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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.

See Less

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.

When it comes to opioid-
induced constipation (OIC),
there’s no more time to wait

When it comes to opioid-induced constipation (OIC), there’s no more time to wait

  • OIC often persists throughout patients’ opioid therapy and is not typically dependent on dose or duration of opioid use2

How long is too long?

~80%

of people in a survey of 322 patients taking oral opioid therapy daily and over-the-counter (OTC) laxatives reported still being constipated1

  • OIC often persists throughout patients’ opioid therapy and is not typically dependent on dose or duration of opioid use2

Despite using OTC laxatives, some patients may still have fewer than 3 bowel movements per week and experience continued discomfort with OIC1,*

*Multinational internet-based survey designed to assess the prevalence, frequency, and severity of opioid-induced bowel dysfunction (OBD) symptoms, specifically constipation, in patients receiving opioid therapy for chronic pain who were taking laxatives; 322 patients taking daily oral opioids and laxatives completed the 45-item questionnaire.1

Patients with OIC often cycle through OTC options without adequate relief 3,4

Laxatives, including stimulants and osmotic laxatives, are typically used as initial treatments for OIC.5-7

Not intended to suggest a comparison of efficacy, safety, or comparability.

Studies have shown that, when combined with a healthy diet and exercise, CYCLOSET helped lower blood sugar levels after each meal throughout the day.

This may help achieve the goals you and your doctor want.

RELISTOR timingRELISTOR timing

Bridging the communication gap with your patients is crucial

In surveys of physicians and patients:

Patients are suffering in silence

In a survey of patients with non-cancer pain and OIC (n=493)3:

0%

of patients did not discuss their constipation-related symptoms with their HCPs3,†

Of those patients who did not discuss OIC:

0%

reported being concerned about having their pain medication changed3,†

HCPs may be unaware

In the physician component of the same survey8:

0%

of HCPs did not know that their patients were experiencing constipation8,†

0%

of HCPs did not know if their patients were on laxatives or not8,†

†Prospective longitudinal survey conducted in the United States, Canada, Germany, and United Kingdom to assess the burden of OIC in patients with non-cancer pain using a combination of patient surveys, retrospective data abstraction from medical records, and physician surveys.3,8 In a study of 493 patient survey participants, baseline patient-reported outcomes were evaluated.3 In a study of 489 patient survey participants, evaluations of physician-completed surveys were conducted.8

It is important for HCPs to initiate discussions about OIC during clinical visits and assess patients’ experiences8
Download Resources
Take a proactive approach to OIC by starting the conversation with your patients
OIC is different from other forms of constipation2,9,10

OIC is caused by opioids binding to mu-opioid receptors in the gastrointestinal (GI) tract, which can slow GI motility2,11

3

effects that can contribute to OIC include

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DECREASED PERISTALTIC MOTION12,13

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INCREASED FLUID ABSORPTION FROM THE GUT12,13

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DECREASED FLUID SECRETION INTO THE GUT12,13

3

effects that can contribute to OIC include

DECREASED
PERISTALTIC MOTION12,13

INCREASED FLUID ABSORPTION FROM THE GUT12,13

DECREASED FLUID SECRETION INTO THE GUT12,13

You have the power to intervene early and address the underlying cause of OIC
RELISTOR timing RELISTOR timing
DISCOVER RELISTOR TABLETS

REFERENCES: 1. 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. 2. Pergolizzi JV Jr, Raffa RB, Pappagallo M, et al. Peripherally acting μ-opioid receptor antagonists as treatment options for constipation in noncancer pain patients on chronic opioid therapy. Patient Prefer Adherence. 2017;11:107-119. 3. Coyne KS, LoCasale RJ, Datto CJ, Sexton CC, Yeomans K, Tack J. Opioid-induced constipation in patients with chronic noncancer pain in the USA, Canada, Germany, and the UK: descriptive analysis of baseline patient-reported outcomes and retrospective chart review. Clinicoecon Outcomes Res. 2014;6:269-281. 4. Emmanuel A, Johnson M, McSkimming P, Dickerson S. Laxatives do not improve symptoms of opioid-induced constipation: results of a patient survey. Pain Med. 2017;18(10):1932-1940. 5. Crockett SD, Greer KB, Heidelbaugh JJ, Falck-Ytter Y, Hanson BJ, Sultan S; American Gastroenterological Association Institute Clinical Guidelines Committee. American Gastroenterological Association Institute guideline on the medical management of opioid-induced constipation. Gastroenterology. 2019;156(1):218-226. 6. Zhao Q, Chen YY, Xu DQ, et al. Action mode of gut motility, fluid and electrolyte transport in chronic constipation. Front Pharmacol. 2021;12:1-15. 7. Brock C, Olesen SS, Olesen AE, et al. Opioid-induced bowel dysfunction: pathophysiology and management. Drugs. 2012;72(14):1847-1865. 8. LoCasale RJ, Datto C, Margolis MK, Coyne KS. Satisfaction with therapy among patients with chronic noncancer pain with opioid-induced constipation. J Manag Care Spec Pharm. 2016;22(3):246-253. 9. Pappagallo M. Incidence, prevalence, and management of opioid bowel dysfunction. Am J Surg. 2001;182(5)(suppl):11S-18S. 10. Cook SF, Lanza L, Zhou X, et al. Gastrointestinal side effects in chronic opioid users: results from a population-based survey. Aliment Pharmacol Ther. 2008;27(12):1224-1232. 11. Galligan JJ, Sternini C. Insights into the role of opioid receptors in the GI tract: experimental evidence and therapeutic relevance. Handb Exp Pharmacol. 2017;239:363-378. 12. Streicher JM, Bilsky EJ. Peripherally acting μ-opioid receptor antagonists for the treatment of opioid-related side effects: mechanism of action and clinical implications. J Pharm Pract. 2018;31(6):658-669. 13. Bader S, Jaroslawski K, Blum HE, Becker G. Opioid-induced constipation in advanced illness: safety and efficacy of methylnaltrexone bromide. Clin Med Insights Oncol. 2011;5:201-211.