The characteristics of the inhibition of serum cholinesterase by metoclopramide

Graham, Shelli; Crossley, A. W. A.

doi:10.1007/bf00198302

Cited by 10 publications

(13 citation statements)

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“…Thus, we initially hypothesized that metoclopramide would prolong the duration of action of landiolol at least by 25%; however, prolongation of its duration of action by metoclopramide was not observed in this study. From previous studies, it can be expected that PCHE activity should be inhibited by 10-20% after administration of 10 mg metoclopramide [6][7][8][9]. Therefore, it is reasonable to think that PCHE activity in this study was inhibited by 10 mg metoclopramide to the same extent as in previous reports, although PCHE activity was not determined in this study.…”

Section: Discussionsupporting

confidence: 41%

“…There was, therefore, a possibility that its duration of beta-blocking action was prolonged by inhibiting PCHE activity. As mentioned before, metoclopramide has been shown to inhibit PCHE in vitro and in vivo [6][7][8][9]. In fact, neuromuscular block caused by succinylcholine and mivacurium, which are also metabolized by PCHE, has been shown to be prolonged by 23 and 30% after metoclopramide administration before induction of anesthesia [7,11].…”

Section: Discussionmentioning

confidence: 99%

“…It has been shown to be metabolized rapidly by plasma cholinesterase (PCHE) [5]. Metoclopramide has been shown to inhibit PCHE in vitro [6][7][8][9]. Its use for preventing postoperative nausea and vomiting in perioperative settings is popular among anesthesiologists although the effect of this drug for that purpose is controversial [10].…”

Section: Introductionmentioning

confidence: 99%

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Metoclopramide does not prolong duration of action of landiolol attenuating the hemodynamic response to induction of anesthesia and tracheal intubation

et al. 2010

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Landiolol is a new ultra-short-acting beta 1-selective adrenoreceptor antagonist, which is metabolized rapidly by plasma cholinesterase (PCHE). Metoclopramide has been shown to inhibit PCHE in vitro. Therefore, metoclopramide might prolong beta blocking effects of landiolol and spoil its ultimate-short-acting property. Just before induction of anesthesia, gynecological patients were randomly assigned to receive 0.2 mg/0.1 ml/kg landiolol and 2 ml saline (Landiolol group; n = 20), 0.2 mg/0.1 ml/kg landiolol and 10 mg metoclopramide/2 ml solution (Landiolol-M group; n = 20), or 0.1 ml/kg saline and 2 ml saline (Control group; n = 20). Tracheal intubation was performed 3 min after induction of anesthesia. Heart rate and blood pressure were recorded. Landiolol with or without metoclopramide similarly inhibited increase in heart rate after induction of anesthesia and tracheal intubation. However, changes in blood pressure were not affected. Metoclopramide at induction of anesthesia did not prolong duration of action of landiolol attenuating the hemodynamic response to induction of anesthesia and tracheal intubation.

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Section: Discussionsupporting

confidence: 41%

Section: Discussionmentioning

confidence: 99%

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Metoclopramide does not prolong duration of action of landiolol attenuating the hemodynamic response to induction of anesthesia and tracheal intubation

et al. 2010

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“…As such, MCP is used clinically owing to its prokinetic and antiemetic effects. Prokinetic effects might be enhanced due to an inhibition of the cholinesterase(s) (Graham and Crossley, 1995;Chemnitius et al, 1996). Although the conventional intravenous dose is ca.…”

Section: Introductionmentioning

confidence: 99%

In vitro protection of red blood cell acetylcholinesterase by metoclopramide from inhibition by organophosphates (paraoxon and mipafox)

Petroianu

Arafat

Kosanović

et al. 2003

J of Applied Toxicology

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Metoclopramide (MCP) is a dopamine receptor antagonist and serotonin receptor agonist widely used as an antiemetic and gastric prokinetic drug. In addition, MCP is a reversible inhibitor of cholinesterases from the human central nervous system and blood, and may have a red blood cell (RBC) acetylcholinesterase (AChE) protective effect against inhibition by organophosphates. The purpose of the study was to quantify 'in vitro', by means of the IC50 shift, the extent of MCP conferred protection, by using paraoxon (POX) and mipafox (MPFX) as inhibitors. Paraoxon is a widely used non-neuropathic organophospate responsible for a large number of accidental or suicidal exposures. Mipafox is a neuropathic organophospate. Red blood cell AChE activities in human plasma were measured photometrically in the presence of different POX, MPFX and MCP concentrations and the IC50 was calculated. Determinations were repeated in the presence of increasing MCP concentrations. It appears that the IC50 shift induced by the presence of MCP increases with the MCP concentration in a linear manner. The protective effect of MCP on cholinesterases could be of practical relevance in the treatment of POX and MPFX poisoning. We conclude that in vivo testing of MCP as an organophosphate protective agent is warranted.

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“…It is used clinically for its gastric prokinetic and antiemetic effects. Prokinetic effects might be enhanced through the inhibition of cholinesterase(s) (6,7).…”

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confidence: 99%

Protective Drugs in Acute Large-Dose Exposure to Organophosphates: A Comparison of Metoclopramide and Tiapride with Pralidoxime in Rats

Petroianu¹,

Al‐Hasan²,

Nurulain³

et al. 2005

Anesthesia & Analgesia

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Weak and reversible inhibitors of cholinesterase(s), when coadministered in excess with a more potent inhibitor such as organophosphates, can act in a protective manner. The benzamide compound, metoclopramide, confers some protection (putatively via this mechanism) for cholinesterases against inhibition by paraoxon both in vitro and in vivo, after chronic small-dose exposure. Tiapride is a related benzamide. In this study, we compared the protection by metoclopramide and tiapride in rats acutely exposed to large doses of paraoxon with the therapeutic "gold standard," pralidoxime. Group 1 received 1 micromol paraoxon (approximately 75% lethal dose), Group 2 received 50 micromol metoclopramide, Group 3 received 50 micromol tiapride, Group 4 received 50 micromol pralidoxime, Group 5 received 1 micromol paraoxon + 50 micromol metoclopramide, Group 6 1 micromol paraoxon + 50 micromol tiapride, and Group 7 1 micromol paraoxon + 50 micromol pralidoxime. All substances were administered intraperitoneally. The animals were monitored for 48 h and mortality was recorded at 30 min, 1, 2, 3, 4, 24, and 48 h. Blood was taken for red blood cell acetylcholinesterase measurements at baseline, 30 min, 24, and 48 h. With the exception of Group 7, in which some late mortality was observed, mortality occurred mainly in the first 30 min after paraoxon administration with minimal changes occurring thereafter. Mortality at 30 min was 0% in the metoclopramide, tiapride, and pralidoxime groups and 73 +/- 20 (paraoxon), 65 +/- 15 (paraoxon + metoclopramide), 38 +/- 14 (paraoxon + tiapride), and 13 +/- 19 (paraoxon + pralidoxime). Mortality at 48 h was 75 +/- 18 (paraoxon), 67 +/- 17 (paraoxon + metoclopramide), 42 +/- 16 (paraoxon + tiapride), and 27 +/- 24 (paraoxon + pralidoxime). Metoclopramide does not significantly influence mortality after acute large-dose paraoxon exposure. Both tiapride and pralidoxime significantly decreased mortality in our model. The protection conferred by tiapride was significantly less than that conferred by pralidoxime at 30 min, but was not significantly different at 24 and 48 h.

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The characteristics of the inhibition of serum cholinesterase by metoclopramide

Cited by 10 publications

References 13 publications

Metoclopramide does not prolong duration of action of landiolol attenuating the hemodynamic response to induction of anesthesia and tracheal intubation

Metoclopramide does not prolong duration of action of landiolol attenuating the hemodynamic response to induction of anesthesia and tracheal intubation

In vitro protection of red blood cell acetylcholinesterase by metoclopramide from inhibition by organophosphates (paraoxon and mipafox)

Protective Drugs in Acute Large-Dose Exposure to Organophosphates: A Comparison of Metoclopramide and Tiapride with Pralidoxime in Rats

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