Through pH determination, acide- color quantification, extraction time and stabilization time of solvent extracting layer, optimal parameters were determined to quantify loperamide. The method could have high sensitive and selectivity with precise and repetitive results; its is appropriate for laboratories at low level of technique equipments
Loperamide ; Pharmaceutical Preparations ; Laboratories

Certain phenolic compounds are known to exhibit laxative properties. Seed sprouts, such as those of peanut, are known to promote de novo biosynthesis of phenolic compounds. This study was conducted to examine the potential laxative properties of 80% (v/v) ethanolic extract of peanut sprout (PSE), which contains a high concentration of phenolic compounds such as resveratrol. For this, SD rats were orally administered PSE while a control group was incubated with saline. Laxative effects were examined in both groups of rats. Constipation induced by loperamide in SD rats was improved by administration of PSE. Constipated rats showed increased intestinal movement of BaSO4 upon administration of PSE compared to the control, and the groups administered 100 or 1,000 mg PSE/kg bw were not significantly different in transit time of the indicator. However, colon length was not statistically different among the experimental groups, although it was longer in the group incubated with 1 g PSE/kg bw compared to other groups. Further, there was no significant difference in stool number among the experimental groups. Taken together, these findings show that PSE has a laxative effect in a rat model of loperamide-induced constipation.
Animals ; Colon ; Constipation ; Ethanol ; Loperamide ; Phenol ; Rats ; Seeds ; Stilbenes

PURPOSE: Some patients who underwent low anterior resection of the rectum do not show satisfying improvement in their anorectal function despite of long-term conservative management. The aim of this prospective study was to evaluate whether loperamide or diazepam could improve anorectal symptoms. METHODS: Fifty-two patients who continued to complain of problems with their anorectal function at least 6 months (mean: 1 year and 2 months) after the operation were recruited. The patients were randomly divided into two groups, and 2 mg of loperamide (loperamide-group, n=24) or diazepam (diazepam-group, n=28) was given orally three times a day for 4 weeks. Standardized interviews concerning anorectal function and anorectal physiologic studies were performed before medication, at the fourth week of medication, and 4 weeks after withdrawal from the medication. RESULTS: In both groups during the medication, daily stool frequency, the number of patients with urgency to defecate, and incontinence score significantly decreased, and maximal resting pressure and urge sensation volume significantly increased. In the diazepam-group, the decrease in daily stool frequency, the number of patients with urgency to defecate, and the increase in urge sensation volume continued after withdrawal from the medication. CONCLUSION: Loperamide or diazepam could improve the long-lasting fecal incontinence symptoms after low anterior resection in patients with rectal cancer. In the process, the increase in maximal resting pressure and urge sensation volume seemed to contribute to a significant degree.
Diazepam* ; Fecal Incontinence* ; Humans ; Loperamide* ; Prospective Studies ; Rectal Neoplasms ; Rectum* ; Sensation

Shouhui Tongbian Capsules was used to explore the therapeutic effect and potential mechanism on slow transit constipation model mice induced by loperamide hydrochloride. In the experiment, loperamide hydrochloride-induced ICR mice were used as the model of slow transit constipation. Fifty ICR mice were divided into the blank group, model group and high, medium and low dose groups of Shouhui Tongbian Capsules extract(100, 200 and 400 mg·kg~(-1)). The model group and the administration groups were then modeled using loperamide hydrochloride intragastrically to obtain slow transit constipation. After successful modeling, high, medium and low doses of drugs were given to each drug group by intragastric administration. After 14 days of administration, the first defecation time, 6 h defecation grain number, 6 h defecation wet weight and dry weight, black feces discharged within 6 h and the fecal water content were measured. Intestinal tissues were taken for c-Kit and SCF immunohistochemical sections to detect the expression of c-Kit and SCF in the blank group, model group and high, medium and low dose groups of the medicinal extract of Shouhui Tongbian Capsules. The tissue changes in the intestinal wall of mice were detected by HE staining. At the same time, partial intestinal tissues were taken to test the activity of ATP synthase and isocitrate dehydrogenase in intestinal tissues of mice. RESULTS:: showed that Shouhui Tongbian Capsules effectively improved the symptoms of slow transit constipation in ICR mice and promoted intestinal movement. Shouhui Tongbian Capsules obviously shortened the time of discharging black stool for the first time, improved the intestinal propulsion rate, increased the water content and amount of feces, and improved the constipation symptoms. Mechanism study revealed that Shouhui Tongbian Capsules increased ATP synthase activity and mitochondrial isocitrate dehydrogenase activity in intestinal tissue, and up-regulated c-Kit/SCF signaling pathway to promote interstitial Cajal cells proliferation, intestinal nerve transmission, intestinal motility and transport capacity.
Animals ; Capsules ; Constipation/drug therapy* ; Gastrointestinal Transit ; Loperamide ; Mice ; Mice, Inbred ICR

Irritable bowel syndrome (IBS) is a common chronic, relapsing functional bowel disorder. IBS can be diagnosed according to the established series of criteria excluding organic diseases, and by institution of a therapeutic trial. Treatment should be tailored to individual patients' needs and fears. Education and reassuring the patients is a simple and effective form of therapy. Correction of precipitating factors can also be therapeutic. Some patients may be helped by changing the diet, avoiding certain drugs, and reducing life stressors. Symptomatic treatment includes fiber for constipation, loperamide for diarrhea, and low-dose antidepressants or antispasmodics for pain; therapeutic efficacy of novel modalities including drugs acting on serotonin receptors are under investigation.
Antidepressive Agents ; Constipation ; Diagnosis* ; Diarrhea ; Diet ; Education ; Humans ; Irritable Bowel Syndrome* ; Loperamide ; Parasympatholytics ; Precipitating Factors ; Receptors, Serotonin

A correlation between endoplasmic reticulum (ER) stress and laxative effects was first reported in a constipation model treated with an aqueous extract of Liriope platyphylla (AEtLP) roots. To investigate the correlation between the laxative effect of uridine (Urd) and ER stress response, alterations in the key parameters for ER stress were measured in loperamide (Lop) induced constipation Sprague Dawley (SD) rats treated with Urd. The efficacy of the laxative effect of Urd was notable on the symptoms of chronic constipation, including alteration of stool parameters and structure of the transverse colon, in Lop induced constipated SD rats. In the PERK/eIF2-ATF4 pathway of ER stress response, the levels of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation and DNA damage-inducible protein (GADD34) transcripts were significantly enhanced in the Lop+Vehicle treated group. However, the levels were restored in the Lop+Urd treated group, although few differences were detected in the decrease rate. Similar changes were observed for levels of inositol-requiring enzyme 1 beta (IRE1β) phosphorylation and X-box binding protein 1 (XBP-1) transcript in the IRE1α/XBP pathway. Furthermore, the number of ER stress-induced apoptotic cells and Bax and Bcl-2 expression were recovered in the Lop+Urd treated group compared to the Lop+Vehicle treated group. The results of the present study therefore provide first evidence that the laxative effects of Urd may be tightly correlated with the recovery of ER stress response in constipation models.
Animals ; Apoptosis ; Carrier Proteins ; Colon, Transverse ; Constipation ; DNA ; Endoplasmic Reticulum ; Eukaryotic Initiation Factor-2 ; Loperamide* ; Phosphorylation ; Rats* ; Uridine*

Regulation of gastrointestinal hormones have been reported in animal models for constipation undergoing laxative therapy when administered herbal products. We undertook to investigate whether the laxative activity of gallotannin-enriched extracts isolated from Galla Rhois (GEGR) affects the regulation of gastrointestinal hormones, by examining the concentration of four hormones and the activation of their receptors in the loperamide (Lop)-induced constipation model. Stool parameters, including number, weight and water content, were significantly recovered in the Lop+GEGR treated group, relative to the Lop+vehicle treated group; however, food intake and water consumption were maintained at a constant level. Also, a similar recovery was detected for thickness of mucosa, muscle and flat luminal surface in the Lop+GEGR treated group. Furthermore, concentration of the four gastrointestinal hormones evaluated, namely, cholecystokinin (CCK), gastrin (GAS), somatostatin (SS) and motilin (MTL), were lower in the Lop+vehicle treated group than the No treated group, but were remarkably enhanced in the Lop+GEGR treated group. Moreover, the downstream signaling pathway of MTL and SS receptors were recovered after GEGR administration. Results of the present study therefore indicate that the laxative effects of GEGR treatment may be tightly related with the regulation of gastrointestinal hormones in the Lop-induced constipation model.
Animals ; Cholecystokinin ; Constipation* ; Drinking ; Eating ; Gastrins ; Gastrointestinal Hormones* ; Loperamide ; Models, Animal ; Motilin ; Mucous Membrane ; Phenobarbital ; Rats* ; Somatostatin ; Water

BACKGROUND/AIMS: Microscopic colitis (MC) encompasses collagenous and lymphocytic colitis and is characterized by chronic diarrhea. In cases of MC, colonic mucosae are macroscopically normal, and diagnostic histopathological features are observed only upon microscopic examination. We designed a prospective multicenter study to determine the clinical features, pathological distribution in the colon and prevalence of MC in Korea. METHODS: We prospectively enrolled patients having watery diarrhea no more than 3 times a day between March 2008 and February 2009. We obtained patient histories and performed colonoscopies with random biopsies at each colon segment. RESULTS: A total of 100 patients with chronic diarrhea were enrolled for a normal colonoscopy and stool exam. MC was observed in 22 patients (22%) (M:F 1.2:1; mean age, 47.5 years). Of those 22 patients, 18 had lymphocytic colitis and 4 had collagenous colitis. The entire colon was affected in only 3 cases (13.6%), the ascending colon in 6 cases (27.2%), the transverse colon in 3 cases (13.6%), and the left colon in 3 cases (13.6%). More than 2 segments were affected in 7 cases (31.8%). Nonsteroidal anti-inflammatory drug-associated MCs were observed in 4 cases (18.2%), 3 of which showed improved diarrhea symptoms following discontinuation of the medication. Frequently associated symptoms were abdominal pain and weight loss. Autoimmune diseases were observed in 4 cases (18.2%). Half of the 22 patients with MC improved with conservative care by loperamide or probiotics. CONCLUSIONS: In a prospective multicenter study of Korean patients with chronic diarrhea, the frequency of MC was found to be approximately 20%, similar to the percentage observed in Western countries. Therefore, the identification of MC is important for the adequate management of Korean patients with chronic diarrhea.
Abdominal Pain ; Autoimmune Diseases ; Biopsy ; Colitis, Collagenous ; Colitis, Lymphocytic ; Colitis, Microscopic ; Collagen ; Colon ; Colon, Ascending ; Colon, Transverse ; Colonoscopy ; Diarrhea ; Humans ; Loperamide ; Mucous Membrane ; Prevalence ; Prospective Studies ; Weight Loss

Irritable bowel syndrome (IBS) is a chronic relapsing disorder of gastrointestinal function, the main features of which are abdominal pain or discomfort and an alteration of the bowel habit. Rome Ⅱ criteria is the most recent international consensus definition for IBS. Rome Ⅱ consensus provides working definitions for constipation-(C-IBS) and diarrhea-predominant (D-IBS) subgroups. Initial management begins with a detailed history taking, including a careful dietary history. The presence of obvious causative factors of stress should be identified. Therapeutic trials may include those of dietary fiber supplementation for C-IBS, dietary manipulation and/or antidiarrheal agents for D-IBS, and antispasmodics for prominent pain. Reassurance of the patient is vital in the initial management. Current approaches to the long-term management of IBS include dietary measures, fiber and bulking agents, antispasmodic agents, antidiarrheal agents, laxatives, psychotroic drugs, and psychological and behavioral therapy. Medications should be prescribed as required, rather than on a regular basis. For moderate or severe abdominal pain, antispasmodics and certain smooth muscle relaxants may be used. These types of drugs are ideally used for a short term during an exacerbation of symptoms. In resistant cases, low-dose antidepressants have been used to treat the abdominal pain of IBS. For diarrhea, loperamide can be used effectively on a p.r.n. basis. For constipation, an increase in dietary fiber and/or dietary fiber supplements should be continued in a long-term basis. If symptoms continue, osmotic laxatives can be tried. Anthraquinone laxatives such as aloe or senna should be avoided in long-term treatment.
Abdominal Pain ; Aloe ; Antidepressive Agents ; Antidiarrheals ; Consensus ; Constipation ; Diarrhea ; Dietary Fiber ; Drug Therapy* ; Humans ; Irritable Bowel Syndrome* ; Laxatives ; Loperamide ; Muscle, Smooth ; Parasympatholytics

BACKGROUND: Constipation is one of the most common disorders in Korea and Western countries. It may be related with life style, diet, physical activity, age, stress and gender, and particularly premenopausal women experience constipation more often than men due to the significant prolongation of the mean colonic transit in women. The aim of this study was to evaluate the effect of a probiotic on constipation in loperamide-induced constipated rats. MATERIALS AND METHODS: The rats were divided into 3 groups. Constipation was induced by administration of loperamide for 5 days, and the excreted amount as well as the number of feces was observed. Lactic acid bacteria as a probiotic were administered orally every day for 5 days. RESULTS: The results showed that loperamide administration induced severe experimental constipation in rats. The amount of feces was decreased and the number of pellets was increased by loperamide. The water content in the feces as a parameter of constipation was also decreased by loperamide. On the other hand, the dry weights of feces were not significantly different among the groups. It represents that the amount of food consumption might have been similar among the groups, and constipation was caused by delayed intestinal movement. CONCLUSION: Probiotic administration for 5 days in rats partly alleviated or prevented the constipation induced by loperamide.
Animals ; Bacteria ; Colon ; Constipation ; Diet ; Feces ; Female ; Hand ; Humans ; Korea ; Lactic Acid ; Life Style ; Loperamide ; Male ; Motor Activity ; Probiotics ; Rats ; Water ; Weights and Measures