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Journal of the American Pharmacists... 2008
Topics: Analgesics, Opioid; Carrier Proteins; Constipation; Familial Mediterranean Fever; Humans; Ileus; NLR Family, Pyrin Domain-Containing 3 Protein; Naltrexone; Narcotic Antagonists; Piperidines; Postoperative Complications; Quaternary Ammonium Compounds; Recombinant Fusion Proteins; Syndrome
PubMed: 18826910
DOI: 10.1331/JAPhA.2008.08537 -
The Medical Letter on Drugs and... Apr 2018
Topics: Abuse-Deterrent Formulations; Acute Pain; Administration, Oral; Analgesics, Opioid; Chronic Pain; Drug Interactions; Drug Tolerance; Humans; Opioid-Related Disorders; Treatment Outcome
PubMed: 29664446
DOI: No ID Found -
Clinical Journal of Oncology Nursing Feb 2013
Review
Topics: Aged; Constipation; Evidence-Based Nursing; Humans; Laxatives; Middle Aged; Naltrexone; Palliative Care; Quaternary Ammonium Compounds; Randomized Controlled Trials as Topic
PubMed: 23372103
DOI: 10.1188/13.CJON.91-92 -
The American Journal of Medicine Apr 2015
Topics: Abdominal Pain; Adult; Analgesics, Opioid; Anorexia; Chronic Disease; Diabetes Mellitus, Type 1; Drug Administration Schedule; Endoscopy, Gastrointestinal; Gastroparesis; Humans; Hypertension; Kidney Failure, Chronic; Male; Naltrexone; Narcotic Antagonists; Nausea; Neuralgia; Quaternary Ammonium Compounds; Substance Withdrawal Syndrome; Treatment Outcome; Vomiting
PubMed: 25460532
DOI: 10.1016/j.amjmed.2014.10.044 -
BMJ Supportive & Palliative Care Sep 2020Opioid-induced constipation (OIC) is common and can significantly affect quality of life. Naloxegol and methylnaltrexone are peripherally acting µ-opioid receptor...
Opioid-induced constipation (OIC) is common and can significantly affect quality of life. Naloxegol and methylnaltrexone are peripherally acting µ-opioid receptor antagonists (PAMORAs) which are effective for the management of OIC. We report on a case in the palliative care setting where a patient with established OIC had an inadequate response to naloxegol but an effective and immediate response to methylnaltrexone at the dose recommended for her weight. This is the first reported case of two PAMORAs used concomitantly.
Topics: Analgesics, Opioid; Female; Humans; Middle Aged; Morphinans; Naltrexone; Narcotic Antagonists; Opioid-Induced Constipation; Palliative Care; Polyethylene Glycols; Quality of Life; Quaternary Ammonium Compounds
PubMed: 32709705
DOI: 10.1136/bmjspcare-2019-002172 -
Gastroenterology Nursing : the Official... 2017
Topics: Humans; Morphinans; Naltrexone; Narcotic Antagonists; Piperidines; Polyethylene Glycols; Quaternary Ammonium Compounds; Receptors, Opioid, mu
PubMed: 29210822
DOI: 10.1097/SGA.0000000000000326 -
Expert Opinion on Investigational Drugs May 2006Methylnaltrexone is an investigational peripheral opioid receptor antagonist, a quaternary derivative of naltrexone. Methylnaltrexone has greater polarity and lower... (Review)
Review
Methylnaltrexone is an investigational peripheral opioid receptor antagonist, a quaternary derivative of naltrexone. Methylnaltrexone has greater polarity and lower lipid solubility, thus it does not cross the blood-brain barrier in humans. Methylnaltrexone offers the therapeutic potential to block or reverse the undesired side effects of opioids that are mediated by receptors located in the periphery (e.g., in the gastrointestinal tract), without affecting analgesia or precipitating the opioid withdrawal symptoms that are predominantly mediated by receptors in the CNS. This article reviews preclinical studies and clinical opioid bowel dysfunction trial data, and briefly discusses other potential roles of this compound in clinical practice.
Topics: Analgesics, Opioid; Animals; Humans; Naltrexone; Narcotic Antagonists; Quaternary Ammonium Compounds; Receptors, Opioid
PubMed: 16634692
DOI: 10.1517/13543784.15.5.541 -
Anesthesiology Oct 1997
Topics: Gastric Emptying; Humans; Naltrexone; Narcotic Antagonists; Narcotics; Quaternary Ammonium Compounds
PubMed: 9357871
DOI: 10.1097/00000542-199710000-00003 -
Expert Review of Gastroenterology &... Oct 2009In April 2008, the US FDA granted approval to methylnaltrexone (Relistor), the first peripheral micro-opioid-receptor antagonist for the treatment of opioid-induced... (Review)
Review
In April 2008, the US FDA granted approval to methylnaltrexone (Relistor), the first peripheral micro-opioid-receptor antagonist for the treatment of opioid-induced constipation in advanced-illness patients receiving palliative care and for whom other laxative therapies failed to achieve adequate results. Methylnaltrexone, a quaternary derivative of naltrexone, introduces a novel mechanism of action that selectively antagonizes the peripheral micro-receptors in the GI tract without effects on the CNS. In clinical trials, subcutaneous methylnaltrexone reversed opioid-induced constipation after the first dose in approximately 50-60% of the patients. In most of the cases, effective laxation occurred within 1 h. The therapeutic benefit was sustained in multiple-dose studies. Owing to the nature of the population studied, safety data are available for approximately 4 months of use. Although it is not the focus of this article, methylnaltrexone's mechanism of action suggests it could be beneficial for other peripheral, opioid-induced adverse effects, such as opioid-related nausea, vomiting, urinary retention, pruritus or postoperative ileus.
Topics: Analgesics, Opioid; Clinical Trials as Topic; Constipation; Defecation; Drug Approval; Gastrointestinal Motility; Humans; Injections, Intravenous; Injections, Subcutaneous; Laxatives; Naltrexone; Narcotic Antagonists; Palliative Care; Quaternary Ammonium Compounds; Treatment Outcome
PubMed: 19817669
DOI: 10.1586/egh.09.42 -
The American Journal of Hospice &... Oct 2023Methylnaltrexone is a peripherally-acting mu-opioid receptor antagonist studied in both cancer and non-cancer patients with opioid-induced constipation (OIC), but...
Methylnaltrexone is a peripherally-acting mu-opioid receptor antagonist studied in both cancer and non-cancer patients with opioid-induced constipation (OIC), but mostly in the outpatient setting. For adult hospitalized cancer patients with OIC, its effectiveness is unknown. Objectives: Describe the efficacy of methylnaltrexone for OIC in the inpatient setting, defined as bowel movement (BM) within 24 hours of methylnaltrexone administration. We performed a single-center, retrospective chart review of all hospitalized, adult patients with a cancer diagnosis who received methylnaltrexone from the palliative care team between January 1st, 2012 and July 1st, 2019. We identified 194 patients. The mean age was 59, 50.5% were male and 88% were white. 192 patients (98%) received the 8 mg dose subcutaneously. The median oral morphine equivalent (OME) was 135 mg (IQR 70-354 mg). 45% (95% confidence interval, 38-53%) had a BM within 24 hours. Higher OME was correlated with successful BM, with a response in 93% (86/92) of patients receiving ≥150 OME and 2% (2/102) of patients receiving <150 OME ( < .0001). Prior laxative use did not predict response at 24 hours whether these were osmotic laxatives (40.7% vs 47.1%, = .52), stimulant laxatives (45.7% vs 45.2%, > .99), or stool softeners (44.7% vs 46.1%, = .89). Methylnaltrexone has a high response rate when used as treatment for OIC in hospitalized adult cancer patients, especially for patients taking ≥150 OME.
Topics: Adult; Humans; Male; Female; Analgesics, Opioid; Laxatives; Retrospective Studies; Constipation; Naltrexone; Narcotic Antagonists; Quaternary Ammonium Compounds; Neoplasms; Morphine
PubMed: 36565253
DOI: 10.1177/10499091221147903