老年稳定型心绞痛患者急性和慢性口服依泮洛尔的药代动力学研究。

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引用

Hosie J, Scott AK, Petrie JC, Cockshott ID

老年稳定型心绞痛患者急性和慢性口服依泮洛尔的药代动力学研究。

临床药物学杂志。1990 3;29(3):333-7。

PubMed ID
1968755 (PubMed视图
摘要

1.依帕洛尔是一种新型抗心绞痛药,它是一种β - 1肾上腺素能受体部分激动剂,具有选择性β - 1肾上腺素能受体拮抗剂和选择性β - 1肾上腺素能受体激动剂活性。它主要代谢为结合物,然后排泄在尿液中,这是有兴趣的,以确定是否有任何积累发生在老年患者。2.在13例稳定性心绞痛老年患者中,研究了依泮洛尔单次口服200mg后72小时和连续每日口服12次后24小时的药代动力学。3.单次给药后(25.7 +/- 17.0 ng ml-1)的峰值血药浓度(平均+/- s.d)与稳态时(32.4 +/- 20.9 ng ml-1)无显著差异(P = 0.35)。在这两种情况下,个体间差异很大。在研究过程中,达到峰值的时间没有显著变化,急性和慢性给药的平均值分别为1.5和1.2小时。4. Plasma concentrations declined biphasically with a mean terminal phase half-life of 17 h and 5 fold inter-individual variation. 5. The mean area under the curve to 24 h was not significantly different (P = 0.26) after the single dose (59.0 +/- 29.8 ng ml-1 h) from that at steady state (78.4 +/- 55.0 ng ml-1 h). There was also wide inter-individual variation in these values. 6. In conclusion, the lack of significant accumulation of epanolol indicates that no alteration of dose is necessary when using epanolol in elderly patients with normal renal and hepatic function.

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