Opioid antagonists for prevention and treatment of opioid-induced gastrointestinal effects

Current Opinion in Anaesthesiology

Volumn 23, Issue 5, 2010, Pages 616-622

  Holzer, Peter ^a  

^a MEDICAL UNIVERSITY OF GRAZ   (Austria)

Author keywords

alvimopan; methylnaltrexone; naloxone; opioid analgesics; opioid induced bowel dysfunction; opioid induced constipation; postoperative ileus

Indexed keywords

17 METHYLNALTREXONE; 17 METHYLNALTREXONE BROMIDE; ALVIMOPAN; NALOXONE; OPIATE ANTAGONIST; OXYCODONE; PEGYLATED NALOXOL; PLACEBO; UNCLASSIFIED DRUG;

ABDOMINAL CRAMP; ABDOMINAL DISCOMFORT; ANALGESIA; CANCER PAIN; CONSTIPATION; COST EFFECTIVENESS ANALYSIS; DIARRHEA; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG INDUCED CONSTIPATION; DRUG INDUCED DISEASE; DRUG MECHANISM; DRUG RELEASE; DRUG SAFETY; DRUG WITHDRAWAL; FLATULENCE; HUMAN; ILEUS; INTESTINE RESECTION; NAUSEA; OPIOID INDUCED CONSTIPATION; POSTOPERATIVE COMPLICATION; POSTOPERATIVE ILEUS; PREVALENCE; PRIORITY JOURNAL; REVIEW; SINGLE DRUG DOSE; TREATMENT RESPONSE; VOMITING;

ANALGESICS, OPIOID; BIOLOGICAL AVAILABILITY; GASTROINTESTINAL DISEASES; HUMANS; NARCOTIC ANTAGONISTS; PERIPHERAL NERVOUS SYSTEM;

EID: 77956458979     PISSN: 09527907     EISSN: None     Source Type: Journal    
DOI: 10.1097/ACO.0b013e32833c3473     Document Type: Review

References (69)

1. Becker G, Blum HE. Novel opioid antagonists for opioid-induced bowel dysfunction and postoperative ileus. Lancet 2009; 373:1198-1206.
2. Reimer K, Hopp M, Zenz M, et al. Meeting the challenges of opioid-induced constipation in chronic pain management: a novel approach. Pharmacology 2009; 83:10-17.
3. Porreca F, Galligan JJ, Burks TF. Central opioid receptor involvement in gastrointestinal motility. Trends Pharmacol Sci 1986; 7:104-107.
4. DeHaven-Hudkins DL, DeHaven RN, Little PJ, Techner LM. The involvement of the mu-opioid receptor in gastrointestinal pathophysiology: therapeutic opportunities for antagonism at this receptor. Pharmacol Ther 2008; 117: 162-187.
5. Thomas JR, Cooney GA, Slatkin NE. Palliative care and pain: new strategies for managing opioid bowel dysfunction. J Palliat Med 2008; 11 (Suppl 1):S1-S19.
6. Holzer P. Opioid receptors in the gastrointestinal tract. Regul Pept 2009; 155:11-17.
7. De Luca A, Coupar IM. Insights into opioid action in the intestinal tract. Pharmacol Ther 1996; 69:103-115.
8. Holzer P. Treatment of opioid-induced gut dysfunction. Expert Opin Investig Drugs 2007; 16:181-194.
9. Panchal SJ, Müller-Schwefe P, Wurzelmann JI. Opioid-induced bowel dysfunction: prevalence, pathophysiology and burden. Int J Clin Pract 2007; 61:1181-1187.
10. Osterbrink J, Haas U. Opioid-induced bowel dysfunction: a literature analysis on pathophysiology and treatment. Wien Med Wochenschr 2008; 158:621-626.
11. Shook JE, Pelton JT, Hruby VJ, Burks TF. Peptide opioid antagonist separates peripheral and central opioid antitransit effects. J Pharmacol Exp Ther 1987; 243:492-500.
12. Cook SF, Lanza L, Zhou X, et al. Gastrointestinal side effects in chronic opioid users: results from a population-based survey. Aliment Pharmacol Ther 2008; 27:1224-1232.
13. Bell T, Annunziata K, Leslie JB. Opioid-induced constipation negatively impacts pain management, productivity, and health-related quality of life: findings from the National Health and Wellness Survey. J Opioid Manag 2009; 5:137-144.
14. Bell TJ, Panchal SJ, Miaskowski C, et al. The prevalence, severity, and impact of opioid-induced bowel dysfunction: results of a US and European Patient Survey (PROBE 1). Pain Med 2009; 10:35-42.
15. Choung RS, Locke GR, Zinsmeister AR, et al. Opioid bowel dysfunction and narcotic bowel syndrome: a population-based study. Am J Gastroenterol 2009; 104:1199-1204.
16. Schutter U, Grunert S, Meyer C, et al. Innovative pain therapy with a fixed combination of prolonged-release oxycodone/naloxone: a large observational study under conditions of daily practice. Curr Med Res Opin 2010; 26: 1377-1387.
17. Tuteja AK, Biskupiak J, Stoddard GJ, Lipman AG. Opioid-induced bowel disorders and narcotic bowel syndrome in patients with chronic noncancer pain. Neurogastroenterol Motil 2010; 22:424-430.
18. Ishihara M, Iihara H, Okayasu S, et al. Pharmaceutical interventions facilitate premedication and prevent opioid-induced constipation and emesis in cancer patients. Support Care Cancer 2009. [Epub ahead of print]
19. Bouras EP, Tangalos EG. Chronic constipation in the elderly. Gastroenterol Clin North Am 2009; 38:463-480.
20. Matsui T, Kojima T, Kojima H, et al. Feasibility study of direct fentanyl patch introduction without prior opioid titration. Int J ClinOncol 2009; 14:202-207.
21. Longstreth GF, Thompson WG, Chey WD, et al. Functional bowel disorders. Gastroenterology 2006; 130:1480-1491.
22. Rentz AM, Yu R, Müller-Lissner S, Leyendecker P. Validation of the bowel function index to detect clinically meaningful changes in opioid-induced constipation. J Med Econ 2009; 12:371-383.
23. Moss J, Rosow CE. Development of peripheral opioid antagonists' new insights into opioid effects. Mayo Clin Proc 2008; 83:1116-1130.
24. Boeckxstaens GE, de Jonge WJ. Neuroimmune mechanisms in postoperative ileus. Gut 2009; 58:1300-1311.
25. Viscusi ER, Gan TJ, Leslie JB, et al. Peripherally acting mu-opioid receptor antagonists and postoperative ileus: mechanisms of action and clinical applicability. Anesth Analg 2009; 108:1811-1822.
26. Schmidt J, Stoffels B, Nazir A, et al. Alvimopan and COX-2 inhibition reverse opioid and inflammatory components of postoperative ileus. Neurogastroenterol Motil 2008; 20:689-699.
27. Iyer S, Saunders WB, Stemkowski S. Economic burden of postoperative ileus associated with colectomy in the United States. J Manag Care Pharm 2009; 15:485-494.
28. Meissner W, Schmidt U, Hartmann M, et al. Oral naloxone reverses opioidassociated constipation. Pain 2000; 84:105-109.
29. Holzer P, Ahmedzai SH, Niederle N, et al. Opioid-induced bowel dysfunction in cancer-related pain: causes, consequences, and a novel approach for its management. J Opioid Manag 2009; 5:145-151.
30. Smith K, Hopp M, Mundin G, et al. Single- and multiple-dose pharmacokinetic evaluation of oxycodone and naloxone in an opioid agonist/antagonist prolonged- release combination in healthy adult volunteers. Clin Ther 2008; 30:2051-2068.
31. Meissner W, Leyendecker P, Mueller-Lissner S, et al. A randomised controlled trial with prolonged-release oral oxycodone and naloxone to prevent and reverse opioid-induced constipation. Eur J Pain 2009; 13:56-64.
32. Nadstawek J, Leyendecker P, Hopp M, et al. Patient assessment of a novel therapeutic approach for the treatment of severe, chronic pain. Int J Clin Pract 2008; 62:1159-1167.
33. Vondrackova D, Leyendecker P, MeissnerW,et al.Analgesic efficacy and safety of oxycodone in combination with naloxone as prolonged release tablets in patients with moderate to severe chronic pain. J Pain 2008; 9:1144-1154.
34. Simpson K, Leyendecker P, Hopp M, et al. Fixed-ratio combination oxycodone/ naloxone compared with oxycodone alone for the relief of opioidinduced constipation in moderate-to-severe noncancer pain. Curr Med Res Opin 2008; 24:3503-3512.
35. Löwenstein O, Leyendecker P, Hopp M, et al. Combined prolonged-release oxycodone and naloxone improves bowel function in patients receiving opioids for moderate-to-severe nonmalignant chronic pain: a randomised controlled trial. Expert Opin Pharmacother 2009; 10:531-543.
36. Sandner-Kiesling A, Leyendecker P, Hopp M, et al. Long-term efficacy and safety of combined prolonged-release oxycodone and naloxone in the management of noncancer chronic pain. Int J Clin Pract 2010; 64:763-774.
37. Clemens KE, Mikus G. Combined oral prolonged-release oxycodone and naloxone in opioid-induced bowel dysfunction: review of efficacy and safety data in the treatment of patients experiencing chronic pain. Expert Opin Pharmacother 2010; 11:297-310.
38. Balsama L, Weese J. Alvimopan: a peripheral acting mu-opioid-receptor antagonist used for the treatment of postoperative ileus. Therapy 2007; 4:653-664.
39. Leslie JB. Alvimopan: a peripherally acting mu-opioid receptor antagonist. Drugs Today (Barc) 2007; 43:611-625.
40. Foss JF, Fisher DM, Schmith VD. Pharmacokinetics of alvimopan and its metabolite in healthy volunteers and patients in postoperative ileus trials. Clin Pharmacol Ther 2008; 83:770-776.
41. Schmith VD, Johnson BM, Vasist LS, et al. The effects of a short course of antibiotics on alvimopan and metabolite pharmacokinetics. J Clin Pharmacol 2010; 50:338-349.
42. Marderstein EL, Delaney CP. Management of postoperative ileus: focus on alvimopan. Ther Clin Risk Manag 2008; 4:965-973.
43. Webster L, Jansen JP, Peppin J, et al. Alvimopan, a peripherally acting muopioid receptor (PAM-OR) antagonist for the treatment of opioid-induced bowel dysfunction: results from a randomized, double-blind, placebo-controlled, dose-finding study in subjects taking opioids for chronic noncancer pain. Pain 2008; 137:428-440.
44. Bell TJ, Poston SA, Kraft MD, et al. Economic analysis of alvimopan in North AmericanphaseIIIefficacytrials.AmJHealthSystPharm2009;66:1362-1368.
45. Bream-Rouwenhorst HR, Cantrell MA. Alvimopan for postoperative ileus. Am J Health Syst Pharm 2009; 66:1267-1277.
46. Wolff BG, Michelassi F, Gerkin TM, et al., Alvimopan Postoperative Ileus Study Group. Alvimopan, a novel, peripherally acting mu-opioid antagonist: results of a multicenter, randomized, double-blind, placebo-controlled, phase III trial of major abdominal surgery and postoperative ileus. Ann Surg 2004; 240:728-734.
47. Delaney CP, Weese JL, Hyman NH, et al., Alvimopan Postoperative Ileus Study Group. Phase III trial of alvimopan, a novel, peripherally acting, muopioid antagonist, for postoperative ileus after major abdominal surgery. Dis Colon Rectum 2005; 48:1114-1125.
48. Herzog TJ, Coleman RL, Guerrieri JP Jr, et al. A double-blind, randomized, placebo-controlled phase III study of the safety of alvimopan in patients who undergo simple total abdominal hysterectomy. Am J Obstet Gynecol 2006; 195:445-453.
49. Viscusi ER, Goldstein S, Witkowski T, et al. Alvimopan, a peripherally acting mu-opioid receptor antagonist, compared with placebo in postoperative ileus after major abdominal surgery: results of a randomized, double-blind, controlled study. Surg Endosc 2006; 20:64-70.
50. Büchler MW, Seiler CM, Monson JR, et al. Clinical trial: alvimopan for the management of postoperative ileus after abdominal surgery: results of an international randomized, double-blind, multicentre, placebo-controlled clinical study. Aliment Pharmacol Ther 2008; 28:312-325.
51. Ludwig K, Enker WE, Delaney CP, et al. Gastrointestinal tract recovery in patients undergoing bowel resection: results of a randomized trial of alvimopan and placebo with a standardized accelerated postoperative care pathway. Arch Surg 2008; 143:1098-1105.
52. Senagore AJ, Bauer JJ, Du W, Techner L. Alvimopan accelerates gastrointestinal recovery after bowel resection regardless of age, gender, race, or concomitant medication use. Surgery 2007; 142:478-486.
53. Tan EK, Cornish J, DarziAW, Tekkis PP.Meta-analysis: alvimopan vs. placebo in the treatment of postoperative ileus. Aliment Pharmacol Ther 2007; 25:47-57.
54. McNicol E, Boyce DB, Schumann R, Carr D. Efficacy and safety of mu-opioid antagonists in the treatment of opioid-induced bowel dysfunction: systematic review and meta-analysis of randomized controlled trials. Pain Med 2008; 9:634-659.
55. Paulson DM, Kennedy DT, Donovick RA, et al. Alvimopan: an oral, peripherally acting, mu-opioid receptor antagonist for the treatment of opioid-induced bowel dysfunction:a 21-day treatment-randomized clinical trial. J Pain 2005; 6:184-192.
56. Yuan CS, Israel RJ. Methylnaltrexone, a novel peripheral opioid receptor antagonist for the treatment of opioid side-effects. Expert Opin Investig Drugs 2006; 15:541-552.
57. Holzer P. Methylnaltrexone for the management of unwanted peripheral opioid effects. Therapy 2008; 5:531-543.
58. Reichle FM, Conzen PF. Methylnaltrexone, a new peripheral mu-receptor antagonist for the prevention and treatment of opioid-induced extracerebral side-effects. Curr Opin Investig Drugs 2008; 9:90-100.
59. Chandrasekaran A, Tong Z, Li H, et al. Metabolism of intravenous methylnaltrexone in mice, rats, dogs, and humans. Drug Metab Dispos 2010; 38:606-616.
60. Tong Z, Chandrasekaran A, Li H, et al. In-vitro metabolism and identification of human enzymes involved in the metabolism of methylnaltrexone. Drug Metab Dispos 2010; 38:801-807.
61. Portenoy RK, Thomas J, Moehl Boatwright ML, et al. Subcutaneous methylnaltrexone for the treatment of opioid-induced constipation in patients with advanced illness: a double-blind, randomized, parallel group, dose-ranging study. J Pain Symptom Manage 2008; 35:458-468.
62. Thomas J, Karver S, Austin Cooney G, et al. Methylnaltrexone for opioidinduced constipation in advanced illness. N Engl J Med 2008; 358:2332-2343.
63. Chamberlain BH, Cross K, Winston JL, et al. Methylnaltrexone treatment of opioid-induced constipation in patients with advanced illness. J Pain Symptom Manage 2009; 38:683-690.
64. Slatkin N, Thomas J, Lipman AG, et al. Methylnaltrexone for treatment of opioid-induced constipation in advanced illness patients. J Support Oncol 2009; 7:39-46.
65. Earnshaw SR, Klok RM, Iyer S, McDade C. Methylnaltrexone bromide for the treatment of opioid-induced constipation in patients with advanced illness: a cost-effectiveness analysis. Aliment Pharmacol Ther 2010; 31:911-921.
66. Kraft MD. Methylnaltrexone, a new peripherally acting mu-opioid receptor antagonist being evaluated for the treatment of postoperative ileus. Expert Opin Investig Drugs 2008; 17:1365-1377.
67. Guay DR. Methylnaltrexone methobromide: the first peripherally active, centrally inactive opioid receptor-antagonist. Consult Pharm 2009; 24:210-226.
68. Clemens KE, Klaschik E. Managing opioid-induced constipation in advanced illness: focus on methylnaltrexone bromide. Ther Clin Risk Manag 2010; 6:77-82.
69. Kraft M, Maclaren R, Du W, Owens G. Alvimopan (entereg) for the management of postoperative ileus in patients undergoing bowel resection. P T 2010; 35:44-49.