Initial U.S. Approval: 2008 [New tablet formulation - 7/2016]
Mechanism of Action:
INDICATIONS AND USAGE:
•Limitations of Use: Use beyond four months has not been studied in the advanced illness population.
DOSAGE AND ADMINISTRATION:
•RELISTOR has been shown to be efficacious in patients who have taken opioids for at least 4 weeks.
•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.
For OIC in adult patients with advanced illness ( 2.3):
Preparation and Administration of RELISTOR Injection (2.6)
| RELISTOR (methylnaltrexone bromide) Subcutaneous Injection
Initial U.S. Approval: 2008
RELISTOR (methylnaltrexone bromide) Subcutaneous Injection, a peripherally-acting mu-opioid receptor antagonist, is a sterile, clear and colorless to pale yellow aqueous solution. The chemical name for methylnaltrexone bromide is (R)-N-(cyclopropylmethyl) noroxymorphone methobromide. The molecular formula is C21H26NO4Br, and the molecular weight is 436.36.
Each 3 mL vial contains 12 mg of methylnaltrexone bromide in 0.6 mL of water. The excipients are 3.9 mg sodium chloride USP, 0.24 mg edetate calcium disodium USP, and 0.18 mg glycine hydrochloride. During manufacture, the pH may have been adjusted with hydrochloric acid and/or sodium hydroxide.
Each 8 mg/0.4 mL pre-filled syringe (1 mL syringe) contains 8 mg of methylnaltrexone bromide in 0.4 mL of water. The excipients are 2.6 mg sodium chloride USP, 0.16 mg edetate calcium disodium USP, and 0.12 mg glycine hydrochloride.
Each 12 mg/0.6 mL pre-filled syringe (1 mL syringe) contains 12 mg of methylnaltrexone bromide in 0.6 mL of water. The excipients are 3.9 mg sodium chloride USP, 0.24 mg edetate calcium disodium USP, and 0.18 mg glycine hydrochloride.
| CLINICAL PHARMACOLOGY
Mechanism of Action
Methylnaltrexone bromide is a selective antagonist of opioid binding at the mu-opioid receptor. As a quaternary amine, the ability of methylnaltrexone bromide to cross the blood-brain barrier is restricted. This allows methylnaltrexone bromide to function as a peripherally-acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids without impacting opioid-mediated analgesic effects on the central nervous system.
| INDICATIONS AND USAGE
RELISTOR® is indicated for the treatment of opioid-induced constipation in patients with advanced illness who are receiving palliative care, when response to laxative therapy has not been sufficient. Use of RELISTOR beyond four months has not been studied.
RELISTOR is contraindicated in patients with known or suspected mechanical gastrointestinal obstruction.
| WARNINGS AND PRECAUTIONS
| ADVERSE REACTIONS
The most common (> 5%) adverse reactions reported with RELISTOR are abdominal pain, flatulence, nausea, dizziness, diarrhea and hyperhidrosis.
| DOSAGE AND ADMINISTRATION
General Dosing Information
FOR SUBCUTANEOUS INJECTION ONLY
RELISTOR should be injected in the upper arm, abdomen or thigh.
The recommended dose of RELISTOR is 8 mg for patients weighing 38 to less than 62 kg (84 to less than 136 lb) or 12 mg for patients weighing 62 to 114 kg (136 to 251 lb). Patients whose weight falls outside of these ranges should be dosed at 0.15 mg/kg. See the table below to determine the correct injection volume. The pre-filled syringe is designed to deliver a fixed dose; therefore, patients requiring dosing calculated on a mg/kg basis should not be prescribed pre-filled syringes.
Use in Patients with Severe Renal Impairment
The pre-filled syringe is designed to deliver a fixed dose; therefore, patients with severe renal impairment should not be prescribed pre-filled syringes unless their body weight calculated dose is 8 mg or 12 mg.
Preparation for Injection
Preparation of RELISTOR Using the Single-use Vial
Preparation of RELISTOR Using the Single-use Pre-filled Syringe
| DOSAGE FORMS AND STRENGTHS
RELISTOR is available in the following dosage forms and strengths. Only patients requiring an 8 mg or 12 mg dose should be prescribed pre-filled syringes.
Single-use vial containing 12 mg/0.6 mL solution for subcutaneous injection.
Single-use pre-filled syringe containing 8 mg/0.4 mL solution for subcutaneous injection, with a 29-gauge x half-inch fixed needle and a needle guard.
Single-use pre-filled syringe containing 12 mg/0.6 mL solution for subcutaneous injection, with a 29-gauge x half-inch fixed needle and a needle guard.
| Package Insert data:
Salix Pharmaceuticals, Inc.
Raleigh, NC 27615
Under license from:
PACKAGE LABEL - PRINCIPAL DISPLAY PANEL - 12 mg/0.6 mL - VIAL
Sterile Single Use Vial
National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
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