Promising medication counteracts constipation caused by opioid painkillers

Opioids – strong morphine-based painkillers – are widely prescribed to patients experiencing chronic severe pain. While these drugs are very effective for treating and managing pain, they have one particularly bothersome side effect: constipation. A new drug, called naloxegol, could bring relief. In stage 3 trials reported in the New England Journal of Medicine, KU Leuven and international researchers provide new evidence that the drug relieves constipation without dulling opioids' pain-relieving effects.

Up until a decade ago, physicians rarely prescribed opioids, reserving them primarily for the terminally sick. Today, opioid-based drugs have proliferated thanks to their 'user-friendliness' and effectiveness. Millions of patients take opioids on a daily basis to manage lower back and chronic joint problems. Opioids also play a critical role in regimes for cancer patients.

However, opioids have a number of side effects, including nausea, vomiting and – notoriously – constipation. Opioids block pain by binding to 'mu-receptors' in the brain. But they also bind to mu-receptors in the bowels, and this causes constipation.

Some sixty percent of patients that take opioid experience constipation. For some, the bother is so great that they choose to stop taking the drug.

A newly developed opioid antagonist called naloxegol may offer relief. Stage 3 testing by an international team of researchers led by Belgian gastroenterologist Jan Tack (University Hospitals Leuven) confirms the drug's efficacy.

Naloxegol is based on the same active molecule as naloxone, a drug developed in the 1960s to counter the effects of opioid overdose. Naloxone is commonly used to wake patients from opioid-induced anesthesia after surgery.

To arrive at naloxegol, the researchers modified the molecular structure of naloxone. The result is an orally administered, once-a-day pill for patients experiencing opioid-induced .

The researchers tested the pill's efficacy in two phase 3 studies – with promising results. Naloxegol was shown to maintain opioids' pain-killing effect in the brain and block their effects in the bowels. Bowel function in all of the 1,400 test subjects returned to normal and accompanying stomach pain and other discomforts decreased. No patients experienced a diminished pain-relieving effect as a result of the drug.

While the studies addressed in the paper focused on patients taking for non-cancer pain such as back pain and other musculoskeletal ailments, similar studies are now underway to examine the effect of naloxegol in patients with chronic cancer-related pain.

Final regulatory approval for the drug is pending in the United States and Europe.

add to favorites email to friend print save as pdf

Related Stories

FDA orders starker warnings on opioid painkillers

Sep 10, 2013

The Food and Drug Administration is requiring stronger warning labels on prescription painkillers like OxyContin, in the government's latest attempt to reduce overdose deaths caused by the long-acting medications.

Recommended for you

Determine patient preferences by means of conjoint analysis

Jul 29, 2014

The Conjoint Analysis (CA) method is in principle suitable to find out which preferences patients have regarding treatment goals. However, to widely use it in health economic evaluations, some (primarily methodological) issues ...

FDA approves hard-to-abuse narcotic painkiller

Jul 25, 2014

(HealthDay)—A new formulation of a powerful narcotic painkiller that discourages potential abusers from snorting or injecting the drug has been approved by the U.S. Food and Drug Administration.

Race affects opioid selection for cancer pain

Jul 25, 2014

(HealthDay)—Racial disparities exist in the type of opioid prescribed for cancer pain, according to a study published online July 21 in the Journal of Clinical Oncology.

FDA approves tough-to-abuse formulation of oxycodone

Jul 25, 2014

(HealthDay)—Targiniq ER (oxycodone hydrochloride and naloxone hydrochloride extended release) has been approved by the U.S. Food and Drug Administration as a long-term, around-the-clock treatment for severe ...

User comments