How does morphine work on colonic motility? An electromyographic study in the human left and sigmoid colon

Schang, J. C.; Hémond, M.; Hébert, Mary F.; Pilote, M.

doi:10.1016/0024-3205(86)90580-1

Cited by 43 publications

(17 citation statements)

References 11 publications

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“…In vivo there is an inhibitory 'opioid tone' in the human colon, especially in the transverse and rectosigmoid regions, which is revealed by administration of naloxone, which would block d-as well as gt-opioid receptors (Kaufman, Krevsky, Malmud, Maurer, Somers, Siegel & Fisher, 1988). Although morphine has an excitatory action in the human colon, as determined electromyographically, it causes a slow transit through the colon (Schang, Hemond, Hebert & Pilote, 1986;Kaufman et al 1988). The decrease in colonic transit is mostly due to a disco-ordination of excitatory activity.…”

Section: Effects Of Enkephalins In the Human Colonmentioning

confidence: 99%

Enkephalins modulate inhibitory neuromuscular transmission in circular muscle of human colon via delta‐opioid receptors.

Hoyle

Kamm

Burnstock

et al. 1990

The Journal of Physiology

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Section: Effects Of Enkephalins In the Human Colonmentioning

confidence: 99%

Enkephalins modulate inhibitory neuromuscular transmission in circular muscle of human colon via delta‐opioid receptors.

Hoyle

Kamm

Burnstock

et al. 1990

The Journal of Physiology

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“…[14][15][16][17][18] Activation of μ opioid receptors on neurons of the myenteric and submucosal plexuses, and in the longitudinal and circular smooth muscle of the GI tract, is associated with increased non-productive smooth muscle contractility that disrupts propagating activity. [19][20][21][22][23] Inhibition of enteric acetylcholine and non-adrenergic non-cholinergic neurotransmitter release is likely to be an important mechanism underlying opioid agonist-induced reductions in motility. 24,25 While there is some evidence that prototypical μ opioid receptor antagonists, such as naltrexone and naloxone, attenuate POI and chronic opioid-induced bowel dysfunction (OBD), [26][27][28] their clinical value in these GI disorders is limited given that these drugs cross the blood brain barrier readily, and thus can attenuate opioid-induced analgesia and provoke an opioid behavioral withdrawal syndrome.…”

Section: Mechanism Of Action Of Alvimopanmentioning

confidence: 99%

Safety and efficacy update: Alvimopan in postoperative ileus

Beattie

2009

Clinical Medicine. Therapeutics

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Postoperative ileus (POI) in patients undergoing abdominal surgery is associated with signifi cant morbidity. In 2008, alvimopan (Entereg ® ) was approved by the Food and Drug Administration (FDA), and is the only available POI therapy in the United States for patients undergoing bowel resection. Data from preclinical studies demonstrate that alvimopan and its primary metabolite, ADL 08-0011, behave as potent μ opioid receptor antagonists. In animals, alvimopan and ADL 08-0011 attenuate opioid agonist-induced reductions in gastrointestinal (GI) transit. Higher doses of alvimopan are required to inhibit opioid-induced analgesia as a result of its inability to penetrate the central nervous system (CNS). ADL 08-0011 is also peripherally selective, although to a lesser degree than alvimopan. In multiple species, including humans, alvimopan has low oral bioavailability, while ADL 08-0011, following its generation by human gut microfl ora, is more readily absorbed and achieves higher exposures. Three Phase 2 and fi ve Phase 3 clinical trials have been conducted to investigate the effi cacy and tolerability of alvimopan in patients undergoing bowel resection. An additional Phase 3 study was conducted in hysterectomy patients. In the majority of the studies, statistically signifi cant, and clinically meaningful, acceleration of GI recovery has been demonstrated. Consistent with animal data, alvimopan has no effect on opioid agonist-induced analgesia in healthy human subjects and POI patients. Clinical experience to date in POI patients indicates that alvimopan is well tolerated when used according to its approved dosing regimen (12 mg b.i.d. for up to 7 days). In this article, the preclinical and clinical properties of alvimopan are reviewed.

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“…1C, right example), when morphine in hibits peristaltic contractions but elicits high-frequency segmentations, while nalox one acts in an opposite fashion. Only recent ly, this mode of action has been described in the human colon in vivo [22]. It may be rec ognized in this context that naloxone also increases the frequency of peristaltic con tractions in the large intestine in vitro [23] ( fig.…”

Section: Functional Role Of Intestinal Opioids In the Control Of Perimentioning

confidence: 99%

Endogenous Opioids, the Enteric Nervous System and Gut Motility

Kromer¹

1990

Dig Dis

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Opium alkaloids have been used for centuries as potent antidiarrheals and analgesics, their constipating action in the latter instance taken as an unwanted effect. It was only during the last decade that the physiological role of opioid peptides present in both neurons and endocrine cells of the gastrointestinal (GI) tract has been defined. The recognition of distinct opioid receptor types which may be differentially involved in the control of motility, acid and electrolyte secretion in the GI tract presently focuses the attention of researchers in this field on the identification of receptor-type-selective opioid agonists in order to free these clinically extremely useful drugs from side effects. The present review provides a survey of mostly physiological data on the functional role of intestinal opioids.

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How does morphine work on colonic motility? An electromyographic study in the human left and sigmoid colon

Cited by 43 publications

References 11 publications

Enkephalins modulate inhibitory neuromuscular transmission in circular muscle of human colon via delta‐opioid receptors.

Enkephalins modulate inhibitory neuromuscular transmission in circular muscle of human colon via delta‐opioid receptors.

Safety and efficacy update: Alvimopan in postoperative ileus

Endogenous Opioids, the Enteric Nervous System and Gut Motility

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