Relistor (methylnaltrexone bromide; Valeant and Progenics) Tablets are now available for the treatment of opioid-induced constipation (OIC) in adults with chronic non-cancer pain. The tablets are available in a 150mg dosage strength.
Methylnaltrexone is a selective antagonist of opioid binding at the mu-opioid receptor. The ability of methylnaltrexone to cross the blood-brain barrier is restricted. This allows it 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.
In addition to the oral formulation, Relistor is also available as a subcutaneous injection in 8mg/0.4mL and 12mg/0.6mg strength solutions. The subcutaneous formulation is indicated for treating OIC in patients with advanced illness and chronic non-cancer pain.
The efficacy of oral methylnaltrexone was similar to that observed in clinical studies of subcutaneous methylnaltrexone in patients with chronic, non-cancer pain. The overall safety profile was also comparable to placebo in patients treated with oral methylnaltrexone.
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