Effect of asimadoline, a κ opioid agonist, on pain induced by colonic distension in patients with irritable bowel syndrome

Alimentary Pharmacology and Therapeutics

Volumn 20, Issue 2, 2004, Pages 237-246

  Delvaux, M ^a,e   Beck, A ^b   Jacob, J ^c   Bouzamondo, H ^d   Weber, F T ^c   Frexinos, J ^a  

^a CHU RANGUEIL   (France)

^b Groupe Sante Recherche   (France)

^c MERCK KGAA   (Germany)

^d Dohme Chibret Centre de Recherche Riom   (France)

^e CHU NANCY BRABOIS   (France)

Author keywords

[No Author keywords available]

Indexed keywords

ASIMADOLINE; OPIATE AGONIST; ORAL CONTRACEPTIVE AGENT; PLACEBO;

ABDOMINAL PAIN; ADULT; AGED; ANALYSIS OF VARIANCE; AREA UNDER THE CURVE; ARTICLE; CLINICAL ARTICLE; CLINICAL TRIAL; COLON DILATATION; COLONOSCOPY; COMPARATIVE STUDY; COMPLIANCE (PHYSICAL); CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIARRHEA; DOUBLE BLIND PROCEDURE; DRUG EFFECT; DRUG SAFETY; EVALUATION; FEMALE; HUMAN; HYPERSENSITIVITY; INTESTINE DIVERTICULOSIS; INTESTINE POLYP; IRRITABLE COLON; MALE; PAIN THRESHOLD; PATIENT; PERCEPTION; PERCEPTIVE THRESHOLD; PRESSURE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SENSATION; STATISTICAL SIGNIFICANCE; ULCERATIVE COLITIS;

ACETAMIDES; ADMINISTRATION, ORAL; ADOLESCENT; ADULT; AGED; DILATATION; DOUBLE-BLIND METHOD; FEMALE; HUMANS; IRRITABLE BOWEL SYNDROME; MIDDLE AGED; NARCOTIC ANTAGONISTS; PAIN; PAIN MEASUREMENT; PAIN THRESHOLD; PRESSURE; PYRROLIDINES;

EID: 3242878696     PISSN: 02692813     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1365-2036.2004.01922.x     Document Type: Article

References (42)

1. Whitehead WE, Crowell MD, Bosmajian L, et al. Existence of irritable bowel syndrome supported by factor analysis of symptoms in two community samples. Gastroenterology 1990; 98: 336-40.
2. Ritchie J. Pain from distension of the pelvic colon by inflating a balloon in the irritable colon syndrome. Gut 1973; 14: 125-32.
3. Whitehead WE, Holtkotter B, Enck P, et al. Tolerance for rectosigmoid distension in irritable bowel syndrome. Gastroenterology 1990; 98: 1187-92.
4. Bradette M, Delvaux M, Staumont G, Fioramonti J, Buéno L, Frexinos J. Evaluation of colonie sensory thresholds in IBS patients using a barostat: definition of optimal conditions and comparison with healthy subjects. Dig Dis Sci 1994; 39; 449-57.
5. Buéno L, Fioramonti J, Delvaux M, Frexinos J. Mediators and pharmacology of visceral sensitivity: from basic to clinical investigations. Gastroenterology 1997; 112: 1714-43.
6. Satoh M, Minami M. Molecular Pharmacology of the opioid receptors. Pharmacol Ther 1995; 68: 343-64.
7. Diop L, Rivière PJ, Pascaud X, Junien JL. Peripheral kappa opioid receptors mediate the antinociceptive effect of fedotozine on the duodenal pain reflex in Rat. Eur J Pharmacol 1994; 271: 65-71.
8. Danzebrink RM, Green SA, Gebhart GF. Spinal mu and delta but not kappa opioid receptor agonists attenuate responses to noxious colorectal distension in the rat. Pain 1995; 63: 39-47.
9. Sproule BA, Busto UE, Somer G, Romach MK, Sellers M. Characteristics of dependent and non-dependent regular users of codeine. J Clin Psychopharmacol 1999; 19: 367-72.
10. Dapoigny M, Abitbol JL, Fraitag B. Efficacy of peripheral kappa agonist fedotozine versus placebo in treatment of irritable bowel syndrome. A multicenter dose-response study. Dig Dis Sci 1995; 40; 2244-8.
11. Delvaux M, Louvel D, Lagier E, Scherrer B, Abitbol JL, Frexinos J. The kappa agonist Fedotozine relieves hypersensitivity to colonic distension in patients with irritable bowel syndrome (IBS). Gastroenterology 1999; 116: 38-45.
12. Gottschlich R, Krug M, Barber A, Devant RM. Kappa opioid activity of the four stereoisomers of the peripherally selective kappa-agonists EMD 60,400 and EMD 61,753. Chirality 1994; 6: 685-9.
13. Barber A, Bartoszyk GD, Bender HM, et al. A pharmacological profile of the novel peripherally selective kappa opioid receptor agonist EMD 61,753. Br J Pharmacol 1994; 113: 1317-27.
14. Burton MB, Gebhart GF. Effects of kappa opioid receptor agonists on responses to colo-rectal distension in rats, with and without acute colonic inflammation. J Pharmacol Exp Ther 1998; 285: 707-15.
15. Sengupta JN, Snider A, Su X, Gebhart GF. Effect of kappa opioids in the inflamed rat colon. Pain 1999; 79: 175-85.
16. Bender HM, Dasenbrock J. Brain concentrations of asimadoline in mice: the influence of coadministration of various P-glycoprotein substrates. Int J Clin Pharmacol Ther 1998; 36: 76-9.
17. Jonker JW, Wagenaar E, vanDeemter L, et al. Role of blood-brain barrier P-glycoprotein in limiting brain accumulation and sedative side-effects of asimadoline, a peripherally acting analgesic drug. Br J Pharmacol 1999; 127: 43-50.
18. Jacob J. EMR 63,320 - Investigator's Brochure version 2.0 Darmstadt: Merck KgaA, July 2002.
19. Thompson WG, Longstreth GF, Drossman DA, Heaton KW, Irvine EJ, Muller-Lisser SA. Functional bowel disorders and functional abdominal pain. Gut 1999; 45 (Suppl II): II43-7.
20. Hachet T, Caussette M. A multifunction and programmable computerised barostat. Gastroenterol Clin Biol 1993; 17: 347-51.
21. CPMP 'Points to consider on missing data', CPMP/EWP/ 1776/99 Draft, 25 January 2001
22. Delvaux M, Louvel D, Lagier E, Fioramonti J, Buéno L, Frexinos J. Reproducibility of sensory thresholds triggered by rectal distension in healthy volunteers. Gastroenterology 1995; 108: A590 (abstract).
23. Kramer HJ, Uhl W, Ladstetter B, Bäcker A. Influence of asimadoline, a new κ agonist on tubular water absorption and vasopressin secretion in man. Br J Clin Pharmacol 2000; 50: 227-35.
24. Whitehead WE, Delvaux M. Standardization of barostat procedures for testing smooth muscle tone and sensory thresholds in the gastrointestinal tract. Dig Dis Sci 1997; 42: 223-41.
25. Blanc C, Delvaux M, Maillot C, et al. Distension protocols for evaluation of rectal sensitivity: the simplest, the best? Gastroenterology 1998; 114: A722 (abstract)
26. Jones KR, Whitehead WE, Meyer K. Agreement between different methods of measuring pain sensitivity. Gastroenterology 1999; 116: A1012 (abstract).
27. Delvaux M, Aggadi Y, Blanc C, Frexinos J. Protocols of distension to evaluate visceral sensitivity in patients with irritable bowel syndrome (IBS): is the simplest, the best? Gastroenterology 2001; 120: A133 (abstract).
28. Haley J, Ketchum S, Dickenson AH. Peripheral kappa-opioid modulation of the formalin response: an electrophysiological study in the rat. Eur J Pharmacol 1990; 191: 437-46.
29. Russel NJW, Schaible HG, Schmidt RF. Opiates inhibit the discharges of fine afferent units from inflamed knee joint of the cat. Neurosci Lett 1987; 765: 107-12.
30. Lembeck F, Donnerer J. Opioid control of the function of primary afferent substance P fibres. Eur J Pharmacol 1985; 114; 241-6.
31. Yaksh TL. Substance P from knee joint afferent terminals: modulation by opioids. Brain Res 1988; 458: 319-24.
32. Rivière P, Pascaud X, Chevalier E, Le Gallou B, Junien JL. Fedotozine reverses ileus by surgery or peritonitis. Action at peripheral kappa opioid receptors. Gastroenterology 1993; 104: 724-31.
33. Delgado-Aros S, Chial HJ, Camilleri M, et al. Effects of a kappa opioid agonist, asimadolime, on satiation and gastrointestinal motor and sensory functions in humans. Am J Physiol 2003; 284: G558-66.
34. Buéno L, Gué M, Fargeas M, Alvinerie M, Junien JL, Fioramonti J. Vagally mediated inhibition of acoustic stress involved cortisol release by orally administered kappa opioid substances in dogs. Endocrinology 1989; 124: 1788-93.
35. Riviere PJM, Pascaud X, Chevalier E, Junien JL. Fedotozine reversal of peritoneal irritation-induced ileus in rats: possible peripheral action on sensory afferents. J Pharmacol Exp Ther 1994; 270: 846-50.
36. Cue M, Junien JL, Buéno L. The kappa agonist fedotozine modulates colonie distension-induced inhibition of gastric motility and emptying in dogs. Gastroenterology 1994; 107: 1327-34.
37. Diop L, Riviere P, Pascaud X, Dassaud M, Junien JL. Role of vagal afferents in the antinociception produced by morphine and U50,488H in the colonic pain reflex in rats. Eur J Pharmacol 1994; 271: 181-7.
38. Ohsawa M, Mizoguchi H, Narita M, Chu M, Nagase H, Tseng LF. Differential mechanisms mediating descending pain controls for antinociception induced by supraspinally administered endomorphin-1 and endomorphin-2 in the mouse. J Pharmacol Exp Ther 2000; 294: 1106-11.
39. Ness TJ. Kappa opioid receptors agonists differentially inhibit two classes of rat spinal neurons, excited by colorectal distension. Gastroenterology 1999; 117: 388-94.
40. Bassotti G, Gaburri M, Imbimbo BP, Morelli A, Whitehead WE. Distension-stimulated propagated contractions in human colon. Dig Dis Sci 1994; 39: 1955-60.
41. Distrutti E, Azpiroz F. Soldevilla A, Malagelada JR. Gastric wall tension determines perception of gastric distention. Gastroenterology 1999; 116: 1035-42.
42. Read NW, Abitbol JL, Bardhan KD, Whorwell PJ, Fraitag B. Efficacy and safety of the peripheral kappa agonist fedotozine versus placebo in the treatment of functional dyspepsia. Gut 1997; 41: 664-68.