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For opioid-induced constipation: Nausea: ~ 11%; 1% severe nausea and 2% discontinued treatment due to nausea. Diarrhea: ~ 8%; 2% severe diarrhea and 1% of patients discontinued treatment due to diarrhea. Less common adverse reactions (<1%): fecal incontinence, blood potassium decreased. For subjects with irritable bowel syndrome with constipation:
Naloxegol (INN; PEGylated naloxol; [4] trade names Movantik and Moventig) is a peripherally acting μ-opioid receptor antagonist developed by AstraZeneca, licensed from Nektar Therapeutics, for the treatment of opioid-induced constipation. [5] It was approved in 2014 in adult patients with chronic, non-cancer pain. [6]
Partial agonists, like the anti-diarrhea drug loperamide and antagonists, like naloxegol for opioid-induced constipation, do not cross the blood–brain barrier, but can displace other opioids from binding to those receptors in the myenteric plexus. Because opioids are addictive and may result in fatal overdose, most are controlled substances.
Results from Phase III Studies of Naloxegol for Treatment of Opioid-Induced Constipation Presented at Digestive Disease Week 2013 ORLANDO, Fla.--(BUSINESS WIRE)-- AstraZeneca (NYS: AZN) today ...
Studies have shown altered muscle contractility and tone, bowel compliance, and transit may contribute to many of the gastrointestinal symptoms of FGID which may include diarrhea, constipation, and vomiting. [20] Visceral hypersensitivity In FGID there is poor association of pain with GI motility in many functional GI disorders.
Methylnaltrexone (MNTX, brand name Relistor), used in form of methylnaltrexone bromide (INN, USAN, BAN), is a medication that acts as a peripherally acting μ-opioid receptor antagonist that acts to reverse some of the side effects of opioid drugs such as constipation without significantly affecting pain relief or precipitating withdrawals.