Effects of methylnaltrexone injection: A Synthesis of Findings from 11 Studies

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Original Abstract of the Article

Major Research Findings

Methylnaltrexone is a peripheral opioid receptor antagonist that has the potential to prevent or reverse the gastrointestinal effects of opioids. 5 Several studies have shown that methylnaltrexone can prevent the delay in oral-cecal transit time caused by morphine, without affecting analgesia. 1 , 3 The safety and tolerance of methylnaltrexone have been investigated in healthy volunteers, with results suggesting it is well-tolerated at doses up to 0.32 mg/kg. 2 Oral methylnaltrexone has also been shown to reduce subjective side effects after morphine administration, such as nausea, itching, stimulation, and flushing. 4 Methylnaltrexone has been studied for the treatment of opioid-induced constipation (OIC) in both chronic and acute settings, demonstrating potential benefits for patients experiencing OIC after orthopedic surgery. 7 , 8 While effective in treating OIC, abdominal pain has been reported as a common side effect. 8

Benefits and Risks

Benefit Summary

Methylnaltrexone has shown promise in preventing opioid-induced constipation and reducing the delay in gastrointestinal transit time caused by opioids, without affecting pain relief. It has also demonstrated potential to reduce subjective side effects associated with opioid use.

Risk Summary

The most common side effect of methylnaltrexone is abdominal pain. Additionally, orthostatic hypotension can occur, which is usually transient and self-limiting.

Comparison between Studies

Commonalities

Multiple studies consistently show that methylnaltrexone can prevent the delay in oral-cecal transit time caused by morphine and improve gastrointestinal motility without affecting analgesia. The safety of methylnaltrexone has been demonstrated in healthy volunteers, suggesting it is generally well-tolerated at specific doses.

Differences

Differences exist in the administration route (oral vs. intravenous), dosage, patient populations, and outcome measures used in the studies. These variations make direct comparison of the results challenging.

Consistency and Contradictions in Results

Several studies consistently show that methylnaltrexone can prevent the delay in oral-cecal transit time caused by morphine. However, the efficacy of methylnaltrexone may vary depending on the dosage, administration route, and patient characteristics. Further research is necessary to fully understand these nuances.

Considerations for Real-Life Application

While methylnaltrexone holds potential for treating opioid-induced constipation, it may not be effective for all patients. It is essential to be aware of potential side effects, such as abdominal pain and orthostatic hypotension, and to follow medical advice when using this medication.

Limitations of Current Research

The current research on methylnaltrexone primarily focuses on healthy volunteers and patients experiencing long-term opioid use. Additional research is needed to assess its effects in patients undergoing short-term opioid use and those with other underlying medical conditions.

Future Research Directions

Future research should investigate the efficacy of methylnaltrexone across various opioid types, dosages, administration routes, and patient populations. Long-term safety and effectiveness studies are also essential.

Conclusion

Methylnaltrexone shows promise as a potential treatment for opioid-induced constipation, but it is not a universal solution. As with any medication, it is crucial to be aware of potential side effects and to consult with a healthcare professional for guidance. Further research will provide a more comprehensive understanding of its safety and efficacy.

Literature analysis of 11 papers
Positive Content
11
Neutral Content
0
Negative Content
0
Article Type
11
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11
1.

Methylnaltrexone prevents morphine-induced delay in oral-cecal transit time without affecting analgesia: a double-blind randomized placebo-controlled trial.

Author: YuanC S, FossJ F, O'ConnorM, ToledanoA, RoizenM F, MossJ

Opioid-induced constipation relief

Methylnaltrexone, a quaternary opioid antagonist, effectively prevented morphine-induced changes in gastrointestinal motility and transit without affecting analgesia in humans. This suggests potential for methylnaltrexone as an adjunct to opioids for managing opioid-induced constipation.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
Research Support, U.S. Gov't, P.H.S.Research funding provided by the Public Health Service (PHS).

Language : English

2.

Safety and tolerance of methylnaltrexone in healthy humans: a randomized, placebo-controlled, intravenous, ascending-dose, pharmacokinetic study.

Author: FossJ F, O'ConnorM F, YuanC S, MurphyM, MossJ, RoizenM F

Opioid side effects treatment
Orthostatic hypotension

This study found that methylnaltrexone, a quaternary opioid antagonist, was well tolerated at doses of 0.32 mg/kg in healthy humans, with the dose-limiting adverse effect being orthostatic hypotension.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
Research Support, U.S. Gov't, P.H.S.Research funding provided by the Public Health Service (PHS).

Language : English

3.

The safety and efficacy of oral methylnaltrexone in preventing morphine-induced delay in oral-cecal transit time.

Author: YuanC S, FossJ F, OsinskiJ, ToledanoA, RoizenM F, MossJ

Oral methylnaltrexone
Prevents constipation

Oral methylnaltrexone, a quaternary opioid antagonist, effectively prevented morphine-induced delay in gastrointestinal transit in healthy volunteers. This suggests its potential use in managing opioid-induced constipation.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
Research Support, U.S. Gov't, P.H.S.Research funding provided by the Public Health Service (PHS).

Language : English

4.

Efficacy of orally administered methylnaltrexone in decreasing subjective effects after intravenous morphine.

Author: YuanC S, FossJ F, O'ConnorM, OsinskiJ, RoizenM F, MossJ

Reduce opioid side effects

Oral methylnaltrexone, a selective peripheral opioid receptor antagonist, significantly decreased subjective ratings of nausea, skin itch, stimulated, and flushing after intravenous morphine injection.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
Research Support, U.S. Gov't, P.H.S.Research funding provided by the Public Health Service (PHS).

Language : English

5.

Effects of enteric-coated methylnaltrexone in preventing opioid-induced delay in oral-cecal transit time.

Author: YuanC S, FossJ F, O'ConnorM, KarrisonT, OsinskiJ, RoizenM F, MossJ

Gastrointestinal effects prevention

Methylnaltrexone, the first peripheral opioid receptor antagonist, has the potential to prevent or reverse the gastrointestinal side effects of opioids. Studies showed that oral methylnaltrexone prevented morphine-induced delays in gastrointestinal transit time.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
Research Support, U.S. Gov't, P.H.S.Research funding provided by the Public Health Service (PHS).

Language : English

6.

The effects of methylnaltrexone alone and in combination with acutely administered codeine on gastrointestinal and colonic transit in health.

Author: WongB S, RaoA S, CamilleriM, ManabeN, McKinzieS, BusciglioI, BurtonD D, RyksM, ZinsmeisterA R

Methylnaltrexone did not affect gastrointestinal or colonic transit and did not reverse acute codeine-associated delayed gut transit in healthy individuals.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

7.

Subcutaneous methylnaltrexone for treatment of acute opioid-induced constipation: phase 2 study in rehabilitation after orthopedic surgery.

Author: AnissianLucas, SchwartzHarry W, VincentKevin, VincentHeather K, CarpenitoJennifer, StamblerNancy, RamakrishnaTage

Laxation
Gastrointestinal side effects

Subcutaneous methylnaltrexone was effective and well tolerated in treating acute opioid-induced constipation (OIC) after orthopedic procedures. Patients receiving methylnaltrexone achieved laxation significantly faster than those receiving placebo.

Clinical Trial, Phase IIA Phase II trial is a trial that further evaluates the efficacy and safety of a new drug or treatment, whose safety has been confirmed to some extent in a Phase I trial, in a small number of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Multicenter StudyResearch conducted in collaboration with multiple research institutions. It aims to collect a wide range of data and obtain more generalizable results.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

8.

Characterization of abdominal pain during methylnaltrexone treatment of opioid-induced constipation in advanced illness: a post hoc analysis of two clinical trials.

Author: SlatkinNeal E, LynnRichard, SuChinyu, WangWenjin, IsraelRobert J

Opioid-induced constipation treatment
Abdominal pain

Methylnaltrexone, a drug for opioid-induced constipation, was found to be associated with abdominal pain as the most common side effect.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

9.

Methylnaltrexone: its pharmacological effects alone and effects on morphine in healthy volunteers.

Author: ZacnyJames P, WroblewskiKristen, CoalsonDennis W

Opioid-induced constipation

This article reviews the use of methylnaltrexone bromide (MTNX) for opioid-induced constipation. Studies suggest that MTNX may alter other opioid-induced effects besides constipation, highlighting the potential role of peripheral opioid actions.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.

Language : English

10.

The effects of morphine and methylnaltrexone on gastrointestinal pain in healthy male participants.

Author: BrokjaerA, OlesenA E, ChristrupL L, DahanA, DrewesA M

Opioid side effect relief
Local analgesia interference

This study explored the effect of rectal morphine before and after blocking opioid receptors outside the central nervous system with methylnaltrexone (MNTX).

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

11.

Protocol for a randomised control trial of methylnaltrexone for the treatment of opioid-induced constipation and gastrointestinal stasis in intensive care patients (MOTION).

Author: PatelParind B, BrettStephen J, O'CallaghanDavid, AnjumAisha, CrossMary, WarwickJane, GordonAnthony C

Gastrointestinal dysmotility treatment

Methylnaltrexone, a peripheral opioid antagonist, may be effective in reversing opioid-induced constipation and gastrointestinal dysmotility in intensive care patients. This trial investigates the potential benefits of methylnaltrexone in managing these common side effects of opioid sedation.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

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