Fidelholtz James, Smith William, Rawls James, Shi Yingqi, Zack Anna, Rüegg Peter, Lefkowitz Martin
Regional Research Department, Hightop Medical Research Center, Cincinnati, Ohio, USA.
Am J Gastroenterol. 2002 May;97(5):1176-81. doi: 10.1111/j.1572-0241.2002.05692.x.
Tegaserod is a selective serotonin (5-HT4) receptor partial agonist effective in providing relief from abdominal pain, bloating, and constipation in patients with irritable bowel syndrome. Tegaserod therapy may be associated with early transient diarrhea, which is related to its mechanism of action. This study was performed in patients with irritable bowel syndrome and symptoms of diarrhea to further assess the safety of tegaserod.
After a 2-wk baseline, patients were randomized (2:2:1) in a double-blind manner to receive 4 mg of tegaserod a day (n = 35), 12 mg of tegaserod a day (n = 34), or placebos (n = 17) for 8 wk. Patients had to fulfill > or =2 Rome diarrhea criteria > or =25% of the time. Adverse events were recorded.
Diarrhea, abdominal pain, headache, flatulence, and fatigue were the most frequently reported adverse events. The frequency rates of diarrhea were 49%, 18%, and 35% for the 4 mg/day, 12 mg/day, and placebo groups, respectively; when the tegaserod data were pooled, the frequency of diarrhea was similar to that of the placebo group (33% and 35%, respectively). No complications of diarrhea (e.g., dehydration and electrolyte abnormalities) were reported. Five patients (6%), all from the tegaserod groups, discontinued study participation because of diarrhea and/or abdominal pain. No serious adverse events were reported.
In this study, tegaserod at doses of 4 and 12 mg/day was safe and not associated with complications of diarrhea or serious adverse events.
替加色罗是一种选择性5-羟色胺（5-HT4）受体部分激动剂，对缓解肠易激综合征患者的腹痛、腹胀和便秘有效。替加色罗治疗可能与早期短暂性腹泻有关，这与其作用机制相关。本研究在有腹泻症状的肠易激综合征患者中进行，以进一步评估替加色罗的安全性。
经过2周的基线期后，患者以双盲方式随机分组（2:2:1），分别接受每日4毫克替加色罗（n = 35）、每日12毫克替加色罗（n = 34）或安慰剂（n = 17）治疗8周。患者必须在≥25%的时间内满足≥2条罗马腹泻标准。记录不良事件。
腹泻、腹痛、头痛、肠胃胀气和疲劳是最常报告的不良事件。4毫克/天、12毫克/天和安慰剂组的腹泻发生率分别为49%、18%和35%；当汇总替加色罗组的数据时，腹泻发生率与安慰剂组相似（分别为33%和35%）。未报告腹泻的并发症（如脱水和电解质异常）。5名患者（6%），均来自替加色罗组，因腹泻和/或腹痛停止参与研究。未报告严重不良事件。
在本研究中，每日剂量为4毫克和12毫克的替加色罗是安全的，且与腹泻并发症或严重不良事件无关。
