RELISTOR Patient Counseling1

Administration

  • Advise patients taking RELISTOR to:
    • Be within close proximity to toilet facilities once RELISTOR is administered.
    • Discontinue RELISTOR if treatment with the opioid pain medication is also discontinued.
  • Advise chronic non-cancer pain patients receiving RELISTOR for OIC to:
    • 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 three days.
    • Inform their healthcare provider if their opioid regimen is changed, to avoid adverse reactions, such as diarrhea.

Tablets

  • Advise patients with chronic non-cancer pain receiving RELISTOR tablets for OIC to take RELISTOR tablets once daily with water on an empty stomach at least 30 minutes before the first meal of the day.

Injection

  • Advise all patients receiving RELISTOR injection to:
    • Inject RELISTOR subcutaneously in the upper arm, abdomen or thigh. Do not inject at the same spot each time (rotate injection sites).
    • Safely dispose of needles by following the sharps disposal recommendations described in the Instructions for Use.
  • Advise chronic non-cancer pain patients receiving RELISTOR injection for OIC to inject one dose every day.
  • Advise patients with advanced illness receiving RELISTOR injection for OIC to inject one dose every other day, as needed, but no more frequently than one dose in a 24-hour period.

Gastrointestinal Perforation

Advise patients to discontinue RELISTOR and to promptly seek medical attention if they develop unusually severe, persistent, or worsening abdominal pain.

Severe or Persistent Diarrhea

Advise patients to discontinue RELISTOR if they experience severe or persistent diarrhea.

Opioid Withdrawal

Advise patients that symptoms consistent with opioid withdrawal may occur while taking RELISTOR, including sweating, chills, diarrhea, abdominal pain, anxiety, and yawning.

Pregnancy

Fetal Opioid Withdrawal

Advise females of reproductive potential, who become pregnant or are planning to become pregnant, that the use of RELISTOR during pregnancy may precipitate opioid withdrawal in a fetus due to the undeveloped blood brain barrier.

Lactation

Advise patients that breastfeeding is not recommended during treatment with RELISTOR.

Information for Adult OIC Patients1

Below is information for patients. It is also provided in the RELISTOR Medication Guide.


What is the most important information I should know about RELISTOR?

RELISTOR can cause serious side effects, including:

  • Tear in your stomach or intestinal wall (perforation). Stomach pain that is severe can be a sign of a serious medical condition. If you get stomach pain that is severe, does not go away, or gets worse, stop taking RELISTOR and get emergency medical help right away.
  • Diarrhea that is severe or that will not go away. Stop taking RELISTOR and call your healthcare provider if you get diarrhea that is severe or that does not go away during treatment with RELISTOR.
  • Opioid withdrawal.You may have symptoms of opioid withdrawal during treatment with RELISTOR including sweating, chills, diarrhea, stomach pain, anxiety, and yawning. Tell your healthcare provider if you have any of these symptoms.
What is RELISTOR?

RELISTOR is a prescription medicine used to treat constipation in adults that is caused by prescription pain medicines called opioids:

  • RELISTOR tablets and RELISTOR injection are used to treat constipation caused by opioids in adults with long-lasting (chronic) pain that is not caused by cancer.
  • RELISTOR injection is used to treat constipation caused by opioids in adults who are receiving treatment for advanced illness, when other medicines for constipation have not worked well enough.

It is not known if RELISTOR is safe and effective if used for longer than 4 months in people with advanced illness.

It is not known if RELISTOR is safe and effective in children.

Who should not use RELISTOR?

Do not use RELISTOR if you have a bowel blockage (intestinal obstruction) or have a history of bowel blockage.

What should I tell my healthcare provider before taking RELISTOR?

Before you start taking RELISTOR, tell your healthcare provider about all of your medical conditions, including if you:

  • have kidney problems.
  • have liver problems.
  • have any stomach or bowel (intestines) problems, including stomach ulcer, Crohn’s disease, diverticulitis, cancer of the stomach or bowel, or Ogilvie’s syndrome.
  • are pregnant or plan to become pregnant. Taking RELISTOR during pregnancy may cause opioid withdrawal symptoms in your unborn baby. Tell your healthcare provider right away if you become pregnant during treatment with RELISTOR.
  • are breastfeeding or plan to breastfeed. It is not known if RELISTOR passes into your breast milk. Taking RELISTOR while you are breastfeeding may cause opioid withdrawal in your baby. You should not breastfeed during treatment with RELISTOR.

Tell your healthcare provider about all of the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

How should I take RELISTOR?
  • Stay close to a toilet after taking RELISTOR.
  • Stop taking RELISTOR if you stop taking your prescription opioid pain medicine. Tell your healthcare provider if your pain medicine changes.
  • If you take too much RELISTOR, call your healthcare provider or go to the nearest emergency room right away.
  • If you take RELISTOR for long-lasting (chronic) pain that is not caused by cancer:
    • RELISTOR has been shown to be effective in people who have taken opioid pain medicines for at least 4 weeks to treat long-lasting (chronic) pain not caused by cancer.
    • Stop taking other laxatives before you start treatment with RELISTOR. You may use other laxatives if RELISTOR does not work after 3 days of treatment.

Tablets:

  • Take RELISTOR tablets 1 time each day with water. Take RELISTOR tablets on an empty stomach at least 30 minutes before your first meal of the day.

Injection (Vials and Pre-filled Syringes):

See the detailed “Instructions for Use” that comes with RELISTOR injection for information about how to prepare and inject RELISTOR injection, and properly throw away (dispose of) used needles and syringes the right way.

  • RELISTOR injection is injected under the skin (subcutaneous injection) of the upper arm, stomach-area (abdomen), or thigh.
  • Inject RELISTOR injection exactly as your healthcare provider tells you.
  • If you use RELISTOR injection for long-lasting (chronic) pain that is not caused by cancer:
    • Inject 1 dose of RELISTOR injection each day.
  • If you use RELISTOR injection and are receiving treatment for advanced illness:
    • Inject 1 dose of RELISTOR injection every other day, as needed. You should not inject more than 1 dose of RELISTOR injection in a 24-hour period.
What are the possible side effects of RELISTOR?

See "What is the most important information I should know about RELISTOR?"

  • The most common side effects of RELISTOR tablets in people with long-lasting (chronic) pain that is not caused by cancer include: stomach-area (abdomen) pain, diarrhea, headache, swelling or a feeling of fullness or pressure in your abdomen, sweating, anxiety, muscle spasms, runny nose, and chills.
  • The most common side effects of RELISTOR injection in people with long-lasting (chronic) pain that is not caused by cancer include: stomach-area (abdomen) pain, nausea, diarrhea, sweating, hot flush, tremor, and chills.
  • The most common side effects of RELISTOR injection in people receiving treatment for their advanced illness include: stomach-area (abdomen) pain, gas, nausea, dizziness, and diarrhea.

Tell your healthcare provider if you have any side effect that bothers you or that does not go away. These are not all of the possible side effects of RELISTOR.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

You may also report side effects to Valeant Pharmaceuticals North America LLC at 1-800-321-4576.

How should I store RELISTOR?

RELISTOR tablets:

  • Store RELISTOR tablets at room temperature between 68°F to 77°F (20°C to 25°C).
  • The bottle of RELISTOR tablets contains 2 desiccant canisters to help keep your medicine dry. Do not remove the desiccant canisters from the bottle.

RELISTOR injection (Vials and Pre-filled Syringes):

  • Store RELISTOR vials and pre-filled syringes at room temperature between 68°F to 77°F (20°C to 25°C).
  • Do not freeze RELISTOR vials or pre-filled syringes.
  • Keep RELISTOR vials and pre-filled syringes away from light until you are ready to use them.
  • If the contents of a RELISTOR vial have been drawn into a syringe and you are not able to use the medicine right away, keep the syringe at room temperature for up to 24 hours.

Keep RELISTOR and all medicines, needles and syringes out of the reach of children.

General information about the safe and effective use of RELISTOR

Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use RELISTOR for a condition for which it was not prescribed. Do not give RELISTOR to other people, even if they have the same symptoms that you have. It may harm them. You can ask your pharmacist or healthcare provider for information about RELISTOR that is written for health professionals.

What are the ingredients in RELISTOR tablets and RELISTOR injection?

Active ingredient: methylnaltrexone bromide

Inactive ingredients (tablets): silicified microcrystalline cellulose, microcrystalline cellulose, sodium lauryl sulfate, croscarmellose sodium, crospovidone, poloxamer 407, stearic acid (vegetable source), colloidal silicon dioxide, edetate calcium disodium, polyvinyl alcohol, titanium dioxide, polyethylene glycol and talc

Inactive ingredients (injection: vials and pre-filled syringes): sodium chloride USP, edetate disodium USP, glycine hydrochloride. During manufacture, the pH may have been adjusted with hydrochloric acid and/or sodium hydroxide.

Indications

  • 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.
  • RELISTOR injection is also indicated for the treatment of OIC in adults with advanced illness who are receiving palliative care, when response to laxative therapy has not been sufficient. Limitations of Use: Use beyond four months has not been studied in the advanced illness population.

IMPORTANT SAFETY INFORMATION - RELISTOR tablets and RELISTOR injection

  • RELISTOR tablets and injection are contraindicated in patients with known or suspected 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.
  • 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 at 1-800-508-0024 or FDA at 1-800-FDA-1088 or www.fda.gov/Safety/MedWatch/

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

REFERENCE:

  1. RELISTOR (methylnaltrexone bromide) Prescribing Information. Bridgewater, NJ: Salix Pharmaceuticals.