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At least 307 records · Page 17Linked to original sources
PubMedDate not supplied

Possible therapeutic use of loperamide for symptoms of lactose intolerance.

OBJECTIVES: To examine a potential practical therapeutic use of loperamide (Lo) to decrease the symptoms of lactose intolerance. SUBJECTS AND METHODS: Nineteen (eight men, 11 women) healthy lactose maldigesters (18 of 19 with symptoms) underwent a 25 g lactose challenge on five separate days. Breath hydrogen was measured, areas under the curve (AUC) were calculated for 4 h, and 4 and 12 h symptom scores were recorded. After establishing baseline measurements, test doses of 4 mg, 8 mg and 12 mg Lo were randomly administered without placebo in a double-blind manner. As well, each subject received seven lactase tablets, in a random, unblinded manner. RESULTS: The median AUC and mean oral cecal transit time followed dose response expectations; however, only lactase treatment achieved significance. Nevertheless, 8 mg Lo significantly improved symptom scores, which were statistically indistinguishable from those of lactase. Four subjects complained of delayed constipation and cramps with various doses of Lo. CONCLUSIONS: Lo monotherapy for lactose intolerance is not economical and may have some side effects. However, Lo may be studied further as an adjunctive treatment of lactose intolerance in an effort to reduce the need for complete lactose digestion. Such a manoeuvre may allow rapid colonic adaptation, which in turn may be beneficial for prophylaxis for a number of colonic diseases.

Adolescent↗
PubMed1986

Secretagogue-induced changes in membrane calcium permeability in chicken and chinchilla ileal mucosa. Selective inhibition by loperamide.

Substance P (SP), neurotensin (NT), bombesin (BB), serotonin (5HT), and carbamylcholine (CCH) transiently increase electrogenic anion secretion in chinchilla and chicken ileum. SP and CCH also transiently inhibit amiloride-sensitive Na/H exchange in isolated chicken enterocytes. Loperamide (LP) inhibits the short-circuit current responses caused by SP, NT, and BB, but not those caused by CCH, 5HT, Ca ionophore, or cyclic nucleotides. Similarly, LP inhibits the effects of SP, but not those of CCH, on Na/H exchange. LP inhibition of the SP effects was further studied in isolated chicken enterocytes. CCH and SP transiently increased cytosolic Ca activity by 20-50 nmol/liter, but only the response to SP was inhibited by LP (10(-5) M) and by the absence of extracellular Ca. We conclude SP and CCH effects on intestinal electrolyte transport are mediated by increasing enterocyte Ca activity and LP specifically inhibits peptide hormone-activated Ca entry by an opiate receptor-independent mechanism.

Amiloride↗
PubMed2004

Loperamide modifies the tissue disposition kinetics of ivermectin in rats.

Ivermectin (IVM) is a broad-spectrum antiparasitic drug extensively used in human and veterinary medicine that is largely excreted in bile and faeces. Loperamide (LPM) is an opioid derivative that reduces gastrointestinal secretions and motility. Both IVM and LPM have been reported to act as P-glycoprotein substrates (P-GP). The goal of the present work was to study the LPM-induced modifications to the pattern of tissue distribution for IVM. Thirty-six Wistar male rats were randomly allocated to two groups (n = 18) and treated subcutaneously with IVM alone or co-administered with LPM. Rats were killed at different times post-treatment and samples (blood and tissues) were collected and analyzed by HPLC. The presence of LPM induced a marked enhancement in the IVM plasma concentrations, resulting in a significantly higher area under concentration time curve (AUC) value (P < 0.01) than that obtained after the administration of IVM alone. Significantly higher IVM availabilities in the liver tissue and small intestine wall (P < 0.05) were obtained in the presence of LPM. There were no statistically significant differences in drug availability in the large intestinal wall after both treatments. However, LPM induced a marked decrease in the amount of IVM recovered in the large intestinal lumen content. The ratio between IVM concentrations in the large intestinal luminal content and plasma at day 1 post-treatment was 4.64-fold higher in the absence of LPM. The delayed intestinal transit time caused by LPM accounting for an extended plasma-intestine recycling time, and a potential competition between IVM and LPM for the P-GP-mediated bile-intestinal secretion processes, may account for the enhanced IVM systemic availability reported in the current study.

Animals↗
PubMed1987

Acute diarrhoeal disease in rabbit: bacteriological diagnosis and efficacy of oral rehydration in combination with loperamide hydrochloride.

Acute outbreaks of diarrhoea with high mortality rates are frequently observed in rabbits. Amongst various aetiological factors Escherichia coli or its toxins have been found to be commonly incriminated. Sulphonamides or antibiotics are used to treat rabbits with bacterial diarrhoea. The result of the antibiotic treatment is moderately successful. We had good results using oral rehydration treatment in combination with loperamide hydrochloride (Immodium) in a colony of rabbits with E. coli diarrhoea.

Acute Disease↗
PubMed1998

Germinated barley foodstuff improves constipation induced by loperamide in rats.

The effects of germinated barley foodstuff (GBF) derived from the aleurone and scutellum fractions of germinated barley low-lignified hemicellulose were examined in Sprague-Dawley rats with constipation induced by loperamide by addition to the diet (2 mg/kg body weight). Bowel movements were higher in the GBF-fed rats than in the cellulose-fed rats used as a control. Fecal water content was also higher in the GBF-fed rats. The concentration of short chain fatty acids in cecal content, especially butyrate, was significantly higher in the GBF-fed rats than in the cellulose-fed rats. These findings suggested that GBF helps normalize defecation not only in diarrhea but also constipation.

Animals↗
PubMed1977

[Effects of loperamide on the motility of the isolated intestine in guinea pigs, rats and dogs (author's transl)].

Effects of Loperamide on the motility of the isolated intestine in guinea-pigs, puppies and rats were examined. The spontaneous contractions of the small intestine and colon in puppies were inhibited at relatively high concentration of the agent (10(-5) g/ml). The peristaltic reflex in the guinea-pig ileum was slightly inhibited at concentrations of 10(-8) to 10(-7) g/ml, and was completely abolished at 10(-6) g/ml. The agent (2X10(-7) g/ml) inhibited the longitudinal contraction of the guinea-pig ileum elicited by transmural electric stimulation. The agent (10(-5) g/ml) inhibited the acetylcholine-induced contraction of the colon and small intestine in puppies, and induced the hyperpolarization of the membrane potential and the abolition of spike potentials of the intestinal muscle in rats.

Action Potentials↗
PubMed1988

Treatment of chronic diarrhoea: loperamide versus ispaghula husk and calcium.

Twenty-five patients with chronic diarrhoea were included in an open, randomized crossover trial comparing the effect of loperamide with ispaghula and calcium. Nineteen patients completed both treatments. Before treatment the median number of daily stools was 7 (range, 4-13), stool consistency was loose in all, and urgency was present in 16 out of 19 patients. Both treatments halved stool frequency, but with regard to urgency and stool consistency ispaghula and calcium was significantly better. A combination of ispaghula and calcium seems to be a cheap and effective alternative to conventional treatment of chronic diarrhoea. Moreover, side effects were minimized.

Adult↗
PubMedDate not supplied

Optimization of the preparation of loperamide-loaded poly (L-lactide) nanoparticles by high pressure emulsification-solvent evaporation.

The entrapment of loperamide hydrochloride (LPM) in biodegradable polymeric drug carriers such as nanoparticles might enable its passage across the blood-brain barrier. The optimization of the preparation of the LPM-loaded PLA nanoparticles was performed employing high pressure emulsification-solvent evaporation. The resulting nanoparticles were characterized by particle size, distribution, thermal analysis, and drug release profiles. The partition of LPM into the organic phase increased with an increase in pH of the aqueous phase and with addition of lipophilic surfactants such as sorbitan fatty acid esters, resulting in an increase in the drug entrapment in the nanoparticles. Evaporation of the organic phase under reduced pressure and the addition of ethanol in the organic phase yielded a high drug entrapment due to the rapid polymer precipitation. The addition of the sorbitan fatty acid esters further increased the drug entrapment even at higher LPM concentrations. The results of thermal analysis suggest that LPM was homogeneously dispersed in the amorphous polymer matrix. The in vitro release of the drug from nanoparticles was biphasic, with a fast initial phase, followed by a second slower phase. Different drug release profiles from nanoparticles can be achieved by addition of sorbitan fatty acid esters, or the employment of different solvents as the organic phase.

Antidiarrheals↗
PubMedDate not supplied

Determination of the active ingredient loperamide hydrochloride in pharmaceutical caplets by high performance thin layer chromatography with ultraviolet absorption densitometry of fluorescence quenched zones.

A quantitative method using silica gel HPTLC plates with fluorescent indicator, automated sample application, and automated UV absorption densitometry of the fluorescence quenching zones was developed and validated for determination of loperamide hydrochloride in anti-diarrheal medications. Samples of three brands of caplets assayed within 96.0-105% of the 2 mg label value. Repeatability was 3.3%, 1.6%, and 2.8% (RSD) for replicate analyses (n=6) of three tablets. The errors of a blank-spike and standard analyses performed to evaluate accuracy were 2.00% and 2.02%, respectively. The method is suitable for application in a drug manufacturing quality control or regulatory analysis laboratory.

Antidiarrheals↗
PubMed1990

Loperamide (imodium)--clinical trial.

1. Imodium (loperamide) produced by Chemical Works of Gedeon Richter, Budapest, is a useful preparation for the symptomatic treatment of both acute and chronic diarrhoea of various etiologies. 2. In chronic diarrhoea cases the best results were obtained in the treatment of functional disorders of the guts. 3. Side effects occurred only in few patients and with low intensity, the treatment had to be interrupted in none of the cases.

Acute Disease↗
PubMed1989

Moderation of urinary and faecal incontinence with loperamide.

The author used Imodium in a clinical trial for the treatment of urinary incontinence following radical prostatectomies, urinary and faecal incontinence due to carcinoma or cerebral accident in history. The drug significantly improved incontinence and did not cause adverse effects. On the basis of the similarity of innervation the author opines that loperamide also influences the function of detrusor and/or bladder orifice besides exerting an antiperistaltic and anal sphincter influencing action.

Aged↗
PubMedDate not supplied

[Clinical evaluation of loperamide (Imodium)].

The clinical usefulness of loperamide (Imodium) was studied. The preparation was given to 35 patients with acute diarrhoea and 34 with chronic diarrhoea. A good effect was obtained in symptomatic treatment of acute and chronic diarrhoea. The best effects were noted in the treatment of diarrhoea due to functional disturbances.

Adult↗
PubMed1978

In vivo antimotility and antidiarrheal activity of lidamidine hydrochloride (WHR-1142A), a novel antidiarrheal agent. Comparison with diphenoxylate and loperamide.

1-(2,6-Dimethylphenyl)-3-methyl-amidinourea hydrochloride (WHR-1142A, lidamidine hydrochloride) was shown to have potent antimotility, antidiarrheal and intestinal antisecretory activity in mice, rats and dogs. Antimotility activity was demonstrated in charcoal intestinal motility, gastric emptying and gastric and intestinal intraluminal pressure studies. Antidiarrheal activity was evaluated in castor oil-, prostaglandin E2-, carbachol-, and serotonin-induced diarrhea. Intestinal secretion induced by cholera toxin was inhibited by WHR-1142A. In general, WHR-1142A was more potent than diphenoxylate and loperamide although species differences were noted. The ED50 for inhibition of castor oil-induced diarrhea was 1.8 mg/kg p.o. and the duration of action at 16 mg/kg p.o. was at least 6 h. Unlike diphenoxylate, WHR-1142A showed no tolerance.

Amidines↗
PubMed1994

Loperamide intoxication in a seven-week-old pup.

A 7-w-old Samoyed-cross pup was presented with central nervous system signs approximately 18 h following administration of the second of 2 doses of loperamide. Circling, vocalization, head pressing and unreactive pupils were present. There was no history of trauma. Improvement was seen shortly following administration of activated charcoal and 0.2 ml naloxone. Naloxone treatment was repeated at 2-h intervals over 12-h. Approximately 20 h following the initial clinical evaluation, the puppy was released to the owner for home care and observation.

Animals↗
PubMed1996

Loperamide poisoning in the dog.

A retrospective study was conducted of 40 loperamide poisoning cases recorded at the Centre National d'Informations Toxicologiques Veterinaires. An apparent breed susceptibility of Collie dogs was observed. Neurologic disturbances (ataxia and prostration) were significant clinical findings. Treatment with naloxone resulted in rapid reversal of signs without sequelae.

Animals↗
PubMed1975

Effect of loperamide, haloperidol and methadone in rats trained to discriminate morphine from saline.

In an operant procedure of lever pressing at FR10 schedule of food reinforcement, rats were trained to respond differentially in order to discriminate the effects of morphine (10 mg/kg) injections from those of saline injection. These rats learned to press a lever on one side after morphine injection and a lever on the opposite side after saline injection. In subsequent testing, these rats reliably emitted responses on the morphine lever after 10 or 20 mg/kg of morphine IP, 50 mg/kg of morphine given orally or 2 mg/kg methadone. Two mg/kg of morphine (or 10 or 20 mg/kg given orall) was recognized as saline. In contrast, after either loperamide (an antidiarrheal drug) given in doses up to 10 mg/kg or haloperidol (a neuroleptic) given in doses up to 0.32 mg/kg, all responses were made on the saline lever. Higher doses suppressed responding. Since neither the antidiarrheal activity nor the neuroleptic activity was sufficient to provide the discriminable cue associated with morphine, it is suggested that specific central effects produced only by narcotic analgesics are the basis for these morphine cues.

Animals↗