Pharmacokinetics of Esmolol in Anesthetized Patients Receiving Chronic Beta Blocker Therapy

Bruljn, N. P. de; Rêves, J. G.; Croughwell, Narda D.; Clements, Fiona M.; Drissel, Debra

doi:10.1097/00000542-198703000-00010

Cited by 24 publications

(5 citation statements)

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“…The V 1 in the present study was lower than that in the previous study (101 ± 8.83 vs 74.9 ± 13.2 mL/kg). Another reason for underestimation might be the CL difference between healthy volunteers and gynecologic patients, since the clearance of esmolol in anesthetized patients has been reported to be lower than that in unanesthetized healthy male volunteers [16]. However, the clearance values obtained for healthy volunteers and gynecology patients were similar (36.6 ± 1.23 vs 34.0 ± 1.96 mL/min/kg).…”

Section: Discussionmentioning

confidence: 94%

Target-controlled infusion and population pharmacokinetics of landiolol hydrochloride in gynecologic patients

et al. 2014

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Section: Discussionmentioning

confidence: 94%

Target-controlled infusion and population pharmacokinetics of landiolol hydrochloride in gynecologic patients

et al. 2014

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“…Pharmacokinetic parameters for esmolol have been studied in healthy subjects and in patients with various diseases, and it is now established that its half-life and volume of distribution are approximately 10 min and 2 l/ kg, respectively (6,15,16). Clinical application of esmolol is maintained in the low micromolar range in plasma, and Sintetos et al (17) reported that a bolus injection of 30 -150 mg esmolol resulted in a blood concentration of 0.8 -1.5 μg/ml (2.4 -4.5 μM).…”

Section: Discussionmentioning

confidence: 99%

Direct Effects of Esmolol and Landiolol on Cardiac Function, Coronary Vasoactivity, and Ventricular Electrophysiology in Guinea-Pig Hearts

et al. 2012

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Abstract. The ultra-short acting, selective β 1 -adrenergic antagonists landiolol and esmolol are widely used perioperatively; however, little is known about their acute direct actions on the heart. The current study utilized the Langendorff perfused heart system to measure changes in cardiac function and hemodynamics in response to each drug. Furthermore, electrophysiological analysis was performed on isolated ventricular myocytes. Direct application of esmolol significantly decreased systolic left ventricular pressure and heart rate at concentrations > 10 μM, while it dosedependently increased coronary perfusion pressure. Esmolol also shortened the action potential duration (APD) in a concentration-dependent manner, an action maintained even when the delayed rectifier K + current or ATP sensitive K + current was blocked. Moreover, esmolol inhibited both the inward rectifier K + current (I K1 ) and the L-type Ca 2+ current (I CaL ) and increased the outward current dose-dependently. In contrast, landiolol had minimal cardiac effects. In the Kyoto Model computer simulation, inhibition of either I K1 or I CaL alone failed to shorten the APD; however, an additional increase in the time-independent outward current caused shortening of the APD, equal to that induced by esmolol. In conclusion, esmolol directly inhibits cardiac performance significantly more so than landiolol, an effect revealed to be at least in part mediated by esmolol-induced APD shortening.

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“…The resulting solutions were applied to the membrane preparations so that a final concentration of drugs was 0.5–200 μM. These drug concentrations were chosen because the tested β 1 -blockers were reported to show blood concentrations of a micromolar level in their pharmacokinetic studies (de Bruijn et al, 1987; Murakami et al, 2005). The concentration of DMSO was adjusted to be 0.25% (v/v) of the total volume so as not to affect the fluidity of intact membranes.…”

Section: Methodsmentioning

confidence: 99%

Characteristic interactivity of landiolol, an ultra-short-acting highly selective β1-blocker, with biomimetic membranes: Comparisons with β1-selective esmolol and non-selective propranolol and alprenolol

Tsuchiya

Mizogami

2013

Front. Pharmacol.

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Although β1-blockers have been perioperatively used to reduce the cardiac disorders associated with general anesthesia, little is known about the mechanistic characteristics of ultra-short-acting highly selective β1-blocker landiolol. We studied its membrane-interacting property in comparison with other selective and non-selective β1-blockers. Biomimetic membranes prepared with phospholipids and cholesterol of varying compositions were treated with β1-selective landiolol and esmolol and non-selective propranolol and alprenolol at 0.5–200 μM. The membrane interactivity and the antioxidant activity were determined by measuring fluorescence polarization and by peroxidizing membrane lipids with peroxynitrite, respectively. Non-selective β1-blockers, but not selective ones, intensively acted on 1,2-dipalmitoylphosphatidylcholine (DPPC) liposomal membranes and cardiomyocyte-mimetic membranes to increase the membrane fluidity. Landiolol and its inactive metabolite distinctively decreased the fluidity of DPPC liposomal membranes, suggesting that a membrane-rigidifying effect is attributed to the morpholine moiety in landiolol structure but unlikely to clinically contribute to the β1-blocking effect of landiolol. Propranolol and alprenolol interacted with lipid raft model membranes, whereas neither landiolol nor esmolol. All drugs fluidized mitochondria-mimetic membranes and inhibited the membrane lipid peroxidation with the potency correlating to their membrane interactivity. Landiolol is characterized as a drug devoid of the interactivity with membrane lipid rafts relating to β2-adrenergic receptor blockade. The differentiation between β1-blocking selectivity and non-selectivity is compatible with that between membrane non-interactivity and interactivity. The mitochondrial membrane fluidization by landiolol independent of blocking β1-adrenergic receptors is responsible for the antioxidant cardioprotection common to non-selective and selective β1-blockers.

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Pharmacokinetics of Esmolol in Anesthetized Patients Receiving Chronic Beta Blocker Therapy

Cited by 24 publications

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Target-controlled infusion and population pharmacokinetics of landiolol hydrochloride in gynecologic patients

Target-controlled infusion and population pharmacokinetics of landiolol hydrochloride in gynecologic patients

Direct Effects of Esmolol and Landiolol on Cardiac Function, Coronary Vasoactivity, and Ventricular Electrophysiology in Guinea-Pig Hearts

Characteristic interactivity of landiolol, an ultra-short-acting highly selective β1-blocker, with biomimetic membranes: Comparisons with β1-selective esmolol and non-selective propranolol and alprenolol

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