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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.

Convenient once-daily RELISTOR dosing1

RELISTOR is available as an oral tablet for adult patients with opioid-induced constipation (OIC) with chronic non-cancer pain (CNCP), including patients with chronic pain related to prior cancer or its treatment who do not require frequent (eg, weekly) opioid dosage escalation.1

RELISTOR tablets

Convenient once-daily RELISTOR dosing1

RELISTOR is available as an oral tablet for adult patients with opioid-induced constipation (OIC) with chronic non-cancer pain (CNCP), including patients with chronic pain related to prior cancer or its treatment who do not require frequent (eg, weekly) opioid dosage escalation.1

double-blue-arrows

RELISTOR helps restore gut function and can increase the number of spontaneous bowel movements (SBMs)1,2

double-blue-arrows double-blue-arrows

RELISTOR helps restore gut function and can increase the number of spontaneous bowel movements (SBMs)1,2

Secondary endpoint, responder analysis: Significantly more patients taking RELISTOR experienced at least 3 SBMs per week1,2,*

0%

RELISTOR tablets 450 mg† (n=200)

0%

Placebo (n=201)

SIGNIFICANT
DIFFERENCE
P=.0052

Percentage of patients

0%
0%

RELISTOR
tablets
450 mg†
(n=200)

Placebo
(n=201)

SIGNIFICANT
DIFFERENCE
P=.00522

Percentage of patients

STUDY DESIGN

In a phase 3, randomized, multicenter, double-blind trial in patients with CNCP (for which they were taking opioids) and OIC, 4 weeks of daily oral RELISTOR (150, 300, or 450 mg) was compared with placebo.1,2,†,‡

*Responder is defined as a patient with 3 or more SBMs per week, with an increase of 1 or more SBMs per week over baseline, for 3 or more out of the first 4 weeks of the treatment period. All patients had OIC, defined as less than 3 SBMs per week and at least 1 additional symptom of constipation.1,2

†Three RELISTOR 150-mg tablets (450 mg total) once daily in the morning with water on an empty stomach at least 30 minutes before the first meal of the day.1

‡SBM is defined as a bowel movement without the use of any laxative in the previous 24 hours.1

*Responder is defined as a patient with 3 or more SBMs per week, with an increase of 1 or more SBMs per week over baseline, for 3 or more out of the first 4 weeks of the treatment period. All patients had OIC, defined as less than 3 SBMs per week and at least 1 additional symptom of constipation.1,2

†Three RELISTOR 150-mg tablets (450 mg total) once daily in the morning with water on an empty stomach at least 30 minutes before the first meal of the day.1

‡SBM is defined as a bowel movement without the use of any laxative in the previous 24 hours.1

Primary endpoint results:

More patients met the primary endpoint of mean percentage of dosing days that resulted in an RFBM within

4

hours
with RELISTOR

during weeks 1 to 42,§

%

of dosing days in the RELISTOR 450 mg/day treatment group (n=200)2

VS

%

of dosing days in the placebo group (n=201)2

Percentages indicative of the number of patients who met the primary endpoint (P<.0001)2

RFBM, rescue-free bowel movement.

§The primary endpoint was the mean percentage of dosing days resulting in a SBM within 4 hours of dosing during the 4-week, double-blind period compared with placebo.2

Additional finding (non-primary or secondary endpoint)

  • 24% of patients experienced a SBM within 4 hours of the first dose of RELISTOR (450 mg/day) oral tablets vs placebo (8%)2
  • SBM within 4 hours of the first dose was an exploratory endpoint. No conclusions about efficacy can be drawn from these descriptive data because they are results from exploratory endpoints2

Convenient once-daily oral therapy1

  • Three (3) 150-mg tablets (450 mg total)
  • RELISTOR therapy should be continued only during opioid use1
Three RELISTOR® (methylnaltrexone bromide) tablets

Not actual size.

ADMINISTRATION:

  • RELISTOR tablets should be taken with water on an empty stomach ≥30 minutes before the first meal of the day1
  • Discontinue all maintenance laxative therapy prior to initiation of RELISTOR. Laxative(s) can be used as needed if there is a suboptimal response to RELISTOR after 3 days1
  • Reevaluate the continued need for RELISTOR when the opioid regimen is changed to avoid adverse reactions1

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RELISTOR subcutaneous injection provides OIC treatment for patients with advanced illness or pain caused by active cancer who require opioid dosage escalation for palliative care1

RELISTOR tablets have a well-established safety profile1

Most common adverse reactions

In the 4-week, double-blind, placebo-controlled period of the clinical study in patients with OIC and CNCP (n=401) (Study 1)1

ADVERSE REACTIONS|| RELISTOR TABLETS
(n=200)		 PLACEBO
(n=201)
ABDOMINAL PAIN 14% 10%
DIARRHEA 5% 2%
HEADACHE 4% 3%
ABDOMINAL DISTENTION 4% 2%
VOMITING 3% 2%
HYPERHIDROSIS 3% 1%
ANXIETY 2% 1%
MUSCLE SPASMS 2% 1%
RHINORRHEA 2% 1%
CHILLS 2% 0%
ADVERSE REACTIONS||
ABDOMINAL PAIN
RELISTOR TABLETS
(n=200)		 14%
Placebo (n=201) 10%
DIARRHEA
RELISTOR TABLETS
(n=200)		 5%
Placebo (n=201) 2%
HEADACHE
RELISTOR TABLETS
(n=200)		 4%
Placebo (n=201) 3%
ABDOMINAL DISTENTION
RELISTOR TABLETS
(n=200)		 4%
Placebo (n=201) 2%
VOMITING
RELISTOR TABLETS
(n=200)		 3%
Placebo (n=201) 2%
HYPERHIDROSIS
RELISTOR TABLETS
(n=200)		 3%
Placebo (n=201) 1%
ANXIETY
RELISTOR TABLETS
(n=200)		 2%
Placebo (n=201) 1%
MUSCLE SPASMS
RELISTOR TABLETS
(n=200)		 2%
Placebo (n=201) 1%
RHINORRHEA
RELISTOR TABLETS
(n=200)		 2%
Placebo (n=201) 1%
CHILLS
RELISTOR TABLETS
(n=200)		 2%
Placebo (n=201)) 0%

||Adverse reactions occurring in at least 2% of patients receiving 3 RELISTOR 150-mg tablets (450 mg total) once daily and at an incidence greater than placebo.1

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

  • Adverse reactions of abdominal pain, diarrhea, hyperhidrosis, anxiety, rhinorrhea, and chills may reflect symptoms of opioid withdrawal1
  • For additional Important Safety Information, please see the sidebar to the right
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REFERENCES: 1. RELISTOR [prescribing information]. Bridgewater, NJ: Salix Pharmaceuticals. 2. Rauck R, Slatkin NE, Stambler N, et al. Randomized, double-blind trial of oral methylnaltrexone for the treatment of opioid-induced constipation in patients with chronic noncancer pain. Pain Pract. 2017;17(6):820-828.