ultrashort-acting Esmolol,选择性β1-adrenoceptor拮抗剂:药效学和药代动力学特性。

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Volz-Zang C, B Eckrich扬P, Schneidrowski B,舒尔特B,棕榈D

ultrashort-acting Esmolol,选择性β1-adrenoceptor拮抗剂:药效学和药代动力学特性。

46欧元中国新药杂志。1994;(5):399 - 404。

PubMed ID

7957532 (在PubMed

]

文摘

esmolol的影响在不同注入率(100、250和500微克。公斤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 selectivity of esmolol. Exercise-induced increases in heart rate and systolic blood pressure were reduced by esmolol in a dose-dependent manner. The estimated EC50 values of rate of infusion for the reduction in heart rate and systolic blood pressure during exercise were 113 and 134 micrograms.kg-1 BW.min-1, respectively. Additionally, heart rate and systolic blood pressure were reduced moderately at rest. Because of the short elimination half-life of esmolol caused by the rapid hydrolysis to its acid metabolite, 45 min after end of infusion high plasma concentrations of the metabolite (maximally 80 micrograms.ml-1) but no esmolol were detectable. Since no in vivo effects have been observed, despite the presence of high plasma concentrations of the metabolite, the metabolite did not participate in the observed effects up to an infusion rate of esmolol of 500 micrograms.kg-1 BW.min-1. The plasma concentrations of antagonist detected by radioreceptor assay and plasma concentrations of esmolol detected by HPLC showed a good correlation (r = 0.97).(ABSTRACT TRUNCATED AT 250 WORDS)

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药物靶点

药物	目标	类	生物	药理作用	行动
Esmolol	beta 1肾上腺素能受体	蛋白质	人类	是的	拮抗剂	细节