Pharmacological studies of loperamide, an anti-diarrheal agent. II. Effects on peristalsis of the small intestine and colon in guinea pigs.

Sohji, Yukinobu; Kawashima, Katsuyoshi; Shimizu, Masanao

doi:10.1254/fpj.74.155

Cited by 28 publications

(20 citation statements)

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“…Loperamide is known to reduce stool frequency in humans and increase colonic contractions in vitro in the guinea pig [9] and in vivo in dogs [23] . Therefore, the loperamide-induced delay of colonic transit in our study could be used as a model of spastic constipation.…”

Section: Discussionmentioning

confidence: 99%

“…The propulsion can be delayed by clonidine and loperamide, an adrenergic ␣ 2 -receptor ag-onist and an -opioid receptor agonist, respectively [6] . It is well known that clonidine relaxes isolated intestine [7,8] and loperamide causes compulsive contractions in the gastrointestinal tract [9] . However, the clonidine-and loperamide-induced delay in the models of colonic propulsion has not been fully characterized.…”

Section: Introductionmentioning

confidence: 99%

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Characterization of Two Models of Drug-Induced Constipation in Mice and Evaluation of Mustard Oil in These Models

et al. 2009

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Although it is known that both clonidine and loperamide cause delayed colonic transit in mice, these models of drug-induced experimental constipation have not yet been fully characterized. Therefore, the aims of this study were to validate the clonidine- and loperamide-induced delays of colonic transit in mice as models of atonic and spastic constipation, respectively, and to evaluate the effect of mustard oil, a TRPA1 agonist, in both models. Colonic transit was evaluated in mice by determining the time needed to evacuate a bead inserted into the distal colon. Both loperamide and clonidine dose-dependently prolonged the evacuation time. Clonidine (10 μg/kg) and loperamide (0.3 mg/kg) tripled the evacuation time compared to controls. These delays were antagonized by the administration of yohimbine and naloxone, respectively. Tegaserod, a gastrointestinal motor-stimulating drug, reversed the delay in both models, but the effects were diminished at high doses. Atropine, an antispastic drug, improved the loperamide-induced delay, but did not affect the clonidine-induced delay. Mustard oil accelerated the colonic transit dose-dependently in both models of drug-induced constipations. These results indicate that clonidine- and loperamide-induced delays in colonic transit are models of atonic and spastic constipation, respectively, and that mustard oil may be effective on both types of constipation.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Characterization of Two Models of Drug-Induced Constipation in Mice and Evaluation of Mustard Oil in These Models

et al. 2009

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“…The drug inhibits intestinal water secretion (8) and colonic peristalsis (9), which extends the fecal evacuation time and delays intestinal luminal transit (10). Thus, loperamide-induced constipation is considered to be a model of spastic constipation (11).…”

Section: Introductionmentioning

confidence: 99%

Laxative effects of fermented rice extract in rats with loperamide-induced constipation

Choi

Kim²,

Cho³

et al. 2014

Experimental and Therapeutic Medicine

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Constipation is a common problem in males and females. The aim of the present study was to evaluate the laxative effects of fermented rice extract (FRe) on rats with loperamide-induced constipation. FRe (100, 200 and 300 mg/kg) was administered orally once per day for six days following 1 h loperamide treatment. The laxative effects of FRe were compared with those of sodium picosulfate (S. picosulfate). Following the induction of constipation in the rats, a marked decrease was observed in the fecal pellet number and water content discharged over 24 h, the surface mucus thickness in the colonic lumen, intestinal charcoal transit ratio, thickness of the colonic mucosa and the number of mucus-producing cells, while an increase was observed in the number of fecal pellets remaining in the colonic lumen and their mean diameter, as compared with the normal vehicle control rats. These conditions were significantly alleviated following the administration of the three doses of FRe when compared with the loperamide control group. However, the alleviating effects were lower than those of S. picosulfate, with the exception of the intestinal charcoal transit ratio. Similar effects on the intestinal charcoal transit ratio were detected for the three doses of FRe when compared with the S. picosulfate-treated rats. In conclusion, the results indicated that FRe exhibits a laxative effect without causing diarrhea, as compared with sodium picosulfate; thus, FRe may be effective as a complementary medicine in patients suffering from lifestyle-induced constipation.

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“…Using these two site-specific methods for the kinetic study of mouse intestine, we have further substantiated in this report that wood creosote and some of its phenolic compounds do have a strong antimotility activity on the colon, but not on the small intestine at an ordinary human therapeutic dose level and that the effect is mediated via blood circulation and not from the luminal side of the colon. As a comparison, a similar experiment was performed on an antidiarrheal agent, loperamide [13,14]. Loperamide did not inhibit the colonic propulsive motility, but it inhibited dose-dependently the propulsive motility of the small intestine.…”

Section: Introductionmentioning

confidence: 99%

Effect of Wood Creosote and Loperamide on Propulsive Motility of Mouse Colon and Small Intestine

Ogata¹,

Ataka²,

Morino³

et al. 1999

Pharmacology

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To elucidate a mechanism of the antidiarrheal activity of wood creosote, its effect on the propulsive motility of mouse colon and small intestine was studied using a charcoal meal test and a colonic bead expulsion test. The effect was compared with that of loperamide. At an ordinary therapeutic dose, wood creosote inhibited the propulsive motility of colon, but not of small intestine. On the other hand, loperamide inhibited the propulsive motility of small intestine, but not of colon. The results indicate that at least a part of the antidiarrheal activity of wood creosote and loperamide is attributable to their antikinetic effect predominantly on colon of the former and predominantly on small intestine of the latter.

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Pharmacological studies of loperamide, an anti-diarrheal agent. II. Effects on peristalsis of the small intestine and colon in guinea pigs.

Cited by 28 publications

References 0 publications

Characterization of Two Models of Drug-Induced Constipation in Mice and Evaluation of Mustard Oil in These Models

Characterization of Two Models of Drug-Induced Constipation in Mice and Evaluation of Mustard Oil in These Models

Laxative effects of fermented rice extract in rats with loperamide-induced constipation

Effect of Wood Creosote and Loperamide on Propulsive Motility of Mouse Colon and Small Intestine

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