RELISTOR Injection Dosing and Administration1

Learn more about the dosing and administration of RELISTOR injection.

Adult opioid-induced constipation (OIC) and chronic non-cancer pain

  • 12 mg subcutaneously once daily

Adult OIC and advanced illness

Weight of Adult Patient Subcutaneous Dose (every other day, as needed) Injection Volume
<38 kg 0.15 mg/kg See below*
38 kg to <62 kg 8 mg 0.4 mL
62 kg to 114 kg 12 mg 0.6 mL
>114 kg 0.15 mg/kg See below*

*The injection volume for these patients should be calculated using the following method: Multiply the patient weight in kilograms by 0.0075 and round up the volume to the nearest 0.1 mL.

When selecting an injection site, choose from the abdomen, thighs, or upper arms.

When selecting an injection site, choose from the abdomen, thighs, or upper arms. Rotate injection sites. Do not inject into areas where the skin is tender, bruised, red, or hard. Avoid areas with scars or stretch marks.

Dosing in moderate to severe renal impairment1

Adult OIC and chronic non-cancer pain

  • 6 mg subcutaneously once daily

Adult OIC and advanced illness with moderate to severe renal impairment

Weight of Adult Patient Subcutaneous Dose Injection Volume
<38 kg 0.075 mg/kg See below
38 kg to <62 kg 4 mg 0.2 mL
62 kg to 114 kg 6 mg 0.3 mL
>114 kg 0.075 mg/kg See below

The injection volume for these patients should be calculated using the following method: Multiply the patient weight in kilograms by 0.00375 and round up the volume to the nearest 0.1 mL.

Dosing in severe hepatic impairment1

Adult OIC and chronic non-cancer pain and severe hepatic impairment

Weight of Adult Patient Subcutaneous Dose Injection Volume
<38 kg 0.075 mg/kg See below
38 kg to <62 kg 4 mg 0.2 mL
62 kg to 114 kg 6 mg 0.3 mL
>114 kg 0.075 mg/kg See below

The injection volume for these patients should be calculated using the following method: Multiply the patient weight in kilograms by 0.00375 and round up the volume to the nearest 0.1 mL.

 

See full Prescribing Information for details on dosing and administration of RELISTOR.

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.