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PubMed2000

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↗
PubMed1982

Loperamide modifies Escherichia coli, heat-stable enterotoxin-induced intestinal secretion.

We have shown previously that loperamide, an opiate analogue, inhibits cholera-toxin- and prostaglandin E2-induced secretion in the rat small intestine. In these studies loperamide modified secretion induced by partially purified Escherichia coli, heat-stable enterotoxin in infant mice. The drug was effective whether administered before or after established secretion. These experiments provide further suggestive evidence that loperamide has a broad spectrum of antisecretory activity.

Animals↗
PubMed1988

A double-blind crossover comparison of lidamidine, loperamide and placebo for the control of chronic diarrhoea.

Fourteen patients with chronic diarrhoea, but no evidence of active organic disease, completed a double-blind crossover comparison of the anti-diarrhoeal effects of loperamide, placebo and the clonidine analogue, lidamidine. Failure of diarrhoea control led to early withdrawals from seven placebo- and six lidamidine-treatment periods, but there was only one early withdrawal during treatment with loperamide. Loperamide was found to be superior to lidamidine or placebo for the control of stool consistency in patients with chronic diarrhoea.

Adult↗
PubMed1979

Naloxone inhibits the anti-diarrhoeal activity of loperamide.

1 Subcutaneous prostaglandin E2 (2.5 mg/kg) produces profuse diarrhoea in fed rats. 2 Pretreatment of rats with subcutaneous loperamide (1.0 mg/kg) completely prevents prostaglandin-induced diarrhoea. If naloxone is administered prior to loperamide injections the activity of the antidiarrhoeal compound is completely destroyed. 3 These data provide strong evidence that the antidiarrhoeal activity of loperamide is mediated via the opiate receptor.

Animals↗
PubMed1996

Antidiarrhoeal activity of new thiazolidinones related to loperamide.

A series of thiazolidinones related to loperamide was synthesized and evaluated for antidiarrhoeal activity in mice, using the castor oil test. Of five compounds tested, antidiarrhoeal activity was found only for 2-(p-nitrophenyl)-3-¿3-[(4-(p-chlorophenyl)-4-hydroxy)piperidino]ethyl¿- 1,3-thiazolidin-4-one. The compound was less active than loperamide (ED50 values = 48.7 (24.8-95.6) and 0.91 (0.24-3.40) mg kg-1 respectively), but was also less toxic (LD50 values = 745.9 (545.2-929.8) and 108.9 (85.5-138.7) mg kg-1, respectively). Its antidiarrhoeal activity was counteracted by naloxone. Our results support the hypothesis that this compound, like loperamide, is an opiate-receptor agonist.

Animals↗
PubMed1977

Double-blind placebo-controlled study of loperamide (Imodium) in chronic diarrhoea caused by ileocolic disease or resection.

Loperamide (R 18 553) was compared with placebo in a double-blind crossover study of 21 patients with chronic diarrhoea caused by ileocolic disease or resection. Eighteen patients completed the trial. At a median daily dose of 6 mg the new antidiarrhoeal preparation was found to be superior to placebo in controlling chronic diarrhoea. The frequency and weight of stools significantly decreased, the stools became more solid, and carmine transit time was prolonged during loperamide therapy. Loperamide was consistently preferred to placebo by the patients. Gastrointestinal side-effects were few and comparable during both treatment periods.

Adult↗
PubMed1981

Effect of loperamide and naloxone on gastric acid secretion in healthy man.

The effect of acute oral administration of three different doses (4, 8, and 16 mg) of loperamide, a peripheral opiate agonist, on basal and submaximal pentagastrin-stimulated gastric acid secretion was evaluated in healthy volunteers. Both basal and stimulated gastric secretion were significantly lowered by 8 and 16 mg of the drug in comparison with a control study, while 4 mg was ineffective. Naloxone, a specific opiate antagonist, decreased slightly but not significantly both basal and pentagastrin-stimulated gastric acid secretion, when infused intravenously at the rate of 30 micrograms/kg/h, but completely abolished the inhibitory effect of loperamide on gastric acidity. These data also suggest that opiates may be involved in the regulation of gastric acid secretion in man by acting at a peripheral site, as loperamide does not cross the blood-brain barrier.

Adult↗
PubMed1999

Effect of wood creosote and loperamide on propulsive motility of mouse colon and small intestine.

To elucidate a mechanism of the antidiarrheal activity of wood creosote, its effect on the propulsive motility of mouse colon and small intestine was studied using a charcoal meal test and a colonic bead expulsion test. The effect was compared with that of loperamide. At an ordinary therapeutic dose, wood creosote inhibited the propulsive motility of colon, but not of small intestine. On the other hand, loperamide inhibited the propulsive motility of small intestine, but not of colon. The results indicate that at least a part of the antidiarrheal activity of wood creosote and loperamide is attributable to their antikinetic effect predominantly on colon of the former and predominantly on small intestine of the latter.

Animals↗
PubMed1977

Long-term survey of the treatment of diarrhoea with loperamide.

42 outpatients with chronic diarrhoea of varying origin received individually adapted doses (2--12 mg) of loperamide for a median time of 543 days (range 140--1,159 days). In most cases, the mean daily stool frequency dropped significantly and stool consistency improved clearly; the beneficial effects of the drug were maintained over the entire treatment period. Also, patients with diarrhoea of organic origin tended to react more favourably to loperamide than patients with functional diarrhoea. No drug-related changes in laboratory parameters could be detected and clinical side effects were virtually nil. No morphine-like effect of loperamide could be evidence by means of the pupil diameter changes after naloxone administration.

Adult↗
PubMed2006

Intrasperm Ca2+ modulation and human ejaculated sperm viability: influence of miconazole, clotrimazole and loperamide.

Elevation of intrasperm Ca(2+) is reported to influence viability of ejaculated spermatozoa. Human spermatozoa possess inositol triphosphate (IP(3))-sensitive Ca(2+) stores, which can be targeted for increasing intrasperm Ca(2+) level. The influence of agents affecting Ca(2+) homeostasis has been investigated. Miconazole nitrate, clotrimazole and loperamide hydrochloride produced a dose- and time-dependent decrease in viability, each requiring respectively 0.5, 1.0 and 1.0 mM for producing death of all sperm cells immediately upon addition to ejaculated human semen samples. The reduction in sperm viability was accompanied by elevation of intrasperm Ca(2+) and was not affected by presence or absence of extracellular Ca(2+). Significantly (P<0.05) less time was required for producing complete loss of sperm viability and increasing intrasperm Ca(2+) when any of these drugs was added to sperm cells previously treated with selected agents affecting Ca(2+) homeostasis. This enhanced spermicidal activity of miconazole, clotrimazole and loperamide appeared to be due to further mobilization of Ca(2+) from partially depleted intrasperm Ca(2+) stores. Synergism of spermicidal activity and intrasperm Ca(2+) elevation by miconazole or clotrimazole was observed when Ca(2+) efflux from sperm cells was simultaneously inhibited by 2',4'-dichlorobenzamil hydrochloride, a Na(+)-Ca(2+) exchange inhibitor. The spermicidal activity of miconazole, clotrimazole or loperamide due to elevation of intrasperm Ca(2+) and its synergism, therefore, has great potential for exploitation of these drugs as contact spermicides.

Adult↗
PubMed1997

Surveillance of loperamide ingestions: an analysis of 216 poison center reports.

BACKGROUND: Loperamide was approved for nonprescription use in 1988. While efficacy is well documented, there are few data on loperamide overdose and management. METHODS: Eight poison centers participated in a prospective study enrolling 216 patients. RESULTS: Where the amount ingested was known, it ranged from 0.03 to 0.94 mg/kg. One- to 3-year-olds were involved in 57.9% of ingestions. Ingestion was unintentional in 182 cases (84.3%), including 59 patients with therapeutic errors (27.3% of all cases). Dispensing cup errors were implicated in 23 cases; 15 patients assumed the dispensing cup was the unit of measure. No symptoms developed in 63.0%; 27.8% had related symptoms. No related symptoms were life-threatening, and no fatalities occurred. The most frequent symptoms were drowsiness (15.7%), vomiting (4.2%), and abdominal pain or burning (3.7%). The frequency of related symptoms was compared in patients receiving the most frequently utilized decontamination modalities: ipecac alone, activated charcoal alone, lavage and activated charcoal, and ipecac and activated charcoal. Compared to the 112 patients who received no decontamination, only the ipecac-treated group demonstrated a significant reduction in the frequency of related symptoms; 13.9% of patients given ipecac alone (without other gastric decontamination) had related symptoms compared to 33.0% of patients who received no decontamination. Three patients received naloxone for CNS symptoms related to loperamide; two responded and the response of the third was unknown. CONCLUSION: Within the range of doses implicated in this study (up to 0.94 mg/kg), there were no life threatening clinical effects and no fatalities. Development of a management protocol is complicated by the absence of a predictable clinical response in each dose range. The data suggest that children over six months with single acute ingestions up to 0.4 mg/kg, and possibly higher, can be safely managed at home, without gastric decontamination.

Adolescent↗
PubMed1975

Loperamide in the symptomatic control of chronic diarrhoea. Double-blind placebo-controlled study.

Fifteen patients (20-66 years) with persistent diarrhoea of varying aetiology were selected for an open trial of loperamide 2 mg capsules. The optimal daily dose for substantial reduction of the diarrhoea ranged from two to seven capsules. Eleven patients showed a significant improvement in stool consistency, a highly significant decrease in stool frequency and a decrease of abdominal cramps. One ileostomy patient with abundant ileostomy output and intermittent leaking of the ileosotmy appliance at night experienced a substantial reduction of the stoma output with virtual disappearance of soiling accidents as night. Loperamide appeared to be ineffective in two patients with cholerrhoeic diarrhoea; in one patient with laxative-induced diarrhoea and in one patient with probable nervous diarrhoea. The eleven successfully treated patients then entered a doubleblind placebo-controlled trial for ten days or util relaps, the daily dose being indentical to the optimal one previously determined in the open phase of the study. The investigator was able to guess the code correctly in ten out of eleven cases. The drug was well tolerated. Because of its considerable efficacy and low side-effect liability, loperamide has to be considered a promising drug in the treatment of chronic diarrhoea.

Adult↗
PubMedDate not supplied

Octreotide long-acting formulation (LAR) in chronic loperamide-refractory diarrhea not related to cancer treatment.

OBJECTIVE: The effectiveness and improvement in quality of life (QOL) of a long-acting formulation of octreotide (LAR) administration for cancer patients, with chronic loperamide-refractory diarrhea not attributed to medical therapy, were investigated. PATIENTS AND METHODS: Twenty-nine patients with chronic loperamide-refractory diarrhea were enrolled to receive octreotide LAR at a starting dose of 30 mg i.m. every 28 days until resolution of the diarrhea for a period of 3 months. RESULTS: Twenty-three patients (79.3%) administered octreotide LAR achieved resolution of diarrhea, while six patients (20.7%) successfully controlled their diarrhea during the study. All patients experienced improved sodium, potassium, albumin and total protein values with improvement in their QOL, as assessed by the Linear Analog Scale Assessment (LASA) (mean values at baseline and at 3 months: energy: 3.2+/-1.1 vs. 6.2+/-1.4; function: 3.1+/-1.3 vs. 6.2+/-1.2; QOL: 3.2+/-0.9 vs. 6.1+/-1.4). No toxicities associated with the administration of octreotide LAR were noted. CONCLUSION: The administration of octreotide LAR at a starting dose of 30 mg i.m. every 28 days efficiently resolved or controlled chronic loperamide-refractory diarrhea, not caused by medical intervention, in cancer patients and improved their QOL.

Adult↗
PubMed1987

Loperamide modifies but does not block the corticotropin-releasing hormone-induced ACTH response in patients with Addison's disease.

The effect of loperamide - a peripheral opiate agonist - on plasma ACTH response to Corticotropin-releasing Hormone (CRH) has been investigated in 6 patients with Addison's disease. After placebo administration CRH induced a marked ACTH increase. After loperamide administration ACTH levels fell to a nadir of 135 +/- 76 pg/ml, and then CRH was still able to induce an ACTH increase; the pattern of ACTH response to CRH was slightly delayed. There was a significant difference between the two ACTH curves after CRH only in the early phase of the response. These data suggest that the inhibitory role of loperamide on ACTH secretion is exerted at supra-pituitary level, although a pituitary site of action can not be excluded.

Addison Disease↗
PubMedDate not supplied

[Effects of loperamide on fecal electrolyte excretion in acute diarrhea in infants].

The effect of loperamide (Imodium) on fecal excretion of electrolytes was studied using a double-blind protocol in 63 infants aged 1 to 32 months, presenting with acute diarrhea. The etiology of these infections was due to virus (n = 9), E. coli (n = 4), Salmonella (n = 4), Shigella (n = 2) or was of undetermined origin (n = 34). The therapeutic protocol was the same for all the infants: ad libitum oral rehydration, with no drug being administered except for Imodium at an average dose of 20 to 25 drops/kg/24 h (0.16 to 0.20 mg/kg/24 h), given every 8 hours for at least 48 hours. Stool Na+ and K+ concentrations were determined in samples taken before and after the double-blind trial. In patients receiving loperamide, we observed a non-significant decrease in fecal Na+ concentration as compared with values before treatment. Comparison of the two groups of infants, one receiving Imodium, the other a placebo, showed a significant difference (p less than 1%) in fecal sodium concentration, due rather to an increase in stool Na+ in the placebo group than to a decrease in the group treated with Imodium. Moreover, the use of loperamide, compared with the placebo, did not result in a significant decrease in the number of stools, modified fecal K+ values, or more rapid recovery from the diarrheal syndrome.

Acute Disease↗
PubMed1986

Effect of loperamide on faecal control after rectoplasty for high imperforate anus.

The effect of loperamide on faecal control after Stephens rectoplasty for high imperforate anus was studied in eight patients more than 8 years after surgery. Clinical assessment and anorectal manometry were performed before and after administration of loperamide for 6 to 8 weeks. Decreased faecal soiling was noted in seven of the eight cases. Obstipation forced two patients to stop the medication. The improved faecal control was verified by an increase in squeeze pressure at anorectal manometry in four patients. When incontinence persists after Stephens rectoplasty, loperamide can improve the faecal control in some cases.

Adolescent↗
PubMed1978

[Studies using loperamide in patients with diarrhea following telecobalt irradiation of malignant abdominal tumors (author's transl)].

45 patients with diarrheas appearing after exposure of the gastro-intestinal region to ionizing radiation were given loperamide in the course of a study. A few days after administration of the loperamide, normalization of the stools took place, except in three cases. Simultaneous tenesmic gripes, some of the patients had also suffered from, disappeared completely, with the exception of two cases where, however, normalization of the stools was obtained by means of the loperamide therapy. Subjective side-effects did not occur. Also no alterations of the blood count, hematological features, liver function tests or urine have been observed.

Abdominal Neoplasms↗
PubMed1982

Diarrhoea following jejuno-ileostomy for morbid obesity. A randomised trial of loperamide and diphenoxylate.

The effect of loperamide and diphenoxylate on diarrhoea following jejuno-ileostomy for morbid obesity was investigated in 27 patients by means of a randomized fixed sample size, three-period cross-over trial. Both loperamide and diphenoxylate had significant effect on the diarrhoeas when compared with no treatment, but no significant difference was found between the two drugs. Loperamide is an acceptable alternative in the treatment of diarrhoea following jejuno-ileostomy.

Adult↗