Naloxone and morphine inhibit gastric emptying of solids

Champion, M C; Sullivan, S; Chamberlain, Marcus; Vezina, William

doi:10.1139/y82-100

Cited by 72 publications

(18 citation statements)

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“…also reported a small but insignificant delay of gastric emptying given naloxone as bolus injection of 1.2 mg and using the paracetamol absorption test to estimate gastric emptying in eight fasted volunteers. In contrast to our study, Champion et al 18 . demonstrated a significant delay of gastric emptying of a solid meal with naloxone 2 mg bolus injection in six volunteers, also using a scintigraphic method.…”

Section: Discussioncontrasting

confidence: 99%

“…demonstrated a significant delay of gastric emptying of a solid meal with naloxone 2 mg bolus injection in six volunteers, also using a scintigraphic method. As it is suggested that naloxone is not a pure opioid receptor antagonist but may also have a weak morphine‐like agonistic effect, they argue that naloxone at this dose (about 2–5 times higher than usually given to reverse narcotic‐induced respiratory depression) may act as a weak opioid agonist instead of an antagonist at lower doses 18,41 . However, using naloxone at a dose of 5 mg bolus injection and a scintigraphic method to estimate gastric emptying time in eight volunteers, Mittal et al 12 .…”

Section: Discussionmentioning

confidence: 99%

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Influence of naloxone on gastric emptying of solid meals, myoelectrical gastric activity and blood hormone levels in young healthy volunteers

Reber¹,

Netzer²,

Gaia³

et al. 2002

Neurogastroenterology Motil

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There is considerable evidence that opioid mechanisms are involved in the mediation of pyloric motor responses that in turn regulate gastric emptying. The purpose of this randomized, placebo-controlled crossover study was to investigate the effect of naloxone on gastric emptying of a solid meal, gastric myoelectrical activity and the postprandial release of gastrointestinal peptides and neuropeptides in 20 healthy volunteers. Naloxone was administered as an intravenous bolus, followed by continuous infusion according to an intravenous dosing nomogram. Gastric emptying time was evaluated by scintigraphy and gastric myoelectrical activity was evaluated by cutaneous electrogastrography. Naloxone did not significantly alter gastric half-emptying time and postprandial dominant gastric electrical frequency compared with placebo. It also did not significantly change the plasma levels of several peptide hormones with the exception of neuropeptide Y, which was significantly increased (P = 0.001). In conclusion, in doses that influence human intestinal motility, naloxone had no effect on gastric motility and release of several peptide hormones in healthy male volunteers. The importance of the isolated increased neuropeptide Y plasma level needs further investigation.

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Section: Discussioncontrasting

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Influence of naloxone on gastric emptying of solid meals, myoelectrical gastric activity and blood hormone levels in young healthy volunteers

Reber¹,

Netzer²,

Gaia³

et al. 2002

Neurogastroenterology Motil

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“…Der obstipierende Effekt der Opioide ist besonders ftir Morphin [4,38,54,56] demonstriert worden und stellt ein obligates Begleitph~inomen bei der chronischen Therapie von Schinerzpatienten dar [42,49]. Da hierftir ursachlich eine Abnahme der Acetylcholinfreisetzung im Plexus myentericus diskutiert wird [27], k6nnte die obstipierende Wirkung durch spezifische Antagonisten wie beispeilsweise Naloxon aufgehoben werden.…”

Section: Diskussionunclassified

“…So ist aus der klinischen Anwendung bekannt, dab die chronische Einnahme von Opioiden bei Schmerzpatienten in fast 95 % aller F~ille zur Obstipa-ti0n ftihrt [5], die so ausgepr/igt sein kann, dab routinem/ii]ig mit dem Opioid Laxanzien verordnet werden miissen [16]. Urs~ichlich liegt dieser obstipierenden Wirkung eine Pyloruskonstriktion mit verz6gerter Magenentleerung [4], eine Hemmung der propulsiven Motorik sowie eine spastische Einschntirung des Dtinndarms zugrunde [27]. Dieser Wirkmechanismus wird dann verst/indlich, wenn man berticksichtigt, dab 0pioide an spezifische Rezeptoren im Plexus myentericus binden, wodurch die Freisetzung von Acetylcholin verhindert wird [11,27].…”

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Die obstipierende Wirkung der Opioide Tilidin-N und Tramadol im Vergleich zu Codein

Freye

Rosenkranz

Neruda

1996

Schmerz

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Tramadol, a mixed mu-opioid agonist and a monoamine-reuptake blocking analgesic, has been supposed to have little effect on propulsive gastrointestinal motility. However, this has not been specifically studied in man. Following institutional approval, 18 human volunteers were given 50 mg of tramadol, tilidine/naloxone, and codeine, respectively, in a double-blind randomised cross-over design. Additionally, 12 further volunteers were given 100 mg of each opioid in a double-blind, randomised fashion, followed by measurement of gastrocoecal transit time. Gastrointestinal transit time was measured using the lactulose H(2)-breath test. A threefold increase in end-expiratory hydrogen when compared to the control value was considered the end point of gastrocoecal transit. At the low dose (50 mg) the three opioids did not differ significantly with regard to their effect on gastrointestinal motility. Gastrocoecal transit time was 90.8 (+/- 10.1 SEM) min for tramadol, 100.6 (+/- 9.8 SEM) min for tilidine/naloxone, and 104.2 (+/- 8.7 SEM) min for codeine. Doubling the dose of each opioid resulted in an increase in mean gastrocoecal transit, namely 97.8 (+/- 11.2 SEM) min for tramadol, 129.2 (+/- 12.2 SEM) min for tilidine/naloxone and 135.9 (+/- 9.2 SEM) min for codeine. The increase in gastrocoecal transit time was significant (P < 0.01) for high doses of tilidine/naloxone and codeine in contrast to the effect of the low doses. This lesser constipation effect may be due to the reduced affinity of tramadol to the mu-opioid receptor. Sedation was significantly higher for codeine after 50 mg (P < 0.05) and 100 mg (P < 0.005) than for tilidine/naloxone and tramadol. Vertigo was significantly higher after 50 mg (P < 0.05) and 100 mg (P < 0.005) of tilidine/naloxone and codeine than after tramadol. Perspiration was significantly higher after tramadol 100 mg (P < 0.005) than after tilidine/naloxone and codeine. Sedation is considered a typical symptom of analgesics interacting with centrally located opioid receptor sites. The higher incidence of perspiration after tramadol suggests that monominergic pathways may be involved in thermoregulation. In conclusion, the opioids tilidine/naloxone and codeine at the doses used significantly prolong gastrointestinal transit time in the high-dose range. Since tramadol does not induce a dose-related increase in gastrocoecal transit time, it may be a useful analgesic in patients who are prone to developing constipation during high-dose opioid therapy.

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“…Dies leuchtet unmittelbar ein, wenn man bedenkt, daß die oroanale Transitzeit zu über 90% auf der Kolontransitzeit beruht [5].…”

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„Die obstipierende Wirkung der Opioide Tilidin-N und Tramadol im Vergleich zu Codein”

Müller-Lissner¹

1997

Der Schmerz

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Naloxone and morphine inhibit gastric emptying of solids

Cited by 72 publications

References 0 publications

Influence of naloxone on gastric emptying of solid meals, myoelectrical gastric activity and blood hormone levels in young healthy volunteers

Influence of naloxone on gastric emptying of solid meals, myoelectrical gastric activity and blood hormone levels in young healthy volunteers

Die obstipierende Wirkung der Opioide Tilidin-N und Tramadol im Vergleich zu Codein

„Die obstipierende Wirkung der Opioide Tilidin-N und Tramadol im Vergleich zu Codein”

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