title: Naloxegol: A Novel Therapy in the Management of Opioid-Induced Constipation.
abstract: Opioid-related bowel dysfunction is a common and potentially severe adverse effect from treatment with opioid analgesics. Its development is not dose related, nor do patients develop tolerance. Opioid-induced constipation (OIC) can lead to fecal impaction, bowel obstruction, and bowel perforation as well as noncompliance with opioid analgesics and poor quality of life. Routine administration of laxatives is necessary to maintain bowel function, and, in refractory cases, other modalities must be pursued. Available options are limited but include peripherally acting μ-opioid receptor antagonists (PAMORAs), including methylnaltrexone. Naloxegol is a newly developed PAMORA that is available through the oral route. At the therapeutic dose of 25 mg daily, naloxegol is effective and safe, with a limited side effect profile and is associated with preservation of centrally mediated analgesia. In this article, we discuss the pharmacokinetics, pharmacodynamics, adverse effects, clinical trials, and cost considerations of naloxegol. Finally, we discuss its potential role as a novel key treatment for OIC in palliative medicine patients.
authors.affiliation: Mayo Clinic Arizona, Palliative Medicine, Phoenix, AZ, USA Rachel.Ellen.Jones@gmail.com.
authors.forename: Rachel
authors.initials: R
authors.lastname: Jones
authors.affiliation: Mayo Clinic Arizona, Palliative Medicine, Phoenix, AZ, USA.
authors.forename: Eric
authors.initials: E
authors.lastname: Prommer
authors.affiliation: Banner University Medical Center, Gastroenterology, Phoenix, AZ, USA.
authors.forename: David
authors.initials: D
authors.lastname: Backstedt
mesh_terms: D000701:Analgesics, Opioid / Q000009:adverse effects* / Q000627:therapeutic use; D003248:Constipation / Q000139:chemically induced* / Q000188:drug therapy*; D004347:Drug Interactions; D006801:Humans; D009019:Morphinans / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D009271:Naltrexone / Q000031:analogs & derivatives / Q000627:therapeutic use; D009292:Narcotic Antagonists / Q000009:adverse effects* / Q000627:therapeutic use; D010146:Pain / Q000188:drug therapy; D011092:Polyethylene Glycols / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D011788:Quality of Life; D000644:Quaternary Ammonium Compounds / Q000627:therapeutic use; D016032:Randomized Controlled Trials as Topic
chemical_list: D000701:Analgesics, Opioid; D009019:Morphinans; D009292:Narcotic Antagonists; D000644:Quaternary Ammonium Compounds; C032257:methylnaltrexone; D011092:Polyethylene Glycols; C000589308:naloxegol; D009271:Naltrexone
keywords: methylnaltrexone; naloxegol; naloxone; opioid-induced constipation; peripherally acting μ-opioid receptor antagonists; μ-opioid receptor