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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Pharmacokinetics, pharmacodynamics, and safety of the 5-HT(1B/1D) agonist eletriptan following intravenous and oral administration.
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Pharmacokinetics, pharmacodynamics, and safety of the 5-HT(1B/1D) agonist eletriptan following intravenous and oral administration.

机译：静脉和口服给药后5-HT（1B / 1D）激动剂依曲曲坦的药代动力学，药效学和安全性。

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Four separate studies were conducted to examine the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of eletriptan, a 5-HT(1B/1D) receptor agonist being developed for the treatment of migraines, after oral and intravenous administration. Fifty-five males received oral (1.5-30 mg or 30-120 mg) or intravenous (1.67-50 microg/kg or 50-102 microg/kg) eletriptan in four double- and single-blind, placebo-controlled, ascending-dose crossover studies. The maximum plasma concentration (Cmax) and area under the concentration curve (AUC) appeared linear over all dose ranges, with an apparent terminal half-life of 4 to 5 hours. Clearance and volume of distribution remained constant with dose. The time to first occurrence of Cmax (tmax) for oral eletriptan was approximately 1 hour and was unaffected by dose. Comparison of AUC values suggested an absolute bioavailability of approximately 50%. A linear PK/PD model, fitted to the data, predicted small, transient elevations in diastolic blood pressure following eletriptan doses > or = 60 mg. These effects were considered unlikely to be clinically significant. Eletriptan was well tolerated, and treatment-related adverse events were mild to moderate and transient. These PK properties should result in eletriptan having a rapid onset and sustained duration of action in terms of migraine efficacy.
机译：进行了四项单独的研究，以检查伊曲曲普坦的安全性，耐受性，药代动力学（PK）和药效动力学（PD），这是一种经口服和静脉内给药后开发的用于治疗偏头痛的5-HT（1B / 1D）受体激动剂。五十五名男性接受了口服依曲曲坦口服（1.5-30 mg或30-120 mg）或静脉注射（1.67-50 microg / kg或50-102 microg / kg）的伊曲坦治疗，四种双盲和单盲，安慰剂对照，递增-剂量交叉研究。在所有剂量范围内，最大血浆浓度（Cmax）和浓度曲线下的面积（AUC）呈线性，表观终末半衰期为4至5小时。清除率和分布体积随剂量保持恒定。口服依曲普坦首次出现Cmax（tmax）的时间约为1小时，不受剂量影响。 AUC值的比较表明绝对生物利用度约为50％。根据数据拟合的线性PK / PD模型预测，在依曲普坦剂量大于或等于60 mg后，舒张压会有短暂的短暂升高。这些作用被认为不太可能具有临床意义。依曲曲坦耐受性良好，与治疗相关的不良事件为轻度至中度和短暂性。这些PK特性应导致依曲普坦具有起效快且持续作用持续时间长的偏头痛功效。

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