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PubMed2005

Presence of antispasmodic, antidiarrheal, antisecretory, calcium antagonist and acetylcholinesterase inhibitory steroidal alkaloids in Sarcococca saligna.

The aim of this investigation was to see if the crude extract of Sarcococca saligna (Ss.Cr) contains chemicals with gut function inhibitory activity by using in vitro and in vivo assays. Ss.Cr caused a dose-dependent (0.03 - 3 mg/mL) inhibitory effect on K+-induced contractions in rat stomach fundus, guinea-pig ileum and rabbit jejunum preparations. The calcium channel blocking(CCB) activity was confirmed when Ss.Cr caused a rightward shift in the Ca++ dose-response curves. It also potentiated, at lower do-ses (0.001 - 0.03 mg/mL), the contractile effect of a fixed dose of acetylcholine (ACh), similar to physostigmine, and suppressed the effect of ACh at higher doses (0.3 - 1.0 mg/mL). Both Ss.Cr and physostigmine inhibited acetylcholinesterase (AChE), in the in vitro assay, confirming the AChE inhibitory activity. In the in vivo studies, Ss.Cr exhibited antidiarrheal and antisecretory activities against castor oil-induced diarrhea and intestinal fluid accumulation in mice. Characteristic steroidal compounds of the plant (saracocine, saracodine, saracorine and alkaloid-C), exhibited a similar combination of AChE inhibitory and CCB activities. Thus this study provides a sound mechanistic base for some of the traditional uses of the plant in hyperactive gut states, in addition to providing the first evidence for verapamil to possess additional AChE inhibitory activity. Furthermore, these characteristic compounds with dual activity may be good candidates for further studies on their usefulness in Alzheimer's disease.

Alkaloids↗
PubMed2005

Antidiarrheal effects of L-histidine-supplemented rice-based oral rehydration solution in the treatment of male adults with severe cholera in Bangladesh: a double-blind, randomized trial.

BACKGROUND: Because of the antisecretory potential of L-histidine in the intestinal tract, its antidiarrheal effects were determined in cholera. METHODS: In a double-blind trial of 126 adult male patients with cholera, L-histidine (2.5 g/L) was mixed with a rice-based oral rehydration solution (ORS) and administered to 62 patients; 64 patients received the same ORS without L-histidine. All patients received ciprofloxacin at a dosage of 500 mg every 12 h for 72 h. Fluid output (of stool, urine, and vomit) and intake (of ORS, water, and intravenous fluid) were determined every 8 h for 72 h. RESULTS: Administration of ORS with L-histidine significantly (P<.05) reduced the frequency of stool output during 32-64 h after initiation of ORS treatment, compared with that in patients given ORS without L-histidine ([all data are means+/-SD] 32-48 h, 11.5+/-6.9 mL/kg vs. 18.8+/-16.0 mL/kg; 40-48 h, 6.7+/-4.4 mL/kg vs. 11.5+/-9.7 mL/kg; and 56-64 h, 6.3+/-5.8 mL/kg vs. 7.8+/-4.1 mL/kg). An overall reduction of 22% in the volume of stool was observed in patients given ORS without L-histidine. The amount of required unscheduled intravenous fluid was lower in patients given ORS with L-histidine, compared with that in patients given ORS without L-histidine (0-24 h, 82.5+/-44.4 mL/kg vs. 158.6+/-72.2 mL/kg [P<.01]; and 24-48 h, 41.6+/-40.4 mL/kg vs. 52.5+/-22.1 mL/kg [P>.05]). Administration of ORS with L-histidine also significantly reduced (P<.05) the intake of ORS and the duration of illness. No adverse effects were observed in these patients. CONCLUSIONS: L-histidine reduces the weight of stool and the frequency of stool output in cholera and could be a useful and safe adjunct treatment that will increase the success rate of ORS and antibiotic therapy in cholera.

Adult↗
PubMed1985

Nigerian geophagical clay: a traditional antidiarrheal pharmaceutical.

The chief geophagical clay entering the West African market system comes from the village of Uzalla, Nigeria. Village inhabitants ascribe antidiarrheal properties to the clay, and they use it in traditional medicinal preparations to counteract intestinal problems. Mineralogical analyses demonstrate a striking similarity between the Uzalla village clay and the clay in the commercial pharmaceutical Kaopectate.

Africa, Western↗
PubMed1986

Role of a novel antidiarrheal agent, BW942C, alone or in combination with trimethoprim-sulfamethoxazole in the treatment of traveler's diarrhea.

The efficacy of BW942C, a novel enkephalinlike pentapeptide antidiarrheal agent, was compared with the efficacy of trimethoprim-sulfamethoxazole (TMP-SMX) and the combination of the two agents in a placebo-controlled trial of the 72-h treatment of acute diarrhea. Subjects with diarrhea but without bloody stools or fever greater than 102 degrees F (38.9 degrees C) were enrolled. Administered to 134 U.S. adults with diarrhea that developed shortly after their arrival in Guadalajara, Mexico, BW942C was more efficacious than TMP-SMX in relieving diarrhea and cramps in the first 12 h of therapy, especially among subjects with diarrhea caused by enterotoxigenic E. coli. In the BW942C treatment group, 25% of subjects eventually took additional therapy because their diarrhea did not respond to BW942C alone. Neurological side effects such as dizziness and light-headedness occurred more frequently among BW942C-treated subjects. Therapy for 3 days with TMP-SMX provided lasting relief comparable with previously reported 5-day therapy. Use of the combination of both agents provided the benefits of prompt relief afforded by BW942C and lasting relief afforded by TMP-SMX. BW942C might prove to be an agent suitable for the treatment of acute diarrhea, with TMP-SMX reserved for treatment of those who do not respond adequately. The empiric use of the combination of BW942C and TMP-SMX appears appropriate for the treatment of severe nondysenteric disease.

Antidiarrheals↗
PubMed1986

Cholesterol: an antidiarrheal agent in rats with short-bowel syndrome fed elemental diets.

Studies show that bile acids and long-chain fatty acids are responsible for diarrhea in certain malabsorption syndromes. Recent reports indicate that substances such as dietary cholesterol, when moderately consumed, can reduce bile-induced excessive mucosal fluid and electrolyte output. This study explores the antidiarrheal effect and dosage of dietary cholesterol in rats following massive bowel resection, co-fed elemental diet. Thirty-five male Sprague-Dawley rats weighing 248-253 g underwent 75% resection of the small bowel and were fed ad libitum for 21 days with 1 of 5 diets (n = 7) of Vivonex HN, supplemented by 0, 2.5, 5, 10 or 15 mM cholesterol/1,000 g of the powdered elemental diet. Parameters measured included daily food and water consumption, daily changes in weight, volume of excrement and stool consistency graded by the same individual (water, semiformed or formed). It was found that 5 mM dietary cholesterol in 1,000 g of the elemental diet produced the most formed stool and significantly improved weight gain in rats with short-bowel syndrome.

Animals↗
PubMed1982

Studies of the mechanism of the antidiarrheal effect of codeine.

To determine whether the antidiarrheal action of opiate drugs in humans is due to enhanced intestinal absorption rates, as suggested by recent experiments in animals, or is due to altered intestinal motility, as traditionally thought, we studied the effect of therapeutic doses of codeine on experimental diarrhea and on the rate of intestinal absorption of water and electrolytes in normal human subjects. Our results show that codeine (30-60 mg i.m.) markedly reduced stool volume during experimental diarrhea induced by rapid intragastric infusion of a balanced electrolyte solution. There was, however, no evidence that codeine stimulated the rate of intestinal absorption in the gut as a whole or in any segment of the gastrointestinal tract, either in the basal state or when absorption rates were reduced by intravenous infusion of vasoactive intestinal polypeptide. We also measured segmental transit times to determine whether and where codeine delayed the passage of fluid through the intestine. Codeine caused a marked slowing of fluid movement through the jejunum, but had no effect on the movement of fluid through the ileum or colon. In other studies, we found that the opiate antagonist naloxone did not significantly affect water or electrolyte absorption rates in the jejunum or ileum. We conclude (a) that therapeutic doses of codeine increase net intestinal absorption (and thereby reduce stool volume) by increasing the contact time of luminal fluid with mucosal cells, not by increasing the rate of absorption by the mucosal cells; and (b) that endogenous opiates do not regulate intestinal absorption in humans.

Adult↗
PubMed1993

[Pharmacological studies on antidiarrheal effects of a preparation containing berberine and geranii herba].

We studied the effects of a preparation containing Berberine and Geranii Herba (BGH) on different diarrheal models of mice and the contractions of isolated guinea pig intestinal smooth muscle, comparing these effects with those of a preparation containing creosote (CSG) and loperamide (LP). BGH, as well as CSG and LP, significantly inhibited the diarrhea induced by castor oil or BaCl2, but not the diarrhea induced by pilocarpine or serotonin. BGH inhibited ACh-, Ba(2+)- or electrical stimulation (ES)-induced contraction of the ileum or colon at concentrations from 10(-6) to 10(-4) g/ml. On the other hand, the inhibitory effect of CSG on the ES-induced contraction was about one hundred times stronger than that on ACh- or Ba(2+)-induced contraction. The order of the inhibitory potency of LP on contractions of the ileum in this test was ES > Ba2+ > ACh, and LP showed stronger inhibition against the contraction of the ileum than that of the colon. These results suggest that BGH exerts its antidiarrheal action by inhibiting intestinal movement, and the mechanism of action of BGH may differ from those of CSG or LP.

Animals↗
PubMed1993

[Pharmacological studies on antidiarrheal effects of berberine and geranii herba].

We studied the effects of berberine and Geranii Herba extract (GH) on different diarrheal models of mice, on the contractions of the isolated guinea pig intestinal smooth muscle and on the peristalsis in the rat intestine, comparing these effects with those of atropine (ATR) and papaverine (PAP). 1) Berberine significantly inhibited both the diarrhea induced by castor oil and that induced by BaCl2 at doses higher than 25 mg/kg, p.o., but did not inhibit diarrhea induced by pilocarpine or serotonin even at 250 mg/kg, p.o. GH exhibited a significant inhibition of BaCl2 induced diarrhea. ATR prevented pilocarpine-induced diarrhea most strongly in diarrheal models. PAP significantly inhibited castor oil-, BaCl2- and pilocarpine-induced diarrhea, but not the serotonin-induced one. 2) Berberine inhibited ACh- or Ba(2+)-induced contractions of the ileum and colon at a concentration of about 10(-5) g/ml, and PAP did so at about 10(-6) g/ml, but GH (10(-3) g/ml) failed to inhibit them. ATR prevented the ACh-induced contraction of the ileum and colon at concentrations 1/1000 of those needed to prevent the Ba(2+)-induced one. On the other hand, berberine as well as PAP exhibited a noncompetitive inhibition of the contractile response induced by ACh, whereas ATR showed a competitive inhibition. 3) Berberine, GH, ATR and PAP showed significantly inhibited the spontaneous peristalsis in the intestine. These results suggest that berberine and GH have antidiarrheal action and that the mechanism of action of berberine may be somewhat differ from that of GH.

Acetylcholine↗
PubMed2000

Effect of zaldaride maleate, an antidiarrheal compound, on fecal pellet output induced by hyperpropulsion in gastrointestine of rats.

The effect of zaldaride, a calmodulin inhibitor, on fecal pellet output in rats was compared with that of loperamide, an antidiarrheal drug. 5-Hydroxytryptamine (10 mg/kg, s.c.), neostigmine (0.3 mg/kg, s.c.) and nicotine (1.0 mg/kg, s.c.) increased fecal pellet output. Zaldaride (> or = 30 mg/kg, p.o.) reduced these increases in fecal pellet outputs. Loperamide (10 mg/kg, p.o.) inhibited fecal pellet output induced by 5-hydroxytryptamine and neostigmine but not nicotine. Under normal conditions, zaldaride and loperamide did not affect fecal pellet output at doses used in these studies. In conclusion, zaldaride may inhibit increases in fecal pellet output induced by hyperpropulsion of the gastrointestinal tract without causing constipation as a side effect.

Animals↗
PubMed2003

Wood creosote, the principal active ingredient of seirogan, an herbal antidiarrheal medicine: a single-dose, dose-escalation safety and pharmacokinetic study.

STUDY OBJECTIVE: To assess the safety, tolerability and pharmacokinetics of escalating single doses of wood creosote, an herbal antidiarrheal and antispasmodic agent. DESIGN: Randomized, double-blind, placebo-controlled study. SETTING: Clinical research center. SUBJECTS: Forty (32 men, 8 women) healthy volunteers aged 19-42 years. INTERVENTION: By random assignment, 22 men and 8 women received escalating single doses of wood creosote (45, 90, 135, 180, and 225 mg) and 10 men received placebo (for each of the five dose levels, 6 subjects received active substance and 2 subjects received placebo). MEASUREMENTS AND MAIN RESULTS: Vital signs, laboratory tests, and electrocardiograms were assessed; no dose-related or clinically significant changes were noted. Serial blood samples were obtained to determine the pharmacokinetics of four major active components of wood creosote: total (conjugated plus free) guaiacol, creosol, o-cresol, and 4-ethylguaiacol. The most common adverse events were mild headache and dizziness, with no dose-related trends being apparent. Area under the concentration-time curve from time zero to infinity increased in a dose-proportional manner for total guaiacol, creosol, and o-cresol and was not assessed for total 4-ethylguaiacol owing to lack of data at the low dose level. No apparent differences by sex were noted for any of the four active components. All four components were rapidly eliminated. CONCLUSION: Single oral doses of wood creosote up to 225 mg were safe and well tolerated in healthy men and women. Also, the doses of wood creosote were rapidly absorbed, conjugated, and eliminated. Such a rapid onset and short duration of action would appear desirable in the treatment of acute nonspecific diarrhea.

Adult↗
PubMed2004

Antidiarrheal drug products for over-the-counter human use; amendment of final monograph. Final rule.

The Food and Drug Administration (FDA) is issuing a final rule amending the final monograph (FM) for over-the-counter (OTC) antidiarrheal drug products to include relief of travelers' diarrhea as an indication for products containing bismuth subsalicylate. Travelers' diarrhea occurs in travelers and is most commonly caused by an infectious agent. This final rule is part of FDA's ongoing review of OTC drug products.

Antidiarrheals↗
PubMed2004

Identification of an N-methyl-4-phenylpyridinium-like metabolite of the antidiarrheal agent loperamide in human liver microsomes: underlying reason(s) for the lack of neurotoxicity despite the bioactivation event.

In contrast with the Parkinson's-like effects associated with the mitochondrial neurotoxin N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and the neuroleptic agent haloperidol, there exist no reports on adverse central nervous system (CNS) effects with the structurally related N-substituted-4-arylpiperidin-4-ol derivative and antidiarrheal agent loperamide. Although this difference can be attributed to loperamide's P-glycoprotein substrate properties that prevent it from accessing the brain, an alternative possibility is that loperamide metabolism in humans is different from that of MPTP and haloperidol and does not involve bioactivation to a neurotoxic pyridinium species. In the current study, loperamide bioactivation was examined with particular focus on identification of pyridinium metabolites. A NADPH-dependent disappearance of loperamide was observed in both rat and human liver microsomes (human t(1/2) = 13 min; rat t(1/2) = 22 min). Loperamide metabolism was similar in human and rat and involved N-dealkylation to N-desmethylloperamide (M3) as the principal metabolic fate. Other routes of loperamide biotransformation included N- and C-hydroxylation to the loperamide-N-oxide (M4) and carbinolamide (M2) metabolites, respectively. Furthermore, the formation of an additional metabolite (M5) was also discernible in human and rat liver microsomes. The structure of M5 was assigned to the pyridinium species (LPP(+)) based on comparison of the liquid chromatography/tandem mass spectrometry characteristics to the pyridinium obtained from loperamide via a chemical reaction. Loperamide metabolism in human microsomes was sensitive to ketoconazole and bupropion treatment, suggesting P4503A4 and -2B6 involvement. Recombinant P4503A4 catalyzed all of the loperamide biotransformation pathways in human liver microsomes, whereas P4502B6 was only responsible for N-dealkylation and N-oxidation routes. The wide safety margin of loperamide (compared with MPTP and haloperidol) despite metabolism to a potentially neurotoxic pyridinium species likely stems from a combination of factors that include a therapeutic regimen normally restricted to a few days and the fact that loperamide and perhaps LPP(+) are P-glycoprotein substrates and are denied entry into the CNS. The differences in safety profile of haloperidol and loperamide despite a common bioactivation event supports the notion that not all compounds undergoing bioactivation in vitro will necessarily elicit a toxicological response in vivo.

1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine↗
PubMed2004

[Controlled clinical testing of an antidiarrheal].

AIM: To identify the efficacy and tolerance of activated charcoal in acute, nonspecific diarrhea. METHOD: Randomized, double-blind study on 100 adults with nonspecific diarrhea, performed in two general practices. 94 were included in the final analysis, 6 patients - all from the placebo group abandoned treatment because of the absence of an effect. RESULTS: The major outcome parameters - reduction of stool frequency and curtailment of the duration of the diarrhea - were unequivocally achieved. Differences between the agent and placebo were great. Stool frequency decreased significantly from the third day in the drug group, and highly significantly from the fourth day. The superiority of the antidiarrheal was also clearly evident in terms of the numbers of days with diarrhea, the clinical findings tympania, nature of the stool and of eight individual symptoms, the summed score of which was improved highly significantly by the test substance. CONCLUSION: The substance tested proved rapidly and reliably effective in the treatment of nonspecific diarrhea, and was well tolerated. Activated charcoal, together with oral rehydration, can therefore be recommended as an initial measure for treating diarrhea with the aim of rapidly and effectively preventing loss of fluid and electrolytes and relieving symptoms.

Adult↗
PubMed1990

[Antibacterial activity of extracts from plants used in preparation as antidiarrheals at Kinshasa, Zaire].

A preliminary and anterior bacteriological study about 38 plant antidiarrheic traditional preparations, has demonstrated that 35 of them have bactericidal activity. Thirty inhibit the growth of all select germs and 5 exert this bactericidal effect on some germs. Some extracts proceeding of these possess a bactericidal activity, specially if they contain polyphenols (flavonoids, catechics tanins), saponins and alkaloids.

Antidiarrheals↗
PubMedDate not supplied

[In vitro study of the adsorption of chloroquine by an antidiarrheal remedy traditionally used in Africa].

Mouboumou is a traditional medicine prepared from the inner part of termitarium and is used in traditional medicine in Zaire. In tropical diseases, antimalarial drugs are often used simultaneously with antidiarrheal absorbent drugs, which might, by their adsorbent properties, compromise the efficacy of the antimalarial treatment. The present in vitro study has allowed to determine the adsorption characteristics of chloroquine on Mouboumou; kaopectate was used a reference adsorbent. The adsorption of chloroquine by these two adsorbents is very important (from 30 to 60%) and fits quite well in with the Langmuir's relation. A decrease of bioavailability of chloroquine, due to the adsorption phenomena, might be observed in vivo and could contraindicate the concomitant administration of these drugs.

Adsorption↗
PubMed1989

Antidiarrheal activity of alpha-2 adrenoceptor agonist SK&F 35886.

Alpha-2 adrenoceptor agonists exhibit antidiarrheal activity in animal models and in humans. However, hypotensive and sedative side effects seriously limit the use of these agents to treat diarrhea. SK&F 35886 (2,6-dimethyl phenylamino imidazoline) is an alpha-2 adrenoceptor agonist with little central nervous system activity. In Ussing chamber preparations of rabbit ileum, SK&F 35886 produces a concentration-dependent decrease in basal short-circuit current (Isc) (EC50 0.2 microM) that is dependent on the presence of mucosal HCO3. This concentration-response curve is shifted to the right of rauwolscine, increasing the EC50 to 30 microM. Prazosin had no effect on this response. Flux studies indicate that SK&F 35886 increases net Cl absorption and enhances HCO3 absorption without altering net Na flux. After PGE2 stimulation of Isc, SK&F 35886, applied either serosally or mucosally, immediately returns the Isc to base line. This effect is due to a reversal of the PGE2-induced inhibition of Na and Cl absorption. In vivo SK&F 35886 dose-dependently inhibits PGE2-induced enteropooling when given orally (ED50 approximately 31 micrograms/kg). This effect is attenuated significantly by rauwolscine (1.0 micrograms/kg s.c.). In cecectomized rats, SK&F 35886 abolishes PGE2-induced diarrhea within 1 hr after oral administration of the drug. SK&F 35886 (500 micrograms/kg p.o.) did not alter hexobarbital sleep time or elicit piloerection or lethargy, whereas clonidine (37.3 micrograms/kg p.o.) significantly enhanced hexobarbital sleep time. These results illustrate the ability of a peripheral acting alpha-2 agonist to promote absorption and inhibit secretion and diarrhea in the mammalian intestine.

16,16-Dimethylprostaglandin E2↗
PubMed1989

[Antidiarrheal agents: tools and therapeutic agents].

A host of chemically diverse compounds have antidiarrheal potency, however, only a fraction of these agents has gained clinical acceptance. But regardless of their therapeutic status, the effects of these drugs have enhanced our understanding of the physiology and pathophysiology of the intestinal mucosa. Fluid- and electrolyte substitution are the primary therapeutic measures in severe diarrhea, for that purpose oral rehydration using glucose-sodium solutions has proven simple and effective. In addition gut-selective opiates, for instance loperamide, are indicated. Opiates not only decrease propulsive motor activity of the bowel but also increase intestinal water and electrolyte absorption, both effects are neuronally mediated. Antimicrobial drugs are necessary in only a small fraction of patients with diarrhea. Experimental findings have indicated possible future candidates for treatment of diarrhea: Besides opiates and glucose-electrolyte solutions water and electrolyte absorption is enhanced by alpha 2-adrenergic agents, corticosteroids, and somatostatin. Inhibitors of electrolyte secretion include phenothiazines and opiates, possibly because of binding to calcium-calmodulin, calcium-channel blockers, membrane-stabilizing agents for instance propranolol and inhibitors of prostaglandin-synthesis such as non-steroidal antirheumatic agents.

Antidiarrheals↗