Colin J N, Farinotti R, Fredj G, Tod M, Clavel J P, Vignon E, Dietlin F
Eur J Clin Pharmacol. 1986;31(1):53-8. doi: 10.1007/BF00870986.
Previous studies have described a pharmacokinetic interaction between probenecid, a uricosuric drug, and oxipurinol, the major metabolite of allopurinol. In single dose studies, no interaction was found to occur between benzbromarone, another uricosuric agent, and oxipurinol. A cross over study was conducted in 12 volunteers to compare the kinetics of allopurinol and oxipurinol following treatment for 7 days with allopurinol alone or combined with benzbromarone 20 or 100 mg. The pharmacokinetic parameters of allopurinol were not modified by the uricosuric therapy, but those of oxipurinol were markedly altered by concurrent administration even of the lower dose of benzbromarone; the average plasma level fell by 30% and the renal elimination rate was increased by 50%. A parallel increase in the renal elimination rate of uric acid was observed (significant only with the higher dose of benzbromarone) and a positive linear correlation between the fractional excretion of uric acid and that of oxipurinol was established.
先前的研究已经描述了促尿酸排泄药丙磺舒与别嘌醇的主要代谢产物氧嘌呤醇之间的药代动力学相互作用。在单剂量研究中，未发现另一种促尿酸排泄药苯溴马隆与氧嘌呤醇之间发生相互作用。对12名志愿者进行了一项交叉研究，以比较单独使用别嘌醇或与20毫克或100毫克苯溴马隆联合治疗7天后别嘌醇和氧嘌呤醇的动力学。促尿酸排泄疗法未改变别嘌醇的药代动力学参数，但即使同时给予较低剂量的苯溴马隆，氧嘌呤醇的药代动力学参数也会发生显著改变；平均血浆水平下降30%，肾脏清除率提高50%。观察到尿酸肾脏清除率平行增加（仅在较高剂量的苯溴马隆时显著），并建立了尿酸分数排泄与氧嘌呤醇分数排泄之间的正线性相关性。
