Ritschel W A, Paulos C, Arancibia A, Agrawal M A, Wetzelsberger K M, Lücker P W
University of Cincinnati, Ohio, USA.
Methods Find Exp Clin Pharmacol. 1998 Mar;20(2):133-7. doi: 10.1358/mf.1998.20.2.485649.
Acetazolamide is recommended for the prophylaxis of acute mountain sickness symptoms which sets in on climbing to high altitudes (H) above 2,500 m. It is primarily excreted unchanged in urine. In a previous study, we reported on the changes in urinary excretion of meperidine and its metabolite normeperidine on exposure to high altitude. In this study, we investigated the effect on urinary excretion of acetazolamide. The study was carried out in three groups of 12 healthy male volunteers each: at sea level (group L), these same volunteers the day after arrival at high altitude of 4,360 m (group HA), and subjects residing for approximately 10 months at high altitude (group HC). Urine was collected for the periods of 0-2, 2-4, 4-8, 8-12, 12-24 and 24-36 h after peroral administration of a single 250 mg dose. Urinary pH was measured and the concentrations of acetazolamide were determined. There were no significant changes observed in the amount of acetazolamide excreted in urine over 36 h. The urinary pH ranged from 4.5 to 7.8 for L, from 4.2 to 6.9 for HA and from 3.1 to 6.7 for HC. The Fel (fraction eliminated unchanged in urine) was calculated from the amount excreted in 36 h in urine and dose, assuming a bioavailability of 1 based on literature data. No significant changes in Fel were seen.
乙酰唑胺被推荐用于预防攀登至海拔2500米以上的高海拔地区（H）时出现的急性高原病症状。它主要以原形经尿液排泄。在之前的一项研究中，我们报告了哌替啶及其代谢产物去甲哌替啶在暴露于高海拔环境时尿排泄的变化。在本研究中，我们调查了对乙酰唑胺尿排泄的影响。该研究在三组健康男性志愿者中进行，每组12人：海平面组（L组）、到达海拔4360米的高海拔地区第二天的同一批志愿者（HA组）以及在高海拔地区居住约10个月的受试者（HC组）。在口服单剂量250毫克后，分别在0 - 2、2 - 4、4 - 8、8 - 12、12 - 24和24 - 36小时收集尿液。测量尿液pH值并测定乙酰唑胺的浓度。在36小时内，尿液中排泄的乙酰唑胺量未观察到显著变化。L组尿液pH值范围为4.5至7.8，HA组为4.2至6.9，HC组为3.1至6.7。根据文献数据假设生物利用度为1，从36小时尿液排泄量和剂量计算出尿中未变化消除分数（Fel）。未观察到Fel有显著变化。
