Absorptive and motor components of the antidiarrhoeal action of loperamide: an in vivo study in pigs.

Abstract

The effects of loperamide (0.1 mg/kg orally) on net colonic water absorption, orocolonic transit time, and intestinal motility were investigated in pigs chronically fitted either with two cannulas in the proximal colon and a catheter in the duodenum and the ileum or with intraparietal electrodes on the duodenum, jejunum, caecum, and proximal colon and a duodenal catheter. Loperamide, given 20 minutes before a meal reduced significantly colonic net water absorption for 10 hours after eating. It also reduced colonic flow rate, increased orocolonic transit time, modified the postprandial intestinal motility by inducing supplementary phase 3 motor complexes and did not affect caecocolonic motility. Intraduodenal infusion of a hypertonic solution of mannitol (900 mOsmfl; 0.6 mi/minute) for the first postprandial hour strongly reduced or reversed net colonic water absorption, increased the colonic flow rate, accelerated the orocolonic transit, and induced profuse diarrhoea. After loperamide administration, all these effects were blocked and the relative colonic water absorption, expressed as the fraction of flow entering the colon, was strongly increased. Mannitol did not modify motility of the small and large intestine, and supplementary phase 3 motor complexes were observed when mannitol infusion was preceded by loperamide administration. It is concluded that in experimental osmotic diarrhoea loperamide causes a reduction in digesta flow entering into the colon, mediated by its action on small intestinal motility, and an increase in colonic water absorption.

Inhibitory effects of zingerone, a pungent component of Zingiber officinale Roscoe, on colonic motility in rats

“…Thus, zingerone seems to be beneficial for patients with colonic disorder related to hyperexcitability of smooth muscles. In support of this notion, it has been reported that some antidiarrheal drugs, such as loperamide and wood creosote, possess inhibitory effects on gut motility in addition to their modulatory effects on fluid absorption/secretion [30][31][32][33][34]. These agents can act directly on intestinal smooth muscles [35,36], being consistent with our results.…”

Investigation On Antidiarrhoeal Activity Of <i>Aristolochia Indica</i> Linn. Root Extracts In Mice

“…Loperamide, a standard antidiarrheal drug is also reported have no effect on colonic motility and incline to slowdown small intestinal transit, reduced colonic rate of flow, and consequently increased colonic water absorption (Theoderau, 1991). EtAI extract also significantly decreased intestinal transit as observed by the decrease in transit motility of charcoal meal.…”

Antidiarrhoeal property of the hydroethanolic extract of the flowering tops of Anthocephalus cadamba

“…of endogenous prostaglandin (Galvez et al, 1993). Loperamide, apart from regulating the gastrointestinal tract, is also reported to slow down transit in the small intestine, reduce colon fl ow rate, and consequently any effect on colonic motility (Theoderau et al, 1991;Salgado et al, 2005). In this study, the hydroethanolic extract of A. cadamba displayed a signifi cant and dose-dependent antidiarrhoeal property.…”