Peripherally restricted μ-opioid receptor antagonists: a review

Techniques in Regional Anesthesia and Pain Management

Volumn 11, Issue 1, 2007, Pages 27-32

  Linn, Andrew J ^a   Steinbrook, Richard A ^a  

^a HARVARD MEDICAL SCHOOL   (United States)

Author keywords

Alvimopan; Gastrointestinal; Methylnaltrexone; Opioid; PAMOR; Postoperative ileus

Indexed keywords

17 METHYLNALTREXONE; ALVIMOPAN; APOMORPHINE; CISPLATIN; CODEINE; LAXATIVE; METHADONE; MORPHINE; MU OPIATE RECEPTOR ANTAGONIST; NALOXONE; OPIATE; PLACEBO;

ABDOMINAL SURGERY; ANALGESIA; ARTICLE; BLOOD BRAIN BARRIER; CANCER GROWTH; CHRONIC PAIN; CLINICAL TRIAL; CONSTIPATION; DRUG ABSORPTION; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG MECHANISM; DRUG STRUCTURE; GASTROINTESTINAL MOTILITY; GASTROINTESTINAL SYMPTOM; GASTROINTESTINAL TRACT FUNCTION; HOSPITAL DISCHARGE; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; ILEUS; IMMUNE DEFICIENCY; NAUSEA; NAUSEA AND VOMITING; NEOVASCULARIZATION (PATHOLOGY); NONHUMAN; PATIENT SATISFACTION; POSTOPERATIVE COMPLICATION; POSTOPERATIVE NAUSEA AND VOMITING; PRURITUS; RESPIRATION DEPRESSION; SEDATION; SIDE EFFECT; STOMACH EMPTYING; UNSPECIFIED SIDE EFFECT; VISUAL ANALOG SCALE; WOUND HEALING;

EID: 34247506326     PISSN: 1084208X     EISSN: None     Source Type: Journal    
DOI: 10.1053/j.trap.2007.02.003     Document Type: Article

References (40)

1. Wood J.D., and Galigan J.J. Function of opioids in the enteric nervous system. Neurogastroenterol Motil 16 (2004) 17-28
2. Holzer P. Opioids and opioid receptors in the enteric nervous system: from a problem in opioid analgesia to a possible new prokinetic therapy in humans. Neurosci Lett 361 (2004) 192-195
3. Levy M.H. Pharmacological treatment of cancer pain. N Engl J Med 335 (1996) 1124-1136
4. Laxatives for the management of constipation in palliative care patients. Cochrane Database Syst Rev 4 (2006) CD003448
5. Bell T., Leslie J., Annunziata K., et al. Opioid-induced constipation compromises pain management and impacts patient quality of life. AAPM (2007) 161
6. Abbound T.K., Lee K., Zhu J., et al. Prophylactic oral naltrexone with intrathecal morphine for cesarean section: effects on adverse reactions and analgesia. Anesth Analg 71 (1990) 367-370
7. Syke N. Oral naloxone in opioid-associated constipation. Lancet 337 (1991) 1475
8. Culpepper-Morgan J.A., Inturrisi C.E., Portenoy R.K., et al. Treatment of opioid-induced constipation with oral naloxone: a pilot study. Clin Pharmacol Ther 52 (1992) 90-95
9. Latasch L., Zimmermann M., Eberhardt B., et al. Treatment of morphine-induced constipation with oral naloxone. Anaesthesist 46 (1997) 191-194
10. Meissner W., Schmidt U., Hartmann M., et al. Oral naloxone reverses opioid-associated constipation. Pain 84 (2000) 105-109
11. Yuan C.S., Foss J.F., Osinski J., et al. The safety and efficacy of oral methylnaltrexone in preventing morphine-induced delay in oral-cecal transit time. Clin Pharmacol Ther 61 (1997) 467-475
12. Yuan C.S., Foss J.F., O'Connor M., et al. Effects of enteric-coated methylnaltrexone in preventing opioid-induced delay in oral-cecal transit time. Clin Pharmacol Ther 67 (2000) 398-404
13. Liu S.S., Hodgson P.S., Carpenter R.L., et al. ADL 8-2698, a trans-3,4-dimethyl-4-(3-hydroxyphenyl) piperidine, prevents gastrointestinal effects of intravenous morphine without affecting analgesia. Clin Pharmacol Ther 69 (2001) 66-71
14. Yuan C.S., Foss J.F., O'Connor M., et al. Methylnaltrexone for reversal of constipation due to chronic methadone use: a randomized controlled trial. J Am Med Assoc 283 (2000) 367-372
15. Yuan C.S., Wei G., Foss J.F., et al. Effects of subcutaneous methylnaltrexone on morphine-induced peripherally mediated side effects: a double-blind randomized placebo-controlled trial. J Pharmacol Exp Ther 300 (2002) 118-123
16. Paulson D.M., Kennedy D.T., Donovick R.A., 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 3 (2005) 184-192
17. Gonenne J., Camilleri M., Ferber I., et al. Effect of alvimopan and codeine on gastrointestinal transit: a randomized controlled study. Clin Gastroenterol Hepatol 8 (2005) 784-791
18. Luckey A., Livingston E., and Tache Y. Mechanisms and treatment of postoperative ileus. Arch Surg 138 (2003) 206-214
19. Delaney C.P., Senagore A.J., Viscusi E.R., et al. Postoperative upper and lower gastrointestinal recovery and gastrointestinal morbidity in patients undergoing bowel resection: pooled analysis of placebo data from 3 randomized controlled trials. Am J Surg 91 (2006) 315-319
20. Livingston EH: personal communication, Sept 29, 2006
21. Kalff J.C., Turler A., Schwarz N.T., et al. Intra-abdominal activation of a local inflammatory response within the human muscularis externa during laparotomy. Ann Surg 237 (2003) 301-315
22. Bult H., Boeckxstaens G.E., Pelcksman P.A., et al. Nitric oxide as an inhibitory non-adrenergic non-cholinergic neurotransmitter. Nature 345 (1990) 346-347
23. DeJonge W., VanDenWijngaard R., The F., et al. Postoperative ileus is maintained by intestinal immune infiltrates that activate inhibitory neural pathways in mice. Gastroenterology 125 (2003) 1137-1147
24. Cali R.L., Meade P.G., Swanson M.S., et al. Effect of morphine and incision length on bowel function after colectomy. Dis Colon Rectum 43 (2000) 163-168
25. Shahbazian A., Heineman A., Schmidhammer H., et al. Involvement of mu- and kappa-, but not delta-, opioid receptors in the peristaltic motor depression caused by endogenous and exogenous opioids in the guinea-pig intestine. Br J Pharmacol 135 (2002) 741-750
26. Wolff B.G., Michelassi F., Gerkin T.M., et al. 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 240 (2004) 728-735
27. Delaney C.P., Weese J., Hyman N., et al. Phase III trial of alvimopan, a novel, peripherally acting, mu opioid antagonist, for postoperative ileus after major abdominal surgery. Dis Colon rectum 48 (2005) 1114-1129
28. Viscusi E.R., Goldstein S., Witkowski T., et al. Alvimopan, a peripherally acting mu-opioid receptor antagonist, compared with placebo in postoperative ileus after major abdominal surgery. Surg Endosc 20 (2006) 64-70
29. Leslie J., Steinbrook R., Viscusi E., et al. Alvimopan oral dosing 30-90 minutes before and BID after bowel resection accelerated GI recovery. Anesthesiology 105 (2006) A122
30. Gan T.J., Isreal R., and Penenberg D.N. Methylnaltrexone in post-operative bowel dysfunction: results of a double-blind, randomized, placebo-controlled trial in segmental colectomy patients. IARS Abstract (2006) S-281
31. Yuan C.S., Foss J.F., O'Connor M., et al. Efficacy of orally administered methylnaltrexone in decreasing subjective effects after intravenous morphine. Drug Alcohol Depend 52 (1998) 161-165
32. Foss J.F., Bass A.S., and Goldberg L.I. Dose-related antagonism of the emetic effect of morphine by methylnaltrexone in dogs. J Clin Pharmacol 33 (1993) 747-751
33. Foss J.F., Yuan C.S., Roizen M.F., et al. Prevention of apomorphine-induced. or cisplatin-induced emesis in the dog by a combination of methylnaltrexone and morphine. Cancer Chemother Pharmacol 33 (1998) 747-751
34. Moerman I., Franck P., and Camu F. Evaluation of methylnaltrexone for the reduction of postoperative vomiting and nausea incidencies. Act Anaesthesiol Belg 46 (1995) 127-132
35. Vallejo R., de Leon-Casasola O., and Benyamin R. Opioid therapy and immunosuppression: a review. Am J Ther 11 (2004) 354-365
36. Ho W.Z., Guo C.J., Yuan C.S., et al. Methylnaltrexone antagonizes opioid-mediated enhancement of HIV infection of human blood mononuclear phagocytes. J Pharmacol Exp Ther 307 (2003) 1158-1162
37. Gupta K., Kshirsagar S., Chang L., et al. Morphine stimulates angiogenesis by activating proangiogenic and survival-promoting signaling and promotes breast tumor growth. Cancer Res 62 (2002) 4491-4498
38. Poonawala T., Levay-Young B.K., Hebbel R.P., et al. Opioids heal ischemic wounds in the rat. Wound Repair Regen 13 (2005) 165-174
39. Moss J., Fekete M.J., and Lingen M. Morphine induced angiogenesis is blocked by methylnaltrexone. Anesthesiology 105 (2006) A1573
40. Singleton P.A., Lingen M.W., Fekete M.J., et al. Methylnaltrexone inhibits opiate and VEGF-induced angiogenesis: role of receptor transactivation. Microvasc Res 72 (2006) 3-11