Methylnaltrexone Bromide
Generic Name: methylnaltrexone bromide
Brand Names:
Relistor
11 DESCRIPTION RELISTOR ® (methylnaltrexone bromide) is a mu-opioid receptor antagonist. The chemical name for methylnaltrexone bromide is ( R )- N -(cyclopropylmethyl) noroxymorphone methobromide. The molecular formula is C 21 H 26 NO 4 Br, and the molecular weight is 436.36. The structural formula is: RELISTOR tablets for oral administration are film-coated and contain 150 mg of methylnaltrexone bromide (equivalent to 122.5 mg methylnaltrexone).
Overview
11 DESCRIPTION RELISTOR ® (methylnaltrexone bromide) is a mu-opioid receptor antagonist. The chemical name for methylnaltrexone bromide is ( R )- N -(cyclopropylmethyl) noroxymorphone methobromide. The molecular formula is C 21 H 26 NO 4 Br, and the molecular weight is 436.36. The structural formula is: RELISTOR tablets for oral administration are film-coated and contain 150 mg of methylnaltrexone bromide (equivalent to 122.5 mg methylnaltrexone).
Uses
1 INDICATIONS AND USAGE RELISTOR is an opioid antagonist. RELISTOR tablets and RELISTOR injection are indicated for the treatment of opioid-induced constipation (OIC) in adults with chronic non-cancer pain, including patients with chronic pain related to prior cancer or its treatment who do not require frequent (e.g., weekly) opioid dosage escalation. ( 1.1 ) RELISTOR injection is indicated for the treatment of OIC in adults with advanced illness or pain caused by active cancer who require opioid dosage escalation for palliative care.
Dosage
2 DOSAGE AND ADMINISTRATION Administration Instructions ( 2.1 ) Be within close proximity to toilet facilities once administered. Discontinue if treatment with opioid pain medication is also discontinued. In adult patients with chronic non-cancer pain and OIC: Patients receiving opioids for less than 4 weeks may be less responsive to RELISTOR. Discontinue all maintenance laxative therapy before starting RELISTOR; may resume laxatives if there is a suboptimal response to RELISTOR after 3 days. Re-evaluate the continued need for RELISTOR when opioid regimen is changed to avoid adverse reactions. In patients with chronic non-cancer pain and OIC, take RELISTOR tablets with water on an empty stomach at least 30 minutes before the first meal of the day.
Side Effects
6 ADVERSE REACTIONS Serious and important adverse reactions described elsewhere in the labeling include: Gastrointestinal perforation [see Warnings and Precautions ( 5.1 )] Severe or persistent diarrhea [see Warnings and Precautions ( 5.2 )] Opioid withdrawal [see Warnings and Precautions ( 5.3 )] The most common adverse reactions are: OIC in adult patients with chronic non-cancer pain ( 6.1 ) RELISTOR tablets (≥ 2%): abdominal pain, diarrhea, headache, abdominal distention, vomiting, hyperhidrosis, anxiety, muscle spasms, rhinorrhea, and chills. RELISTOR injection (≥ 1%): abdominal pain, nausea, diarrhea, hyperhidrosis, hot flush, tremor, and chills. OIC in adult patients with advanced illness ( 6.1 ) RELISTOR injection (≥ 5%): abdominal pain, flatulence, nausea, dizziness, and diarrhea.
Interactions
7 DRUG INTERACTIONS Other Opioid Antagonists : Potential for additive effect and increased risk of opioid withdrawal; avoid concomitant use. ( 7.1 ) 7.1 Other Opioid Antagonists 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. 7.2 Drugs Metabolized by Cytochrome P450 Isozymes In healthy subjects, a subcutaneous dose of 0.3 mg/kg of RELISTOR did not significantly affect the metabolism of dextromethorphan, a CYP2D6 substrate.
Warnings
5 WARNINGS AND PRECAUTIONS Gastrointestinal Perforation : Consider the overall risk benefit in patients with known or suspected lesions of the GI tract. Monitor for severe, persistent or worsening abdominal pain; discontinue if development of symptoms. ( 5.1 ) Severe or Persistent Diarrhea : Discontinue if severe or persistent diarrhea occurs during treatment. ( 5.2 ) Opioid Withdrawal : Consider the overall risk benefit in patients with disruptions to the blood-brain barrier. Monitor closely for symptoms of opioid withdrawal. 4 CONTRAINDICATIONS RELISTOR 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 [see Warnings and Precautions ( 5.1 )] . Patients with known or suspected mechanical gastrointestinal obstruction and at increased risk of recurrent obstruction. ( 4 , 5.1 )
Pregnancy
8.1 Pregnancy Risk Summary The limited available data with RELISTOR in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriages. There are clinical considerations when RELISTOR is used by pregnant women [see Clinical Considerations].
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied NDC Number Pack Size Contents 65649-150-90 90-count bottle 100-mL bottle containing 90 tablets and 2 silica gel desiccant canisters. Each 150 mg film-coated tablet is white, round, biconvex, and debossed with “REL” on one side and plain on the other side.
Frequently Asked Questions
What is Methylnaltrexone Bromide used for?▼
1 INDICATIONS AND USAGE RELISTOR is an opioid antagonist. RELISTOR tablets and RELISTOR injection are indicated for the treatment of opioid-induced constipation (OIC) in adults with chronic non-cancer pain, including patients with chronic pain related to prior cancer or its treatment who do not require frequent (e.g., weekly) opioid dosage escalation. ( 1.1 ) RELISTOR injection is indicated for the treatment of OIC in adults with advanced illness or pain caused by active cancer who require opioid dosage escalation for palliative care.
What are the side effects of Methylnaltrexone Bromide?▼
6 ADVERSE REACTIONS Serious and important adverse reactions described elsewhere in the labeling include: Gastrointestinal perforation [see Warnings and Precautions ( 5.1 )] Severe or persistent diarrhea [see Warnings and Precautions ( 5.2 )] Opioid withdrawal [see Warnings and Precautions ( 5.3 )] The most common adverse reactions are: OIC in adult patients with chronic non-cancer pain ( 6.1 ) RELISTOR tablets (≥ 2%): abdominal pain, diarrhea, headache, abdominal distention, vomiting, hyperhidrosis, anxiety, muscle spasms, rhinorrhea, and chills. RELISTOR injection (≥ 1%): abdominal pain, nausea, diarrhea, hyperhidrosis, hot flush, tremor, and chills. OIC in adult patients with advanced illness ( 6.1 ) RELISTOR injection (≥ 5%): abdominal pain, flatulence, nausea, dizziness, and diarrhea.
Can I take Methylnaltrexone Bromide during pregnancy?▼
8.1 Pregnancy Risk Summary The limited available data with RELISTOR in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriages. There are clinical considerations when RELISTOR is used by pregnant women [see Clinical Considerations].
What are the important warnings for Methylnaltrexone Bromide?▼
5 WARNINGS AND PRECAUTIONS Gastrointestinal Perforation : Consider the overall risk benefit in patients with known or suspected lesions of the GI tract. Monitor for severe, persistent or worsening abdominal pain; discontinue if development of symptoms. ( 5.1 ) Severe or Persistent Diarrhea : Discontinue if severe or persistent diarrhea occurs during treatment. ( 5.2 ) Opioid Withdrawal : Consider the overall risk benefit in patients with disruptions to the blood-brain barrier. Monitor closely for symptoms of opioid withdrawal. 4 CONTRAINDICATIONS RELISTOR 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 [see Warnings and Precautions ( 5.1 )] . Patients with known or suspected mechanical gastrointestinal obstruction and at increased risk of recurrent obstruction. ( 4 , 5.1 )
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.