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PubMed1996

A volunteer model for the comparison of laxatives in opioid-related constipation.

Loperamide was used to provide a source of opioid-induced constipation in healthy volunteers. Each volunteer took a sequence of three dose levels of loperamide. One of three laxatives was used to counterbalance the effect of loperamide and restore bowel function to what the individual considered normal at each stage before the dose of loperamide was increased. Lactulose, senna, and codanthrusate were selected as examples of a softening, a stimulant, and a combination laxative, respectively. Outcome measures were the doses of laxative used, stool form and frequency, ease of defecation, a rating scale of subjective bowel function, and the occurrence of adverse effects. Each laxative was taken by ten volunteers, and all proved capable of maintaining normal bowel function. A combination of stimulant and softening laxatives was most likely to maintain normal bowel function at the lowest dose and least adverse effects. The mean final dose of lactulose was excessive for use in ill patients. Senna was associated with significantly more adverse effects than the other laxatives, mainly abdominal pain (P < 0.001). This model of constipation may provide a standardized means of assaying the clinical effectiveness of oral laxatives.

Adolescent↗
PubMed1988

Methylene blue protects intestinal mucosa from free radical-mediated sublethal radiation damage.

Susceptibility of the intestine to radiation damage is a primary reason for the failure of external beam radiation to cure intra-abdominal cancer. High-dose irradiation causes intestinal denudation, fluid loss, and resultant shock. Simple and effective methods for protecting the intestine from irradiation damage are not available. Many biological effects of ionizing irradiation are caused by free radical intermediates. We have previously reported that many of the toxicities of doxorubicin, a classic free radical generating anticancer agent, are blocked by methylene blue pretreatment. We have now found that pretreatment with methylene blue protects rats from intestinal damage, as measured histologically and by quantitative stool blood determinations. Whereas the exact mechanisms of this protection remain elusive, we believe this method of modulating the therapeutic index of ionizing radiation deserves additional preclinical and clinical study.

Animals↗
PubMed1988

Development of a Crohn's index for survey research.

Current Crohn's disease activity indices are not suitable for survey research because they rely on information from the laboratory or physical examination. We used data from a multicenter controlled trial of adjuvant sulfasalazine to develop an index of Crohn's disease activity based on information which could be obtained exclusively by interview. The study population consisted of 89 actively symptomatic patients seen on 1082 occasions in eight medical centers. Multiple regression analyses identified three variables which predicted the ratings of physicians: stool frequency, abdominal pain and sense of well-being. The new index correlated very well (r = 0.87, p less than 0.001) with the Crohn's Disease Activity Index from which it was derived. The index may be used in epidemiologic studies to accurately place patients into quartiles of disease severity which correspond to similar quartiles of the CDAI.

Abdomen↗
PubMed2004

[Management of acute infantile diarrhoea: a study on community pharmacy counseling in the Midi-Pyrenees region].

UNLABELLED: Counselling by community pharmacists is becoming an accepted standard for pharmacy practice. However, drugs available in children without prescription form are scarce, and most of the over-the-counter drugs have not been tested and approved in children. OBJECTIVES: The aim of this study was to investigate attitude and knowledge of community pharmacists about advice and treatment in children with acute diarrhoea. MATERIAL AND METHODS: We sent a postal questionnaire to a sample of 176 community pharmacies in the Midi-Pyrénées area (South western France), asking what they would give as advice and/or drugs in a simulated case of acute diarrhoea in an eight-month-old baby. For each question (interview of the mother, counselling about hygiene and dietetics, monitoring and drugs), we compared pharmacists answers to available evidence-based data and/or guidelines in the literature and to Summary Products Characteristics (SPC) for each reported drug. Forty one percent of pharmacies answered, giving 101 exploitable questionnaires. RESULTS: Only 48.5% of subjects have recommended a rehydration solution. 71.3% recommended an inadequate beverage (soda) and 40% recommended stopping food intake despite WHO guidelines. Most of pharmacists (77%) noticed a drug with an appropriate indication and a paediatric mention in the SPC. However, in 12.9% of cases, drugs were contra-indicated or inadequate (loperamide, nifuroxazide, microorganisms available in capsules). CONCLUSION: Even if an appropriate advice was given by most of the responders, improvements in advice are needed: too many pharmacists recommended anti-diarrhoeal drugs and withholding milk despite evidence about their lack of effectiveness on dehydration prevention. Conversely, rehydration solutions, which have been proved their effectiveness since many years, are not sufficiently proposed.

Acute Disease↗
PubMed2003

CFTR pharmacology and its role in intestinal fluid secretion.

The cystic fibrosis transmembrane conductance regulator (CFTR) is a cAMP-activated Cl(-) channel expressed in epithelial cells in the airways, pancreas, intestine and other fluid-transporting tissues. Cystic fibrosis is caused by mutations in the CFTR, resulting in impaired Cl(-) transport and plasma membrane targeting. CFTR is expressed in the lumenal membrane of enterocytes, where it functions as the principal pathway for secretion of Cl(-) and fluid in enterotoxin-induced secretory diarrheas such as cholera. Small-molecule CFTR inhibitors reduce enterotoxin-induced intestinal fluid secretion in animal models. CFTR inhibition might also reduce intestinal fluid losses in cholera and possibly in other infectious and non-infectious diarrheas.

Animals↗
PubMed2006

Brain damage in neonatal rats following kaolin induction of hydrocephalus.

Neonatal and congenital hydrocephalus are common problems in humans. Hydrocephalus was induced in 1-day-old rats by injection of kaolin into the cisterna magna. At 7 and 21 days, magnetic resonance (MR) imaging was used to assess ventricle size, then brains were subjected to histopathological and biochemical analyses. Hydrocephalic pups did not exhibit delays in righting or negative geotaxis reflexes during the first week. At 7 days, there was variable ventricular enlargement with periventricular white matter edema, axon damage, reactive astrogliosis, and accumulation of macrophages in severe but not mild hydrocephalus. Cellular proliferation in the subependymal zone was significantly reduced. The cortical subplate neuron layer was disrupted. In rats allowed to survive to 21 days, weight was significantly lower in severely hydrocephalic rats. They also exhibited impaired memory in the Morris water maze test. Despite abnormal posture, there was minimal quantitative impairment of walking ability on a rotating cylinder. At 21 days, histological studies showed reduced corpus callosum thickness, fewer mature oligodendrocytes, damaged axons, and astroglial/microglial reaction. Reduced myelin basic protein, increased glial fibrillary acidic protein, and stable synaptophysin content were demonstrated by immunochemical methods. In conclusion, impairment in cognition and motor skills corresponds to ventricular enlargement and white matter destruction. Quantitative measures of weight, memory, ventricle size, and myelin, and glial proteins in this neonatal model of hydrocephalus will be useful tools for assessment of experimental therapeutic interventions.

Age Factors↗
PubMed2004

Antidiarrhoeal activity of Rhus javanica ripen fruit extract in albino mice.

The antidiarrhoeal effects of the methanolic extract of Rhus javanica ripen fruits (MERJ) were investigated by employing four experimental models of diarrhoea in Swiss albino mice. MERJ treated mice, showed significant reduction in the faecal output and protected them from castor oil-induced diarrhoea. The extract also reduced the intestinal fluid secretion induced by MgSO4 and gastrointestinal motility after charcoal meal administration in the albino mice. No mortality and visible signs of general weakness was observed in the mice following the test extract administration up to 2000 mg/kg dose.

Administration, Oral↗
PubMed2005

Antidiarrhoeal activity of Cyperus rotundus.

The methanol extract of Cyperus rotundus rhizome, given orally at the doses of 250 and 500 mg/kg b.w., showed significant antidiarrhoeal activity in castor oil induced diarrhoea in mice. Among the fractions, tested at 250 mg/kg, the petroleum ether fraction (PEF) and residual methanol fraction (RMF) were found to retain the activity, the latter being more active as compared to the control. The ethyl acetate fraction (EAF) did not show any antidiarrhoeal activity.

Animals↗
PubMed2005

Efficacy of current drug therapies in irritable bowel syndrome: what works and does not work.

Based on current evidence, bulking agents are not more effective than placebo at improving global irritable bowel syndrome (IBS)symptoms, although they may increase stool frequency in large doses. Tricyclic antidepressants are more effective than placebo for patients with diarrhea-predominant IBS. Imodium is more effective than placebo at improving stool consistency and decreasing stool frequency in patients with IBS, and it may be an important component for treating diarrhea-predominant IBS. Antispasmodics agents available in the United States are not more effective than placebo for treating IBS, although the studies are small and poorly designed. There are no randomized controlled trials examining the efficacy of laxatives for managing IBS. Tegaserod is more effective than placebo at improving global IBS symptoms in women with nondiarrhea-predominant IBS. Alosetron is more effective than placebo in women with diarrhea-predominant IBS, although its use should be limited to patients who have failed conventional therapy because of its adverse event profile.

Antidepressive Agents↗
PubMed2004

Liquid chromatography-tandem mass spectrometry determination of loperamide and its main metabolite desmethylloperamide in biological specimens and application to forensic cases.

A liquid chromatographic mass spectrometric (LC/MS/MS) method has been developed for the determination of loperamide in whole blood and other biological specimens. The procedure involves liquid-liquid extraction of loperamide, desmethylloperamide and methadone-D3 (internal standard) with butyl acetate. Confirmation and quantification was done by positive electrospray ionisation with a triple quadrupole mass spectrometer operating in multiple reaction-monitoring (MRM) mode. Two MRM transitions of each compound were established and identification criteria were set up based on the ratio of the responses between the two MRM transitions of each compound. The standard curves were linear over a working range of 0.1-500 microg/kg for all transitions. The limit of quantification was 0.1 microg/kg in whole blood. The repeatability and reproducibility within the laboratory expressed by relative standard deviation were less than 5 and 11%, respectively, and the accuracy was better than 9%. The method was developed to examine a feces sample from a child whose mother was suspected of Münchausen syndrome by proxy and it proved to be suitable for forensic cases being simple, selective and reproducible. The method was also applied for a case investigation involving a overdose of loperamide.

Antidiarrheals↗
PubMed2005

Validation of a liquid chromatographic-tandem mass spectrometric method for the determination of loperamide in human plasma.

A sensitive and selective method based on liquid chromatography-tandem mass spectrometry (LC-MS/MS) has been developed for the quantitative determination of loperamide in human plasma. Automated solid-phase extraction (SPE) on disposable extraction cartridges (DEC) is used to isolate the compounds from the biological matrix and to prepare a cleaner sample before injection and analysis in the LC-MS/MS system. After conditioning, the plasma sample is loaded on the DEC filled with endcapped ethyl silica (C2(EC)) and washed twice with water. The analytes are therefore eluted by dispensing methanol. The eluate is then collected and added with ammonium acetate solution in order to inject an aliquot of this final extract in the LC-MS/MS system. On-line LC-MS/MS system using atmospheric pressure chemical ionization (APCI) has been developed for the determination of loperamide. The separation is obtained on a octadecylsilica based stationary phase using a mobile phase consisting in a mixture of methanol and 5mM ammonium acetate solution (25:75, v/v). Clonazepam is used as internal standard (IS). The MS/MS ion transitions monitored are m/z 477--> 266 and 316--> 270 for loperamide and clonazepam, respectively. The most appropriate regression model of the response function as well as the limit of quantitation were first selected during the pre-validation step. These latter criteria were then assessed during the formal validation step. The limit of quantitation (LOQ) was around 50 pg/ml for loperamide. The method was also validated with respect to recovery, precision, trueness, accuracy and linearity.

Antidiarrheals↗
PubMed2004

Anti-diarrheal and spasmolytic activities and acute toxicity study of Soonkijangquebo, a herbal anti-diarrheal formula.

The anti-diarrheal and spasmolytic activities of Soonkijangquebo (SKJQB), a Korean herbal anti-diarrheal formulation, were subjected to pharmacological evaluation. SKJQB, at a dose of 50-200 mg/kg, inhibited castor oil-induced diarrhea in mice. The median effective dose (ED50) for the anti-diarrheal effect was 93 mg/kg. In isolated rabbit jejunum preparations, SKJQB produced a spasmolytic effect by the relaxation of spontaneous contractions in a dose-dependent manner. The median effective concentration (EC50) for the spasmolytic effect was 3.6 mg/ml. In isolated guinea pig ileum preparations, SKJQB also produced a spasmolytic effect by reduction of acetylcholine-induced contractions. When tested against calcium channel blockade in rabbit jejunum, SKJQB caused a dose-dependent rightward shift in the Ca2+ dose-response curves, similar to that produced by verapamil, a well-known calcium antagonist. In an acute toxicity study in Sprague-Dawley rats, the median lethal dose (LD50) of SKJQB was greater than 2000 mg/kg, and no pathological changes were noticed in macroscopic examination by necropsy of rats treated with SKJQB. Thus, SKJQB may be safely used as a spasmolytic as well as an anti-diarrheal agent.

Animals↗
PubMed2004

Evaluation of the bioactivity of triterpene mixture isolated from Carmona retusa (Vahl.) Masam leaves.

The major constituent of Carmona retusa (Vahl.) Masam. leaves is an intractable mixture of triterpenes, namely alpha-amyrin (43.7%), beta-amyrin (24.9%), and baurenol (31.4%). At a dosage of 100mg/kg mouse, the triterpene mixture exhibited 51% analgesic activity but only showed 20% anti-inflammatory activity. Kruskal-Wallis one-way analysis of variance by ranks showed that the triterpene mixture is as active as mefenamic acid, a commercially available analgesic, at alpha = 0.01. The charcoal tracing test showed a 29% anti-diarrheal activity for the triterpene mixture, which increased to 55% at a dosage of 250 mg/kg mouse. At the higher dosage, the triterpene mixture differed significantly from its solvent control at alpha = 0.01. Results of the micronucleus test showed that the triterpene mixture did not exhibit mutagenic nor anti-mutagenic activity at alpha = 0.001. There was no significant decrease in blood glucose levels (bgl) in alloxan-induced diabetic mice after administration of the triterpene mixture. The triterpene mixture was inactive against Escherichia coli and possessed moderate activities against Staphylococcus aureus, Candida albicans, and Trichophyton mentagrophytes.

Acetic Acid↗
PubMed2004

Antidiarrhoeal activity of some Egyptian medicinal plant extracts.

The antidiarrhoeal activity of six Egyptian medicinal plant extracts (200 and 400 mg kg(-1)) and their effect on motility of isolated rabbit's duodenum was investigated. Phytochemical screening of the plant extracts for their active constituents was also carried out by TLC. Oral administration of methanol extract from Conyza dioscoridis (CD) or Alhagi maurorum (AM) in a 200 mg kg(-1) dose exhibits a significant antidiarrhoeal effect against castor oil-induced diarrhoea, while Mentha microphylla (MM), Convolvulus arvensis (CA), Conyza linifolia (CL) produced no significant effect. In a dose of 400 mg kg(-1), Mentha microphylla, Conyza dioscoridis, Alhagi maurorum, Zygophyllum album (ZA), and Conyza linifolia produced a significant (P<0.01) effect, while Convolvulus arvensis produced no antidiarrhoeal effect in rats. Methanol extract of Mentha microphylla, Conyza dioscoridis, Zygophyllum album, and Convolvulus arvensis induced a dose-dependent (0.4-2.8 mg ml(-1)) relaxation of rabbit's duodenal smooth muscle. Alhagi maurorum and Conyza linifolia increased the contractile force in concentrations between 0.4 and 1.6 mg ml(-1). Higher concentrations (>3.2 mg ml(-1)) caused a rapid depressant effect. The depressant effect induced by Alhagi maurorum (in a higher dose) and Zygophyllum album appeared to be due to calcium channel blocking effect, since CaCl(2) could not restore the contractile response of the tissue impregnated in calcium free-medium. However, a ganglionic blocking effect appeared to be a possible mechanism of action of Mentha microphylla and Conyza dioscoridis since a stimulant dose of nicotine could not restore the contractile response of the tissue. The effect of Convolvulus arvensis and Conyza linifolia was not through any of the common mediators. Phytochemical screening revealed the presence of tannins, flavonoids, unsaturated sterols/triterpenes, carbohydrates, lactones and proteins/amino acids as major constituents.

Animals↗
PubMed2005

Anti-diarrhoeal activity of Butea monosperma in experimental animals.

The anti-diarrhoeal potential of the ethanolic extract of stem bark of Butea monosperma (Lam) Kuntz has been evaluated using several experimental models in Wistar albino rats. The extract inhibited castor oil induced diarrhoea and PGE(2) induced enteropooling in rats; it also reduced gastrointestinal motility after charcoal meal administration. The results obtained establish the efficacy and substantiate the use of this herbal remedy as a non-specific treatment for diarrhoea in folk medicine.

Animals↗