RELISTOR Targets the Underlying Cause of
RELISTOR can help treat opioid-induced constipation without compromising analgesia because of its restricted ability to cross the blood-brain barrier and its ability to block opioids from binding in tissues such as the GI tract.1,2
Opioid-Induced Constipation (OIC) and RELISTOR
The Science of OIC and Why Opiates Cause Constipation
Nearly all opioids are small molecules that can easily permeate the blood-brain barrier. Within the central nervous system, these molecules interact with mu-opioid receptors to exert an analgesic effect.
Opioid receptors can also be found in the periphery, such as the gastrointestinal tract.
While opioids are exerting their desirable analgesic effects centrally at the mu-opioid receptor, they are also causing undesirable adverse effects peripherally, including gastrointestinal function.
A goal for opioid-induced constipation should be to separate the undesirable peripheral effect of opioids on the gastrointestinal tract from the central analgesic effect.
Targeting the Source of Opioid-Induced Constipation
RELISTOR is indicated for the treatment of opioid-induced constipation for adult patients with chronic non-cancer pain.
RELISTOR is indicated for the treatment of opioid-induced constipation in patients with advanced illness who are receiving palliative care, when response to laxative therapy has not been sufficient. Use of RELISTOR beyond four months has not been studied.
RELISTOR (methylnaltrexone bromide) is a peripherally acting selective antagonist of opioid binding at the mu-opioid receptor.
The molecular structure of RELISTOR restricts it from crossing the blood-brain barrier; therefore, it does not interfere with the desired action of opioids on the centrally located mu-opioid receptors.
RELISTOR is a competitive antagonist that occupies the mu-receptors in the GI tract.
This targeted action of RELISTOR blocks opioids from binding to decrease their constipating effects on the GI tract.
Therefore, RELISTOR can help treat the constipation initiated by the peripheral action of opioids to mu-receptors in the GI tract without compromising opioid-mediated analgesic effects on the central nervous system.
By occupying the mu-receptor in the GI tract, RELISTOR may help restore your patient's bowel function.
The most common adverse reactions in adult patients with OIC and chronic non-cancer pain are abdominal pain, nausea, diarrhea, hyperhidrosis, hot flush, tremor, and chills.
The most common adverse reactions in adult patients with OIC and advanced illness are abdominal pain, flatulence, nausea, dizziness, and diarrhea.
- RELISTOR® (methylnaltrexone bromide) Prescribing Information, Salix Pharmaceuticals.
- Michna E, Blonsky ER, Schulman S, et al. Subcutaneous methylnaltrexone for the treatment of opioid-induced constipation in patients with chronic nonmalignant pain: a randomized controlled study. J Pain. 2011;12(5):554-562.