RELISTOR Targets the Underlying Cause of
Opioid-Induced Constipation

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
Targeting the Source of OIC

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.

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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.

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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.

INDICATIONS

RELISTOR is indicated for the treatment of opioid-induced constipation for adult patients with chronic non-cancer pain.

RELISTOR is also indicated for the treatment of opioid-induced constipation in adult 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.

IMPORTANT SAFETY INFORMATION

RELISTOR® (methylnaltrexone bromide) Subcutaneous Injection is contraindicated in patients with known or suspected gastrointestinal obstruction and patients at increased risk of recurrent obstruction, due to the potential for gastrointestinal perforation.

Cases of gastrointestinal perforation have been reported in adult patients with opioid-induced constipation and advanced illness with conditions that may be associated with localized or diffuse reduction of structural integrity in the wall of the gastrointestinal tract (e.g., peptic ulcer disease, Ogilvie's syndrome, diverticular disease, infiltrative gastrointestinal tract malignancies or peritoneal metastases). Take into account the overall risk-benefit profile when using RELISTOR in patients with these conditions or other conditions which might result in impaired integrity of the gastrointestinal tract wall (e.g., Crohn's disease). Monitor for the development of severe, persistent, or worsening abdominal pain; discontinue RELISTOR in patients who develop this symptom.

If severe or persistent diarrhea occurs during treatment, advise patients to discontinue therapy with RELISTOR and consult their physician.

Symptoms consistent with opioid withdrawal, including hyperhidrosis, chills, diarrhea, abdominal pain, anxiety, and yawning have occurred in patients treated with RELISTOR. Patients having disruptions to the blood-brain barrier may be at increased risk for opioid withdrawal and/or reduced analgesia and should be monitored for adequacy of analgesia and symptoms of opioid withdrawal.

Avoid concomitant use of RELISTOR with other opioid antagonists because of the potential for additive effects of opioid receptor antagonism and increased risk of opioid withdrawal.

RELISTOR may precipitate opioid withdrawal in a fetus and should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. In nursing mothers, a decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

In the clinical study in adult patients with opioid-induced constipation and chronic non-cancer pain, the most common adverse reactions (≥ 1%) were abdominal pain, nausea, diarrhea, hyperhidrosis, hot flush, tremor, and chills.

In clinical studies in adult patients with opioid-induced constipation and advanced illness, the most common adverse reactions (≥ 5%) were abdominal pain, flatulence, nausea, dizziness, and diarrhea.

Click here for Prescribing Information.

For product information, adverse event reports, and product complaint reports, please contact:

Salix Product Information Call Center
Phone: 1-800-508-0024
Fax: 1-510-595-8183
Email: customerservice@salix.com

References:

  1. RELISTOR® (methylnaltrexone bromide) Prescribing Information, Salix Pharmaceuticals.
  2. 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.
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