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西咪替丁和雷尼替丁对奎宁药代动力学的影响。

Effects of cimetidine and ranitidine on the pharmacokinetics of quinine.

作者信息

Wanwimolruk S, Sunbhanich M, Pongmarutai M, Patamasucon P

出版信息

Br J Clin Pharmacol. 1986 Sep;22(3):346-50. doi: 10.1111/j.1365-2125.1986.tb02898.x.

Abstract

The pharmacokinetics of orally administered quinine were determined in six normal volunteers before and after a 7-day course of cimetidine (1 g day-1) or ranitidine (300 mg day-1). Peak plasma quinine concentration and the time of peak concentration were not altered after cimetidine or ranitidine pretreatment. After cimetidine pretreatment there was a significant reduction in the apparent oral clearance of quinine, from 0.182 +/- 0.063 (mean +/- s.d.) to 0.133 +/- 0.055 1 h-1 kg-1 (P less than 0.05). This was reflected in a 49% (range 17 to 90%) increase in the mean elimination half-life from 7.6 +/- 1.3 to 11.3 +/- 3.7 h (P less than 0.05). In contrast to cimetidine, ranitidine had no significant effect on the clearance or half-life of quinine. The apparent interaction between quinine and cimetidine may have therapeutic implications. Special care should be taken in patients taking these two common drugs concomitantly. Additionally, to avoid unnecessary risks due to drug interaction, the use of ranitidine may be preferable in the patients in whom it is desirable to administer an H2-receptor antagonist together with quinine.

摘要

在6名正常志愿者中,测定了口服奎宁在服用西咪替丁(1克/天)或雷尼替丁(300毫克/天)7天疗程前后的药代动力学。西咪替丁或雷尼替丁预处理后,血浆奎宁峰值浓度和达峰时间未改变。西咪替丁预处理后,奎宁的表观口服清除率显著降低,从0.182±0.063(均值±标准差)降至0.133±0.055升/小时·千克-1(P<0.05)。这反映在平均消除半衰期增加了49%(范围为17%至90%),从7.6±1.3小时增至11.3±3.7小时(P<0.05)。与西咪替丁不同,雷尼替丁对奎宁的清除率或半衰期无显著影响。奎宁与西咪替丁之间明显的相互作用可能具有治疗意义。同时服用这两种常用药物的患者应特别注意。此外,为避免因药物相互作用带来不必要的风险,在希望将H2受体拮抗剂与奎宁一起给药的患者中,使用雷尼替丁可能更为可取。

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本文引用的文献

2
Drug interactions with cimetidine.西咪替丁的药物相互作用。
Clin Pharmacokinet. 1982 Jan-Feb;7(1):23-41. doi: 10.2165/00003088-198207010-00002.
3
Clinical pharmacokinetics of quinidine.奎尼丁的临床药代动力学。
Clin Pharmacokinet. 1980 Mar-Apr;5(2):150-68. doi: 10.2165/00003088-198005020-00003.
7
Quinine disposition kinetics.奎宁处置动力学。
Br J Clin Pharmacol. 1983 Oct;16(4):399-403. doi: 10.1111/j.1365-2125.1983.tb02184.x.
8
Effect of cimetidine on quinidine clearance.西咪替丁对奎尼丁清除率的影响。
Ther Drug Monit. 1984;6(3):306-12. doi: 10.1097/00007691-198409000-00009.
10
Interactions and non-interactions with ranitidine.与雷尼替丁的相互作用及非相互作用
Clin Pharmacokinet. 1984 Nov-Dec;9(6):493-510. doi: 10.2165/00003088-198409060-00002.

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