Ultra-short acting beta-blockers: A proposal for the treatment of the critically ill patient

Zaroslinski, John F.; Borgman, Robert J.; O’Donnell, John P.; Anderson, W. Gary; Erhardt, Paul; Kam, Sheung-Tsam; Reynolds, Robert D.; Lee, Robert J.; Gorczynski, Richard J.

doi:10.1016/0024-3205(82)90547-1

Cited by 71 publications

(14 citation statements)

References 18 publications

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“…Thus the effective beta-blocking dose range of esmolol is between 5.0 and 160 pg/kg/min; a dose of 30 to 50 pg/kg/min is generally found to produce 50% blockade of cardiac responses to large but submaximal doses of catecholamines. The cardioselectivity of esmolol observed in vitro was confirmed in vivo using a constant flow, perfused hindlimb preparation in pentobarbital-anesthetized, ganglion-blocked dogs (14,41). A submaximal dose of isoproterenol (0.27 pg/kg) was administered intravenously before and during constant intravenous infusion of esmolol.…”

Section: Beta-blockade and Duration Of Actionmentioning

confidence: 83%

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Esmolol

Gorczynski¹,

Quon²,

Krasula³

et al. 1985

Cardiovascular Drug Reviews

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Section: Beta-blockade and Duration Of Actionmentioning

confidence: 83%

“…To facilitate safe, rapid induction of beta-blockade in acute therapy situations, American Critical Care has introduced the concept of ultrashort-acting beta-blockers (41). Recent reports (7-9,16) have outlined molecular approaches toward the design of metabolically labile beta-blockers.…”

mentioning

confidence: 99%

Esmolol

Gorczynski¹,

Quon²,

Krasula³

et al. 1985

Cardiovascular Drug Reviews

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“…Although esmolol is of clinical interest and its betablocking potency and "cardioselectivity" have been evaluated using standard procedures both in vitro and in vivo [3,18]; radioligand binding studies have revealed the 30-to 40-fold higher affinity of esmolol for/31-adrenoceptors than for/32-adrenoceptors [19]. The acid metabolite of esmolol had a 400-fold lower affinity than the parent compound.…”

Section: Esmolol (Methyl 3-[4-[2-hydroxy-3-(isopropylamino)mentioning

confidence: 99%

Esmolol, an ultrashort-acting, selective ?1-adrenoceptor antagonist: pharmacodynamic and pharmacokinetic properties

Volz-Zang

Eckrich

Jahn

et al. 1994

Eur J Clin Pharmacol

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The effects of esmolol at different rates of infusion (100, 250 and 500 micrograms.kg-1 BW.min-1) were compared with beta-adrenoceptor occupancy (beta 1 and beta 2, estimated by a subtype selective radioreceptor assay) and plasma concentrations of esmolol and its acid metabolite were measured by HPLC. Up to a rate of infusion of esmolol of 500 micrograms.kg-1 BW.min-1 there was a maximal beta 1-receptor occupancy of 84.7% while beta 2-receptor occupancy was below the detection limit; confirming the beta 1 selectivity of esmolol. Exercise-induced increases in heart rate and systolic blood pressure were reduced by esmolol in a dose-dependent manner. The estimated EC50 values of rate of infusion for the reduction in heart rate and systolic blood pressure during exercise were 113 and 134 micrograms.kg-1 BW.min-1, respectively. Additionally, heart rate and systolic blood pressure were reduced moderately at rest. Because of the short elimination half-life of esmolol caused by the rapid hydrolysis to its acid metabolite, 45 min after end of infusion high plasma concentrations of the metabolite (maximally 80 micrograms.ml-1) but no esmolol were detectable. Since no in vivo effects have been observed, despite the presence of high plasma concentrations of the metabolite, the metabolite did not participate in the observed effects up to an infusion rate of esmolol of 500 micrograms.kg-1 BW.min-1. The plasma concentrations of antagonist detected by radioreceptor assay and plasma concentrations of esmolol detected by HPLC showed a good correlation (r = 0.97).(ABSTRACT TRUNCATED AT 250 WORDS)

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“…It has a plasma half-life of approximately 10 min and is available only in parenteral form [36]. The drug appears to be metabolized by blood, tissue, and hepatic esterases.…”

Section: Esmolol -Ultrashort-acling ¡I-blockermentioning

confidence: 99%

Beta-Adrenergic Blockade

Frishman¹,

Teicher²

1985

Cardiology

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β-Adrenergic blockade represents a major pharmacologic advance. These drugs bind to membrane adrenergic receptors interfering with the effects of endogenous catechol-amines. Eight β-blockers are available in the United States, and others are being studied. The drugs have varying pharmacodynamic properties that may modify certain side effects: β₁- selectivity, partial agonism, alpha-adrenergic blocking activity, membrane stabilization, and varying pharmacokinetic characteristics. The drugs have been shown to be relatively safe and useful for a wide variety of cardiovascular and noncardiovascular disease states, and their wide spectrum of therapeutic activity illustrates the importance of the sympathetic nervous system in the pathophysiology of medical illness.

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Ultra-short acting beta-blockers: A proposal for the treatment of the critically ill patient

Cited by 71 publications

References 18 publications

Esmolol

Esmolol

Esmolol, an ultrashort-acting, selective ?1-adrenoceptor antagonist: pharmacodynamic and pharmacokinetic properties

Beta-Adrenergic Blockade

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