Dobutamine Alters the Pharmacokinetic and Pharmacodynamic Behavior of Esmolol

Krumpl, Günther; Ulč, Ivan; Trebs, Michaela; Hodisch, Juri; Kadlecová, Pavla; Husch, Bernhard

doi:10.7759/cureus.12217

Cited by 1 publication

(3 citation statements)

References 28 publications

(48 reference statements)

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“…The pharmacokinetic results and individual PD results have already been published separately. 26,27 One key finding was that the elimination of esmolol, and less so of landiolol, is accelerated in the presence of dobutamine, which has a marked effect on steady-state concentrations. This report focuses on the PD differences between the 2 drugs.…”

Section: Discussionmentioning

confidence: 99%

“…Between March and September 2011, we performed a prospective, randomized, double-blinded, single-center clinical trial with 2 crossover-periods at the Center for Pharmacology and Analysis (CEPHA s.r.o. ), Plze ň, Czech Republic, in compliance with the respective study protocol, the Declaration of Helsinki, and Good Clinical Practice and Good Laboratory Practice guidelines, as well as other applicable international and national regulatory requirements and local laws after 27…”

Section: Methodsmentioning

confidence: 99%

“…The pharmacokinetic results obtained in this study have been published elsewhere. 26,27 A key finding was the fact that the pharmacokinetics of both β-blockers are affected in the presence of dobutamine, which results in a marked reduction of steady-state concentrations. The steady-state concentrations of esmolol and landiolol in the presence of dobutamine are ≈120 ng/mL and ≈160 ng/mL, respectively, whereas in an earlier head-to-head comparison between esmolol and landiolol under similar conditions but without dobutamine, the steady-state concentrations had been ≈200 ng/mL for both drugs.…”

Section: Pharmacokineticsmentioning

confidence: 99%

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Blood Pressure Recovery After Dobutamine Antagonism: Partial With Landiolol, None With Esmolol

Krumpl¹,

Ulč²,

Trebs

et al. 2021

Clinical Pharm in Drug Dev

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We investigated the hemodynamic effects of 2 short-acting β 1 -blockers,landiolol and esmolol,in the continuous presence of dobutamine in a prospective, single-center, randomized, crossover study in 16 healthy White volunteers. Dobutamine was infused at a rate sufficient to increase the heart rate by at least 30 beats per minute, followed by a 60-minute infusion of 50 μg/kg/min esmolol or 10 μg/kg/min landiolol on top of the unchanged dobutamine infusion. Concentrations of β-blockers and their metabolites in blood, heart rate, and blood pressure were followed for 180 minutes. Landiolol reduced the dobutamine-induced heart rate and blood pressure increases better than esmolol. After discontinuation of β-blocker administration, heart rate recovered swiftly to preinfusion values in both study arms. Systolic and diastolic blood pressure recovered partially after landiolol but showed a continued reduction after esmolol. No serious adverse events were observed. The heart rate effect is characteristic for β-blockers, whereas the blood pressure effects are likely due to direct and indirect β-blocker effects as well as influences on various ion channels. This may explain why landiolol that is devoid of effects on renin and sodium, calcium, and potassium channels behaves different from esmolol with respect to blood pressure recovery.

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Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Pharmacokineticsmentioning

confidence: 99%

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