Esmolol, an ultrashort-acting, selective β1-adrenoceptor antagonist: pharmacodynamic and pharmacokinetic properties

@article{VolzZang2004EsmololAU,
  title={Esmolol, an ultrashort-acting, selective $\beta$1-adrenoceptor antagonist: pharmacodynamic and pharmacokinetic properties},
  author={Corinna Volz‐Zang and Bridget Eckrich and P. Jahn and B. Schneidrowski and Britta Schulte and Dieter Palm},
  journal={European Journal of Clinical Pharmacology},
  year={2004},
  volume={46},
  pages={399-404}
}
The effects of esmolol at different rates of infusion (100, 250 and 500 μg·kg−1 BW·min−1) were compared with β-adrenoceptor occupancy (β1 and β2, 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 μg·kg−1 BW·min−1 there was a maximal β1-receptor occupancy of 84.7% while β2-receptor occupancy was below the detection limit; confirming the β1 selectivity of esmolol… 
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Esmolol infusion versus propranolol infusion: effects on heart rate and blood pressure in healthy volunteers.
TLDR
Test data indicate that infusion of ~160 mg of esmolol acutely and selectively blocks β1-adrenergic receptors in healthy humans, and changes in femoral blood flow and hematological parameters in response to epinephrine infusion were not different between es Molol and saline infusion, indicating that the esmoll infusion paradigm does not block β2-receptors.
Dobutamine Alters the Pharmacokinetic and Pharmacodynamic Behavior of Esmolol
TLDR
The accelerated elimination of esmolol was likely due to higher cleavage through tissue esterases induced by dobutamine-induced increased tissue passage cycles per time unit, and the HR effect was characteristic of a beta-blocker, whereas the blood pressure effect was probably due to a mechanism other than direct Beta-blockade.
Neuroprotective effects of selective beta-1 adrenoceptor antagonists, landiolol and esmolol, on transient forebrain ischemia in rats; a dose–response study
EFFECT OF ESMOLOL ON FLUID THERAPY IN NORMOVOLEMIA AND HYPOVOLEMIA
TLDR
It is suggested that esmolol impairs the vascular retention of fluid and may increase the amount of volume support during fluid resuscitation.
Nociceptive Effects of Locally Treated Metoprolol
TLDR
The results can demonstrate that peripheral β-adrenergic receptors can play important roles in nociceptive process and suggest that locally treated metoprolol may cause hyperalgesic and allodynic actions.
Effects of esmolol on systemic and pulmonary hemodynamics and on oxygenation in pigs with hypodynamic endotoxin shock
TLDR
In large animals with endotoxemic shock, continuous infusion of esmolol, a selective beta-1 adrenergic blocker, titrated to decrease heart rate by 20%, was well tolerated and may offset LPS-induced cardiac dysfunction by a preload positive effect.
Bolus application of landiolol and esmolol: comparison of the pharmacokinetic and pharmacodynamic profiles in a healthy Caucasian group
TLDR
Compared to esmolol, landiolol shows a more prominent and pronounced bradycardic effect in relation to its blood pressure-lowering effect, an action profile that might be of specific advantage in the perioperative setting.
High‐Dose Glucagon Has Hemodynamic Effects Regardless of Cardiac Beta‐Adrenoceptor Blockade: A Randomized Clinical Trial
TLDR
High‐dose glucagon boluses had significant hemodynamic effects regardless of beta‐blockade, and a glucagon infusion had comparable and apparently longer‐lasting effects compared with bolus, indicating that infusion may be preferable to bolus injections.
Comparative effects of ultra-short-acting β1-blockers on voltage-gated tetrodotoxin-resistant Na+ channels in rat sensory neurons
TLDR
Esmolol, but not landiolol, may have useful effects against pain related to TTX-r Na+ channel activity, and is compared with ultra-short-acting β1-blockers on tetrodotoxin-resistant sodium channels in rat dorsal root ganglion neurons, which are important for nociception.
Role of the β1-Adrenergic Pathway in Anesthetic and Ischemic Preconditioning against Myocardial Infarction in the Rabbit Heart In Vivo
TLDR
The results demonstrate that anesthetic preconditionsing is mediated by the β1-adrenergic pathway, whereas this pathway is not essential for ischemic preconditioning.
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References

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Beta-adrenoreceptor antagonist potency and pharmacodynamics of ASL-8123, the primary acid metabolite of esmolol.
TLDR
ASL-8123 is a weak beta-adrenoreceptor antagonist which is approximately 1,600-1,900 times less potent than its parent, esmolol.
Esmolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy.
TLDR
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-adsenoceptor antagonism for short durations.
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TLDR
Esmolol was followed by a significant reduction of isoproterenol‐induced increase in heart rate and systolic blood pressure at doses of 50, 150, and 400 μg/kg/min, indicating that nonhepatic routes play a predominant role in its clearance.
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TLDR
Esmolol appears to be a potent β1‐selective adrenoceptor antagonist with a particularly strong hypotensive effect and 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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TLDR
Esmolol dosage would probably not require adjustment in patients with renal failure maintained on hemodialysis or CAPD, and ASL‐8123 has shown very limited β‐blocking activity in animals and human beings and its toxicity is currently unknown.
Effects of bolus injection of esmolol in healthy, exercising subjects
TLDR
The rapid onset and disappearance of esmolol effects may make it an appealing drug in acute care settings, and this study investigated the effect of a bolus dose of es Molol on heart rate, blood pressure, and PR interval in healthy, exercising male subjects.
Beta adrenoceptor subtype binding activity in plasma and beta blockade by propranolol and beta-1 selective bisoprolol in humans. Evaluation with Schild-plots.
TLDR
In vitro receptor occupancy can predict beta blockade in humans for propranolol and a selective antagonist and a refined analysis of Schild-plot data is concluded.
Esmolol‐Digoxin Drug Interaction
TLDR
Although digoxin did not influence the kinetics of esmolol, the small increase seen in digoxin serum concentration during the combination therapy warrants that caution be exercised during concurrent administration of es Molol and digoxin to patients.
Esmolol: a short-acting titratable beta-blocker in acute myocardial ischemia.
TLDR
A brief summary of the pharmacology of esmolol, as well as experimental and clinical evidence on the use of es Molol in acute myocardial ischemia are provided.
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