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PubMed1993

Gastrointestinal function in chronic radiation enteritis--effects of loperamide-N-oxide.

The effects of loperamide-N-oxide, a new peripheral opiate agonist precursor, on gastrointestinal function were evaluated in 18 patients with diarrhoea caused by chronic radiation enteritis. Each patient was given, in double-blind randomised order, loperamide-N-oxide (3 mg orally twice daily) and placebo for 14 days, separated by a washout period of 14 days. Gastrointestinal symptoms; absorption of bile acid, vitamin B12, lactose, and fat; gastric emptying; small intestinal and whole gut transit; and intestinal permeability were measured during placebo and loperamide-N-oxide phases. Data were compared with those obtained in 18 normal subjects. In the patients, in addition to an increased frequency of bowel actions (p < 0.001), there was reduced bile acid absorption, (p < 0.001) a higher prevalence of lactose malabsorption (p < 0.05) associated with a reduced dietary intake of dairy products (p < 0.02), and faster small intestinal (p < 0.001) and whole gut transit (p < 0.05) when compared with the normal subjects. There was no significant difference in gastric emptying between the two groups. Treatment with loperamide-N-oxide was associated with a reduced frequency of bowel actions (p < 0.001), slower small intestinal (p < 0.001), and total gut transit (p < 0.01), more rapid gastric emptying (p < 0.01), improved absorption of bile acid (p < 0.01), and increased permeability to 51Cr EDTA (p < 0.01). These observations indicate that: (1) diarrhoea caused by chronic radiation enteritis is associated with more rapid intestinal transit and a high prevalence of bile acid and lactose malabsorption, and (2) loperamide-N-oxide slows small intestinal transit, increases bile acid absorption, and is effective in the treatment of diarrhoea associated with chronic radiation enteritis.

Adult↗
PubMed1994

In man the mu-opiate agonist loperamide specifically inhibits ACTH secretion induced by the cholecystokinin-like peptide ceruletide.

Ceruletide, a cholecystokinin-8-like peptide, was recently reported to stimulate ACTH secretion in man. The aim of this study was to investigate the effect of the mu-opiate agonist, loperamide, and the opiate antagonist, naloxone, on ceruletide-induced ACTH secretion in man. In 6 normal subjects, basal ACTH and cortisol plasma levels were significantly suppressed 3 h after loperamide administration (16 mg, orally) from 5 +/- 0 to 2 +/- 0 pmol/l and from 356 +/- 44 to 154 +/- 16 nmol/l. After stimulation with 8 ng ceruletide/kg body weight/min over a period of 5 min, the maximum ACTH levels (at 7.5 min) were significantly reduced by loperamide from 26 +/- 7 to 6 +/- 1 pmol/l and the maximum cortisol levels (at 30 min) were significantly reduced from 676 +/- 47 to 392 +/- 58 nmol/l. Furthermore, the ACTH peak (delta = 7.5 min) was significantly blunted by loperamide from 21 +/- 7 to 5 +/- 1 pmol/l and the integrated area under the curve from 0 to 120 min (delta AUC) of ACTH was significantly reduced from 40 +/- 11 to 14 +/- 4 pmol x 120 min/l. The cortisol peak (delta = 30 min) and the AUC of cortisol were not significantly diminished. The suppressive effect of loperamide on basal and ceruletide-induced ACTH and cortisol secretion was completely reversed by the administration of 0.8 mg naloxone, 20 min before and during infusion of ceruletide. The administration of naloxone itself had no significant effect on ACTH or cortisol levels. In conclusion, ACTH is released by peripherally administered ceruletide within a short period.(ABSTRACT TRUNCATED AT 250 WORDS)

Adrenocorticotropic Hormone↗
PubMed1989

The effect of loperamide on bowel habits and anal sphincter function in patients with ileoanal anastomosis.

The effect of loperamide on stool frequency, volume, and weight and on the function of the internal (IAS) and the external (EAS) anal sphincter was investigated in 19 patients with straight ileoanal anastomosis. Nine patients had intact anal sphincter function (group I), and in the other 10 the function of the anal sphincters was impaired (group II). After 72 h without any medication, the patients were investigated on a standard diet on 2 consecutive days: the 1st day with placebo, and the 2nd day with loperamide (16 mg). Stool collection and anal sphincter manometry/electromyography (EMG) were done on both days. The median number of stools was reduced from 10 and 13.5 to 6 and 7 per 24 h (p less than 0.01), and the fecal weight reduced from 600 and 900 g to 400 and 500 g (p less than 0.01) from the placebo day to the loperamide day in groups I and II, respectively. The tone of the IAS was significantly increased by loperamide in group I but remained unchanged in group II patients. The EAS function, determined by EMG and pressure measurements, was not significantly changed in any group by loperamide.

Adult↗
PubMed1997

Effects of loperamide oxide on gastrointestinal transit time and anorectal function in patients with chronic diarrhoea and faecal incontinence.

BACKGROUND: Loperamide improves anorectal function in patients with chronic diarrhoea. We wished to investigate whether the prodrug loperamide oxide has similar effects. METHODS: Eleven patients with chronic diarrhoea and faecal incontinence participated in a randomized, placebo-controlled, double-blind, crossover study of the effects of loperamide oxide (4 mg twice daily for 1 week). RESULTS: Loperamide oxide reduced wet stool weight and improved the patients' ratings of symptoms. Mouth-to-caecum transit time was not altered, but whole-gut transit time was prolonged. There were limited effects on anorectal function, but the mean minimum basal pressure mainly contributed by the internal anal sphincter (IAS) was increased, as was the mean volume infused before leakage occurred in the saline continence test. CONCLUSION: Loperamide oxide is effective in the treatment of diarrhoea with faecal incontinence; normalization of colon transit time and an increase in the tone of the IAS seem to be the main determinants of efficacy.

Adult↗
PubMed1993

Ciprofloxacin and loperamide in the treatment of bacillary dysentery.

OBJECTIVE: To compare the safety and efficacy of loperamide plus ciprofloxacin with those of ciprofloxacin alone in the treatment of bacillary dysentery. DESIGN: Double-blind, placebo-controlled, randomized clinical trial. SETTING: Hospital in Thailand. PARTICIPANTS: Eighty-eight adults with dysentery seeking medical care between November 1990 and February 1992. Patients who had received prior antibiotics or antimotility drugs were excluded. INTERVENTION: All 88 patients with dysentery were treated with ciprofloxacin, 500 mg twice daily for 3 days. Forty-two of these patients were randomly assigned to receive loperamide, a 4-mg initial dose followed by 2 mg after every loose stool (as many as eight caplets [16 mg] daily), and 46 were randomly assigned to receive placebo. MEASUREMENTS: Stools were collected daily until resolution of diarrhea and again after 10 days. The time to passage of the last unformed stool, number of unformed stools, and symptoms were recorded after treatment. RESULTS: Shigella or enteroinvasive Escherichia coli (53%), Vibrio parahaemolyticus (16%), and Salmonella (7%) were the most common bacterial enteric pathogens identified in 88 patients with dysentery. In patients infected with Shigella or enteroinvasive E. coli, the median duration of diarrhea was 19 hours (25th to 75th percentiles, 6 to 42 hours) for those receiving loperamide plus ciprofloxacin compared with 42 hours (21 to 46 hours) for those receiving ciprofloxacin alone (P = 0.028). The median number of diarrheal stools for those receiving ciprofloxacin and loperamide was 2.0 (1 to 5 stools) compared with 6.5 (2 to 9 stools) for those receiving ciprofloxacin alone (P = 0.016). None of the participants had a temperature greater than 38 degrees C after 24 hours of treatment. None of the patients was infected with the same bacterial enteric pathogen more than 1 day after receiving treatment. CONCLUSIONS: Loperamide decreases the number of unformed stools and shortens the duration of diarrhea in dysentery caused by Shigella in adults treated with ciprofloxacin.

Adult↗
PubMed1987

[Effect of loperamide on fecal flora of children with severe prolonged diarrhea].

Loperamide has recently been proposed in the management of infants with severe protracted diarrhea. The purpose of this study was to determine the effect of loperamide (0.5 mg/kg/d) on fecal flora in 19 cases of severe protracted diarrhea. Criteria analysed were: clinical tolerance (vomiting and abdominal distension) and efficacy (number of stools, transit time and Na/k in stools); complete identification and counts of aerobic and strict anaerobic bacteria in fresh stools before and 4 to 8 days after the beginning of loperamide. Parental and/or oral alimentation remained unchanged during the entire study. Clinical resolution of diarrhea was rapid (less than 24 h) in 9 of 14 patients. In 2 cases ileus was observed and resolved when loperamide was discontinued. Although important changes in specific fecal flora counts was noticed for streptococcus D and proteus as compared to 5 controls, no bacterial overgrowth appeared or was worsened during loperamide treatment.

Child, Preschool↗
PubMed1984

Mechanisms of action of loperamide.

The pharmacology of loperamide is discussed, with particular reference to the drug's antidiarrhoeal properties. Its absorption, distribution, metabolism and excretion are considered and rapid concentration in the small intestine is described. The mechanism of action of loperamide on fluid and electrolyte transport is examined with reference to opiate agonism, calcium-channel blocking, calmodulin inhibition, and paracellular permeability. The colon appears to be the main site of action of loperamide on gut motility and transit. In the proximal colon, the drug accentuates segmenting motor activity. Work relating to the activity of loperamide on bacterial toxins and other secretory agents is outlined. Diarrhoea induced by prostaglandins can be prevented by pretreatment with the drug. Details are given of clinical applications of loperamide for diarrhoea control in children and adults. The drug has no significant side-effects and presents no serious threat of abuse.

Absorption↗
PubMed1981

A comparative study of loperamide and diphenoxylate in the treatment of chronic diarrhoea caused by intestinal resection.

A double-blind cross-over study of the antidiarrhoeal effects of loperamide and diphenoxylate in 29 patients with chronic diarrhoea due to intestinal resection is presented. Most of these subjects had had surgery for Crohn's disease which was in a stable and nonactive phase during the study. Loperamide and diphenoxylate were presented as identical capsules. Each was administered for a minimum duration of 25 days. The number of capsules required to control diarrhoea was significantly smaller in the loperamide group than in the diphenoxylate group. Loperamide was also statistically superior to diphenoxylate at reducing the number of stools and improving the faecal consistency. Nineteen of the 29 patients considered loperamide to be the most effective antidiarrhoeal drug, five preferred diphenoxylate and five did not notice any difference.

Adult↗
PubMed1980

Double-blind cross-over study comparing loperamide, codeine and diphenoxylate in the treatment of chronic diarrhea.

As no adequate comparison of these widely used drugs has been made, we have performed a double-blind cross-over trial in 30 individuals with chronic diarrhea. Each underwent three randomized treatment periods of 4 wk duration. Patients were instructed to increase the daily dose gradually until control was achieved or side effects became intolerable. Stool frequency, consistency, urgency, and incontinence were then compared when a stable dose was reached. Though 2.3 capsules (4.6 mg) of loperamide, 2.3 capsules (103.5 mg) of codeine and 2.5 capsulses (12.5 mg) of diphenoxylate all reduced stool frequency to the same extent, diphenoxylate was significantly less effective in producing a solid stool. Before treatment 95% of patients experienced urgency, sometimes associated with fecal incontinence, often as their major diability. Loperamide and codeine were more effective in relieving this than was diphenoxylate. Side effects, particularly central nervous effects, were greatest with diphenoxylate and least with loperamide. Approximately equal numbers discontinued each preparation; poor control and central-nervous-system side effects were the usual reasons for stopping diphenoxylate and codeine, and abdominal pain and constipation for stopping loperamide. We conclude that both loperamide and codeine phosphate are superior to diphenoxylate in the symptomatic treatment of chronic diarrhea.

Antidiarrheals↗
PubMed1978

Interaction of loperamide and diphenoxylate with ethanol and methohexital.

The antidiarrheal drugs loperamide and diphenoxylate were tested for their ability to potentiate central nervous system depression induced by ethanol in mice and nethohexital in rats. Oral diphenoxylate potentiated the loss of righting reflex (hypnosis) at 10 mg/kg in mice and at 5 mg/kg in rats, doses which were considerably lower than those required to induce morphine-like behavior in mice and rats. Oral loperamide did not potentiate hypnosis. Increased incidence and duration of hypnosis was observed with loperamide only at very high, nearly toxic doses (100 mg/kg in mice and 80 mg/kg in rats) and these doses induced only nonspecific central nervous system depression. The failure of loperamide to potentiate the action of hypnotics confirms data from clinical trials which showed that loperamide is essentially free of central depressant effects when given orally.

Animals↗
PubMedDate not supplied

[The delivery of loperamide to the brain by using polybutyl cyanoacrylate nanoparticles].

The possibility of using polysorbate 80-coated nanoparticles for the delivery of the water insoluble opioid (lyonist loperamide across the blood-brain barrier was investigated. The analgesic effect after i.v. injection of the preparations was used as the indication of drug transport through this barrier. Intravenous injection of the particulate formulation resulted in a long and significant analgesic effect. A polysorbate 80 loperamide solution induced a much less pronounced and very short analgesia. Uncoated nanoparticles loaded with loperamide were unable to produce analgesia. Polysorbate 80-coated PBCA nanoparticles loaded with loperamide led to the transport of loperamide to the brain.

Analgesics↗
PubMed1994

Opioid pharmacology of the antinociceptive effects of loperamide in mice.

Loperamide (0.1-3.2mg/kg i.p.) produced dose-dependent and complete suppression of writhing in the acetic acid-induced writhing assay in mice. Naltrexone (NTX; 0.1-10.0mg/kg s.c.) and its N-methylated derivative quaternary naltrexone (QNTX; 1.0 and 10.0mg/kg s.c.) were roughly equipotent in antagonizing the antinociceptive effects of loperamide. In contrast, NTX was approximately 100-fold more potent than QNTX in antagonizing the antinociceptive effects of the classical mu agonist morphine. Furthermore, the antinociceptive effects of loperamide were not antagonized by central administration of the selective mu antagonist D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH(2) (CTAP; 300ng i.c.v.), or by systemic administration of either the kappa selective antagonist nor-binaltorphimine (nor-BNI; 32.0mg/kg s.c.), or the delta antagonist naltrindole (NTI; 10.0mg/kg s.c.). These doses of CTAP, nor-BNI and NTI were effective antagonists of morphine, the kappa agonist U69,593 and the delta agonist BW 373U86 [(+/-)-4-((R*)-a-((2S*5R*)-4-allyl-2,5-dimethyl-1- piperazinal)-3-hydroxybenzyl)-N, N-diethylbenzamide dihydrochloride], respectively. These results indicate that the antinociceptive effects of loperamide in mice are mediated, at least in part, by opioid receptors; however, these receptors are distinct from the opioid receptors mediating the effects of morphine, U69,593 and BW 373U86. These results are consistent with the hypothesis that loperamide produces its antinociceptive effects by acting, at least in part, at peripheral opioid receptors.

Journal Article↗
PubMed1993

Effect of metoclopramide and loperamide on the pharmacokinetics of didanosine in HIV seropositive asymptomatic male and female patients.

The pharmacokinetics of orally-administered didanosine were evaluated in 6 male and 6 female HIV seropositive patients to determine the effect of pretreatment with metoclopramide, an inducer of gastrointestinal motility, and loperamide, which retards motility. Using a randomized, balanced, crossover design, each patient received the following three treatments under fasting conditions: didanosine as a single agent, didanosine 5 min after a single 10 mg intravenous dose of metoclopramide, and didanosine 1 h after the final of 4 doses, 4 mg each, of loperamide. Serial blood and urine samples were collected for up to 12 h after each dose. Plasma and urine aliquots were analysed for intact didanosine using HPLC with UV detection. Pharmacokinetic parameter values were calculated using noncompartmental methods. The mean Cmax values were significantly greater for the didanosine single agent (2.04 micrograms.ml-1) and didanosine with metoclopramide (2.30 micrograms.ml-1) treatments than for the combination of didanosine with loperamide (1.57 microgram.ml-1). The t1/2 in males was significantly greater than in females for the didanosine (1.75 vs 1.12 h, respectively) and didanosine with metoclopramide treatments (1.74 vs 1.20 h, respectively). No significant treatment or gender effects were observed for AUC or UR (urinary recovery). The pharmacokinetics of didanosine were not altered appreciably by dosing with metoclopramide. Administration with loperamide affected the rate but not the extent of absorption. There were no clinically relevant differences between males and females in the disposition of didanosine.

Administration, Oral↗
PubMed1984

Inhibition by loperamide of deoxycholic acid induced intestinal secretion.

The effect of loperamide on deoxycholic acid (DOC)-induced secretion was studied in ligated loops of the rat jejunum and colon in vivo. In controls, loperamide slightly augmented fluid absorption. 3 mmol DOC caused net fluid secretion. Loperamide reduced this secretion in the colon and reversed it to absorption in the jejunum. Na-K-ATPase specific activity and cAMP levels were measured in the jejunum, and [14C]erythritol clearance as an index of mucosal permeability in the colon. In the jejunum this opiate analogue affected neither basal or DOC-depressed Na-K-ATPase, nor mucosal cAMP. In the colon it reduced a large increase of the erythritol clearance caused by DOC. It is suggested that loperamide interferes with DOC-induced intestinal secretion in part by lowering mucosal permeability.

Animals↗
PubMed1986

Loperamide inhibits gallbladder inflammatory fluid secretion in experimental cholecystitis.

Fluid secretion by the gallbladder mucosa is suggested to have a key pathophysiological role in acute cholecystitis, since it causes distension of the obstructed gallbladder. The present study investigates the actions of loperamide on the gallbladder function in experimental cholecystitis. Gallbladder fluid transport and motility were studied in vivo with a continuous perfusion technique. A net fluid secretion by the gallbladder mucosa was seen in cats in which cholecystitis was induced whereas there was a net fluid absorption from the gallbladder lumen in the control animals. The net fluid secretion in experimental cholecystitis was inhibited by loperamide (1 mg/kg), an effect that was blocked by naloxone (1 mg/kg), suggesting an involvement of specific opiate receptors. Loperamide (1 mg/kg) relaxed the normal gallbladder but had no significant effects on its fluid absorption. Since loperamide reduces mucosal fluid secretion in experimental cholecystitis without contracting the gallbladder wall, it is suggested that this peripherally acting opiate agonist could be useful in the treatment of patients with acute cholecystitis.

Animals↗
PubMed1990

Loperamid, an efficacious drug against fish-pathogenic acanthocephalans.

A total of 20 drugs were tested for their efficacy in the treatment of infections involving the two major acanthocephalans infesting rainbow trout in European trout farms. In in vitro experiments, the antidiarrhoeic loperamid and the well-known anthelminthic drug niclosamide showed the best efficacy. Worms treated with loperamid contracted the posterior end of their body, in which severe necrosis of the tegument caused the death of the worms. In in vivo experiments, loperamid was the most efficacious drug: 50 mg/kg given to rainbow trout on 3 consecutive days led to a complete cure. According to preliminary tolerance tests in water baths, the toxicity of this drug is low as compared with that of niclosamide, which is very toxic. Thus, loperamid can be recommended as the drug of choice for therapy of acanthocephalan infections in fish.

Acanthocephala↗
PubMed1987

Stimulation of gastrointestinal motility by loperamide in dogs.

The effects of loperamide on gastrointestinal motility were investigated in conscious fasted dogs chronically fitted with strain-gauge transducers on the antrum, the jejunum, and the colon. Oral administration of loperamide (0.1 mg/kg) induced, after a delay of 20-30 min, a long-lasting (8-12 hr) stimulation of gastrointestinal motility associated with a disorganization of the cyclic activity at the three levels investigated. These effects were reproduced by a subcutaneous administration at the same dose and were antagonized by previous intravenous administration of naloxone or a quaternary opiate antagonist. Intracolonic administration (0.1 mg/kg) stimulated, after a delay of 20-30 min, colonic motility only. Intracerebroventricular loperamide (1 microgram/kg) induced a long-lasting (15-20 hr) inhibition of the gastric motility and a short (2-hr) disorganization of the jejunal motor profile. These data show that oral loperamide stimulates gastrointestinal motility in dogs and involves peripheral opiate receptors.

Administration, Oral↗
PubMed1982

Effects of loperamide on anal sphincter function in patients complaining of chronic diarrhea with fecal incontinence and urgency.

We have investigated the effect of loperamide (4 mg tds) on the continence to a standard volume of rectally infused saline and anorectal manometry in 26 patients complaining of chronic diarrhea complicated by fecal incontinence and severe urgency. Each patient was treated for one week with loperamide (4 mg tds) and for one week with an identical placebo in a double-blind cross-over trial. Our results showed that as well as its established effects of improving stool consistency and reducing stool weight, frequency and episodes of incontinence and severe urgency, loperamide also significantly improved continence to a standard volume of rectally infused saline. This action was associated with an increase in the maximum basal sphincter pressure, an increase in the rectal volume required to abolish recovery of the rectoanal inhibitory reflex, and a reduction in rectal compliance. These results suggest that loperamide may have a specific action on the anal sphincter, which may aid continence in patients who complain of diarrhea and fecal incontinence.

Adult↗