Antidiarrheal activity

Rolgamidine (14) is a dihydropyrrole derivative which has antidiarrheal activity It can be synthesized by alkylation of trans 2,5-dimethyl-3 pyrroline (12) with methyl bromoacefate to give 13 An amide-ester exchange reaction with guanidine hydrochloride completes the synthesis of rolgamidine (14) [3]... 

Gupta, S., J. N. S. Yadava, and J. S. Tandon. Antisecretory (antidiarrheal) activity of Indian medicinal plants against Escherichia coli enterotoxin-in-duced secretion in rabbit and Guinea pig ileal loop models. Int J Pharmacog 1993 31(3) 198-204-... 

Antidiarrheal activity. Decoction of the dried rhizome, taken orally hy children, was active. Infantile diarrhea was treated with kexieding capsule composed of 5 plant materials, including roasted ginger, clove, and fruit peel of Punica granatum. Of the 234 infants and 71 children treated, 281 (92%) were cured in 1-3 days and 9 (3%) were significantly improved. The total effective rate was 95% . Water extract of the dried rhizome, administered hy gastric intubation to mice at a dose of 0.5 mg/g, was active vs castor oil-induced diarrhea . 

The antidiarrheal activity of codeine results from two actions. First, there is a decrease in the propulsive contractile activity of the small and large intestines, which delays the forward movement of the contents of the intestines. Second, codeine causes an increase in the absorption of water from the intestinal contents. These gastrointestinal effects are mediated by specific opioid receptors in the gut (as we will see in... 

There are many peripheral organs that possess enkephalin opiate receptors the ileum, the most distal part of the small intestine, and the vas deferens are the most significant. The receptors in the ileum are responsible for the antidiarrheal activity of opiates. This is also the explanation for the severe constipation that may occur when people use opiates for pain relief. 

Despite the lack of studies correlating the antidiarrheic activity of crude drugs with the presence of flavonoids, these have been also studied as pure compounds in this regard. The most used assay of antidiarrhoeic activity is the castor oil test, in which diarrhea is induced by the oral administration of castor oil to mice. Different flavonoids have been shown to possess antidiarrheal activity in this test quercetin, kaempferol, morin, myricetin, rutin (i.p.) [117,118], quercitrin (p.o.) [114,119], and tematin (i.p.) [44], all showing a dose-dependent activity in the range between 25 and 100 mg/kg. However, flavonoids are not only able to exert a preventive antidiarrheal effect in this acute model of experimentally-induced diarrhea, but also in chronic models. Thus quercitrin showed beneficial effects in a model of lactose-induced chronic diarrhea in rats, since it reduced the diarrheal output and facilitated colonic mucosal repair in lactose fed [120]. 

A. Diphenoxylate is an opioid analog of meperidine. It is metabolized to difenoxin, which has fivefold the antidiarrheal activity of diphenoxylate. Both agents have opioid effects (see p 286) in overdose. 

Antidiarrheal activity, 1408 Antidiarrheic, 2000 Anti-DNA Topoisomerase II, 2422 Anti-doping tests, 287 Antidote, 63 Antiepilepsirine, 1352 Antiepileptic activity, 1515 Antiestrogenic, 2408 action, 2400 effects, 2412 Antifeedant, 3488 Antifeedant effect, 4091 Antifertility agents, 2388, 2417 Antiflogistic, 2906... 

Berberine is currently being used to treat gastrointestinal-related medical disorders due to infections including bacterial diarrhea caused by Vibrio cholerae and Escherichia coli and intestinal parasites. The mechanism of the antidiarrheal activity of berberine has not been described yet. According to the study performed by Baker et al., berberine significantly inhibits myoelectric activity and transit of the small intestine that appears to be partially mediated by opioid and a-adrenergic receptors, concluding that the antidiarrheal properties of berberine may be mediated, at least in part, by its ability to delay small intestinal transit [67]. 

Peppers are added in traditional antidiarrheal formulations of different herbs. In a study made in experimental mice, the antidiarrheal activity of piperine against diarrhea produced by castor oil, MgS04, and arachidonic acid has been evidenced at 8 and 32 mg/kg p.o. dose [51]. Inhibition of castor oil-induced entero pooling by piperine suggests its inhibitory effect on prostaglandins. Piperine (2.5-20 mg/kg, i.p.) dose-dependently reduced castor oil-induced intestinal fluid accumulation in experimental mice piperine reduces castor oil-induced fluid secretion with a mechanism involving capsaicin-sensitive neurons [43]. 

Dietary Supplements/Health Foods. Root bark used in capsules, tablets, tinctures, and infusion, primarily for uterine-relaxant and antidiarrheal activity (wren). 

Further effects on the GIT include antiamoebic and antidiarrheal activities as reported by Tona et al. and by Galvez et al., whereby euphorbia polyphenolic extract inhibited the growth of Entamoeba histolytica at a concentration below 10 pg/ mL, ° and the lyophilized decoction and one of its constituents, quercitrin, displayed antidiarrheal effect in experimental animal models. 

---