Newton P, Keeratithakul D, Teja-Isavadharm P, Pukrittayakamee S, Kyle D, White N
Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand.
Trans R Soc Trop Med Hyg. 1999 Jan-Feb;93(1):69-72. doi: 10.1016/s0035-9203(99)90184-0.
The plasma concentrations of quinine and its main metabolite, 3-hydroxyquinine (3OHQn), were measured in 5 adult Thai patients with severe Plasmodium falciparum malaria and acute renal failure. Two patients required peritoneal dialysis but all survived. During acute renal failure plasma concentrations of 3OHQn rose to reach up to 45% of the levels of the parent compound. The estimated median (range) quinine clearance was 0.83 mL/kg/min (0.58-1.16), and 3OHQn clearance/fraction of quinine converted was 3.40 mL/kg/min (2.58-4.47). The estimated 3OHQn terminal elimination half-life was 21 h (16.5-32.5). These data suggest that 3OHQn contributes about 12% of the antimalarial activity of the parent compound in patients with falciparum malaria and acute renal failure. It is also likely that 3OHQn contributes to adverse effects, although this metabolite is not quantitated routinely by current high-performance liquid chromatography quinine assays.
在5例患有严重恶性疟原虫疟疾和急性肾衰竭的成年泰国患者中，测量了奎宁及其主要代谢产物3 - 羟基奎宁（3OHQn）的血浆浓度。2例患者需要进行腹膜透析，但均存活。在急性肾衰竭期间，3OHQn的血浆浓度上升，达到母体化合物水平的45%。估计奎宁清除率的中位数（范围）为0.83 mL/kg/分钟（0.58 - 1.16），3OHQn清除率/奎宁转化分数为3.40 mL/kg/分钟（2.58 - 4.47）。估计3OHQn的终末消除半衰期为21小时（16.5 - 32.5）。这些数据表明，在患有恶性疟和急性肾衰竭的患者中，3OHQn对母体化合物抗疟活性的贡献约为12%。3OHQn也可能导致不良反应，尽管目前的高效液相色谱法奎宁检测通常不对这种代谢产物进行定量。
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