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

Have a cold? Don't ask your doctor for antibiotics

4 hours ago

Antibiotic resistance is a major threat to public health. Resistance makes it harder for physicians to treat infections and can increase the chance patients will die from an infection. What is more, the treatment ...

Powdered measles vaccine found safe in early clinical trials

Nov 25, 2014

A measles vaccine made of fine dry powder and delivered with a puff of air triggered no adverse side effects in early human testing and it is likely effective, according to a paper to be published November 28 in the journal ...

Health care M&A leads global deal surge

Nov 23, 2014

In a big year for deal making, the health care industry is a standout. Large drugmakers are buying and selling businesses to control costs and deploy surplus cash. A rising stock market, tax strategies and ...

User comments

Please sign in to add a comment. Registration is free, and takes less than a minute. Read more

Click here to reset your password.
Sign in to get notified via email when new comments are made.