Naloxegol: First oral peripherally acting mu opioid receptor antagonists for opioid-induced constipation
Tejus Anantharamu1★, Sushil Sharma1, Ajay Kumar Gupta1, Navdeep Dahiya1, Dick B. Singh Brashier1★ Corresponding author
- 1Ashok Kumar Sharma Department of Pharmacology, Armed Forces Medical College, Pune, Maharashtra, India.
CORRESPONDENCE
Tejus Anantharamu
Ashok Kumar Sharma Department of Pharmacology, Armed Forces Medical College, Pune, Maharashtra, India.
Received: 25-09-2014; Revised: 09-02-2015; Accepted: 29-05-2015.
Volume 6, Issue 3 · pp. 188–192 · PUBLISHED 2015 · DOI: 10.4103/0976-500X.162015
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ABSTRACT
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.
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Anantharamu, T., Sharma, S., Gupta, A. K., Dahiya, N., & Brashier, D. B. S. (2015). Naloxegol: First oral peripherally acting mu opioid receptor antagonists for opioid-induced constipation. Journal of Pharmacology and Pharmacotherapeutics, 6(3), 188–192. https://doi.org/10.4103/0976-500X.162015