Alvimopan
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| Clinical data | |
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| Trade names | Entereg |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a608051 |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Bioavailability | 6% |
| Protein binding | 80% (parent drug), 94% (metabolite) |
| Metabolism | Gut microflora-mediated hydrolysis to active metabolite |
| Biological half-life | 10-17 hours |
| Excretion | Faeces, urine (35%) |
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| Synonyms | Alvimopan, Entereg |
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| Chemical and physical data | |
| Formula | C25H32N2O4 |
| Molar mass | 424.53 g/mol |
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Alvimopan (trade name Entereg) is a drug which behaves as a peripherally acting μ-opioid antagonist. With the limited ability to cross the blood–brain barrier and reach the μ-opioid receptors of the central nervous system, many of the clinically undesirable side-effects (such as euphoria and withdrawal) of centrally acting opioid agonists are minimized without affecting the intended activation of μ-opioid receptors of the peripheral nervous system in the gastrointestinal tract. For the same reason, alvimopan has no analgesic properties at therapeutic doses. It is currently only Food and Drug Administration approved for the treatment of postoperative ileus which it received in May 2008.
Alvimopan is indicated in people to avoid postoperative ileus following partial large or small bowel resection with primary anastomosis. Alvimopan accelerates the gastrointestinal recovery period as defined by time to first bowel movement or flatus.
The most common side effects associated with alvimopan are:
Alvimopan is absolutely contraindicated in patients who have taken therapeutic doses of opioids for more than seven consecutive days immediately prior to when alvimopan would be initiated because individuals with recent exposure to opioids are expected to be more sensitive to the effects of mu-opioid receptor antagonists. The peripheral site of action of alvimopan suggests that such a heightened sensitivity would precipitate gastrointestinal effects beyond dyspepsia.
Alvimopan is not substrate for the enzyme system. Therefore, no interactions are expected with hepatically metabolized drugs. Alvimopan is substrate for P-glycoprotein. Expect interactions with known P-glycoprotein inhibitors such as amiodarone, bepridil, diltiazem, ciclosporin, itraconazole, quinine, quinidine, spironolactone, and verapamil.
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