The Central and Peripheral Influences of Opioids on Gastrointestinal Propulsion

Manara, L.; Bianchetti, A.

doi:10.1146/annurev.pa.25.040185.001341

Cited by 198 publications

(44 citation statements)

References 41 publications

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“…Because opioid receptors and endorphins are widely distributed in the central nervous system and throughout the gastrointestinal tract [Manara and Bianchetti, 1985], an endogenous opioid system may participate at either level in the regulation of gut function, including motility. On the other hand, the dominant site of effect (central vs. peripheral) of exogenous opioid-induced gut motility change or constipation remains a matter of speculation.…”

Section: Opioids and Constipationmentioning

confidence: 99%

Methylnaltrexone: Investigation of clinical applications

Yuan

Foss

2000

Drug Dev. Res.

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Morphine and related opioids are widely used medications that are associated with a number of limiting side effects. In the last three decades significant progress has been achieved in our understanding of the mechanisms of action of these opioids; however, these advances have yielded few new approaches to the management of opioid side effects. Methylnaltrexone, the first peripheral opioid antagonist currently under clinical investigation, has the potential to prevent or treat opioid‐induced peripherally mediated side effects without interfering with analgesia. This article reviews data obtained from preclinical and clinical studies on methylnaltrexone that focus on the antagonism of opioid‐induced constipation. Other potential clinical applications of the compound are also discussed. Drug Dev. Res. 50:133–141, 2000. © 2000 Wiley‐Liss, Inc.

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Section: Opioids and Constipationmentioning

confidence: 99%

Methylnaltrexone: Investigation of clinical applications

Yuan

Foss

2000

Drug Dev. Res.

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“…The naloxone-buprenorphine interaction was studied in the present work using a second classical (and clinically important) property of opioidsslowing of transit along the gastrointestinal tract (Manara & Bianchetti 1985). A primary aim of this work was to characterize the change in shape and/or A. Cowan position of the buprenorphine DRC in a nonbehavioural test and to interpret any alteration in the light of current receptor theory and corresponding findings from antinociceptive assays.…”

Section: Introductionmentioning

confidence: 99%

Buprenorphine and Gastrointestinal Transit in Rats: Effect of Naloxone on the Biphasic Dose‐response Curve

Cowan

1992

Clin Exp Pharma Physio

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1. Buprenorphine (0.01-10 mg/kg, subcutaneous [s.c.]) slowed the passage of a charcoal meal along the gastrointestinal tract in rats. The dose-response relationship was U-shaped. 2. When rats were pretreated with naloxone (0.30 mg/kg, s.c.), both the descending and ascending components of the buprenorphine dose-response curve were displaced to the right. 3. Buprenorphine-induced delay of transit was maximal at a dose of 0.10 mg/kg. In rats pretreated with naloxone, a 30-fold higher dose of buprenorphine was required for a comparable peak effect. 4. Moderate-high doses of buprenorphine may be acting on a functionally related binding site which non-competitively inhibits the usual buprenorphine-mu opioid receptor interaction.

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“…Opioids exert significant effects through direct activation of opioid receptors in the gastrointestinal tract. With activation of these receptors, patients experience decreased gastric acid secretion, delayed intestinal transit time, increased absorption of fluids from the intestinal lumen, and a harder, dryer stool (1).…”

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confidence: 99%

“…Naloxone is a relatively pure competitive antagonist with a significantly greater affinity for opioid receptors than most analgesics (1,2). Because it has activity inside as well as outside the central nervous system, it has been used safely and effectively to reverse the symptomatology associated with narcoticinduced adverse effects, specifically respiratory and central nervous system depression (3,4).…”

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confidence: 99%