Wanwimolruk S, Sunbhanich M, Pongmarutai M, Patamasucon P
Br J Clin Pharmacol. 1986 Sep;22(3):346-50. doi: 10.1111/j.1365-2125.1986.tb02898.x.
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.
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。