Saunders D R, Sillery J, Rachmilewitz D, Rubin C E, Tytgat G N
Gastroenterology. 1977 May;72(5 Pt 1):849-56.
The effect of bisacodyl on intestinal structure and function was investigated. Net water transport was measured under steady state conditions in vivo during single pass infusions of rodent and of human intestinal segments. Each segment served as its own control. Bisacodyl inhibited water absorption in rat jejunum, ileum, and colon. The degree of inhibition was linearly related to the logarithm of the bisacodyl concentration over the range of 0.05 to 2.0 mg per 100 ml. In human jejunal segments, bisacodyl, 1 mg per 100 ml, caused net water secretion. Bisacodyl, 5 mg every 6 hr, increased ileostomy output by 15% when it was fed to 5 patients with established ileostomies. By light microscopy, bisacodyl, 2 mg per 100 ml, erased cytoplasmic and nuclear detail within surface absorptive cells of rat intestine. By electron microscopy, the involved cells contained sparse and abnormal cytoplasmic organelles and nuclei which were deficient in chromatin. These results suggest that the laxative effect of bisacodyl is related to its ability to inhibit intestinal water absorption. Reduced absorption may be secondary to changes in surface absorptive cells.
研究了比沙可啶对肠道结构和功能的影响。在对啮齿动物和人类肠段进行单程灌注的体内稳态条件下,测量了净水转运。每个肠段都作为自身的对照。比沙可啶抑制大鼠空肠、回肠和结肠的水吸收。在每100毫升0.05至2.0毫克的浓度范围内,抑制程度与比沙可啶浓度的对数呈线性关系。在人类空肠段中,每100毫升1毫克的比沙可啶会引起净水分泌。每6小时服用5毫克比沙可啶,给5名已建立回肠造口术的患者服用时,回肠造口术的排出量增加了15%。通过光学显微镜观察,每100毫升2毫克的比沙可啶会使大鼠肠道表面吸收细胞内的细胞质和细胞核细节消失。通过电子显微镜观察,受累细胞含有稀疏且异常的细胞质细胞器和缺乏染色质的细胞核。这些结果表明,比沙可啶的泻药作用与其抑制肠道水吸收的能力有关。吸收减少可能是表面吸收细胞变化的继发结果。