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PubMed1999

Antidiarrheal effects of zaldaride maleate after oral, intravenous and subcutaneous administration to rats.

The antidiarrheal action of zaldaride maleate (ZAL) after oral, intravenous and subcutaneous administration was examined to determine whether ZAL acts systemically or locally in the intestine of rats. Oral administration of ZAL inhibited castor oil- and 16,16-dimethyl prostaglandin E2-induced diarrhea; however, intravenous or subcutaneous administration of ZAL was ineffective. When ZAL was orally administered, the area under the plasma concentration time curve of the compound was lower than that of ZAL following intravenous or subcutaneous administration at the maximum doses studied. The antidiarrheal effect of ZAL was not dependent on its plasma concentration level. These results suggest that ZAL acts locally in the intestinal tract in rats.

16,16-Dimethylprostaglandin E2↗

PubMed2005

Evaluation of antidiarrheal potential of trichodesma indicum root extract in rats.

Trichodesma indicum is found as a weed throughout the greater part of India. The decoction of the root is used for diarrhea, dysentery, and fever in Indian traditional medicine. However, the traditional claims need to be validated by suitable experimental animal models. Therefore, this study was undertaken to evaluate its antidiarrheal potential in several animal models. The extract significantly inhibited the castor oil-induced diarrhea and decreased propulsion of charcoal meal through the gastrointestinal tract; it also reduced the castor oil-induced small intestinal fluid accumulation (enteropooling). The ethanol extract of T. indicum root has significant antidiarrheal activity and substantiates the use of this herbal remedy as a nonspecific treatment for diarrhea in folk medicine.

Administration, Oral↗

PubMed2003

[Mechanism of quercetin as an antidiarrheal agent].

OBJECTIVE: To investigate the antidiarrheal mechanism of quercetin extracted from Psidium guajava L. METHODS: The effects of quercetin on the contractility of guinea pig ileum in vitro and on the peristaltic motion of mouse small intestine in vivo were observed, and the peak value of contractility and peristaltic distance recorded. The inhibitory effect of quercetin on the permeability of the abdominal capillaries was also observed. RESULTS: Quercetin inhibited the contraction of guinea pig ileum in vitro and the peristaltic motion of mouse small intestine, and reduced the permeability of abdominal capillaries. CONCLUSION: Quercetin can inhibit the intestinal movement and reduce capillary permeability in the abdominal cavity, which may be the antidiarrheal mechanism of Psidium guajava L extract.

Animals↗

PubMed1989

Antidiarrheal properties of supraspinal mu and delta and peripheral mu, delta and kappa opioid receptors: inhibition of diarrhea without constipation.

We evaluated the ability of mu [morphine, Tyr-Pro-N-MePhe-D-Pro-NH2 (PLO17)], delta (Tyr-D-Pen-Gly-Phe-D-Pen) (DPDPE) and kappa [U50,488H, (trans-3,4-dichloro-N-methyl-N-(2-(1-pyr-rolidinyl) cyclo-hexyl)benzeneacetamine)] opioid receptor selective agonists to inhibit diarrhea induced by castor oil (0.6 ml p.o.) in mice after supraspinal (i.c.v.) and peripheral (s.c.) administration. The antidiarrheal potency of each compound was compared to its analgesic and gastrointestinal antitransit potency when given by the same route of administration. When administered i.c.v., morphine, PLO17 and DPDPE inhibited diarrhea in a dose-related fashion. The mu agonists, morphine and PLO17, given i.c.v, inhibited diarrhea at doses much lower than those needed to produce analgesia or to inhibit gastrointestinal transit. DPDPE (i.c.v.) was equipotent in inhibiting diarrhea and in eliciting analgesia, but did not effect the rate of transit. U50,488H (i.c.v.) inhibited diarrhea only at extremely high doses which also caused profound postural-motor incapacitance. U50,488H given i.c.v. had no effect on transit at any dose. When given peripherally, morphine, PLO17, DPDPE and U50,488H all inhibited diarrhea in a dose-related fashion. All four compounds inhibited diarrhea at doses much below those needed to cause analgesia. Morphine s.c. and PLO17 s.c. both inhibited diarrhea at doses lower than those required to inhibit transit. DPDPE s.c. and U50,488H s.c. had no effect on transit at any dose. The antidiarrheal effects of i.c.v. morphine, i.c.v. PLO17 and i.c.v. DPDPE were antagonized by pretreatment with 1 microgram i.c.v. of naltrexone.(ABSTRACT TRUNCATED AT 250 WORDS)

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗

PubMed1988

WHR 1049, a potent metabolite of lidamidine, has antidiarrheal and antimotility effects on the small intestine in rats.

Lidamidine HCl has been suggested to be effective in treating certain motor disorders of the gastrointestinal tract. Lidamidine has alpha-2 agonist as well as local anesthetic properties. We studied the antimotility and antidiarrheal activity of WHR 1049, a hepatic metabolite of lidamidine known to have some activity and to persist longer in the serum than does lidamidine. We recorded the intestinal myoelectric activity of fasted unanesthetized rats with bipolar electrodes implanted on their proximal jejunum. We found that lidamidine HCl, given by gavage, inhibited fasting myoelectric activity in a dose-dependent manner (using 0.5-4.0 mg/kg). Neither saline nor tetracaine inhibited myoelectric activity. WHR 1049 given by gavage also inhibited myoelectric activity and was 30 times as potent as lidamidine (milligram per milligram, using 0.0625- to 0.25-mg/kg doses). Pretreatment with yohimbine (5 mg/kg s.c.), before administration of WHR 1049, decreased the myoelectric activity inhibition by two-thirds (but did not completely block it). Castor oil (1 ml/200 g b.wt.) was given to induce diarrhea and did so when given alone or with saline (vehicle) pretreatment. When these animals were pretreated with 0.25 mg/kg of WHR 1049, the same dose of castrol oil did not induce diarrhea for a 6-hr observation period. We conclude that WHR 1049 is a potent metabolite of lidamidine that inhibits myoelectric activity, has significant alpha-2 agonist activity and blocks induced diarrhea. Because tetracaine does not inhibit myoelectric activity we suggest that the local anesthetic properties of lidamidine do not account for any of the myoelectric activity inhibition. WHR 1049 may account for much of the antimotility and antidiarrheal activity of lidamidine.

Action Potentials↗

PubMed1985

Different actions of 2 antidiarrheal agents, lidamidine and loperamide, on motility of the isolated cat colon muscle.

Besides their action on intestinal absorption and secretion antidiarrheal agents may affect gastrointestinal motility. Little is known about motor actions in the large intestine. Therefore, the effects of loperamide and lidamidine on contractile and myoelectrical activity were studied in strips of the circular muscle of the cat colon in vitro. Both drugs caused a concentration dependent increase in spontaneous contractions, but the potency of loperamide was greater than that of lidamidine and the efficacy of lidamidine greater than that of loperamide. The corresponding EC50 were 2.9 X 10(-9) M and 1.4 X 10(-5) M, respectively, and the EC100 2.7 X 10(-7) M and 10(-4) M, respectively. In the myoelectrical tracings loperamide stimulated predominantly spike activity, lidamidine oscillatory potentials. The effect of loperamide was antagonized by naloxone, thus indicating an action on opiate receptors. The effect of lidamidine was not inhibited by a variety of drugs. Tetrodotoxin and alpha-adrenergic inhibitors even exaggerated the lidamidine effect, probably by a suppression of tonic nervous inhibition. The receptor for the lidamidine action has yet to be determined. In conclusion, the motor effects may play an important role in the antidiarrheal action of loperamide, but probably not in that of lidamidine, at least not within the range of clinically used doses.

Animals↗

PubMed1977

Methods for the study of antidiarrheal agents. Study of commonly used protective and adsorbent agents.

Several agents were employed to induce diarrhea in squirrel monkeys: (1) diarrhaogenic diets, (2) various doses of cholera toxin, (3) prostaglandin derivatives, (4) bile, (5) lactulose, (6) phenolphthalein, (7) castor oil. Kaolin, pectin, Kaopectate and placebo were used as antidiarrheal treatment. Evaluation was based on (a) frequency, (b) consistency, (c) total and dry weight of the stools, and (d) electrolyte loss. The spectrum of procedures employed appeared to be suitable for the evaluation of antidiarrheal agents of the protective and adsorbent class.

Animals↗

PubMed1978

Mechanism of action studies of lidamidine hydrochloride (WHR-1142A), a novel antidiarrheal agent.

1-(2,6-Dimethylphenyl)-3-methylamidinourea hydrochloride (WHR-1142A), lidamidine hydrochloride), a novel antidiarrheal agent, inhibited contractile activity in isolated guinea pig ileum stimulated by acetylcholine, histamine, serotonin, dimethylphenylpiperazinium, prostaglandin E2, BaCl2 and KCl. WHR-1142A also blocked spontaneous and stimulated contractile activity measured with extraluminal strain gauges in the duodenum, ileum and colon of dogs. Studies on the autonomic effects of WHR-1142A indicated little, if any, peripheral adrenergic stimulatory or cholinergic blocking activity. Inhibition of intestinal motility by WHR-1142A was not antagonized by naloxone. WHR-1142A also showed no morphine-like analgesic effects and was devoid of any H1-antihistamine activity. WHR-1142A appears to be a pharmacologically unique antidiarrheal agent.

Amidines↗

PubMed1997

[The clinical and experimental evaluation of the pharmacological efficacy of the new antidiarrheal preparation ftorazol].

A clinical trial of the new antidiarrheal drug of antisecretory action fluorasol was studied with patients with salmonellosis and food toxic infections. 65 patients had moderate and 53 severe symptoms. It was established that fluorasol was superior to basic rehydration therapy in relieving diarrheal syndrome irrespective of severity of acute intestinal infections. Clinical effects on intoxication were not registered. Antidiarrheal activity of fluorasol was confirmed on the model of experimental diarrhea on isolated loops of the rat small intestine. Liquid secretion into the lumen of small intestinal isolated loops in the presence of fluorasol substance fell twofold compared to control loops.

Acute Disease↗

PubMed1987

Naloxone-reversible antidiarrheal effects of enkephalinase inhibitors.

Thiorphan and acetorphan, two potent inhibitors of enkephalinase (EC 3.4.24.11 membrane-metalloendopeptidase) significantly reduced the castor oil-induced diarrhea in rats when administered intravenously (or orally, for acetorphan) but not when administered intracerebroventricularly. These effects were more marked during the 90 min period following the castor oil challenge but were still significant up to 4-8 h after the latter. Acetorphan was about 6 times more potent than thiorphan. The antidiarrheal activity of both compounds was completely prevented in rats receiving naloxone subcutaneously but not intracerebroventricularly (in the case of thiorphan). In contrast to loperamide, a peripherally acting opiate receptor agonist, the enkephalinase inhibitors did not significantly reduce gastrointestinal transit as measured in the charcoal meal test. The antidiarrheal activity of enkephalinase inhibitors therefore seems attributable to protection of endogenous opioids, presumably outside the brain, and to reduction of intestinal secretion rather than transit.

Amino Acids, Sulfur↗

PubMed1985

Synthesis and antidiarrheal activity of N-(aminoiminomethyl)-1H-pyrrole-1-acetamides related to guanfacine.

A series of N-(aminoiminomethyl)-1H-pyrrole-1-acetamides, related to guanfacine, were prepared and tested for antidiarrheal activity in castor oil dosed rats. trans-N-(Aminoiminomethyl)-2,5-dihydro-2,5-dimethyl-1H-pyrrole-1-acetami de (2), in which the dichlorophenyl ring of guanfacine is replaced by 2,5-dimethyl-2,5-dihydropyrrole, showed potent antidiarrheal activity but possessed only minimal cardiovascular activity in rats.

Animals↗

PubMed1996

Pharmacological studies on antidiarrheal effects of Hange-shashin-to.

We attempted to characterize the antidiarrheal action of Hange-shashin-to (TJ-14), a kampo medicine, by comparing its action with that of loperamide. The oral administration of TJ-14 caused the dose-dependent suppression of castor oil-induced diarrhea at 250 to 1000 mg/kg. No significant repression was noted by TJ-14 even at 1000 mg/kg, p.o. for diarrhea induced by pilocarpine, serotonin or barium chloride. Oral treatment with loperamide at 5 mg/kg markedly suppressed diarrhea induced by castor oil and barium chloride. Contractions of isolated guinea pig ileum in response to acetylcholine (1 x 10(-7) g/ml), histamine (1 x 10(-7) g/ml) or barium chloride (3 x 10(-4) g/ml) were little affected by TJ-14 at 10(-4) g/ml. The responses elicited by the three contractive drugs were dose-dependently suppressed by loperamide. TJ-14 did not affect the small intestinal transit even at an oral dose of 1000 mg/kg. On the other hand, the small intestinal transit was significantly suppressed by loperamide (5 mg/kg, p.o.). These results indicate that TJ-14 can effectively control castor oil-induced diarrhea, and that its antidiarrheal action was not based on the suppression of intestinal motility.

Animals↗

PubMed1977

Effect of antidiarrheal and antimotility drugs on ileal excreta.

Commonly used antimotility and antidiarrheal drugs were administered to six ileostomized subjects to determine whether their normal ileal excreta and that induced by prune juice could be altered. A total of 49 studies were performed, 21 with and 28 without prune juice. Bismuth subgallate was the only drug which significantly reduced the normal ileal excreta (P less than 0.05). Codeine sulfate decreased the ileal excreta in two of three subjects in either type of study. The third subject was a nonresponder to drugs. Deodorized tincture of opium (DTO) and diphenoxylate (Lomotil) were also effective in some subjects. Propantheline, tincture of belladonna, Sorboquel, and Kaopectate did not appear to decrease ileal excreta. Calcium carbonate, on the other hand, increased ileal excreta; fat excretion was also increased.

Adult↗

PubMed1991

Ethnobotanical review of medicinal plants from Thai traditional books, Part II: Plants with antidiarrheal, laxative and carminative properties.

A survey of medicinal plants used in Thailand has been made from Thai books on traditional herbal medicine. In this part of the survey, 326 plants with antidiarrheal, laxative and/or carminative properties are described. Information provided for each species includes plant part used, methods of preparation and administration and literature references to Thai books, together with indications of usage in other Southeast Asian countries and of phytochemical work which has been performed.

Antidiarrheals↗

PubMed2005

A study of the antidiarrheal properties of Loeselia mexicana on mice and rats.

Antidiarrheal properties of hexane, chloroform, methanol and aqueous extracts from Loeselia mexicana were studied using mice and rats as animal models. Flavones and sesquiterpenlactones were detected in the chemical screening of the aqueous extract. Diarrhea was induced by castor oil or MgSO4. The methanol extract diminished diarrhea in mice induced by MgSO4, while the aqueous extract showed an effect on castor-oil-induced. The aqueous extract also reduced castor-oil-enhanced intestinal transit and inhibited defecation of normal mice. The results obtained showed a symptomatic relief of diarrhea.

Administration, Oral↗

PubMed1996

Metabolically programmed polyamine analogue antidiarrheals.

The design, synthesis, and testing of a novel class of antidiarrheal drugs based on a tetraamine pharmacophore are reported. While N1,N14-diethylhomospermine (DEHSPM) (5 mg/kg) completely prevents diarrhea in rodents, tissue distribution studies demonstrated that the principal metabolite of DEHSPM, homospermine (HSPM), accumulates and persists in tissues for a protracted period of time. This accumulation accounts for a large part of the chronic toxicity of DEHSPM. Thus a major objective was to develop a metabolically labile analogue of DEHSPM which retained the desirable biological properties of the parent drug. Hydroxyl groups, sites vulnerable to further metabolic transformation, were introduced into the external aminobutyl segments providing N1,N14-diethyl-(3R),(12R)-dihydroxyhomospermine [(HO)2-DEHSPM]. The design concept was assisted by molecular modeling, which predicted that (HO)2DEHSPM would have a Ki for polyamine transport essentially identical with that of DEHSPM. The experimentally measured Ki and also the observed values of other biological properties of (HO)2DEHSPM were in fact identical with those of DEHSPM, including IC50 against L1210 cells, impact on the NMDA receptor, and impact on L1210 native polyamine pools. Most significantly, however, there was no accumulation of the dideethylated metabolite in tissues from mice treated chronically with (HO)2DEHSPM, and (HO)2DEHSPM was 3-fold less toxic than DEHSPM. Finally, (HO)2DEHSPM completely prevented diarrhea in the castor oil-treated rat model at a dose of 5 mg/kg, just as did DEHSPM.

Animals↗

PubMed1982

A simple controlled method for the clinical evaluation of antidiarrheal drugs.

A castor oil model induced diarrhea was used to evaluate dose regimens of the standard antidiarrheal polycarbophil. The study population consisted of 100 healthy volunteers, divided into five groups of 20 each, in whom diarrhea was induced by 120 ml flavored 36.4% castor oil. The polycarbophil dose regimens evaluated were 1, 1.5, 2, or 3 gm at 30-min intervals after castor oil to total the usual prescribed dose of 6 gm/day. One gram taken every 30 min for six doses lowered the number of bowel movements and also induced the least number of cramps and lowest cramp severity rating (reported by subjects). The same total dose over a different dosing interval was no more effective then placebo.

Acrylic Resins↗

PubMed2001

Study of Ligmed-A, an antidiarrheal drug based on lignin, on rat small intestine enzyme activity and morphometry.

This study aimed to determine the potential toxic effect of 4-day oral treatment with a lignin-based formulation on the enzymatic activity and morphology of the small intestine of rat. Ligmed-A is collected from sugarcane and is used to treat diarrhea in weaning pigs. The compound is about 90% lignin, an insoluble polyphenolic constituent of plants and a component of dietary fiber. The duodenal, jejunal and ileal mucosa of control rats and those receiving 2 g/kg Ligmed-A showed similar protein contents of about 100 mg/g. The sucrase and alkaline phosphatase activities of the three intestinal segments were unaltered after administration of the compound. Nonhistological alterations were observed after treatment. Our results, together with those of previous studies which found no toxicological effects, indicate that Ligmed-A could provide a potent antidiarrheal treatment in the veterinary area. However, further studies are required to examine its use in humans.

Administration, Oral↗