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PubMed1979

Dissociation between opiate-like and antidiarrheal activities of antidiarrheal drugs.

Three synthetic antidiarrheals, diphenoxylate, loperamide and SC 27166, and two narcotics, morphine and codeine, were evaluated in rats by the intravenous and oral route for specificity and duration of their antidiarrheal, opiate-like and acute toxic effects. The activity in the castor oil test, the tail withdrawal test and the acute toxicity test was used to determine the relative antidiarrheal specificity and relative safety margins. An analysis of animal and clinical data indicate these tests to be excellent indicators of clinical usefulness and specificity. Intravenously, all five agents induced opiate-like central effects, loperamide and SC 27166 at near toxic doses only. When administered orally loperamide and SC 27166 were devoid of opiate-like central nervous system activity. Analysis of the plasma levels after oral loperamide indicated that this drug does not attain a concentration high enough to induce opiate-like central effects. All agents were effective antidiarrheals by the oral route with loperamide being the most potent (ED50 = 0.15 mg/kg), longest acting (ED50 8 hr = 1.81 mg/kg) and most specific (relative antidiarrheal specificity, 8 hr greater than or equal to 88) and having the greatest relative safety margin (8 hr = 102).

Administration, Oral↗
PubMed1995

Observational Study of Travelers' Diarrhea.

Background: European air travelers returning from Algeria, Egypt, Mexico, Morocco, and Tunisia were interviewed about their experience of travelers' diseases upon arrival in Brussels. Diarrhea was mentioned by 37% of the adults and 27% of the children. These subjects were questioned about the types of measures taken, type and duration of drug treatment (if any), and about duration of diarrhea and side effects experienced. Methods: Final analysis was performed based on 2160 interviews. The largest proportion of diarrhea was reported in the age group 15-24 years (46%). Results: The majority of the 2160 subjects had opted for drug treatment (81%): 927 subjects for loperamide alone, 235 for loperamide in combination with nifuroxazide, and 178 for nifuroxazide alone. Other drugs had been used less frequently. The median time to recovery was 2.4 days with loperamide compared to 3.2 days with nifuroxazide and to 3.4 days for the no-treatment group. Conclusions: A stratification of the results by severity of the diarrhea suggests a rank of antidiarrheal potency as follows: loperamide > nifuroxazide > no-drug treatment. The side effect with the highest incidence was constipation (2.4% with loperamide). (J Travel Med 2:11-15, 1995) Travelers' diarrhea is usually defined as the passage of at least three unformed stools per day or any number of such stools when accompanied by fever, abdominal cramping, or vomiting. The definition may be broadened to include more trivial bowel disturbance.1,2 The duration of this self-limited disease generally is 3 to 5 days. Medical intervention aims at shortening the duration of disease, thus allowing the sufferer to resume his or her usual activities at an early stage. A shortened period of recovery to physical well-being has obvious favorable economic implications if the traveler is on business and may help the maintenance of a desired level of quality of life while a traveler is on holiday. An observational study of various medical complaints made by European travelers about their stay in areas outside Europe (Algeria, Egypt, Mexico, Morocco, and Tunisia) was conducted. Air travelers returning from these areas between July 15 and August 16, 1992, were interviewed upon arrival at Brussels airport by means of a standardized questionnaire written up in lay language. As shown in Table 1, the total number of complaints in the adult group (>= 15 years of age, n = 5373) was 4919 and 446 in the pediatric group (n = 818). With fever as an exception, there were fewer complaints in children. Only approximately 50% of the travelers did not suffer

Journal Article↗
PubMed1989

Effect of altering small bowel transit time on sustained release theophylline absorption.

The relationship between variations in small bowel transit time (SBTT) and the absorption of theophylline from a sustained-release product was evaluated in a three-way, randomized, crossover study in 12 healthy male nonsmokers. Subjects received sustained-release theophylline (600 mg) with loperamide (8 mg every 6 hour x 8 doses). metoclopramide (15 mg every 6 hour x 8 doses) or placebo (every 6 hour x 8 doses). Theophylline solution (400 mg) was used as a reference standard. Serum samples were collected periodically for 72 hours for theophylline concentration determinations. SBTT was measured by the lactulose hydrogen breath test. Compared with placebo (98 +/- 53 min), SBTT was increased with loperamide (211 +/- 87 min; P less than 0.001) and decreased with metoclopramide (55 +/- 18 min; P less than 0.001). Loperamide decreased the rate, but not the extent of theophylline absorption from this product. This was evident from the reduced Cmax, the prolonged Tmax, and the decreased fraction of the dose absorbed at 24 hours, while the area under the curves remained the same. In contrast, metoclopramide had no effect either on rate or extent of absorption. The data suggest that the effect of loperamide on these absorption parameters was due to an increase in the dissolution time of this sustained-release product.

Adult↗
PubMed1981

Subcutaneous morphine reduces intestinal propulsion in rats partly by a central action.

Rats were given intracerebroventricular or intravenous injections of the quarternary opioid receptor antagonist N,N-diallyl-normorphinium (DANM. 100 microgram). Ten min later morphine (7.5 mg/kg) or loperamide (10 mg/kg) was injected subcutaneously. Intestinal propulsion was assessed by measuring the progress of radioactive chromium (Na51(2) CrO4, 0.5 microCi) along the small intestine. The radioactive chromium was instilled into the proximal duodenum 20 min after injection of morphine or loperamide, and the animals sacrificed 35 min after giving radioactive chromium. Morphine and loperamide both inhibit intestinal propulsion. DANM (100 microgram i.c.v.) reduces the effect of morphine but not loperamide. Intravenous injection of DANM does not reduce anti-propulsive action of morphine. By itself DANM neither increases nor decreases intestinal propulsion. These experiments indicate that morphine, when administered by a peripheral route, reduces small intestinal propulsion in the rat partly through an action on brain opioid receptors.

Animals↗
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↗
PubMed2003

Morphine and d-amphetamine nullify each others' hypothermic effects in mice.

We have examined the effects of the psychostimulant d-amphetamine and the neuroleptic haloperidol on hypothermia induced by intraperitoneal injection of the centrally penetrating opioids morphine, fentanyl and sufentanil and the peripherally acting opioid loperamide. Measuring rectal body temperatures, dose-response relationships were established for all compounds. Morphine and sufentanil produced hyperthermia at low doses and dose-related hypothermia at higher doses. Fentanyl and loperamide produced dose-related hypothermia. Fixed doses of each opioid producing significant hypothermia were selected for interaction studies. The psychostimulant d-amphetamine was found t o produce biphasic effects with low doses inducing hypothermia and higher doses inducing hyperthemia. Haloperidol produced dose-related hypothermia. The selected doses of the opioids were then injected followed after 15 min. by injection of hypothermia producing doses of d-amphetamine or haloperidol. Hypothermia induced by morphine, fentanyl and sufentanil was reversed by d-amphetamine whereas loperamide-induced hypothermia was unaffected. Rebound hyperthermia was also measured with fentanyl and sufentanil. Haloperidol increased the hypothermic effects of morphine, fentanyl and sufentanil but not of loperamide. In conclusion, the central stimulating effects of opioids and amphetamine may combine resulting in thermogenesis and reversal of hypothermia. Central mechanisms of opioid-induced hypothermia in mice are influenced by drugs which alter the dopamine system, whereas peripheral mechanisms are unaffected. A possible clinical implication for this dopaminergic interaction may be toxicity associated with hyperpyrexia caused by psychostimulant misuse, which is increasingly occurring concomitantly with abuse of opioids.

Analgesics, Opioid↗
PubMed1997

Lower serum oestrogen concentrations associated with faster intestinal transit.

Increased fibre intake has been shown to reduce serum oestrogen concentrations. We hypothesized that fibre exerts this effect by decreasing the time available for reabsorption of oestrogens in the colon. We tested this in volunteers by measuring changes in serum oestrogen levels in response to manipulation of intestinal transit times with senna and loperamide, then comparing the results with changes caused by wheat bran. Forty healthy premenopausal volunteers were placed at random into one of three groups. The first group took senna for two menstrual cycles then, after a washout period, took wheat bran, again for two menstrual cycles. The second group did the reverse. The third group took loperamide for two menstrual cycles. At the beginning and end of each intervention a 4-day dietary record was kept and whole-gut transit time was measured; stools were taken for measurement of pH and beta-glucuronidase activity and blood for measurement of oestrone and oestradiol and their non-protein-bound fractions and of oestrone sulphate. Senna and loperamide caused the intended alterations in intestinal transit, whereas on wheat bran supplements there was a trend towards faster transit. Serum oestrone sulphate fell with wheat bran (mean intake 19.8 g day(-1)) and with senna; total- and non-protein-bound oestrone fell with senna. No significant changes in serum oestrogens were seen with loperamide. No significant changes were seen in faecal beta-glucuronidase activity. Stool pH changed only with senna, in which case it fell. In conclusion, speeding up intestinal transit can lower serum oestrogen concentrations.

Adult↗
PubMed1987

Effect of two potent calmodulin antagonists on calcium transport of brush border and basolateral vesicles from human duodenum.

In the present in-vitro study we investigated the possible role of the calmodulin-antagonistic drugs loperamide and calmidazolium in the regulation of transepithelial Ca2+ transport of human duodenum. Brush border membrane vesicles and basolateral membrane vesicles were simultaneously prepared from surgically resected pieces of morphologically intact human duodenum with a modified Percoll-gradient centrifugation method. Brush border and basolateral membrane vesicles were characterized using enzyme marker analysis and electron microscopy: alkaline phosphatase was enriched 20-fold in brush border membrane vesicles, whereas [Na+ + K+]-stimulated adenosine triphosphatase was enriched 15-fold in basolateral membrane vesicles. Calmodulin activity was determined by a specific radioimmunoassay after solubilizing brush border and basolateral membrane vesicles in 1% Triton X-100. In basolateral membrane vesicles, we found no calmodulin activity. In brush border membrane vesicles calmodulin activity was impaired by 50% after pre-incubation with loperamide or calmidazolium. We measured calcium, sodium, D-glucose and D-mannitol uptake with a rapid filtration technique. Before the transport experiments, brush border and basolateral membrane vesicles were pre-incubated with 5 microM loperamide or 5 microM calmidazolium for 60 min at 5 degrees C. In drug-pretreated, brush border membrane vesicles calcium uptake was significantly reduced after 1 min incubation (-25% +/- 5%, P less than 0.05); this effect was completely reversed in the presence of 5 microM calmodulin. In basolateral membrane vesicles, we found two Ca2+ transport systems: (1) Na+/Ca2+ exchange and (2) ATP-dependent Ca2+ transport. In basolateral membrane vesicles loperamide had no effect. Calmidazolium had no effect on Na+/Ca2+ exchange, but significantly inhibited ATP-dependent Ca2+ transport. This effect could not be reversed by calmodulin.

Biological Transport, Active↗
PubMed1983

The effects of an opiate agonist and antagonist on the human upper gastrointestinal tract.

Endogenous opiates may play a role in regulating intestinal function and we have investigated this possibility in the human upper gastrointestinal tract using loperamide as a locally-acting opiate agonist and naloxone as antagonist. Loperamide (4 mg) had no effect on the fasting pattern of motor activity in the antrum, duodenum and proximal jejunum. However, naloxone (40 micrograms kg-1 h-1, i.v.) abolished interdigestive motor activity in five of ten subjects and reduced antroduodenal motility index per cycle in all subjects (antrum: 1230 +/- 120 to 130 +/- 140 mm2; duodenum: 1120 +/- 150 to 225 +/- 160 mm2; P less than 0.005). These effects were not significantly affected by loperamide. Plasma motilin exhibited cyclic variation with significantly higher concentrations during antroduodenal phase 3 than during phases 1 and 2 of the interdigestive cycle. Plasma motilin was not altered by naloxone or loperamide, and neither drug had any effect on basal gastric acid secretion, duodenal output of amylase and bile salt or duodenogastric reflux. The results suggest that endogenous opiates regulate fasting motor activity in the human gastrointestinal tract but do not influence basal secretory function of the stomach, pancreas or biliary tree.

Adult↗
PubMed2006

Differential in vivo sensitivity to inhibition of P-glycoprotein located in lymphocytes, testes, and the blood-brain barrier.

A major functional component of the blood-brain barrier is P-glycoprotein. In principle, inhibition of this efflux transporter would permit greater distribution of its substrates into the brain and increased central effects. Tariquidar and elacridar, potent and selective P-glycoprotein inhibitors, were investigated in this regard using the opioid loperamide as an in vivo probe in mice. Pretreatment with both inhibitors converted intravenous loperamide from a drug without central effects to one producing antinociception. Radiolabeled loperamide tissue distribution studies indicated that inhibition was associated with increased uptake into brain and testes in the absence of changes in plasma levels, along with enhanced efflux of rhodamine 123 from CD3e+ T-lymphocytes. However, with tariquidar, the loperamide dose-response curves for testes/plasma and brain/plasma concentration ratios were shifted 6- (p = 0.07) and 25-fold (p < 0.01) to the right, respectively (ED50 = 1.48 and 5.65 mg/kg), compared with the rhodamine 123 efflux curve (ED50 0.25 mg/kg). Less pronounced shifts were noted with elacridar where the brain/plasma ratio was shifted only 2-fold relative to the rhodamine 123 efflux data (ED50 = 2.36 versus 1.34 mg/kg, respectively; p 0.01). These results indicate that the P-glycoprotein localized in the blood-brain barrier and, to a lesser extent, the testes-blood barrier is more resistant to inhibition than at other tissue sites such as the lymphocyte; moreover, the extent of this effect depends on the inhibitor. Such resistance can be overcome by a sufficiently high dose of an inhibitor; however, whether this is safely attainable in the clinical situation remains to be determined.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed1996

Relations between transit time, fermentation products, and hydrogen consuming flora in healthy humans.

BACKGROUND/AIMS: To investigate whether transit time could influence H2 consuming flora and certain indices of colonic bacterial fermentation. METHODS: Eight healthy volunteers (four methane excretors and four non-methane excretors) were studied for three, three week periods during which they received a controlled diet alone (control period), and then the same diet with cisapride or loperamide. At the end of each period, mean transit time (MTT) was estimated, an H2 lactulose breath test was performed, and stools were analysed. RESULTS: In the control period, transit time was inversely related to faecal weight, sulphate reducing bacteria counts, concentrations of total short chain fatty acids (SCFAs), propionic and butyric acids, and H2 excreted in breath after lactulose ingestion. Conversely, transit time was positively related to faecal pH and tended to be related to methanogen counts. Methanogenic bacteria counts were inversely related to those of sulphate reducing bacteria and methane excretors had slower MTT and lower sulphate reducing bacteria counts than non-methane excretors. Compared with the control period, MTT was significantly shortened (p < 0.05) by cisapride and prolonged (p < 0.05) by loperamide (73 (11) hours, 47 (5) hours and 147 (12) hours for control, cisapride, and loperamide, respectively, mean (SD)). Cisapride reduced transit time was associated with (a) a significant rise in faecal weight, sulphate reducing bacteria, concentrations of total SCFAs, and propionic and butyric acids and breath H2 as well as (b) a significant fall in faecal pH and breath CH4 excretion, and (c) a non-significant decrease in the counts of methanogenic bacteria. Reverse relations were roughly the same during the loperamide period including a significant rise in the counts of methanogenic bacteria and a significant fall in those of sulphate reducing bacteria. CONCLUSIONS: Transit time differences between healthy volunteers are associated with differences in H2 consuming flora and certain indices of colonic fermentation. Considering the effects of some fermentation products on intestinal morphology and function, these variations may be relevant to the pathogenesis of colorectal diseases.

Adult↗
PubMed1997

Increasing butyrate concentration in the distal colon by accelerating intestinal transit.

BACKGROUND: Populations at low risk of colonic cancer consume large amounts of fibre and starch and pass acid, bulky stools. One short chain fatty acid (SCFA), butyrate, is the colon's main energy source and inhibits malignant transformation in vitro. AIM: To test the hypothesis that altering colonic transit rate alters colonic pH and the SCFA content of the stools. PATIENTS: Thirteen healthy adults recruited by advertisement. METHODS: Volunteers consumed, in turn, wheat bran, senna and loperamide, each for nine days with a two week washout period between study periods, dietary intake being unchanged. Before, and in the last four days of each intervention, whole gut transit time (WGTT), defaecation frequency, stool form, stool beta-glucuronidase activity, stool pH, stool SCFA concentrations and intracolonic pH (using a radiotelemetry capsule for continuous monitoring) were assessed. RESULTS: WGTT decreased, stool, output and frequency increased with wheat bran and senna, vice versa with loperamide. The pH was similar in the distal colon and stool. Distal colonic pH fell with wheat bran and senna and tended to increase with loperamide. Faecal SCFA concentrations, including butyrate, increased with senna and fell with loperamide. With wheat bran the changes were non-significant, possibly because of the short duration of the study. Baseline WGTT correlated with faecal SCFA concentration (r = -0.511, p = 0.001), with faecal butyrate (r = -0.577, p < 0.001) and with distal colonic pH (r = 0.359, p = 0.029). CONCLUSION: Bowel transit rate is a determinant of stool SCFA concentration including butyrate and distal colonic pH. This may explain the inter-relations between colonic cancer, dietary fibre intake, stool output, and stool pH.

Adult↗
PubMed1996

Pharmacological studies on antidiarrheal effects of Hange-shashin-to.

We attempted to characterize the antidiarrheal action of Hange-shashin-to (TJ-14), a kampo medicine, by comparing its action with that of loperamide. The oral administration of TJ-14 caused the dose-dependent suppression of castor oil-induced diarrhea at 250 to 1000 mg/kg. No significant repression was noted by TJ-14 even at 1000 mg/kg, p.o. for diarrhea induced by pilocarpine, serotonin or barium chloride. Oral treatment with loperamide at 5 mg/kg markedly suppressed diarrhea induced by castor oil and barium chloride. Contractions of isolated guinea pig ileum in response to acetylcholine (1 x 10(-7) g/ml), histamine (1 x 10(-7) g/ml) or barium chloride (3 x 10(-4) g/ml) were little affected by TJ-14 at 10(-4) g/ml. The responses elicited by the three contractive drugs were dose-dependently suppressed by loperamide. TJ-14 did not affect the small intestinal transit even at an oral dose of 1000 mg/kg. On the other hand, the small intestinal transit was significantly suppressed by loperamide (5 mg/kg, p.o.). These results indicate that TJ-14 can effectively control castor oil-induced diarrhea, and that its antidiarrheal action was not based on the suppression of intestinal motility.

Animals↗
PubMed1983

Abnormalities in gastrointestinal motor activity in patients with short bowels: effect of a synthetic opiate.

We have investigated the fasting and postprandial patterns of gastrointestinal pressure activity in a group of patients with extensive (greater than 100 cm) resections of the distal small bowel. Each short bowel patient was studied on 2 consecutive days with random single blind administration of either loperamide (6 mg at 5 h and at 30 min before the meal) or placebo, and 20 healthy controls were studied on single days (13 basal fasting, 7 placebo). During fasting, the duration of the interdigestive motor complex was significantly shorter in patients with short bowel syndrome (71.1 +/- 15.6 min vs. 109 +/- 7.8 min for controls, p less than 0.03); hence, the frequency of complexes was increased. The duration of phase 2 was strikingly shorter in patients (18.7 +/- 7.0 min vs. 52.9 +/- 8.5 min for controls, p less than 0.03). Gastric emptying and postprandial motor activity were identical in patients and controls. During fasting, loperamide prolonged phase 3 (7.6 +/- 2.2 min vs. 4.3 +/- 1.1 min for placebo, p less than 0.03). Postprandially, loperamide shortened the time from meal ingestion to the first phase 3 by 50% (p less than 0.003), and increased motility index and frequency of contraction in the gut (p less than 0.01). Thus, gut motor activity in the short bowel syndrome is characterized by more frequent interdigestive motor complexes, marked reduction in phase 2 activity, and a normal feeding pattern. Loperamide therapy increases feeding activity while at the same time shortening its duration.

Adult↗
PubMed2001

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↗
PubMed1998

Intestinal absorption of oestrogen: the effect of altering transit-time.

OBJECTIVE: The mechanism by which a high fibre diet may reduce serum oestrogens is unknown. We hypothesized that time is a rate-limiting factor in oestrogen absorption from the colon so that changes in colonic transit-rate affect the proportion of oestrogen that is deconjugated and/or absorbed. AIM: To determine if alteration of intestinal transit rate would influence the absorption of an oral dose of oestradiol glucuronide. PARTICIPANTS: Twenty healthy postmenopausal women recruited by advertisement. SETTING: Department of Medicine, Bristol Royal Infirmary. METHODS: Volunteers consumed, in turn, wheat bran, senna, loperamide and bran shaped plastic flakes, each for 10 days with a minimum 2 week washout period between study periods, dietary intake being unchanged. Before and in the last 4 days of each intervention whole-gut transit-time, defecation frequency, stool form, stool beta-glucuronidase activity, stool pH and the absorption of a 1.5 mg dose of oestradiol glucuronide were measured. RESULTS: Wheat bran, senna and plastic flakes led to the intended reduction in whole-gut transit-time, increase in defecatory frequency and increase in stool form score. Loperamide caused the opposite effect. The length of time the absorbed oestrogen was detectable in the serum fell with wheat bran and senna, although this was only significant for oestradiol. Oestrone, but not oestradiol, was detectable for a longer time with loperamide. Plastic flakes had no effect on either oestrogen. Areas under the curve did not change significantly but tended to fall with the three transit-accelerating agents and to rise with loperamide. CONCLUSION: Our data indicate there is likely to be an effect of intestinal transit on the absorption of oestrogens but more refined techniques are needed to characterize this properly.

Dietary Fiber↗
PubMed2000

Racecadotril.

Racecadotril is an oral enkephalinase inhibitor used in the treatment of acute diarrhoea. It prevents the degradation of endogenous opioids (enkephalins), thereby reducing hypersecretion of water and electrolytes into the intestinal lumen. In a randomised double-blind study in 6 adult volunteers with castor oil-induced diarrhoea, racecadotril significantly reduced stool weight and stool number in comparison with placebo. Similar results have been obtained in treating castor oil-induced diarrhoea in rats. Racecadotril was significantly more effective than placebo in randomised double-blind studies in adults or children with diarrhoea (of infectious origin or in adults with HIV infection). In well controlled trials, racecadotril had efficacy similar to that of loperamide and was generally as effective as loperamide-oxide. Racecadotril had a similar tolerability profile to placebo, and was better tolerated than loperamide, in adults and children with diarrhoea. It caused significantly less constipation after resolution of diarrhoea than loperamide.

Animals↗
PubMed1988

A new suspension form of smectite (Liquid 'Diasorb') for the treatment of acute diarrhoea: a randomized comparative study.

An open, multi-centre, general practice study was carried out in 80 patients with acute diarrhoea to compare the effectiveness and tolerability of treatment with a liquid formulation of smectite, a hydrated aluminium-magnesium silicate (Liquid 'Diasorb'), and loperamide. Patients were allocated at random to receive one or other treatment for a maximum of 48 hours. Thirty-three of the patients on the smectite preparation and 30 of those on loperamide had acute diarrhoea of at least 24 hours but no longer than 48 hours in duration. Patients received a daily dose of 6 to 9 g smectite or 8 to 12 mg loperamide, depending on the symptoms. Details of red and white cell counts, serum electrolyte concentrations and stool culture for pathogens and parasites were recorded on entry and after 1 week. The results, judged in terms of resolution of symptoms after 2 and 7 days, doctor and patient assessment of response to therapy, and incidence of side-effects, showed that both treatments were equally effective and well-tolerated. Two patients were withdrawn, 1 patient (Liquid 'Diasorb') because of lack of response and the other (loperamide) because of dryness of the mouth and nausea. Laboratory parameters remained unchanged apart from a slight decrease in leucocytes in both groups.

Acute Disease↗