Rees P H, Keating M I, Kager P A, Hockmeyer W T
Lancet. 1980 Aug 2;2(8188):226-9. doi: 10.1016/s0140-6736(80)90120-8.
Kenyan kala-azar is sometimes unresponsive to a standard course of sodium stibogluconate. The renal excretion of sodium stibogluconate was therefore studied in patients with kala azar and in volunteers; both urine and serum levels of sodium stibogluconate were measured. After intravenous injection sodium stibogluconate seemed to be distributed throughout the extracellular fluid and to have a renal clearance similar to that of inulin. At 6 h blood levels had fallen to less than 1% of peak values. After intramuscular injection, peak blood levels were lower and more sustained. However, more than 80% was excreted in the first 6 h, and blood levels fell to around 1% of peak values in 16 h. The dangers of cumulative toxicity may be exaggerated, and restriction of courses of sodium stibogluconate to 30 days or even to 10 days (in the U.S.A.) may not be necessary. If shorter courses are ineffective prolonged and continued courses may be given provided that renal function is assessed and the dosage is adjusted when indicated.
肯尼亚黑热病有时对标准疗程的葡萄糖酸锑钠无反应。因此,对黑热病患者和志愿者的葡萄糖酸锑钠肾排泄情况进行了研究;同时测量了尿液和血清中的葡萄糖酸锑钠水平。静脉注射后,葡萄糖酸锑钠似乎分布于整个细胞外液,其肾脏清除率与菊粉相似。6小时后,血药浓度降至峰值的1%以下。肌肉注射后,血药峰值较低且维持时间更长。然而,超过80%的药物在最初6小时内排出,16小时后血药浓度降至峰值的1%左右。累积毒性的危险性可能被夸大了,将葡萄糖酸锑钠疗程限制在30天甚至10天(在美国)可能没有必要。如果较短疗程无效,在评估肾功能并在必要时调整剂量的情况下,可以给予延长和持续的疗程。