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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.

When speed is clinically useful1

RELISTOR is also available as a subcutaneous injection for adult patients with opioid-induced constipation (OIC) and chronic non-cancer pain (CNCP) and advanced illness or pain caused by active cancer who require opioid dosage escalation for palliative care.1

RELISTOR subcutaneous injection

When speed is clinically useful1

RELISTOR is also available as a subcutaneous injection for adult patients with opioid-induced constipation (OIC) and chronic non-cancer pain (CNCP) and advanced illness or pain caused by active cancer who require opioid dosage escalation for palliative care.1

Efficacy: RELISTOR subcutaneous injection

Significant increases in weekly spontaneous bowel movements (SBMs) in adults with OIC and CNCP1

0%

RELISTOR 12 mg subcutaneous once daily (n=150)

0%

Placebo (n=162)

P<0.001

Percentage of responders during the double-blind treatment period (defined as a patient with 3 or more SBMs per week for each of the 4 weeks in the double-blind period)1,*,†,‡

0%
0%

RELISTOR
12 mg
subcutaneous
once daily
(n=150)

Placebo
(n=162)

P<0.001

Percentage of responders during the double-blind treatment period (defined as a patient with 3 or more SBMs per week for each of the 4 weeks

in the double-blind period)1,*,†,‡

Percentage of responders during the double-blind treatment period (defined as a patient with 3 or more SBMs per week for each of the 4 weeks in the double-blind period)1,*,†,‡

STUDY DESIGN: IN ADULT PATIENTS WITH OIC AND CNCP

Study 2 was a 4-week, multicenter, double-blind, randomized, placebo-controlled, phase 3 study. The efficacy of RELISTOR injection was evaluated in 312 patients with CNCP for which they were taking opioids. All patients had OIC, defined as less than 3 spontaneous bowel movements (SBMs) per week and at least one additional symptom of constipation.1

*Data from the modified intent-to-treat (mITT) population (all randomized patients who received ≥1 dose of double-blind study medication) are shown.1

A responder was defined as a patient with 3 or more SBMs per week for each of the 4 weeks in the double-blind period.1

A SBM was defined as a bowel movement that occurred without laxative use during the previous 24 hours.1

When speed is clinically useful in adults with OIC and CNCP1,2

Following the first dose, more patients experienced a SBM§ within

4

hours
with RELISTOR

subcutaneous injection1,2

compared with placebo

%

of patients receiving RELISTOR 12 mg subcutaneous injection once daily (n=150)1,2

VS

%

of patients in the placebo group (n=162)1,2

Percentages indicative of the number of patients who met the primary endpoint (P<.001)1,2

Percentages indicative of the number of patients who met the primary

endpoint (P<.001)1,2

§SBM defined as occurring without laxative use during the previous 24 hours.1

Learn about RELISTOR subcutaneous injection in oncology and emergency medicine

Once-daily dosing options for patients with CNCP1

  • Administer 12 mg subcutaneously once daily||
  • Dose reduction to 6 mg once daily is recommended in patients with moderate to severe renal impairment
  • Dose reduction is recommended in patients with severe hepatic impairment
  • 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 days

ADMINISTRATION: IN ADULT PATIENTS WITH CNCP

  • Should be administered subcutaneously in patients’ abdomen, thigh, or upper arm1
  • Should not be injected at the exact same spot each time (rotate injection sites)1
  • Please see Instructions For Use in the full Prescribing Information

||The pre-filled syringe is only for patients who require a RELISTOR subcutaneous injection dose of 8 mg or 12 mg. Do not use the pre-filled syringe and attached needle more than 1 time, even if there is medicine left in the syringe. Use the vial for patients who require other doses of RELISTOR subcutaneous injection. Do not use a RELISTOR vial more than 1 time, even if there is medicine left in the vial.1

Refer to the Prescribing Information for more information on weight-based dosing in patients with severe hepatic impairment and CNCP, advanced illness, and dosing in patients with renal impairment and advanced illness.1

RELISTOR syringe and bottle

Not actual size.

ADMINISTRATION: IN ADULT PATIENTS WITH CNCP

  • Should be administered subcutaneously in patients’ abdomen, thigh, or upper arm1
  • Should not be injected at the exact same spot each time (rotate injection sites)1
  • Please see Instructions For Use in the full Prescribing Information
RELISTOR injection for patients with advanced illness or pain caused by active cancer who require opioid dosage escalation for palliative care1

RELISTOR subcutaneous injection: Most common adverse reactions

Adverse reactions occurring in ≥1% of patients at an incidence greater than placebo1

4-week, double-blind, placebo-controlled clinical study in adults with OIC and CNCP
ADVERSE REACTIONS# RELISTOR INJECTION
12 MG (n=150)
PLACEBO
(n=162)
ABDOMINAL PAIN** 21% 7%
NAUSEA 9% 6%
DIARRHEA 6% 4%
HYPERHIDROSIS 6% 1%
HOT FLUSH 3% 2%
TREMOR 1% <1%
CHILLS 1% 0%
ADVERSE REACTIONS#
ABDOMINAL PAIN**
RELISTOR INJECTION
12 MG (n=150)
21%
Placebo (n=162) 7%
NAUSEA
RELISTOR INJECTION
12 MG (n=150)
9%
Placebo (n=162) 6%
DIARRHEA
RELISTOR INJECTION
12 MG (n=150)
6%
Placebo (n=162) 4%
HYPERHIDROSIS
RELISTOR INJECTION
12 MG (n=150)
6%
Placebo (n=162) 1%
HOT FLUSH
RELISTOR INJECTION
12 MG (n=150)
3%
Placebo (n=162) 2%
TREMOR
RELISTOR INJECTION
12 MG (n=150)
1%
Placebo (n=162) <1%
CHILLS
RELISTOR INJECTION
12 MG (n=150)
1%
Placebo (n=162) 0%

#Adverse reactions occurring in at least 1% of patients receiving RELISTOR injection 12 mg subcutaneously 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

  • For additional Important Safety Information, please see the sidebar to the right
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    Information, please see bottom of page
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REFERENCES: 1. RELISTOR [prescribing information]. Bridgewater, NJ: Salix Pharmaceuticals. 2. Michna E, Blonsky ER, Schulman S, et al. Subcutaneous methylnaltrexone for treatment of opioid-induced constipation in patients with chronic, nonmalignant pain: a randomized controlled study. J Pain. 2011;12(5):554-562.