Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Antidiarrheals”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 865 records · Page 48Linked to original sources

Identification of an active site in the antisecretory factor protein.

The antisecretory factor (AF) is a new regulatory protein, produced in the human pituitary gland, which reverses intestinal fluid secretion induced by cholera toxin. We have previously described the cDNA-cloning and characterization of the expressed gene. The aim of this study was to identify the region responsible for the antisecretory activity in the AF-molecule. The recombinant full-length AF has an increased ability to inhibit hypersecretion after treatment with trypsin, indicating that the activity of AF is achieved by smaller peptide fragments. To localize the active region of AF, we expressed truncated forms of the recombinant protein and examined their antisecretory activity against cholera toxin-induced fluid secretion in rat. Nine recombinant AF peptides and four smaller peptides made by solid phase synthesis were tested. Five of the peptides lacked all activity, whereas seven of them were highly active, a dose between 4 and 15 pmol causing a half-maximal inhibition. All the active peptides contained amino acid 36-42 of the AF sequence, whereas none of the inactive peptides contained this sequence. Our results suggest that the site of the antisecretory activity resides in a small region (I)VCHSKTR between position 35 and 42 of the AF molecule.

Amino Acid Sequence↗

A scintigraphic study to investigate the potential for altered gut distribution of loperamide from a loperamide-simethicone formulation in man.

A loperamide simethicone combination formulation has recently been demonstrated to have significant clinical advantages compared to loperamide alone in the relief of diarrhoea and related symptoms. The product visualisation technique of gamma scintigraphy has been used to investigate the interaction of the formulation with the heterogenous environment of the human gut in a group of 12 healthy volunteers. The results suggest that changes in the intestinal kinetics of loperamide from the combination product, e.g. jejunal coating, could be contributing to the improved efficacy.

Antidiarrheals↗

[Drug treatment of acute infectious diarrhea in infants and children].

In this paper written by the Groupe francophone d'hépatologie, gastroentérologie et nutrition pédiatriques, recommendations are given on the indications of drugs in infant and child infectious acute diarrhea, based upon the current scientific knowledge on their effectiveness and tolerance. This paper complements an article on nutritional treatment of acute diarrhea written by the Comité de nutrition de la Société française de pédiatrie, and published in the same issue of the Archives de Pédiatrie.

Acute Disease↗

[Effect of racecadotril in the management of acute diarrhea in infants and children].

BACKGROUND: The treatment of diarrhoea relies on the maintenance or restoration of hydration with maintenance of an adequate nutritional intake. Racecadotril has been shown to reduce the stools output during acute diarrhoea. The present work was aimed at measuring the number of emergency department visits for acute diarrhoea either the children received racecadotril or not. METHOD: Racecadotril and rehydration were compared with rehydration alone in children aged three months to three years who had acute diarrhoea and were evaluated in the emergency department (ED). The primary end point was the number of medical exams during the week after starting treatment. Secondary end points were the number of stools during the first 48 hours, the duration of the diarrhoea and the weight on day 7. RESULTS: One hundred and sixty-six children were alternatively randomized to the treated and the control groups. There was no difference for age, degree of dehydration and length of illness before the first visit between the groups. Whatever type of rehydration (oral or i.v.), the treated group had a significant lower number of stools (p < 0.001) and a faster recovery (p < 10(-9)). The children receiving racecadotril needed less additional ED visits for the same episode (p < 0.05). There was no difference for the weight-gain on day 7. CONCLUSIONS: This study demonstrates the efficacy of racecadotril as adjuvant therapy to oral and i.v. rehydration in the treatment of acute diarrhoea and a fewer emergency department second visit before recovery.

Acute Disease↗

In vitro evaluation of pectin-HPMC compression coated 5-aminosalicylic acid tablets for colonic delivery.

In this study, we report pectin-HPMC compression coated core tablets of 5-aminosalicylic acid (5-ASA) for colonic delivery. Each 100 mg core tablet contained 5-ASA and was compression coated at 20 kN or 30 kN using 100% pectin, 80% pectin-20% HPMC, or 60% pectin-40% HPMC, at two different coat weights as 400 or 500 mg. Drug dissolution/system erosion/degradation studies were carried out in pH 1.2 and 6.8 buffers using a pectinolytic enzyme. The system was designed based on the gastrointestinal transit time concept, under the assumption of colon arrival times of 6 h. It was found that pectin alone was not sufficient to protect the core tablets and HPMC addition was required to control the solubility of pectin. The optimum HPMC concentration was 20% and such system would protect the cores up to 6 h that corresponded to 25-35% erosion and after that under the influence of pectinase the system would degrade faster and delivering 5-ASA to the colon. The pectin-HPMC envelope was found to be a promising drug delivery system for those drugs to be delivered to the colon.

Anti-Inflammatory Agents, Non-Steroidal↗

Antiamoebic and spasmolytic activities of extracts from some antidiarrhoeal traditional preparations used in Kinshasa, Congo.

Three major extracts from some traditional preparations, based on medicinal plants, used as antidiarrhoeal agents were investigated for their putative antiamoebic and spasmolytic activities in vitro. Results indicated that both biological activities are concentrated in the polyphenolic fraction, and not in the saponin or alkaloid containing fractions. The most active polyphenolic extracts were those from Euphorbia hirta whole plant, leaves of Alchornea cordifolia, Crossopteryx febrifuga, Nauclea latifolia, Psidium guajava, Tithonia diversifolia, stem bark of Harungana madagascariensis, Mangifera indica, Maprounea africana and Psidium guajava, inhibiting Entamoeba histolytica growth with MAC < 10 micrograms/ml. The same extracts, at a concentration of 80 micrograms/ml in an organ bath, also exhibited more than 70% inhibition of acetylcholine and/or KCl solution-induced contractions on isolated guinea-pig ileum.

Amebicides↗

Biological screening of traditional preparations from some medicinal plants used as antidiarrhoeal in Kinshasa, Congo.

Forty six aqueous extracts from 38 medicinal plant species belonging to different families were selected on the basis of their traditional medicinal use as antidiarrhoeic agents. They were submitted in a broad biological screening including antibacterial, antiamoebic and antispasmodic activities. The results of the testing have indicated that 37 extracts (80.43%), 33 (71.74%) and 32 (69.54%) exhibited some level of antibacterial, antiamoebic and antispasmodic activity respectively. Only 8 plant extracts (17.39%) would act as antidiarrhoeic agents by a triple pronounced antibacterial, antiamoebic and antispasmodic action. They include aqueous extracts from Euphorbia hirta whole plant, leaves of Psidium guajava and Tithonia diversifolia, root bark of Alchornea cordifolia, Heinsia pulchella, Paropsia brazzeana, Rauwolfia obscura and Voacanga africana.

Amebicides↗

Decreased colonic mucus in rats with loperamide-induced constipation.

Constipation is a risk factor of colorectal cancer. Mucin is a major component of lumenal mucus, which protects the colorectal mucosa against mechanical and chemical damage. The aim of this study was to evaluate mucus production and to quantitate lumen mucus in a rat model of spastic constipation. We induced constipation with loperamide (1.5 mg/kg), and histochemically evaluated mucus production and the thickness of the mucus layer at the fecal surface. We quantitated the mucus attached to the mucosal surface using colonic perfusion with N-acetylcysteine. While more feces remained in the colon, there was less fecal excretion and lower fecal water content in loperamide-administered rats than in control rats. Crypt epithelial cells contained less mucus in constipated rats than in control rats. The mucus layer at the fecal surface was thinner and less mucus was recovered from the mucosal surface in constipated rats than in control rats. Mucus production of crypt epithelial cells and mucus at the fecal and mucosal surface were reduced by loperamide-induced constipation.

Animals↗

Irritable bowel syndrome.

Irritable bowel syndrome (IBS) is one of the most common diagnoses made in the primary care setting and is responsible for up to 40% of referrals to gastroenterologists. Approximately 70% of persons who meet the diagnostic criteria for IBS do not seek health care, and the remaining account for 12% of visits to primary care providers. IBS is a functional bowel disordered comprising abdominal pain associated with defecation or a change in bowel habit with features of disordered defecation and distension in the absence of any demonstrable abnormality. The diagnosis is based on clinical findings and the exclusion of other disorders. New pharmaceutical agents are available to treat the underlying disorder; however, the treatment of IBS still involves a comprehensive, multicomponent approach that includes medical management of dominant symptoms, dietary modifications, and, possibly, psychotherapy.

Antidepressive Agents↗

Herbal agents and over-the-counter medications in pregnancy.

Exposures to over-the-counter and herbal products are frequent in pregnant women. Limited information exists on the effects of many of these agents during pregnancy; it is not safe to assume that because these products are available without a prescription that they are without danger to the pregnant woman and her fetus. The basic principles utilized in deciding whether to employ prescription medications such as dose, embryological timing and potential toxic fetal effects also apply to herbal medications and over-the-counter agents. Conventional reasoning indicates that maternal exposure to poorly studied medications should be limited; therefore, many of these agents should be used sparingly or not at all by pregnant women. This chapter includes a review of selected herbal and over-the-counter agents, including those which are considered to be acceptable for use in pregnancy.

Adult↗

Effect of the prebiotic oligofructose on relapse of Clostridium difficile-associated diarrhea: a randomized, controlled study.

BACKGROUND & AIMS: Ten percent to 20% of patients relapse after successful treatment of their Clostridium difficile -associated diarrhea. We set out to determine if the prebiotic oligofructose could alter the fecal bacterial flora and, in addition to antibiotic treatment, reduce the rate of relapse from C difficile infection. METHODS: Consecutive inpatients with C difficile -associated diarrhea were randomly allocated to receive oligofructose or placebo for 30 days in addition to specific antibiotic treatment. Patients were followed up for an additional 30 days. The main end point was the development of further diarrhea. Stools were collected for bacterial culture and C difficile toxin measurement. RESULTS: One hundred forty-two patients were recruited. Stool culture confirmed the probiotic effect of oligofructose with an increase in fecal bifidobacteria from baseline 8.68 log(10) colony-forming units (cfu)/g to 9.37 log(10) cfu/g at discharge (P < .0001; 95% confidence interval [CI], 0.45-0.94), 9.64 log(10) cfu/g at 30 days (P < .0001; 95% CI, 0.74-1.18), and 9.42 log(10) cfu/g at 60 days (P < .0001; 95% CI, 0.56-0.93). Thirty patients experienced a relapse of diarrhea after a median of 18 days (range, 8-34 days). Relapse of diarrhea was more common in those taking placebo (8.3% oligofructose vs 34.3% placebo, P < .001, chi(2) = 14.35). Patients who relapsed stayed in the hospital longer than those who did not (53 vs 26 days, P = .021; 95% CI, 2-28), and there was a longer period of time from commencing metronidazole or vancomycin and their diarrhea settling (6 vs 3 days; P = .007; 95% CI, 1.0-5.0). CONCLUSIONS: Fecal cultures confirmed the prebiotic effect of oligofructose. Patients taking oligofructose were less likely to develop further diarrhea than those taking the placebo.

Aged↗

Structure-activity studies of 16-methoxy-16-methyl prostaglandins.

The synthesis of the pure diastereoisomer of 16-methoxy-16-methyl-PGF2 alpha, -PGE2, and -PGE1 is described. The absolute configuration of C-16 was established by chemical methods, while the absolute C-15 configurations of the diastereoisomers were assigned tentatively on the basis of their chromatographic behavior and NMR spectra. The synthetic prostaglandin analogues were evaluated for antisecretory, antifertility, and diarrheogenic effects. Both the C-15 and C-16 configurations were found to be critical for the biological activities. These studies indicate that the introduction of the methyl and methoxy groups at C-16 into the prostaglandin analogues markedly increases the ratio of antisecretory to diarrheogenic action. One of the PGE1 derivatives, 9f(15 alpha, 16R) (MDL 646, mexiprostil), was selected for further pharmacological evaluation and is currently under clinical investigation.

Alprostadil↗

Octreotide in the treatment of severe chemotherapy-induced diarrhea.

BACKGROUND: Chemotherapy-induced diarrhea (CID) is a common side effect of a number of chemotherapeutic agents. Conventional therapy for severe CID with opioids or loperamide is moderately effective. A prospective trial was conducted using octreotide acetate for treatment of severe CID refractory to loperamide. PATIENTS AND METHODS: Thirty-two patients with grade 2 and 3 CID refractory to loperamide were treated with octreotide at a dosage of 100 microg subcutaneously 3x/day for three days followed by 50 microg 3x/day for three days. Previous chemotherapy consisted of regimens containing fluorouracil, leucovorin, CPT-11, cyclophosphamide, methotrexate and cisplatin. Primary tumors were colorectal (n = 23), gastric (n = 3), and other cancers (n = 6). RESULTS: Complete resolution of diarrhea was obtained in 30 of 32 patients (94%); 5 within 24 hours, 14 within 48 hours, and 11 within 72 hours of treatment. Nineteen patients were treated as outpatients. Thirteen were hospitalized for a median of three days. Response was unaffected by age, gender, performance status, previous chemotherapy or primary tumor site. No side effects related to octreotide were observed. CONCLUSIONS: Octreotide 100 microg subcutaneously 3x/day for three days is an effective, safe treatment for CID given primarily or as a second-line therapy after loperamide failure.

Adult↗

Therapeutic response to octreotide in patients with refractory CPT-11 induced diarrhea.

PURPOSE: Severe diarrhea can represent a dose-limiting toxicity with the use of CPT-11. Conventional therapy is ineffective in some patients and is also limited by patient compliance. We report our observation on the effectiveness of octreotide acetate in the treatment of CPT-11-induced diarrhea refractory to opioids. PATIENTS AND METHODS: We describe 4 patients with metastatic gastrointestinal tumors who developed severe diarrhea following treatment with CPT-11 (65-125 mg/m2/weekly for 4 weeks every 6 weeks). Diarrhea was refractory to treatment with loperamide and diphenoxylate and was treated with octreotide acetate. RESULTS: Complete resolution of diarrhea was observed within 2-4 days of octreotide acetate treatment. Three patients responded to SC octreotide given every 8 hours and the 4th patient to octreotide given by continuous s.c. infusion. CONCLUSIONS: Our preliminary observation suggests value of octreotide in the control of CPT-11 induced refractory diarrhea. Prospective studies are warranted.

Adult↗