Oral Treatment for Opioid-Induced Constipation Approved

DEERFIELD, IL – Lubiprostone, marketed as Amitiza by Sucampo Pharmaceuticals Inc. and its partner Takeda Pharmaceuticals USA Inc., has been approved by the Food and Drug Administration (FDA) as the first oral treatment for opioid-induced constipation in adults with chronic noncancer pain.

The drug is a specific activator of ClC-2 chloride channels in the intestinal epithelium, and, through activation of apical ClC-2 channels in the intestinal epithelium, bypasses the antisecretory action of opiates.The new approval came after a Supplemental New Drug Application that received a priority review. The drug already is approved in the United States for the treatment of chronic idiopathic constipation in adults, also at a dose of 24 μg twice daily, and irritable bowel syndrome with constipation in women 18 years of age and older at a dose of 8 μg twice daily.

FDA approval was based on results from 12-week, Phase 3 studies in patients taking opioids, including morphine, oxycodone and fentanyl for chronic noncancer pain and a long-term open-label safety study. Two of the Phase 3 studies met the overall efficacy endpoint, although a third study did not, according to a Sucampo press release.

The manufacturer points out that the effectiveness of the drug in patients taking diphenylheptane opioids, such as methadone, hasn’t been established and that concomitant use of these opioids might interfere with its effectiveness.

Opioid-induced constipation is a common adverse effect of long-term opioid use because the binding of opioids to peripheral opioid receptors in the gastrointestinal (GI) tract results in absorption of electrolytes, such as chloride, with a subsequent reduction in small intestinal fluid. Activation of enteric opioid receptors also results in abnormal GI motility. 

Comments (1)

Trackback URL | Comments RSS Feed

  1. Robert says:

    You might need a stool softener, not a laxative. I had oral surgery and was prescribed amoxicillin (antibiotic) and endocet (pain reliever containing acetaminophen and oxycodone). In the patient prescription information for endocet it lists constipation as a possible side effect, and goes on to say “To prevent constipation, eat a diet adequate in fiber, drink plenty of water, and exercise.” I had not had side effects from medication before that I can remember, and unfortunately, I did not read all of this prior to using this medication. After the surgery I became severely constipated.

    I had not eaten anything for several days, so when my bowl movements stopped I did not notice. Rarely in my life have I been constipated. Once I started eating again, I became uncomfortable within a few days and realized that I was constipated. I tried prune juice, laxatives such as Ex-Lax, Phillips Milk of Magnesia, SenokotXtra, and a self-administered rectal suppository. Nothing worked. Days were going by and I was becoming extremely uncomfortable and was very close to going to the emergency room for a rectal water enema. I decided to call my doctor (general practitioner) first to ask his advice, but he was on vacation so I spoke to another doctor in the office. I related the story above. Although I was seeking advice on what over the counter medication I should take, I was advised instead to go to the emergency room and have an x-ray because I might have a tumor. Of course, I thought that was ridiculous. I did not suddenly develop a tumor. Although I had not read it, it seemed to me my problem was the result of taking pills for several days while not eating much of anything. Then I called a pharmacist, who then recommended medications that I had already taken. No new ideas there either. Finally I called the oral surgeon who operated on me. This seemed at the time to be an odd question for him, but I was getting desperate.

    He immediately said I needed a stool softener and recommended Colace. He said such problems were common in hospitals and this is what patients were often given. I bought it, took it, went for a long walk around the neighborhood and periodically walked around the perimeter of the backyard for 15 minutes at a time, and in 12-18 hours began to have relief. The stool came out in hard compact clay-like nuggets. It was difficult and a bit painful to pass and I squatted in the shower to do it, but once the process started I experienced relief in increments over the next 12 hours.

Share Your Thoughts