Tegaserod: A review of its use in the management of irritable bowel syndrome with constipation in women

Drugs

Volumn 63, Issue 11, 2003, Pages 1101-1120

  Wagstaff, Antona J ^a   Frampton, James E ^a   Croom, Katherine F ^a  

^a ADIS INTERNATIONAL LIMITED   (New Zealand)

Author keywords

Constipation; Irritable bowel syndrome; Pharmacodynamics; Pharmacokinetics; Tegaserod; Therapeutic use; Women

Indexed keywords

BULKING AGENT; LAXATIVE; PLACEBO; SEROTONIN 4 RECEPTOR; TEGASEROD;

ABDOMINAL PAIN; CLINICAL TRIAL; CONSTIPATION; COST EFFECTIVENESS ANALYSIS; DIARRHEA; DIET THERAPY; DISEASE ASSOCIATION; DISEASE SEVERITY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG MECHANISM; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG TOLERABILITY; DRUG WITHDRAWAL; FEMALE; FLATULENCE; GASTROINTESTINAL MOTILITY; HEADACHE; HUMAN; INTESTINE SECRETION; IRRITABLE COLON; MALE; META ANALYSIS; OVARY CYST; PALLIATIVE THERAPY; PATIENT EDUCATION; PHARMACODYNAMICS; QUALITY OF LIFE; RECEPTOR AFFINITY; REVIEW; TREATMENT OUTCOME;

BIOLOGICAL AVAILABILITY; COLONIC DISEASES, FUNCTIONAL; CONSTIPATION; FEMALE; GASTROINTESTINAL AGENTS; GASTROINTESTINAL MOTILITY; HUMANS; INDOLES; INTESTINAL ABSORPTION; MEDLINE; RANDOMIZED CONTROLLED TRIALS; TREATMENT OUTCOME;

EID: 0038509016     PISSN: 00126667     EISSN: None     Source Type: Journal    
DOI: 10.2165/00003495-200363110-00013     Document Type: Review

References (81)

1. Forbes A. IBS: guide to diagnosis and recommended treatment. Prescriber 1997 Apr 19; 8: 67-72
2. Badia X, Mearin F, Balboa A, et al. Burden of illness in irritable bowel syndrome comparing Rome I and Rome II criteria. Pharmacoeconomics 2002; 20 (11): 749-58
3. Farthing MJG. New drugs in the management of the irritable bowel syndrome. Drugs 1998 Jul; 56: 11-21
4. Crowell MD. The role of serotonin in the pathophysiology of irritable bowel syndrome. Am J Manag Care 2001 Jul; 7 (8 Suppl.): S252-60
5. Fass R, Longstreth GF, Pimentel M, et al. Evidence- and consensus-based practice guidelines for the diagnosis of irritable bowel syndrome. Arch Intern Med 2001 Sep 24; 161 (17): 2081-8
6. American Gastroenterological Association. American Gastroenterological Association medical position statement: irritable bowel syndrome. Gastroenterology 1997 Jun; 112: 2118-9
7. Hungin APS, Whorwell PJ, Tack J, et al. The prevalence, patterns and impact of irritable bowel syndrome: an international survey of 40 000 subjects. Aliment Pharmacol Ther 2003; 17: 643-50
8. Mayer EA, Naliboff B, Lee O, et al. Review article: gender-related differences in functional gastrointestinal disorders. Aliment Pharmacol Ther 1999; 13 Suppl. 2: 65-9
9. Degen LP, Phillips SF. Variability of gastrointestinal transit in healthy women and men. Gut 1996; 39: 299-305
10. Scott LJ, Perry CM. Tegaserod. Drugs 1999 Sep; 58 (3): 491-6; discussion 497-8
11. Bucheit K-H, Gamse R, Giger R, et al. The serotonin 5-HT4 receptor: 1. Design of a new class of agonists and receptor map of the agonist recognition site. J Med Chem 1995; 38: 2326-30
12. Buchheit K-H, Gamse R, Giger R, et al. The serotonin 5-HT4 receptor: 2. Structure-activity studies of the indole carbazimidamide class of agonists. J Med Chem 1995; 38: 2331-8
13. Norman P. Tegaserod Novartis. Current Opin Central Peripheral Nervous System Investig Drugs 2000; 2 (3): 344-54
14. Hoyer D, Fehlmann D, Langenegger D, et al. High affinity of SDZ HTF-919 and related molecules for calf and human caudate 5-HT4 receptors. Ann N Y Acad Sci 1998 Dec 15; 861: 267-8
15. Appel S, Kumle A, Hubert M, et al. First pharmacokinetic-pharmacodynamic study in humans with a selective 5-hydroxytryptamine4 receptor agonist. J Clin Pharmacol 1997 Mar; 37 (3): 229-37
16. Pfannkuche H-J, Buchheit K-H, Buhl T, et al. Substituted carbazimidamides, a new class of potent and selective 5-HT4 receptor agonists and antagonists [abstract no. 329]. Naunyn Schmiedebergs Arch Pharmacol 1996; 353 (4 Suppl.): R90
17. Kuemmerle JF, Murthy KS, Grider JR, et al. Human intestinal muscle cells express a rapidly desensitizing long splice variant of the 5-HT4 receptor. Gastroenterology 1996 Apr; 110 (4 Suppl.): A1091
18. Zimmermann AE. Tegaserod: a 5-HT4 agonist for women with constipation-predominant irritable bowel syndrome. Formulary 2002 Sep; 37: 449-61
19. Lacy BE. Tegaserod. Clin Perspect Gastroenterol 2002; 5 (4): 251-5
20. Grider JR. A rapidly desensitizing 5-HT4 receptor mediates the peristaltic reflex induced by mucosal stimuli [abstract no. G3121]. Gastroenterology 1998 Apr 15; 114 (4 Suppl. Pt 2): A757
21. Grider JR, Foxx-Orenstein AE, Jin J-G. 5-Hydroxytryptamine4 receptor agonists initiate the peristaltic reflex in human, rat, and guinea pig intestine. Gastroenterology 1998 Aug; 115 (2): 370-80
22. Pfannkuche H J, Buhl T, Gamse R, et al. The properties of a new prokinetically active drug: SDZ HTF 919. Neurogastroenterol Motil 1995 Dec; 7 (4): 280
23. Fioramonti J, Million M, Bueno L. Investigations on a 5HT4 agonist (SDZ HTF 919) and its main metabolite in conscious dogs: effects on gastrointestinal motility and impaired gastric emptying [abstract no. G3103]. Gastroenterology 1998 Apr 15; 114 (4 Suppl. Pt 2): A752
24. Huge A, Zittel TT, Kreis ME, et al. Effects of tegaserod (HTF 919) on gastrointestinal motility and transit in awake rats [abstract no. 2100]. Gastroenterology 2000 Apr; 118 Suppl. 2, Pt 1: A403
25. Nguyen A, Camilleri M, Kost LJ, et al. SDZ HTF 919 stimulates canine colonic motility and transit in vivo. J Pharmacol Exp Ther 1997 Mar; 280 (3): 1270-6
26. Jin J-G, Foxx-Orenstein AE, Grider JR. Propulsion in guinea pig colon induced by 5-hydroxytryptamine (HT) via 5-HT4 and 5-HT3 receptors. J Pharmacol Exp Ther 1999 Jan; 288 (1): 93-7
27. Appel S, Kumle A, Meier R. Clinical pharmacodynamics of SDZ HTF 919, a new 5-HT4 receptor agonist, in a model of slow colonic transit. Clin Pharmacol Ther 1997 Nov; 62 (5): 546-55
28. Degen L, Matzinger D, Merz M, et al. Tegaserod, a 5-HT4 receptor partial agonist, accelerates gastric emptying and gastrointestinal transit in healthy male subjects. Aliment Pharmacol Ther 2001 Nov; 15 (11): 1745-51
29. Petrig C, Templeton J, Matzinger D, et al. Effect of tegaserod on gastrointestinal transit in male and female subjects [abstract no. MON-G-512, poster]. Gut 2002; 51 Suppl. III: A138
30. Prather CM, Camilleri M, Zinsmeister AR, et al. Tegaserod accelerates orocecal transit in patients with constipation-predominant irritable bowel syndrome. Gastroenterology 2000 Mar; 118 (3): 463-8
31. Petrig C, Templeton J, Matzinger D, et al. Effect of tegaserod on faecal water and electrolyte secretion in male and female subjects [abstract no. WED-G-322, poster]. Gut 2002; 51 Suppl. III: A249
32. Coelho AM, Rovira P, Fioramonti J, et al. Antinociceptive properties of HTF 919 (tegaserod), a 5-HT4 receptor partial agonist, on colorectal distension in rats [abstract no. 4393]. Gastroenterology 2000 Apr; 118 Suppl. 2, Pt 1: A835
33. Schikowski A, Thewissen M, Mathis C, et al. Serotonin type-4 receptors modulate the sensitivity of intramural mechanoreceptive afferents of the cat rectum. Neurogastroenterol Motil 2002 Jun; 14 (3): 221-7
34. Camilleri M. Serotonergic modulation of visceral sensation: lower gut. Gut 2002; 51 Suppl. 1: 81-6
35. Coffin B, Farmachidi JP, Rueegg P, et al. Tegaserod, a 5-HT4 receptor partial agonist, decreases sensitivity to rectal distension in healthy subjects. Aliment Pharmacol Ther 2003; 17: 577-85
36. Dunger-Baldauf C, Rueegg PC, Lefkowitz M. Is relief from abdominal discomfort/pain in tegaserod treated IBS-C patients due to an increased frequency of bowel movements? [abstract no. 838]. Am J Gastroenterol 2002 Sep; 97 Suppl.: S275
37. Morganroth J, Ruegg PC, Dunger-Baldauf C, et al. Tegaserod, a 5-hydroxytryptamine type 4 receptor partial agonist, is devoid of electrocardiographic effects. Am J Gastroenterol 2002 Sep; 97 (9): 2321-7
38. Drici MD, Ebert SN, Wang WX, et al. Comparison of tegaserod (HTF 919) and its main human metabolite with cisapride and erythromycin on cardiac repolarization in the isolated rabbit heart. J Cardiovasc Pharmacol 1999 Jul; 34 (1): 82-8
39. Appel-Dingemanse S, Lemarechal M-O, Kumle A, et al. Integrated modelling of the clinical pharmacokinetics of SDZ HTF 919, a novel selective 5-HT4 receptor agonist, following oral and intravenous administration. Br J Clin Pharmacol 1999 May; 47 (5): 483-91
40. Appel-Dingemanse S, Hirschberg Y, Osborne S, et al. Multiple-dose pharmacokinetics confirm no accumulation and dose proportionality of the novel promotile drug tegaserod (HTF 919). Eur J Clin Pharmacol 2001 Mar; 56 (12): 889-91
41. Appel-Dingemanse S, Rawls J, Heggland J, et al. Similar pharmacokinetics of tegaserod (HTF 919) in patients with constipation- and diarrhea-predominant irritable bowel syndrome [abstract no. 5340]. Gastroenterology 2000 Apr; 118 Suppl. 2, Pt 2 (4): A1160
42. Zhou H, McLeod J, Alladina L, et al. Pharmacokinetics (PK) of SDZ HTF 919 (HTF) not altered in subjects with severe renal insufficiency requiring hemodialysis [abstract no. PIII-108]. Clin Pharmacol Ther 1999 Feb; 65 (2): 203
43. Appel-Dingemanse S, Horowitz A, Campestrini J, et al. The pharmacokinetics of the novel promotile drug, tegaserod, are similar in healthy subjects-male and female, elderly and young. Aliment Pharmacol Ther 2001 Jul; 15 (7): 937-44
44. Appel-Dingemanse S, Hubert M, Alladina L, et al. Pharmacokinetics and safety of SDZ HTF 919, a new promotile drug: in healthy subjects and patients with hepatic cirrhosis [abstract no. ExhB5331]. Digestion 1998; 59 Suppl. 3: 736-7
45. Zhou H, Khalilieh S, Lau H, et al. Effect of meal timing not critical for the pharmacokinetics of tegaserod (HTF 919). J Clin Pharmacol 1999 Sep; 39 (9): 911-9
46. Zhou H, Khalilieh S, Campestrini J, et al. Effect of gastric pH on plasma concentrations of tegaserod (HTF 919) and its major metabolite in healthy subjects [abstract no. no. 5538]. Gastroenterology 2000 Apr; 118 Suppl. 2, Pt 2: A1206-7
47. Appel-Dingemanse S, Campestrini J, Rawls J, et al. Tegaserod pharmacokinetics (PK) are similar in different types of irritable bowel syndrome (IBS) and gastroesophageal reflux disease (GERD) [abstract no. A443]. J Gastroenterol Hepatol 2000 Mar; 15 Suppl.: B123
48. Appel-Dingemanse S. Clinical pharmacokinetics of tegaserod, a serotonin 5-HT4 receptor partial agonist with promotile activity. Clin Pharmacokinet 2002; 41 (13): 1021-42
49. Novartis Pharmaceuticals Corporation. Zelnorm™ (tegaserod maleate) tablets; prescribing information. East Hanover (NJ): Novartis Pharmaceuticals Corporation, 2002 Jul 22
50. Vickers AE, Zollinger M, Dannecker R, et al. In vitro metabolism of tegaserod in human liver and intestine: assessment of drug interactions. Drug Metab Dispos 2001 Oct; 29 (10): 1269-76
51. Zhou H, Khalilieh S, Svendsen K, et al. Tegaserod coadministration does not alter the pharmacokinetics of theophylline in healthy subjects. J Clin Pharmacol 2001 Sep; 41 (9): 987-93
52. Kalbag J, Migoya E, Osborne S, et al. Tegaserod does not significantly affect the pharmacokinetics of dextromethorphan in healthy subjects [abstract no. 5422]. Gastroenterology 2000 Apr; 118 (4 Suppl. 2, Pt 2): A1179
53. Zhou H, Horowitz A, Ledford PC, et al. The effects of tegaserod (HTF 919) on the pharmacokinetics and pharmacodynamics of digoxin in healthy subjects. J Clin Pharmacol 2001 Oct; 41 (10): 1131-9
54. Ledford P, On N, Ligueros-Saylan M, et al. Tegaserod does not significantly affect the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects [abstract no. 5445]. Gastroenterology 2000 Apr; 118 (4 Suppl. 2, Pt 2): A1184
55. Zhou H, Walter YH, Hubert M, et al. Tegaserod (HTF 919) does not decrease the effectiveness of an oral contraceptive when coadministered to healthy female subjects [abstract no. 5539]. Gastroenterology 2000 Apr; 118 (4 Suppl. 2, Pt 2): A1207
56. Kellow J, Lee OY, Chang FY, et al. An Asia-Pacific, double blind, placebo controlled, randomised study to evaluate the efficacy, safety, and tolerability of tegaserod in patients with irritable bowel syndrome. Gut 2003; 52: 671-6
57. Müller-Lissner SA, Fumagalli I, Bardhan KD, et al. Tegaserod, a 5-HT4 receptor partial agonist, relieves symptoms in irritable bowel syndrome patients with abdominal pain, bloating and constipation. Aliment Pharmacol Ther 2001 Oct; 15 (10): 1655-66
58. Novick J, Miner P, Krause R, et al. A randomized, double-blind, placebo-controlled trial of tegaserod in female patients suffering from irritable bowel syndrome with constipation. Aliment Pharmacol Ther 2002 Nov; 16 (11): 1877-88
59. Hamling J, Bang CJ, Tarpila S, et al. Titration regimen indicates partial 5-HT4 agonist HTF 919 improves symptoms of constipation predominant irritable bowel syndrome (C-IBS) [abstract no. ExhB5324]. Digestion 1998; 59 Suppl. 3: 735
60. Langaker KJ, Morris D, Pruitt R, et al. The partial 5-HT4 agonist (HTF 919) improves symptoms in constipation-predominant irritable bowel syndrome (C-IBS) [abstract no. GaPP0064]. Digestion 1998; 59 Suppl. 3: 20
61. Bardhan KD, Forbes A, Marsden CL. A clinical investigation of the effects of tegaserod treatment regimen on the symptoms of IBS-C in tegaserod responsive patients [abstract no. 053]. Gut 2003; 52 Suppl. 1: A14-5
62. Spiller RC. Problems and challenges in the design of irritable bowel syndrome clinical trials: experience from published trials. Am J Med 1999 Nov 8; 107 (5A): 91S-7S
63. De Ponti F, Tonini M. Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs 2001; 61 (3): 317-32
64. Poole RM. Tegaserod relieves global symptoms of irritable bowel syndrome. Inpharma 2002 Aug 10; 1350: 13-4
65. Novartis. Integrated summary of safety - update. 2002
66. Tougas G, Snape Jr WJ, Otten MH, et al. Long-term safety of tegaserod in patients with constipation-predominant irritable bowel syndrome. Aliment Pharmacol Ther 2002 Oct; 16 (10): 1701-8
67. Whorwell PJ, Krumholz S, Mueller Lissner S, et al. Tegaserod has a favorable safety & tolerability profile in patients with constipation predominant and alternating forms of irritable bowel syndrome (IBS) [abstract no. 5529]. Gastroenterology 2000 Apr; 118 Suppl. 2, Pt 2: A1204
68. Ruegg P, Lefkowitz M, Drossman D, et al. Tegaserod alone or in combination with antidepressant drugs is well tolerated in patients with IBS-C [abstract no. 851]. Am J Gastroenterol 2002 Sep; 97 Suppl.: S279-80
69. Earnest D, Rueegg PC, Dunger Baldauf C, et al. Diarrhea in patients treated with tegaserod for irritable bowel syndrome with constipation (IBS-C) is infrequent and usually self-limited [abstract no. 843]. Am J Gastroenterol 2002 Sep; 97 Suppl.: S277
70. Plebani G, Fried M, Michetti P, et al. Safety of tegaserod in patients with irritable bowel syndrome: the Swiss experience [abstract no. WED-G-323]. Gut 2002; 51 Suppl. III: A249
71. Fidelholtz J, Smith W, Rawls J, et al. Safety and tolerability of tegaserod in patients with irritable bowel syndrome and diarrhea symptoms. Am J Gastroenterol 2002 May; 97 (5): 1176-81
72. Novartis Pharmaceuticals Canada Inc. Prescribing information; Zelnorm™ (tegaserod hydrogen maleate) tablets. Dorval (Quebec): Novartis Pharmaceuticals Canada Inc., 2002 Feb 27
73. American Gastroenterological Association. American Gastroenterological Association medical position statement: irritable bowel syndrome. Gastroenterology 2002; 123: 2105-7
74. Jones J, Boorman J, Cann P, et al. British Society of Gastroenterology guidelines for the management of the irritable bowel syndrome. Gut 2000 Nov; 47 Suppl. 2: 1-19
75. Talley NJ. Serotoninergic neuroenteric modulators. Lancet 2001 Dec 15; 358 (9298): 2061-8
76. Harris MS. Irritable bowel syndrome: a cost-effective approach for primary care physicians. Postgrad Med 1997 Mar; 101 (3): 215-26
77. Lefkowitz MP, Rueegg PC, Shi Y, et al. Validation of a global relief measure in two clinical trials of irritable bowel syndrome with tegaserod [abstract no. 855]. Gastroenterology 2000 Apr; 118 Suppl. 2, Pt 1: A145 (plus poster)
78. Camilleri M. Management of the irritable bowel syndrome. Gastroenterology 2001 Feb; 120 (3): 652-68
79. Levy RL, Von Korff M, Whitehead WE, et al. Costs of care for irritable bowel syndrome patients in a health maintenance organization. Am J Gastroenterol 2001; 96 (11): 3122-9
80. Longstreth GF, Wilson A, Knight K, et al. Irritable bowel syndrome, health care use, and costs: a U.S. managed care perspective. Am J Gastroenterol 2003; 98 (3): 600-7
81. Leong SA, Barghout V, Birnbaum HG, et al. The economic consequences of irritable bowel syndrome: a US employer perspective. Arch Intern Med 2003; 163 (8): 929-35