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Constipation and bowel cleansers
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Generic Name and Formulations:

Methylnaltrexone bromide 150mg; tabs.

Select therapeutic use:

Indications for RELISTOR:

Opioid-induced constipation (OIC) in adults with chronic non-cancer pain, including chronic pain related to prior cancer or its treatment in patients who do not require frequent opioid dosage escalation.


Discontinue all maintenance laxatives prior to initiation; may be used if suboptimal methylnaltrexone response after 3 days. Reevaluate if opioid regimen is changed. Take on an empty stomach with water ≥30mins before first meal of day. 450mg once daily in the AM. Moderate or severe renal (CrCl<60mL/min) or hepatic (Child-Pugh B or C) impairment: 150mg once daily.


Not established.


Known or suspected GI obstruction and at increased risk of recurrent obstruction.


Discontinue if concurrent opioid pain medication is also discontinued. GI perforation; monitor for severe, persistent, or worsening abdominal pain; discontinue if occurs. Discontinue if severe or persistent diarrhea occurs. Increased risk of opioid withdrawal and/or reduced analgesia in those with blood-brain barrier disruptions; monitor for symptoms. Bowel movement may occur within 30 mins of dosing. Elderly. Pregnancy. Nursing mothers: not recommended.


Potential additive effects and increased risk of opioid withdrawal with concomitant other opioid antagonists; avoid.

See Also:


Pharmacological Class:

Opioid antagonist (peripheral).

Adverse Reactions:

Abdominal pain, flatulence, nausea, dizziness, diarrhea, headache, abdominal distention, vomiting, hyperhidrosis, anxiety, muscle spasms, rhinorrhea, chills, tremor, hot flush; GI perforation, opioid withdrawal.

Generic Availability:


How Supplied:

Tabs—60, 90; Single-use vial (12mg/0.6mL)—1; Prefilled syringes (8mg/0.4mL)—7; Prefilled syringes (12mg/0.6mL)—1, 7

RELISTOR 0.6ml of 12mg/0.6ml syringes (Qty:28)

appx. price $3122.00