Methylnaltrexone bromide

Methylnaltrexone bromide is an opioid antagonist medication used to treat opioid-induced constipation. It is a peripherally-acting μ-opioid receptor antagonist, meaning that it binds to the μ-opioid receptor but does not activate it. This prevents the opioid from binding to the μ-opioid receptors in the gastrointestinal tract, thus reversing the opioid-induced constipation without affecting the opioid's effects on pain. It is typically used in patients with advanced illness who are taking opioids for pain relief, and can be used in both adults and children.

Methylnaltrexone bromide, also known by the brand name Relistor, is a medication specifically used to address opioid-induced constipation (OIC) in adults.

Here's a breakdown of its key points:

  • Function: It acts as a peripherally acting mu-opioid receptor antagonist. This means it primarily targets opioid receptors outside the central nervous system (CNS), particularly in the gut.
  • Mechanism of action: By blocking these receptors in the gut, Methylnaltrexone bromide weakens the constipating effects of opioids without affecting their pain-relieving properties in the brain.

Key points to remember:

  • Treated condition: OIC, a common side effect experienced by individuals taking opioid medications for pain management.
  • Administration: Available as a subcutaneous injection administered by a healthcare professional.
  • Not a pain reliever: It does not manage pain and should not be used as a substitute for prescribed pain medication.

Additional information:

  • FDA approved: Methylnaltrexone bromide was approved by the US Food and Drug Administration (FDA) in 2008.
  • Not for everyone: It may not be suitable for all individuals suffering from OIC, and consultation with a doctor is crucial before using this medication.
Anatomical Therapeutic Chemical Classification
A - Alimentary tract and metabolism
A06 Drugs for constipation
A06A - Drugs for constipation
A06AH Peripheral opioid receptor antagonists
External Links