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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 and pharmacodynamics of irbesartan in healthy subjects.
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Pharmacokinetics and pharmacodynamics of irbesartan in healthy subjects.

机译：厄贝沙坦在健康受试者中的药代动力学和药效学。

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摘要

The safety, pharmacokinetics, and pharmacodynamics of single and multiple doses of the angiotensin II (AII) AT1 blocker irbesartan were assessed in healthy subjects. In this single-center, placebo-controlled, double-blind within dose group, sequential, dose-ascending study, 48 men were randomized to receive irbesartan at doses of 150 mg, 300 mg, 600 mg, or 900 mg daily. Subjects received a single dose of irbesartan (n = 9 per group) or placebo (n = 3 per group), followed by 3 days of placebo, and then multiple doses of irbesartan or placebo once daily for 7 days. The values for plasma area under the concentration-time curve (AUC) of irbesartan were dose proportional up to 600 mg. There were no significant differences between the dose groups in time to maximum concentration (tmax) or half-life (t1/2) after single and multiple doses. After multiple doses, urinary recovery was significantly lower in the 600-mg and 900-mg dose groups compared with the 150-mg and 300-mg dose groups. Steady-state concentrations of irbesartan were achieved within 3 days of administration with no clinically important accumulation. Irbesartan produced dose-dependent increases in plasma renin activity and AII levels. Irbesartan was well tolerated at doses from 150 mg to 900 mg daily; a maximally tolerated dose was not reached. Modest decreases in blood pressure without orthostatic symptoms were observed at irbesartan doses of 300 mg or higher. These results demonstrated the dose-proportionality of irbesartan 150 mg to 600 mg and indicated that doses up to 900 mg daily were well tolerated.
机译：在健康受试者中评估了单次和多次剂量的血管紧张素II（AII）AT1阻断剂厄贝沙坦的安全性，药代动力学和药效学。在该单中心，安慰剂对照，双盲的剂量组内，连续，剂量增加的研究中，随机分配48名男性接受厄贝沙坦，剂量分别为每天150 mg，300 mg，600 mg或900 mg。受试者接受单剂量的厄贝沙坦（每组n = 9）或安慰剂（每组n = 3），然后接受3天的安慰剂，然后每天多次给予厄贝沙坦或安慰剂，共7天。厄贝沙坦的浓度-时间曲线（AUC）下的血浆面积值与剂量成比例，最高为600 mg。各剂量组在单次和多次给药后的最大浓度（tmax）或半衰期（t1 / 2）的时间上无显着差异。多次给药后，与150 mg和300 mg剂量组相比，600 mg和900 mg剂量组的尿液恢复明显降低。厄贝沙坦在给药后3天内达到稳态浓度，没有临床上的重要积累。厄贝沙坦引起血浆肾素活性和AII水平的剂量依赖性增加。每天150 mg至900 mg的剂量对厄贝沙坦具有良好的耐受性;未达到最大耐受剂量。在300 mg或更高的厄贝沙坦剂量下观察到血压适度下降而无直立性症状。这些结果证明了150 mg至600 mg厄贝沙坦的剂量比例，并表明每天耐受高达900 mg的剂量具有良好的耐受性。

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