esterase in the erythrocyte cytosol to an inactive acid metabolite. Its hemodynamic and electrophysiologic effects are similar to those of other beta blockers. Unlike the effects of other beta blockers, however, the effects of esmolol dissipate rapidly to baseline within 30 minutes after its discontinuation. Evidence obtained from clinical studies indicates that esmolol is effective and safe in reducing the ventricular rate in patients with supraventricular tachyarrhythmias, and in reducing the heart rate in patients with acute myocardial infarction and/or unstable angina. Esmolol has also been shown to be effective and safe in attenuating the tachycardia and hypertension seen during the intraoperative period. Data from postoperative patients indicate that esmolol is ideal as sole-agent therapy for the treatment of moderate postoperative hypertension associated with a hyperdynamic state. The short duration of action and titratability of esmolol make it an ideal drug for use in patients in whom the clinical need for beta blockade is limited in duration, and it offers additional safety in patients in whom beta blockade is beneficial; however, it might be precluded because of coexisting contraindications. To date, experience with esmolol in over 1200 patients has been gathered, and the adverse effect profile is basically similar to that reported here.
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PMID:Esmolol: a titratable short-acting intravenous beta blocker for acute critical care settings. 288 41

Esmolol is a new intravenous beta-adrenergic blocker with an ultrashort (nine-minute) elimination half-life, which has been studied predominantly for control of supraventricular tachycardia and management of certain types of hypertension. Clinical studies indicate that the efficacy of esmolol is equivalent to that of propranolol and verapamil for control of supraventricular tachycardia and to sodium nitroferricyanide (sodium nitroprusside) for control of postoperative hypertension. Esmolol also has been shown to control heart rate and blood pressure during episodes of acute myocardial ischemia. Cardioselectivity is similar to that of metoprolol, and the ability to titrate the effect of esmolol may provide additional assurance that beta-adrenergic blockade will remain within the cardioselective range. The most commonly observed adverse effect seen in clinical trials was asymptomatic hypotension. Hypotension may be minimized by titrating to the minimum effective dose and is readily reversed within 10 to 30 minutes of discontinuing the infusion of esmolol. These unique features represent advantages of great potential merit in critical care medicine.
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PMID:Managing critically ill patients with esmolol. An ultra short-acting beta-adrenergic blocker. 289 47

The ultra-short-acting beta-adrenergic blockers are parenteral agents that can be rapidly titrated in clinical situations where immediate beta-adrenergic blockade is warranted. The effects of those drugs rapidly dissipate after termination of treatment, providing an important safety feature. Esmolol, the prototype drug of this class, is approved for treatment of supraventricular tachyarrhythmias but also has potential use in treatment of patients with perioperative hypertension and acute myocardial ischemia.
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PMID:Ultra-short-acting beta-adrenergic blockers. 289 87

We sought to evaluate the effectiveness of esmolol vs placebo in 40 patients emerging from general anesthesia for neurosurgery. Efficacy was defined as a decrease in systolic blood pressure to within 20% above average ward pressure. The need for additional antihypertensive agents to control blood pressure was also used to define efficacy. During the infusion period 20 of 21 (95%) of the esmolol-treated patients and two of 19 (11%) of the patients receiving placebo had return of systolic blood pressure to within 20% of average ward pressure (p less than 0.001). One out of 21 (5%) esmolol-treated patients and 14 of 19 (74%) of the placebo group required intervention with additional antihypertensive medications (p less than 0.001). Esmolol was found to be effective in controlling hypertension that develops on emergence from general anesthesia in patients undergoing neurosurgery.
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PMID:Esmolol for the control of hypertension after neurologic surgery. 290 10


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