Methylnaltrexone

What it is used for

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, 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 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. Opioid-Induced Constipation in Adult Patients with Chronic Non-Cancer Pain RELISTOR tablets and RELISTOR injection are indicated for the treatment of opioid-induced constipation (OIC) in adult patients 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.

Opioid-Induced Constipation in Adult Patients with Advanced Illness RELISTOR injection is indicated for the treatment of OIC in adult patients with advanced illness or pain caused by active cancer who require opioid dosage escalation for palliative care.

2.1 Important Administration Information

• Be within close proximity to toilet facilities once RELISTOR is administered.
• Discontinue RELISTOR if treatment with the opioid pain medication is also discontinued.
• In adult patients with chronic non-cancer pain and OIC:
  • o Patients receiving opioids for less than 4 weeks may be less responsive to RELISTOR.
  • o 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.
  • o Re-evaluate the continued need for RELISTOR when the opioid regimen is changed to avoid adverse reactions.
  • o In patients with chronic non-cancer pain and OIC, take RELISTOR tablets with water on an empty stomach at least 30 minutes before the first meal of the day.

2.3 Opioid-Induced Constipation in Adult Patients with Advanced Illness

The pre-filled syringe is only for patients who require a RELISTOR injection dose of 8 mg or 12 mg. Use the vial for patients who require other doses of RELISTOR injection.

Table 1 below shows the recommended weight-based dose of RELISTOR injection and the corresponding injection volume. The recommended dosage regimen is one dose administered subcutaneously every other day, as needed. Do not administer more frequently than one dose per 24-hour period.

2.4 Dosage in Patients with Renal Impairment

The recommended dosage of RELISTOR in patients with moderate and severe renal impairment (i.e., creatinine clearance less than 60 mL/minute as estimated by Cockcroft-Gault), is shown below by indication:

OIC in Adult Patients with Chronic Non - Cancer Pain

• RELISTOR tablets: 150 mg once daily in the morning.
• RELISTOR injection: 6 mg administered subcutaneously once daily

OIC in Adult Patients with Advanced Illness

RELISTOR injection: The recommended dosage regimen is one dose every other day, as needed is shown in Table 2.

*Calculate the injection volume for these patients by multiplying the patient weight in kilograms by 0.00375 and then rounding up the volume to the nearest 0.1 mL.