Naldemedine

From WikiMD
Jump to navigation Jump to search

Information about Naldemedine

Naldemedine is a peripherally acting opioid antagonist which is used to treat constipation caused by chronic opioid use.

Liver safety of Naldemedine

Naldemedine has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury.

Mechanism of action of Naldemedine

Naldemedine (nal dem' e deen) is a semisynthetic opiate receptor antagonist which is similar structurally to naltrexone and blocks mu receptors in the enteric nervous system of the gastrointestinal tract resulting in an inhibition of opioid induced slowing of peristalsis. Naldemedine has a large polar side chain that does not block its engagement with opioid receptors, but does prevent it from crossing the blood brain barrier. As a consequence, naldemedine reverses the peripheral but not the central nervous system effects of opiates, such as pain relief and euphoria. In large preregistration trials, naldemedine was found to increase spontaneous bowel movement frequency and reduce constipation related side effects of opiates used for analgesia in patients with chronic, non-cancer pain.

FDA approval information for Naldemedine

Naldemedine was approved for this use in the United States in 2017 and is currently available as tablets of 0.2 mg under the brand name Symproic.

Dosage and administration for Naldemedine

The recommended dose regimen is 0.2 mg once daily.

Side effects of Naldemedine

Side effects can include abdominal pain, diarrhea, nausea, flatulence, anxiety, restlessness and sweating. Rare but potentially severe adverse events include withdrawal symptoms, hypersensitivity reactions and gastrointestinal perforation. Naldemedine has minimal effects on constipation in persons not taking opioids.

Antidiarrheal agents

Antidiarrheal agents include bulk forming agents, hydroscopic agents, bile acid resins, bismuth, inhibitors of intestinal motility, non-absorbed antibiotics and hormones. Bulk forming agents include methylcellulose; hydroscopic agents include pectin and kaolin; bile acid resins are cholestyramine, colestipol and colesevalam; inhibitors of intestinal motility include opioids such as diphenoxylate and loperamide. Antibiotics include rifamycin and rifaximin which are non-absorbed and are used for travelers' diarrhea. Hormones with antidiarrheal activity include octretide and somatostatin. Most antidiarrheal agents are active locally in the small intestine and colon and are largely not absorbed. Some, however, have been implicated in rare causes of liver injury (senna, cascara, cholestyramine). Telotristat is a relatively new agent that inhibits the synthesis of serotonin and is used specifically for the diarrhea of carcinoid syndrome.

Antiemetics are a diverse group of medications that act at different points in the pathways that regulate nausea and vomiting. These include antihistamines, anticholinergic agents, phenothiazines, serotonin type 3 receptor blockers, centrally acting benzamides, cannabinoid receptor agonists, substance P antagonists and miscellaneous.

Anticholinergic Agents

Antihistamines

Cannabinoid Receptor Agonists

Serotonin 5-HT3 Receptor Antagonists

Substance P/Neurokinin 1 Receptor Antagonists

Miscellaneous

Acid peptic disease/antiulcer agents that include antacids, the histamine type 2 receptor blockers (H2 blockers), and the proton pump inhibitors (PPIs). These agents are some of the most commonly taken medications and are very well tolerated, most being available both by prescription and over-the-counter. While many of these drugs are approved for use in duodenal and gastric ulcer disease, their major use is for acid reflux and indigestion.

Histamine H2 Receptor Antagonists (H2 Blockers) Cimetidine, Famotidine, Nizatidine, Ranitidine

Proton Pump Inhibitors

Cathartics, laxatives or agents for constipation include bulk forming agents, osmotic agents, stool wetting agents, nonspecific stimulants, prokinetic agents and agents that increase fluid secretion. Many of these therapies are not systemically absorbed and none are considered particularly hepatotoxic. Naldemedine and naloxegol are opioid antagonists and are used to treat the constipation associated with opioid use.

Inflammatory bowel disease encompasses several disorders, most commonly ulcerative colitis and Crohn colitis. Agents can be classified as 5-aminosalicyclic acid (5-ASA) based agents, immunosuppressive drugs, antitumor necrosis factor agents, corticosteroids, antibiotics and miscellaneous.

5-Aminosalicyclic Acid (5-ASA) Derivatives

Immunosuppressive Agents

Tumor Necrosis Factor Antagonists

Miscellaneous

Irritable Bowel Syndrome Agents Antimuscarinics/Antispasmodics [See Anticholinergic agents

Prokinetic Agents - See Serotonin 5-ht4 receptor agonists Alosetron, Cisapride, Domperidone, Linaclotide, Lubiprostone, Metoclopramide, Plecanatide, Prucalopride, Tegaserod

Other

Cost and Coupons - Naldemedine

Reviews for Naldemedine

This article is a stub. YOU can help Wikimd by expanding it!

Articles on Naldemedine

Wikipedia

Learn more about Naldemedine

Help WikiMD

Find something you can improve? Join WikiMD as an an editor and help improve this page or others.

Apple bitten.svg

WikiMD is a free medical encyclopedia and wellnesspedia moderated by medical professionals.

W8MD weight loss logo

Ad. Tired of being overweight?. W8MD's insurance Weight loss program can HELP*

Quick links: Medicine Portal | Encyclopedia‏‎‏‎ | Gray's Anatomy‏‎ | Topics‏‎ |‏‎ Diseases‏‎ | Drugs | Wellness | Obesity‏‎ | Metabolic syndrome | Weight loss*
Disclaimer: The entire contents of WIKIMD.ORG are for informational purposes only and do not render medical advice or professional services. If you have a medical emergency, you should CALL 911 immediately! Given the nature of the wiki, the information provided may not be accurate, misleading and or incorrect. Use the information on this wiki at your own risk! See full Disclaimer.
Link to this page: <a href="http://www.wikimd.org/wiki/Naldemedine">Naldemedine</a>

  • Individual results may vary for weight loss from our sponsors.