RELISTOR

Between the oral dosage range of 150 mg to 450 mg for RELISTOR tablets and the subcutaneous dosage range of 0.15 mg/kg to 0.50 mg/kg for RELISTOR injection, the mean C max and area under the plasma concentration-time curve (AUC) of methylnaltrexone increased in a dose-proportional manner. There was no significant accumulation of methylnaltrexone following once-daily oral dosing of 450 mg RELISTOR tablets or subcutaneous dosing of 12 mg RELISTOR injection for seven consecutive days in healthy sub...

14.1 Opioid-Induced Constipation in Adult Patients with Chronic Non-Cancer Pain RELISTOR Tablets The efficacy of RELISTOR tablets in the treatment of OIC in patients with chronic non-cancer pain was evaluated in a randomized, double-blind, placebo-controlled study (Study 1). This study compared 4-week treatment of RELISTOR tablets 450 mg orally once daily with placebo. A total of 401 patients (200 RELISTOR, 201 placebo) were enrolled and treated in the double-blind period. Patients had a history of chronic non-cancer pain for which they were taking opioids. The most common pain condition requi...

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...

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 )

Gastrointestinal Perforation : Consider the overall risk benefit in patients with known or suspected lesions of the GI tract. Monitor for severe, persistent or worsening abdominal pain; discontinue if development of symptoms. ( 5.1 ) Severe or Persistent Diarrhea : Discontinue if severe or persistent diarrhea occurs during treatment. ( 5.2 ) Opioid Withdrawal : Consider the overall risk benefit in patients with disruptions to the blood-brain barrier. Monitor closely for symptoms of opioid withdr...

7 DRUG INTERACTIONS 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 ...