Alvimopan, Entereg

  • Indications
  1. Promotion of upper and lower gastrointestinal recovery following partial bowel resection with primary anastomosis
    1. Approved only for short-term management (15 doses) of post-operative ileus
    2. Only hospitals FDA approved may dispense Alvimopan
  • Contraindications
  1. Continuous Opioids at therapeutic dosess >7 days
  2. Severe hepatic dysfunction
  3. Severe renal dysfunction
  • Mechanism
  1. Synthetic piperidine that is peripherally, a selective and Competitive Antagonist at the Opioid mu receptor
    1. Active at the myenteric and submucosal Neurons and the immune cells of the lamina propria in the Gastrointestinal Tract
    2. Alvimopan is more potent than Naloxone by a factor of 3 to 9
  2. Block Opioid binding in the intestinal tract
    1. Decreases mu-Opioid receptor mediated bowel paralysis
  • Dosing
  • Perioperative
  1. Start 12 mg orally 30 min to 5 hours prior to surgery (partial bowel resection with primary anastomosis)
  2. Next: 12 mg orally twice daily on the day after surgery for up to 7 days (15 doses)
  • Pharmacokinetics
  1. Serum concentrations may be 2 fold higher in patients of Japanese descent
  • Adverse Effects
  1. Myocardial Infarction risk
    1. FDA enforces restricted prescribing of Alvimopan
  • Safety
  1. Pregnancy Category B
  2. Unknown safety in Lactation