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Abstract
Loperamide is opioid-related and like meperidine (pethidine) is a piperidine derivative. It is available without prescription. It is used for the treatment of acute diarrhea and for control of some chronic conditions, such as diarrhea associated with inflammatory bowel disease. It acts on opioid receptors in the intestinal wall with lesser effects on muscarinic receptors to inhibit peristalsis; it may also have an inhibitory effect on secretions. The effects of loperamide are rapid, and are relatively selective for the intestine; it causes significantly lower central opioid-like side effects in comparison to diphenoxylate and codeine in therapeutic doses. The oxide form of loperamide is an investigational drug designed to slowly release loperamide in the intestine.
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This study investigated the effect of loperamide on the motor function of small intestine and J-pouch. Proctocolectomy and ileal pouch-anal anastomosis were performed in four dogs. Motility was recorded by serosal electrodes and strain gauge transducers. The intestinal transit time was determined radiologically. Multiple measurements were performed before and during chronic administration of loperamide. This treatment led to a significant decrease in median stool frequency from 11 (10-13) to 9 stools/day (8-12) and a tendential increase in intestinal transit time from 60 (50-105) to 70 min (60-90). This was not accompanied by significant changes in fasted or postprandial motility. There were no significant differences in the characteristics of the migrating myoelectric complex or in the fed pattern, either in the small intestine or in the pouch. Loperamide thus does not significantly affect intestinal motility after ileal pouch-anal anastomosis. The reduction in stool frequency seems to be due to antisecretory effects in the first line.
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-chloro-phenyl)-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.
Acute uncomplicated diarrhoea is commonly treated by self-medication. Guidelines for treatment exist, but are inconsistent, sometimes contradictory, and often owe more to dogma than evidence. An ad hoc multidisciplinary group has reviewed the literature to determine best practice.
In general it is recognized that treatment of acute episodes relieves discomfort and social dysfunction. There is no evidence that it prolongs the illness. Self-medication in otherwise healthy adults is safe.
Oral loperamide is the treatment of choice. Older anti-diarrhoeal drugs are also effective in the relief of symptoms but carry the risk of unwanted adverse effects. Oral rehydration solutions do not relieve diarrhoea, and confer no added benefit for adults who can maintain their fluid intake. Probiotic agents are, at present, limited in efficacy and availability. Antimicrobial drugs, available without prescription in some countries, are not generally appropriate for self-medication, except for travellers on the basis of medical advice prior to departure.
Medical intervention is recommended for the management of acute diarrhoea in the frail, the elderly (> 75 years), persons with concurrent chronic disease, and children. Medical intervention is also required when there is no abatement of the symptoms after 48 h, or when there is evidence of deterioration such as dehydration, abdominal distension, or the onset of dysentery (pyrexia > 38.5 °C and/or bloody stools).