Oral naloxone antagonizes loperamide-induced delay of orocecal transit

Abstract

Orocecal transit time was determined by the lactulose hydrogen breath test in nine healthy volunteers after administration of placebo, loperamide (16 mg per os), and loperamide (16 mg per os) followed by oral naloxone at doses of 16 and 32 mg. The four tests were performed in double-blind conditions and in random sequences. Transit time (mean, SD) after loperamide (128.8 min, 32.9) was significantly increased (P less than 0.05) compared with placebo (85.5 min, 35.7), loperamide followed by naloxone 16 mg (88.8 min, 46.2), and loperamide followed by naloxone 32 mg (84.4 min, 40.6). These results show that the peripheral opioid agonist loperamide delays orocecal transit in healthy subjects and that naloxone per os at adequate doses antagonizes this effect.

Prospective randomized double-blind trial of racecadotril compared with loperamide in elderly people with gastroenteritis living in nursing homes

“…No ineffectiveness was recorded during this treatment. Loperamide is a selective mu-opiate-receptor agonist that is able to prolong orocecal and colonic transit times by disrupting the gut's electrical activity, increasing gut capacity, and delaying the passage of fluids through the small intestine [35]. Several studies reported that loperamide is able to reduce diarrhea manifestations in adults, with or without antibiotic treatments [36].…”

Single doses of ritodrine delay orocaecal transit in patients with irritable bowel syndrome.

“…We studied eleven patients (three men, eight women) with irritable bowel syndrome in view of a suggested clinical application of 3-adrenoceptor agonists in these patients (Lyrenas et al, 1985 a (Basilisco et al, 1987). At 09.30 h the fasting subjects ingested 10 g of lactulose suspended in 100 ml of tap water.…”

Management of opioid-induced bowel dysfunction in cancer patients

“…Thus, the amount of this drug that crosses the blood-brain barrier (BBB) is minimal and no antagonism is observed in the CNS receptors [49]. Several studies have shown that naloxone is effective in OBD [2,9,29,30,46]. The dose range used to reduce the incidence of OBD varies: an 8-10 mg dose [2], or 10-20% of the daily morphine dose [19,30].…”

“…Several studies have shown that naloxone is effective in OBD [2,9,29,30,46]. The dose range used to reduce the incidence of OBD varies: an 8-10 mg dose [2], or 10-20% of the daily morphine dose [19,30]. In order to prevent the opioid withdrawal syndrome (OWS) and slowly increase the amount of drug to obtain a satisfactory response, an initial maximum dose of 5 mg is recommended [47].…”