Abstract: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 sele… Show more
“…At therapeutic doses, it has no intrinsic sympathomimetic activity or membrane-stabilizing effect. Its half-life of distribution is very fast (approximately 2 min) [28]. These pharmacokinetic properties allowed gentle titration and rapid resolution of any potential negative effects after stopping treatment.…”
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.
“…At therapeutic doses, it has no intrinsic sympathomimetic activity or membrane-stabilizing effect. Its half-life of distribution is very fast (approximately 2 min) [28]. These pharmacokinetic properties allowed gentle titration and rapid resolution of any potential negative effects after stopping treatment.…”
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.
“…The positive chronotrophic effect was abolished by esmolol, a selective b 1 -antagonist [8], in both sexes, suggesting that the effect was mediated through noradrenaline on b 1 -adrenoreceptors.…”
“…Esmolol, a cardioselective beta 1 -blocker [26], shows good controllability after intravenous application. But there are few clinical trials and case reports about its use in children.…”
The actual treatment approaches vary widely, demonstrating the lack of hard science on which current treatment of hypertensive emergencies in children is based. The hypotensive agent for the individual situation should be chosen considering the properties, side effects, the limited experiences with its use and the patient's anamnesis.
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