Naloxegol: First oral peripherally acting mu opioid receptor antagonists for opioid-induced constipation

• Published in: Journal of pharmacology & pharmacotherapeutics Vol. 6; no. 3; pp. 188 - 192
• Main Authors: Anantharamu, Tejus, Sharma, Sushil, Gupta, Ajay Kumar, Dahiya, Navdeep, Brashier, Dick B. Singh, Sharma, Ashok Kumar
• Format: Journal Article
• Language: English
• Published: India Medknow Publications and Media Pvt. Ltd 01.07.2015; Sage Publications Ltd; Medknow Publications & Media Pvt Ltd
• Subjects: Analgesics; Blood-brain barrier; Cancer; Cancer therapies; Complications and side effects; Constipation; Dosage and administration; Drug dosages; Drug therapy; FDA approval; Heart attacks; Molecules of the Millennium; Motility; Naloxegol; Narcotics; Opioids; Pain management; Palliative care; Studies; Naloxegol; peripherally acting mu opioid receptor antagonists; opioid-induced constipation
• ISSN: 0976-500X; 0976-5018
• DOI: 10.4103/0976-500X.162015

Opioid-induced constipation (OIC) is one of the most troublesome and the most common effects of opioid use leading to deterioration in quality of life of the patients and also has potentially deleterious repercussions on adherence and compliance to opioid therapy. With the current guidelines advocating liberal use of opioids by physicians even for non-cancer chronic pain, the situation is further complicated as these individuals are not undergoing palliative care and hence there cannot be any justification to subject these patients to the severe constipation brought on by opioid therapy which is no less debilitating than the chronic pain. The aim in these patients is to prevent the opioid-induced constipation but at the same time allow the analgesic activity of opioids. Many drugs have been used with limited success but the most specific among them were the peripherally acting mu opioid receptor antagonists (PAMORA). Methylnaltrexone and alvimopan were the early drugs in this group but were not approved for oral use in OIC. However naloxegol, the latest PAMORA has been very recently approved as the first oral drug for OIC. This article gives an overview of OIC, its current management and more specifically the development and approval of naloxegol, including pharmacokinetics, details of various clinical trials, adverse effects and its current status for the management of OIC.