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Indications

IMPORTANT SAFETY INFORMATION

  • RELISTOR® (methylnaltrexone bromide) 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.
  • RELISTOR injection is also 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.
  • RELISTOR tablets and injection are contraindicated in patients with known or suspected mechanical gastrointestinal obstruction and patients

IMPORTANT SAFETY INFORMATION

  • RELISTOR tablets and injection are contraindicated in patients with known or suspected mechanical 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 healthcare provider.
  • 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.
  • The use of RELISTOR during pregnancy may precipitate opioid withdrawal in a fetus due to the immature fetal blood-brain barrier and should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Because of the potential for serious adverse reactions, including opioid withdrawal, in breastfed infants, advise women that breastfeeding is not recommended during treatment with RELISTOR. 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.
  • A dosage reduction of RELISTOR tablets and RELISTOR injection is recommended in patients with moderate and severe renal impairment (creatinine clearance less than 60 mL/minute as estimated by Cockcroft-Gault). No dosage adjustment of RELISTOR tablets or RELISTOR injection is needed in patients with mild renal impairment.
  • A dosage reduction of RELISTOR tablets is recommended in patients with moderate (Child-Pugh Class B) or severe (Child-Pugh Class C) hepatic impairment. No dosage adjustment of RELISTOR tablets is needed in patients with mild hepatic impairment (Child-Pugh Class A). No dosage adjustment of RELISTOR injection is needed for patients with mild or moderate hepatic impairment. In patients with severe hepatic impairment, monitor for methylnaltrexone-related adverse reactions and dose adjust per Prescribing Information as may be indicated.
  • In the clinical studies, the most common adverse reactions were:

OIC in adult patients with chronic non-cancer pain

  • RELISTOR tablets (≥ 2% of RELISTOR patients and at a greater incidence than placebo): abdominal pain (14%), diarrhea (5%), headache (4%), abdominal distention (4%), vomiting (3%), hyperhidrosis (3%), anxiety (2%), muscle spasms (2%), rhinorrhea (2%), and chills (2%).
  • RELISTOR injection (≥ 1% of RELISTOR patients and at a greater incidence than placebo): abdominal pain (21%), nausea (9%), diarrhea (6%), hyperhidrosis (6%), hot flush (3%), tremor (1%), and chills (1%).

OIC in adult patients with advanced illness

  • RELISTOR injection (≥ 5% of RELISTOR patients and at a greater incidence than placebo): abdominal pain (29%), flatulence (13%), nausea (12%), dizziness (7%), and diarrhea (6%).

To report SUSPECTED ADVERSE REACTIONS, contact Salix Pharmaceuticals at 1-800-321-4576 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Please click here for full Prescribing Information for RELISTOR tablets and RELISTOR injection.

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IMPORTANT SAFETY INFORMATION

  • RELISTOR tablets and injection are contraindicated in patients with known or suspected mechanical 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 healthcare provider.
  • 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.
  • The use of RELISTOR during pregnancy may precipitate opioid withdrawal in a fetus due to the immature fetal blood-brain barrier and should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Because of the potential for serious adverse reactions, including opioid withdrawal, in breastfed infants, advise women that breastfeeding is not recommended during treatment with RELISTOR. 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.
  • A dosage reduction of RELISTOR tablets and RELISTOR injection is recommended in patients with moderate and severe renal impairment (creatinine clearance less than 60 mL/minute as estimated by Cockcroft-Gault). No dosage adjustment of RELISTOR tablets or RELISTOR injection is needed in patients with mild renal impairment.
  • A dosage reduction of RELISTOR tablets is recommended in patients with moderate (Child-Pugh Class B) or severe (Child-Pugh Class C) hepatic impairment. No dosage adjustment of RELISTOR tablets is needed in patients with mild hepatic impairment (Child-Pugh Class A). No dosage adjustment of RELISTOR injection is needed for patients with mild or moderate hepatic impairment. In patients with severe hepatic impairment, monitor for methylnaltrexone-related adverse reactions and dose adjust per Prescribing Information as may be indicated.
  • In the clinical studies, the most common adverse reactions were:

OIC in adult patients with chronic non-cancer pain

  • RELISTOR tablets (≥ 2% of RELISTOR patients and at a greater incidence than placebo): abdominal pain (14%), diarrhea (5%), headache (4%), abdominal distention (4%), vomiting (3%), hyperhidrosis (3%), anxiety (2%), muscle spasms (2%), rhinorrhea (2%), and chills (2%).
  • RELISTOR injection (≥ 1% of RELISTOR patients and at a greater incidence than placebo): abdominal pain (21%), nausea (9%), diarrhea (6%), hyperhidrosis (6%), hot flush (3%), tremor (1%), and chills (1%).

OIC in adult patients with advanced illness

  • RELISTOR injection (≥ 5% of RELISTOR patients and at a greater incidence than placebo): abdominal pain (29%), flatulence (13%), nausea (12%), dizziness (7%), and diarrhea (6%).

Indications

  • RELISTOR® (methylnaltrexone bromide) 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.
  • RELISTOR injection is also 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.

To report SUSPECTED ADVERSE REACTIONS, contact Salix Pharmaceuticals at 1-800-321-4576 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Please click here for full Prescribing Information for RELISTOR tablets and RELISTOR injection.

What happens if patients forego treatment of opioid-induced constipation (OIC) for fear of blunting the analgesic effects of their pain medication? What if these patients present in an emergency department setting or are receiving palliative care at home for advanced cancer?

Special considerations for these OIC treatment scenarios are explored below.

Oncology and
emergency medicine

What happens if patients forego treatment of opioid-induced constipation (OIC) for fear of blunting the analgesic effects of their pain medication? What if these patients present in an emergency department setting or are receiving palliative care at home for advanced cancer?

Special considerations for these OIC treatment scenarios are explored below.

When facing active cancer pain1

Cancer-related pain and OIC Cancer-related pain and OIC
60%

of patients treated with morphine for cancer-related pain experienced OIC, per a 2006 study2

STUDY DESIGN: IN ADULT PATIENTS WITH CHRONIC CANCER PAIN

Study, published in 2006, consisted of 42 adult patients with chronic cancer pain and advanced cancer taking morphine regularly throughout the time of the 4-week study, as prescribed solely by the Palliative Medicine Program physicians at the Cleveland Clinic Foundation. Symptoms were self-reported by the patients using an empirical 33-item questionnaire. The first question was a categorical global rating of overall pain intensity during the previous week (none, mild, moderate, severe). The remaining 32 questions asked about 27 potential symptoms already reported in the literature as morphine side effects; there were 2 questions each about constipation, nausea, vomiting, and hearing problems.2

Study, published in 2006, consisted of 42 adult patients with chronic cancer pain and advanced cancer taking morphine regularly throughout the time of the 4-week study, as prescribed solely by the Palliative Medicine Program physicians at the Cleveland Clinic Foundation. Symptoms were self-reported by the patients using an empirical 33-item questionnaire. The first question was a categorical global rating of overall pain intensity during the previous week (none, mild, moderate, severe). The remaining 32 questions asked about 27 potential symptoms already reported in the literature as morphine side effects; there were 2 questions each about constipation, nausea, vomiting, and hearing problems.2

RELISTOR subcutaneous injection is the first and only PAMORA available for adult patients with OIC and active cancer pain who require opioid dosage escalation for palliative care1,3-6

PAMORA, peripherally acting mu-opioid receptor antagonist.

Oncology and Emergency Medicine

RELISTOR injection: When speed is clinically useful1,7,8

Advanced illness*: In focus

RELISTOR timingRELISTOR timing

RELISTOR injection: When speed is clinically useful1,7,8

Advanced illness*: In focus

0%

of patients (n=47) in Study 4 receiving 0.15 mg/kg dose of RELISTOR experienced a spontaneous bowel movement (SBM)† within 4 hours of first dose vs 14% receiving placebo (n=52; P<.0001)1,7

0%

of patients (n=62) in Study 5 receiving 0.15 mg/kg dose of RELISTOR experienced a SBMǂ within 4 hours of first dose vs 16% receiving placebo (n=71; P<.0001)1,8

In Study 5, significantly more patients in the RELISTOR injection cohort (52%; n=62) experienced laxation within the first 4 hours after at least 2 of the first 4 doses vs 9% for placebo (n=71; P<.0001)1

STUDY DESIGNS: IN ADULT PATIENTS WITH ADVANCED ILLNESS

Study 4 was a multicenter, double-blind, randomized, placebo-controlled study where 154 patients with advanced illness and OIC received a single subcutaneous RELISTOR injection 0.15 mg/kg or 0.3 mg/kg or placebo, followed by an open-label 4-week dosing period where RELISTOR injection could be used as needed, no more frequently than 1 dose in a 24-hour period.1,7

Study 5 was a 2-week, multicenter, double-blind, randomized, placebo-controlled trial comparing RELISTOR injection 0.15 mg/kg or 0.3 mg/kg given every other day vs placebo in 133 patients, followed by a subsequent 3-month open-label extension study.1,8

*In patients who require opioid dosage escalation for palliative care.1

†SBM is defined as laxation without the use of a rescue laxative during the previous 24 hours.1

~0%

of patients with advanced illness in Study 4 who responded to RELISTOR injection (0.15 or 0.3 mg/kg) experienced a SBM‡ within 30 minutes of first dose7

-

Limitations of data: The proportion of patients who experienced a SBM within 30 minutes is an exploratory endpoint. No conclusions about efficacy can be drawn from these descriptive data because they are results from exploratory endpoints7

‡SBM is defined as laxation without the use of a rescue laxative during the previous 24 hours.1

Once-daily dosing options for patients with chronic non-cancer pain1

RELISTOR has a well-established safety profile1

Adverse reactions from all doses in double-blind placebo-controlled clinical studies of RELISTOR injection in adult patients with OIC and advanced illness (Studies 4 and 5)1

ADVERSE REACTIONS§ RELISTOR INJECTION
(n=165)		 PLACEBO
(n=123)
ABDOMINAL PAIN|| 29% 10%
FLATULENCE 13% 6%
NAUSEA 12% 5%
DIZZINESS 7% 2%
DIARRHEA 6% 2%
ADVERSE REACTIONS§
ABDOMINAL PAIN||
RELISTOR INJECTION (n=165) 29%
Placebo (n=123) 10%
FLATULENCE
RELISTOR INJECTION (n=165) 13%
Placebo (n=123) 6%
NAUSEA
RELISTOR INJECTION (n=165) 12%
Placebo (n=123) 5%
DIZZINESS
RELISTOR INJECTION (n=165) 7%
Placebo (n=123) 2%
DIARRHEA
RELISTOR INJECTION (n=165) 6%
Placebo (n=123) 2%

§Adverse reactions occurring in at least 5% of patients receiving all doses of RELISTOR injection (0.075, 0.15, and 0.3 mg/kg) and at an incidence greater than placebo.1

||Includes abdominal pain, upper abdominal pain, lower abdominal pain, abdominal discomfort, and abdominal tenderness.1

.For additional Important Safety Information, please see the sidebar to the right

.For additional Important Safety Information, please see bottom of the page

Emergency Medicine

When working in the emergency department (ED)

The ED often sees patients with OIC. OIC occurs in 40% to 80% of all patients receiving an opioid medication for chronic pain.9-11

Oncology and Emergency Medicine

Not actual size.

RELISTOR injection is available in vials and pre-filled syringes1

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REFERENCES: 1. RELISTOR [prescribing information]. Bridgewater, NJ: Salix Pharmaceuticals. 2. Glare P, Walsh D, Sheehan D. The adverse effects of morphine: a prospective survey of common symptoms during repeated dosing for chronic cancer pain. Am J Hosp Palliat Care. 2006;23(3):229-235. 3. Amitiza. Prescribing information. Sucampo Pharma Americas, LLC; 2020. 4. Movantik. Prescribing information. RedHill Biopharma Inc; 2023. 5. Symproic. Prescribing information. Collegium Pharmaceutical, Inc; 2020. 6. Pergolizzi JV Jr, Christo PJ, LeQuang JA, Magnusson P. The use of peripheral μ-opioid receptor antagonists (PAMORA) in the management of opioid-induced constipation: an update on their efficacy and safety. Drug Des Devel Ther. 2020;14:1009-1025. 7. Slatkin N, Thomas J, Lipman AG, et al. Methylnaltrexone for treatment of opioid-induced constipation in advanced illness patients. J Support Oncol. 2009;7(1):39-46. 8. Thomas J, Karver S, Cooney GA, et al. Methylnaltrexone for opioid-induced constipation in advanced illness. N Engl J Med. 2008;358(22):2332-2343. 9. Bell TJ, Panchal SJ, Miaskowski C, Bolge SC, Milanova T, Williamson R. The prevalence, severity, and impact of opioid-induced bowel dysfunction: results of a US and European patient survey (PROBE 1). Pain Med. 2009;10(1):35-42. 10. Kalso E, Edwards JE, Moore AR, McQuay HJ. Opioids in chronic non-cancer pain: systematic review of efficacy and safety. Pain. 2004;112(3):372-380. 11. Hjalte F, Berggren AC, Bergendahl H, Hjortsberg C. The direct and indirect costs of opioid-induced constipation. J Pain Symptom Manage. 2010;40(5):696-703.