II. 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

III. Contraindications

  1. Continuous Opioids at therapeutic dosess >7 days
  2. Severe hepatic dysfunction
  3. Severe renal dysfunction

IV. 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

V. 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)

VI. Pharmacokinetics

  1. Serum concentrations may be 2 fold higher in patients of Japanese descent

VII. Adverse Effects

  1. Myocardial Infarction risk
    1. FDA enforces restricted prescribing of Alvimopan

VIII. Safety

  1. Pregnancy Category B
  2. Unknown safety in Lactation

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Related Studies

Ontology: alvimopan (C1508750)

Definition (NCI) A synthetic trans-3,4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons and the immune cells of the lamina propria in the human gut. Upon administration, this agent binds to mu-opioid receptors in the gut, thereby reversing opioid-related disturbances in gut motility. Alvimopan is approximately three to nine times more potent than naloxone.
Definition (PDQ) A synthetic trans-3,4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons andthe immune cells of the lamina propria in the human gut. Upon administration, this agent binds to mu-opioid receptors in the gut, thereby reversing opiod-related disturbances in gut motility. Alvimopan is approximately three to nine times more potent than naloxone. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=453551&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=453551&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C49096" NCI Thesaurus)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C419502
SnomedCT 437917007, 437886007
English Alvimopan, Alvimopan (substance), Alvimopan (product), ALVIMOPAN, alvimopan [Chemical/Ingredient], trans-3,4-dimethyl-4-(3-hydroxyphenyl) piperidine, alvimopan
Spanish alvimopán (producto), alvimopán, alvimopán (sustancia)