The effects of cimetidine, ranitidine and famotidine on the single-dose pharmacokinetics of naproxen and its metabolites in humans.

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-12-01

T B Vree, M van den Biggelaar-Martea, C P Verwey-van Wissen, M L Vree, P J Guelen

引用次数: 0

Abstract

We studied the effects of cimetidine, ranitidine and famotidine on the kinetics of naproxen. The mean t1/2 beta of naproxen in 6 subjects was 25.7 +/- 5.4 h (range 16 to 36). Naproxen acyl glucuronide accounts for 50.9 +/- 6.9% of the dose, its isomerized isoglucuronide for 6.8 +/- 2.6%, O-desmethylnaproxen acyl glucuronide for 14.3 +/- 4.1% and its isoglucuronide for 5.5 +/- 1.5% (n = 6). Naproxen (1.3 +/- 1.1%) and O-desmethylnaproxen (0.6 +/- 0.4%) are excreted in negligible amounts. Cimetidine, ranitidine and famotidine all reduced significantly the t1/2 beta of naproxen by 50% from 25 h to 13 h and the t1/2 alpha from 4.0 h to 1.1 h. No effect of the H2 antagonists was observed on the absorption of naproxen. They also reduced the Vss of naproxen by 50%. The amount of naproxen acyl glucuronide, naproxen isoglucuronide and O-desmethylnaproxen acyl glucuronide excreted in the urine, remained unchanged, 60%, 7%, and 14% respectively.

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西咪替丁、雷尼替丁和法莫替丁对萘普生及其代谢物在人体内单剂量药代动力学的影响。

研究了西咪替丁、雷尼替丁和法莫替丁对萘普生动力学的影响。6例受试者中，萘普生的平均t1/2 β为25.7±5.4 h(范围16 ~ 36)。萘普生酰基葡萄糖醛酸酯占50.9 +/- 6.9%，其异构化异葡萄糖醛酸酯占6.8 +/- 2.6%，o -去甲基萘普生酰基葡萄糖醛酸酯占14.3 +/- 4.1%，异葡萄糖醛酸酯占5.5 +/- 1.5% (n = 6)。萘普生(1.3 +/- 1.1%)和o -去甲基萘普生(0.6 +/- 0.4%)的排泄量可以忽略不计。西咪替丁、雷尼替丁和法莫替丁在25 ~ 13 h显著降低了50%的t1/2 β，在4.0 ~ 1.1 h显著降低了50%的t1/2 α。H2拮抗剂对萘普生吸收无影响。他们还将萘普生的Vss降低了50%。尿中萘普生酰基葡萄糖醛酸盐、萘普生异葡萄糖醛酸盐和o -去甲基萘普生酰基葡萄糖醛酸盐的排泄量保持不变，分别为60%、7%和14%。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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International journal of clinical pharmacology, therapy, and toxicology

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