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… 
Esmolol infusion versus propranolol infusion: effects on heart rate and blood pressure in healthy volunteers.
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TLDR
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References

SHOWING 1-10 OF 31 REFERENCES
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.
Kinetics of esmolol, an ultra‐short‐acting beta blocker, and of its major metabolite
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.
Ultra‐short‐acting beta‐blockade: A comparison with conventional beta‐blockade
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.
Esmolol: a titratable short-acting intravenous beta blocker for acute critical care settings.
Pharmacokinetics of esmolol and ASL‐8123 in renal failure
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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