Karbwang J, Bunnag D, Harinasuta T, Chittamas S, Berth J, Druilhe P
Department of Clinical Tropical Medicine, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand.
Southeast Asian J Trop Med Public Health. 1992 Dec;23(4):773-6.
Pharmacokinetics of quinine, quinidine and cinchonine when given as a combination were evaluated in Thai patients with falciparum malaria during acute infection and convalescence. The combination of quinine, quinidine and cinchonine was randomly given to thirteen patients at 400 mg or 600 mg (consisting of one-third of each component; 7 patients were enrolled in 400 mg regimen and 6 in 600 mg regimen) intravenously every 8 hours for 7 days. The drug combination was given again at day 35 to define the pharmacokinetics of each drug during convalescence. All patients with the 600 mg regimen had good response with 100% cure rate while patients with the 400 mg regimen had a good initial response but one patient recrudesed on day 46. This particular patient had plasma concentrations of all three drugs lower than the mean values of patients with sensitive responses. The plasma levels of quinine and quinidine obtained from the present study were higher than that expected from one-third of the conventional dose (600 mg) when given alone, suggesting drug combination interaction. The terminal half-lives of each of the three components were prolonged during acute malaria when compared to those obtained during convalescence.
在泰国急性感染期和恢复期的恶性疟患者中,评估了奎宁、奎尼丁和辛可宁联合使用时的药代动力学。将奎宁、奎尼丁和辛可宁的组合以400毫克或600毫克(每种成分各占三分之一;7名患者采用400毫克方案,6名患者采用600毫克方案)随机给予13名患者,每8小时静脉注射一次,共7天。在第35天再次给予该药物组合,以确定恢复期每种药物的药代动力学。所有采用600毫克方案的患者反应良好,治愈率为100%,而采用400毫克方案的患者初始反应良好,但有一名患者在第46天复发。该特定患者三种药物的血浆浓度均低于反应敏感患者的平均值。本研究中获得的奎宁和奎尼丁的血浆水平高于单独给予常规剂量(600毫克)的三分之一时预期的水平,提示药物组合存在相互作用。与恢复期相比,三种成分在急性疟疾期间的终末半衰期均延长。