relistor

Administration Instructions ( 2.1 ) • Be within close proximity to toilet facilities once administered. • Discontinue if treatment with 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 before starting RELISTOR; may resume laxatives if there is a suboptimal response to RELISTOR after 3 days. o Re-evaluate the continued need for RELISTOR when opioid regimen is changed to avoid adverse reactions. • 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. Dosing • For OIC in adult patients with chronic non-cancer pain ( 2.2 ): o RELISTOR tablets: The recommended dosage is 450 mg once daily in the morning. o RELISTOR injection: The recommended dosage is 12 mg subcutaneously once daily. • For OIC in adult patients with advanced illness ( 2.3 ): o 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. o RELISTOR injection: See Table 1 in the full prescribing information for the recommended dosage; administer one dose every other day, as needed, but no more frequently than one dose in a…

Serious and important adverse reactions described elsewhere in the labeling include: • Gastrointestinal perforation [see Warnings and Precautions ( 5.1 )] • Severe or persistent diarrhea [see Warnings and Precautions ( 5.2 )] • Opioid withdrawal [see Warnings and Precautions ( 5.3 )] The most common adverse reactions are: OIC in adult patients with chronic non-cancer pain ( 6.1 ) • RELISTOR tablets (≥ 2%): abdominal pain, diarrhea, headache, abdominal distention, vomiting, hyperhidrosis, anxiety, muscle spasms, rhinorrhea, and chills. • RELISTOR injection (≥ 1%): abdominal pain, nausea, diarrhea, hyperhidrosis, hot flush, tremor, and chills. OIC in adult patients with advanced illness ( 6.1 ) • RELISTOR injection (≥ 5%): abdominal pain, flatulence, nausea, dizziness, and diarrhea. 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. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Opioid-Induced Constipation in Adult Patients with Chronic Non-Cancer Pain The safety of RELISTOR tablets was evaluated in a double-blind, placebo-controlled trial in…

RELISTOR is contraindicated in patients with known or suspected gastrointestinal obstruction and patients at increased risk of recurrent obstruction, due to the potential for gastrointestinal perforation [see Warnings and Precautions ( 5.1 )] . Patients with known or suspected mechanical gastrointestinal obstruction and at increased risk of recurrent obstruction. ( 4 , 5.1 )

During clinical trials of RELISTOR administered orally and subcutaneously, one accidental case of methylnaltrexone bromide overdose was reported and no adverse events were reported as a result of the overdosage. A study of healthy subjects noted orthostatic hypotension associated with a dose of 0.64 mg/kg administered as an intravenous bolus. Monitor for signs or symptoms of orthostatic hypotension and initiate treatment as appropriate. If a patient on opioid therapy receives an overdose of RELISTOR, the patient should be monitored closely for potential evidence of opioid withdrawal symptoms such as chills, rhinorrhea, diaphoresis or reversal of central analgesic effect. Base treatment on the degree of opioid withdrawal symptoms, including changes in blood pressure and heart rate, and on the need for analgesia.

U.S. Poison Control: call or text 1-800-222-1222 (free, 24/7). In an emergency call 911. From the FDA label; not medical advice.

Other Opioid Antagonists : Potential for additive effect and increased risk of opioid withdrawal; avoid concomitant use. ( 7.1 ) 7.1 Other Opioid Antagonists 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. 7.2 Drugs Metabolized by Cytochrome P450 Isozymes In healthy subjects, a subcutaneous dose of 0.3 mg/kg of RELISTOR did not significantly affect the metabolism of dextromethorphan, a CYP2D6 substrate. 7.1 Other Opioid Antagonists 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. 7.2 Drugs Metabolized by Cytochrome P450 Isozymes In healthy subjects, a subcutaneous dose of 0.3 mg/kg of RELISTOR did not significantly affect the metabolism of dextromethorphan, a CYP2D6 substrate.