Naldemedine - new choice for treatment of opioid-related constipation January 25, 2018 Source: CPhI Pharma Online Author: Tim Zhu laugh Effective prevention and treatment of opioid-related constipation can improve the quality of life of patients. Naldemedine can significantly increase the number of bowel movements in patients, has the advantage of no effect on pain and does not cause opiate withdrawal symptoms. The treatment of chronic cancer pain is aimed at relieving pain and improving the quality of life. Opioids are commonly used painkillers for moderate to severe pain. They play an analgesic effect through the combination with opioid receptors. The patient has adverse reactions such as constipation, nausea and vomiting, muscle spasm, and drug resistance. The most important adverse reaction is constipation, which in turn leads to depression, abdominal distension, abdominal pain, and even parasitic intestinal obstruction. Some patients prefer to suffer from pain and do not accept constipation caused by long-term use of opioids. The work brings new challenges. Effective prevention and treatment of opioid-related constipation can improve the quality of life of patients. At present, the most commonly used treatment for opioid-induced constipation is extraintestinal laxatives. In addition, existing opioid-related constipation treatments include laxatives (osmotic laxatives, stimulating laxatives, lubricative laxatives, etc.). Medicine (mosapride, tegaserod, etc., dopamine receptor antagonists: itopride, domperidone, etc.), probiotics (Lactobacillus, Bacillus subtilis, Bifidobacterium, etc.), opioid receptor antagonists Loxos, oxycodone, methylnaltrexone, avimopan, etc.), traditional Chinese medicine (Mairen Runchang Pills), secretagogues (lubi prostaglandin, linaclotide, etc.). Newer drugs include Axelopran, Linaclotide, and TRV-130. In March 2017, the FDA approved the treatment of constipation drug Symproic (naldemedine), which was approved on the basis of the Compose clinical program, which is a global comprehensive clinical trial in patients with chronic non-cancerous pain and opioid-induced constipation. Development research. Naldemedine is an opioid receptor antagonist that acts primarily on the μ receptor in the gastrointestinal tract, thereby alleviating opioid-related constipation. Naldemedine is a derivative of naltrexone that greatly reduces its ability to cross the blood-brain barrier by increasing the molecular weight and surface polarity of naltrexone. Symproic is approved for the treatment of constipation caused by opioids in patients with chronic non-cancerous pain in adults. Japanese scholars recently reported the results of a phase III clinical trial using the μ-opioid receptor antagonist Naldemedine (S-297995) for opioid-induced constipation in patients with cancer pain. This phase III clinical trial consisted of two parts, one was a two-week randomized double-blind controlled trial of 194 patients, and patients with constipation were randomized. The intervention group received oral naldemedine 0.2 mg daily, and the control group received placebo. The outcome measure was the proportion of spontaneous defecation (≥ 3 weekly or weekly increases compared to baseline), and the improvement in the intervention group was significantly better than the placebo group, with 71.1% and 34.4%, respectively. The other part was a 12-week open randomized expansion study of 131 patients. The primary outcome measure was drug safety. Diarrhea is the most common adverse reaction that has been reported to be abdominal pain, diarrhea, and nausea. Naldemedine does not cross the blood-brain barrier, does not cause withdrawal of opioids, and has no effect on the analgesic effect of opioids. These indicate that oral naldemedine 0.2 mg daily can effectively treat opioid-induced constipation, which is good. It is tolerated by patients who use opioids and is safe. Naldemedine can significantly increase the number of bowel movements in patients, has the advantage of no effect on pain and does not cause opiate withdrawal symptoms. However, although the drug has been successfully approved for marketing in the United States, its efficacy in patients from different regions and ethnic groups still needs further research. Naldemedine will provide doctors and cancer patients with new options for the treatment of μ-opioid receptor antagonists. References: Katakami N, Harada T, Murata T, et al. Randomized Phase III and Extension Studies of Naldemedine in Patients With Opioid-Induced Constipation and Cancer. J Clin Oncol. 2017, 1,35(34):3859-3866. Livestock Industry Nitrile Gloves Livestock Industry Nitrile Gloves,Blue Nitrile Exam Gloves,Powder Free Nitrile Medical Gloves,Latex Free Powder Free Nitrile Gloves Puyang Linshi Medical Supplies Co., Ltd. , https://www.linshimedicals.com