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Relistor

Relistor (methylnaltrexone bromide) is a peripherally acting opioid receptor antagonist used to treat opioid-induced constipation (OIC) in adult patients with chronic pain who are receiving opioid therapy. It works by blocking the effects of opioids on the gut, helping to relieve constipation without affecting the analgesic effects of opioids in the central nervous system.



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Frequently Asked Questions

How quickly does Relistor work?
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Relistor typically begins to work within 30 minutes to 4 hours after administration, depending on the formulation.

Can I stop taking Relistor suddenly?
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Relistor can generally be discontinued without tapering; however, consult your healthcare provider if you have any concerns

Are there any specific dietary restrictions while taking Relistor?
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There are no specific dietary restrictions associated with Relistor, but maintaining a healthy diet can support overall gastrointestinal health.

What should I do if I miss a dose of Relistor?
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If you miss a dose of the injectable form, administer it as soon as you remember. If it’s close to the time for your next dose, skip the missed dose and continue with your regular schedule. For the oral form, follow your healthcare provider's instructions.

Is Relistor safe for long-term use?
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Relistor is intended for use as needed for opioid-induced constipation. Long-term use should be discussed with a healthcare provider to evaluate benefits and risks. Regular monitoring for effectiveness and any potential side effects is essential.

Comprehensive Drug Guide

How Does Relistor Work?

Methylnaltrexone selectively binds to and blocks mu-opioid receptors in the gastrointestinal tract, counteracting the constipating effects of opioids. Unlike other opioid antagonists, Relistor does not significantly cross the blood-brain barrier, which allows it to block peripheral opioid effects without interfering with central pain relief.

Common Dosages

  • Injectable solution: 12 mg/0.6 mL (subcutaneous injection).
  • Oral tablets: 150 mg.

Typical Dosing

  • For the injectable form: The recommended dose is 12 mg administered subcutaneously once a day as needed for OIC.
  • For the oral form: The recommended dose is 450 mg taken once daily with or without food.


Typical Dosing

FDA Approved Indications

  • Treatment of opioid-induced constipation (OIC) in adult patients with chronic pain who are on opioid therapy.

Who Shouldn't Take Relistor?

  • Known hypersensitivity to methylnaltrexone or any components of the formulation.
  • Gastrointestinal obstruction (e.g., bowel obstruction), as it may worsen the condition.

Advice From The Pharmacist

  • Instruct patients on the proper administration technique for both the injectable and oral forms of Relistor.
  • Advise patients to use Relistor only as directed and to consult their healthcare provider if symptoms do not improve or worsen.
  • Monitor for signs of gastrointestinal obstruction, especially in patients with a history of such conditions.


Side Effects of Relistor

Common Side Effects

  • Abdominal pain
  • Flatulence
  • Diarrhea
  • Nausea
  • Headache


Uncommon/Severe Side Effects

  • Severe allergic reactions (such as rash, itching, or difficulty breathing)
  • Withdrawal symptoms in patients who are physically dependent on opioids.


Risks and Warnings of Relistor

  • Gastrointestinal Risks: Patients should be monitored for signs of bowel obstruction, especially those with a history of gastrointestinal disorders.
  • Withdrawal Symptoms: Patients who are physically dependent on opioids may experience withdrawal symptoms after taking Relistor.

Interactions with Relistor

Common Drug Interactions

  • Opioids: Relistor may not be effective if there is an ongoing need for opioid analgesia, and its use should be carefully monitored in patients with concurrent opioid therapy.

Other Gastrointestinal Agents: Caution is advised when combining with other gastrointestinal medications, as this may increase the risk of side effects.

Alternatives to Relistor

  • Laxatives: Such as polyethylene glycol or docusate sodium may be used to manage opioid-induced constipation.
  • Other Opioid Receptor Antagonists: Such as naloxone, which may be used in specific cases of opioid-induced side effects.