Mesalamine in the treatment and maintenance of remission of ulcerative colitis

Expert Review of Clinical Pharmacology

Volumn 5, Issue 2, 2012, Pages 113-123

  Ham, Maggie ^a   Moss, Alan C ^a  

^a BETH ISRAEL DEACONESS MEDICAL CENTER   (United States)

Author keywords

5 ASA; inflammatory bowel disease; mesalamine; ulcerative colitis

Indexed keywords

AMINOSALICYLIC ACID; AZATHIOPRINE; BUDESONIDE; CYCLOSPORIN; DIVISTYRAMINE; HYDROCORTISONE; INFLIXIMAB; MERCAPTOPURINE; MESALAZINE; PLACEBO; PREDNISONE; SALAZOSULFAPYRIDINE; TIOGUANINE; TRANSFORMING GROWTH FACTOR BETA1;

ABDOMINAL PAIN; ACNE; ACUTE PANCREATITIS; AREA UNDER THE CURVE; ARTHRALGIA; ARTHRITIS; ASTHENIA; BACKACHE; BLOOD DYSCRASIA; CANCER PREVENTION; CELL CYCLE CHECKPOINT; CHEMOPROPHYLAXIS; CHILL; CLINICAL PRACTICE; COLITIS; COLORECTAL CANCER; CONJUNCTIVITIS; CONSTIPATION; COST EFFECTIVENESS ANALYSIS; COUGHING; DIARRHEA; DISEASE SEVERITY; DIZZINESS; DNA REPAIR; DRUG COST; DRUG DELIVERY SYSTEM; DRUG EFFICACY; DRUG ERUPTION; DRUG EXCRETION; DRUG FORMULATION; DRUG HYPERSENSITIVITY; DRUG METABOLISM; DRUG RELEASE; DRUG SAFETY; DRUG TOLERABILITY; DRUG UPTAKE; DYSMENORRHEA; DYSPEPSIA; ERUCTATION; FEVER; FLATULENCE; FLU LIKE SYNDROME; FOLLOW UP; HEADACHE; HEARING IMPAIRMENT; HEMOLYTIC ANEMIA; HEPATITIS; HOSPITALIZATION; HUMAN; IN VITRO STUDY; INSOMNIA; INTERSTITIAL NEPHRITIS; INTESTINE MUCOSA; LEUKOPENIA; LIVER INJURY; LIVER TOXICITY; LONG TERM CARE; MALAISE; META ANALYSIS (TOPIC); MUSCLE HYPERTONIA; MYALGIA; NAUSEA; NEPHROTOXICITY; NONHUMAN; PANCREATITIS; PATIENT COMPLIANCE; PERIPHERAL EDEMA; PH; PHARMACODYNAMICS; PHARYNGITIS; PNEUMONIA; POSTMARKETING SURVEILLANCE; PRURITUS; QUALITY OF LIFE; RANDOMIZED CONTROLLED TRIAL (TOPIC); REMISSION; REVIEW; RHINITIS; RISK REDUCTION; SELF REPORT; SIDE EFFECT; SIGNAL TRANSDUCTION; SKIN MANIFESTATION; SWEATING; THORAX PAIN; TREATMENT DURATION; TREATMENT RESPONSE; ULCERATIVE COLITIS; URINARY EXCRETION; VOMITING;

ADOLESCENT; ADULT; AGED; AGED, 80 AND OVER; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; CHILD; CHILD, PRESCHOOL; COLITIS, ULCERATIVE; HUMANS; INFANT; MESALAMINE; MIDDLE AGED; PATIENT COMPLIANCE; RANDOMIZED CONTROLLED TRIALS AS TOPIC; REMISSION INDUCTION; SEVERITY OF ILLNESS INDEX; THERAPEUTIC EQUIVALENCY; TREATMENT OUTCOME; YOUNG ADULT;

EID: 84858386221     PISSN: 17512433     EISSN: 17512441     Source Type: Journal    
DOI: 10.1586/ecp.12.2     Document Type: Review

References (86)

1. Loftus EV. Clinical epidemiology of inflammatory bowel disease: Incidence, prevalence, and environmental influences. Gastroenterology 126, 1504-1517 (2004).
2. Kornbluth A, Sachar DB. Ulcerative colitis practice guidelines in adults: American College of Gastroenterology, practice parameters committee. Am. J. Gastroenterol. 105, 501-523 (2010).
3. Loftus CG, Loftus EV, Harmsen WS et al. Update on the incidence and prevalence of Crohn's disease and ulcerative colitis in Olmsted County, Minnesota, 1940-2000. Inflamm. Bowel Dis. 13, 254-261 (2007).
4. Jess T, Loftus EV, Velayos FS et al. Risk of intestinal cancer in inflammatory bowel disease: A population-based study from Olmsted County, Minnesota. Gastroenterology 130, 1039-1046 (2006).
5. Burger D, Travis S. Conventional medical management of inflammatory bowel disease. Gastroenterology 140, 1827-1837 (2011).
6. Travis SP, Stange EF, Lemann M et al. European evidence-based consensus on the management of ulcerative colitis: Current management. J. Crohns Colitis 2, 24-62 (2008).
7. Moss AC, Cheifetz AS, Peppercorn MA. Combined oral and topical mesalazine treatment for extensive ulcerative colitis. Nat. Clin. Pract. Gastroenterol. Hepatol. 3, 290-293 (2006).
8. Moss AC, Peppercorn MA. Steroid-refractory severe ulcerative colitis: what are the available treatment options? Drugs 68, 1157-1167 (2008).
9. Lichtenstein GR, Abreu MT, Cohen R, Tremaine W. American Gastroenterological Association Institute technical review on corticosteroids, immunomodulators, and infliximab in inflammatory bowel disease. Gastroenterology 130, 940-987 (2006).
10. Lead Discovery UK. Inflammatory Bowel Diseases: World Market Report 2009-2024. Lead Discovery, Sussex, UK (2009).
11. Sonu I, Lin MV, Blonski W, Lichtenstein GR. Clinical pharmacology of 5-ASA compounds in inflammatory bowel disease. Gastroenterol. Clin. N. Am. 39, 559-599 (2010).
12. Peppercorn MA. Sulfasalazine. Pharmacology, clinical use, toxicity, and related new drug development. Ann. Intern. Med. 101, 377-386 (1984).
13. Sandborn WJ, Hanauer SB. Systematic review: The pharmacokinetic profiles of oral mesalazine formulations and mesalazine pro-drugs used in the management of ulcerative colitis. Aliment. Pharmacol. Ther. 17, 29-42 (2003).
14. Akiho H, Ihara E, Motomura Y, Nakamura K. Cytokine-induced alterations of gastrointestinal motility in gastrointestinal disorders. World J. Gastrointest. Pathophysiol. 2, 72-81 (2011).
15. Fujiwara M, Mitsui K, Yamamoto I. Inhibition of proliferative responses and interleukin 2 productions by salazosulfapyridine and its metabolites. Jap. J. Pharmacol. 54, 121-131 (1990).
16. Doering J, Begue B, Lentze MJ et al. Induction of T lymphocyte apoptosis by sulphasalazine in patients with Crohn's disease. Gut 53, 1632-1638 (2004).
17. Liptay S, Bachem M, Hacker G, Adler G, Debatin KM, Schmid RM. Inhibition of nuclear factor kB and induction of apoptosis in T-lymphocytes by sulfasalazine. Br. J Pharmacol. 128, 1361-1369 (1999).
18. Dubuquoy L, Rousseaux C, Thuru X et al. PPARg as a new therapeutic target in inflammatory bowel diseases. Gut 55, 1341-1349 (2006).
19. Pedersen G, Brynskov J. Topical rosiglitazone treatment improves ulcerative colitis by restoring peroxisome proliferator-activated receptor-g activity. Am. J. Gastroenterol. 105, 1595-1603 (2010).
20. Rousseaux C, Lefebvre B, Dubuquoy L et al. Intestinal antiinflammatory effect of 5-aminosalicylic acid is dependent on peroxisome proliferator- activated receptor-g. J. Exp. Med. 201, 1205-1215 (2005).
21. Fernandez-Becker NQ, Moss AC. Improving delivery of aminosalicylates in ulcerative colitis: Effect on patient outcomes. Drugs 68, 1089-1103 (2008).
22. Brunner M, Greinwald R, Kletter K et al. Gastrointestinal transit and release of 5-aminosalicylic acid from 153Sm-labelled mesalazine pellets vs. tablets in male healthy volunteers. Aliment. Pharmacol. Ther. 17, 1163-1169 (2003).
23. Layer PH, Goebell H, Keller J, Dignass A, Klotz U. Delivery and fate of oral mesalamine microgranules within the human small intestine. Gastroenterology 108, 1427-1433 (1995).
24. Lichtenstein GR, Kamm MA. Review article: 5-aminosalicylate formulations for the treatment of ulcerative colitis - methods of comparing release rates and delivery of 5-aminosalicylate to the colonic mucosa. Aliment. Pharmacol. Ther. 28, 663-673 (2008).
25. Yang LP, McCormack PL. MMX® mesalazine: A review of its use in the management of mild to moderate ulcerative colitis. Drugs 71, 221-235 (2011).
26. Lawlor G, Ahmed A, Moss AC. Once-daily mesalamine granules for ulcerative colitis. Expert Rev. Clin. Immunol. 6, 521-526 (2010).
27. Rasmussen SN, Bondesen S, Hvidberg EF et al. 5-aminosalicylic acid in a slow-release preparation: bioavailability, plasma level, and excretion in humans. Gastroenterology 83, 1062-1070 (1982).
28. Ford AC, Achkar JP, Khan KJ et al. Efficacy of 5-aminosalicylates in ulcerative colitis: systematic review and meta-analysis. Am. J. Gastroenterol. 106, 601-616 (2011).
29. Sutherland L, Macdonald JK. Oral 5-aminosalicylic acid for induction of remission in ulcerative colitis. Cochrane Database Syst. Rev. CD000543 (2006).
30. Lichtenstein GR, Rutgeerts P. Importance of mucosal healing in ulcerative colitis. Inflamm. Bowel Dis. 16, 338-346 (2010).
31. Hanauer SB, Sandborn WJ, Dallaire C et al. Delayed-release oral mesalamine 4.8 g/day (800 mg tablets) compared to 2.4 g/day (400 mg tablets) for the treatment of mildly to moderately active ulcerative colitis: The ASCEND I trial. Can. J. Gastroenterol. 21, 827-834 (2007).
32. Kruis W, Bar-Meir S, Feher J et al. The optimal dose of 5-aminosalicylic acid in active ulcerative colitis: A dose-finding study with newly developed mesalamine. Clin. Gastroenterol. Hepatol. 1, 36-43 (2003).
33. Hanauer S, Schwartz J, Robinson M et al. Mesalamine capsules for treatment of active ulcerative colitis: Results of a controlled trial. Pentasa study group. Am. J. Gastroenterol. 88, 1188-1197 (1993).
34. Sandborn WJ, Kamm MA, Lichtenstein GR, Lyne A, Butler T, Joseph RE. MMX multi matrix system mesalazine for the induction of remission in patients with mild-to-moderate ulcerative colitis: A combined analysis of two randomized, double-blind, placebo-controlled trials. Aliment. Pharmacol. Ther. 26, 205-215 (2007).
35. Orchard TR, van der Geest SA, Travis SP. Randomised clinical trial: Early assessment after 2 weeks of high-dose mesalazine for moderately active ulcerative colitis - new light on a familiar question. Aliment. Pharmacol. Ther. 33, 1028-1035 (2011).
36. Lichtenstein GR, Ramsey D, Rubin DT. Randomised clinical trial: Delayed-release oral mesalazine 4.8 g/day vs. 2.4 g/day in endoscopic mucosal healing - ASCEND I and II combined analysis. Aliment. Pharmacol. Ther. 33, 672-678 (2011).
37. Siegel CA. Accidentally ASCENDing into comparative effective research for inflammatory bowel disease. Gastroenterology 137, 1880-1882 (2009).
38. Cooney RM, Warren BF, Altman DG, Abreu MT, Travis SP. Outcome measurement in clinical trials for ulcerative colitis: Towards standardisation. Trials 8, 17 (2007).
39. Ito H, Iida M, Matsumoto T et al. Direct comparison of two different mesalamine formulations for the induction of remission in patients with ulcerative colitis: A double-blind, randomized study. Inflamm. Bowel Dis. 16, 1567-1574 (2010).
40. Harris MS, Lichtenstein GR. Review article: Delivery and efficacy of topical 5-aminosalicylic acid (mesalazine) therapy in the treatment of ulcerative colitis. Aliment. Pharmacol. Ther. 33, 996-1009 (2011).
41. Hoivik ML, Moum B, Solberg IC et al. Health-related quality of life in patients with ulcerative colitis after a 10-year disease course: Results from the IBSEN study. Inflamm. Bowel Dis. doi:10.1002/ibd.21863 (2011) (Epub ahead of print).
42. Guyatt G, Mitchell A, Irvine EJ et al. A new measure of health status for clinical trials in inflammatory bowel disease. Gastroenterology 96, 804-810 (1989).
43. Prantera C, Kohn A, Campieri M et al. Clinical trial: ulcerative colitis maintenance treatment with 5-ASA: A 1-year, randomized multicentre study comparing MMX with Asacol. Aliment Pharmacol. Ther. 30, 908-918 (2009).
44. [No authors listed]. An oral preparation of mesalamine as long-term maintenance therapy for ulcerative colitis. A randomized, placebo-controlled trial. The Mesalamine Study Group. Ann. Intern. Med. 124, 204-211 (1996).
45. Mulder CJ, Tytgat GN, Weterman IT et al. Double-blind comparison of slow-release 5-aminosalicylate and sulfasalazine in remission maintenance in ulcerative colitis. Gastroenterology 95, 1449-1453 (1988).
46. Moss AC, Peppercorn MA. The risks and the benefits of mesalazine as a treatment for ulcerative colitis. Expert Opin. Drug Saf. 6, 99-107 (2007).
47. Gupta MK, Pollack S, Hutchings JJ. Mesalamine induced symptom exacerbation of ulcerative colitis: Case report and brief discussion. World J. Gastrointest. Pharmacol. Ther. 1, 132-134 (2010).
48. Ransford RA, Langman MJ. Sulphasalazine and mesalazine: serious adverse reactions re-evaluated on the basis of suspected adverse reaction reports to the Committee on Safety of Medicines. Gut 51, 536-539 (2002).
49. Pitchumoni CS, Rubin A, Das K. Pancreatitis in inflammatory bowel diseases. J. Clin. Gastroenterol. 44, 246-253 (2010).
50. Marteau P, Nelet F, Le Lu M, Devaux C. Adverse events in patients treated with 5-aminosalicyclic acid: 1993-1994 pharmacovigilance report for pentasa in France. Aliment. Pharmacol. Ther. 10, 949-956 (1996).
51. Gisbert JP, Gonzalez-Lama Y, Mate J. 5-aminosalicylates and renal function in inflammatory bowel disease: A systematic review. Inflamm. Bowel Dis. 13, 629-638 (2007).
52. Patel H, Barr A, Jeejeebhoy KN. Renal effects of long-term treatment with 5-aminosalicylic acid. Can. J. Gastroenterol. 23, 170-176 (2009).
53. Van Staa TP, Travis S, Leufkens HG, Logan RF. 5-aminosalicylic acids and the risk of renal disease: A large British epidemiologic study. Gastroenterology 126, 1733-1739 (2004).
54. Alivanis P, Aperis G, Lambrianou F et al. Reversal of refractory sulfasalazine-related renal failure after treatment with corticosteroids. Clin. Ther. 32, 1906-1910 (2010).
55. Khokhar OS, Lewis JH. Hepatotoxicity of agents used in the management of inflammatory bowel disease. Dig. Dis. 28, 508-518 (2010).
56. Hauser R, Duty S, Godfrey-Bailey L, Calafat AM. Medications as a source of human exposure to phthalates. Environ. Health Perspect. 112, 751-753 (2004).
57. Huang PC, Kuo PL, Chou YY, Lin SJ, Lee CC. Association between prenatal exposure to phthalates and the health of newborns. Environ. Int. 35, 14-20 (2009).
58. Swan SH. Environmental phthalate exposure in relation to reproductive outcomes and other health endpoints in humans. Environ. Res. 108, 177-184 (2008).
59. Gearry RB, Barclay ML. Azathioprine and 6-mercaptopurine pharmacogenetics and metabolite monitoring in inflammatory bowel disease. J. Gastroenterol. Hepatol. 20, 1149-1157 (2005).
60. Hande S, Wilson-Rich N, Bousvaros A et al. 5-aminosalicylate therapy is associated with higher 6-thioguanine levels in adults and children with inflammatory bowel disease in remission on 6-mercaptopurine or azathioprine. Inflamm. Bowel Dis. 12, 251-257 (2006).
61. Lowry PW, Franklin CL, Weaver AL et al. Leucopenia resulting from a drug interaction between azathioprine or 6-mercaptopurine and mesalamine, sulphasalazine, or balsalazide. Gut 49, 656-664 (2001).
62. Campbell S, Ghosh S. Effective maintenance of inflammatory bowel disease remission by azathioprine does not require concurrent 5-aminosalicylate therapy. Eur. J. Gastroenterol. Hepatol. 13, 1297-1301 (2001).
63. Mantzaris GJ, Sfakianakis M, Archavlis E et al. A prospective randomized observer-blind 2-year trial of azathioprine monotherapy versus azathioprine and olsalazine for the maintenance of remission of steroid-dependent ulcerative colitis. Am. J. Gastroenterol. 99, 1122-1128 (2004).
64. Katsanos KH, Tatsioni A, Pedersen N et al. Cancer in inflammatory bowel disease 15 years after diagnosis in a population-based European collaborative follow-up study. J. Crohns Colitis 5, 430-442 (2011).
65. Terdiman JP. The prevention of colitis-related cancer by 5-aminosalicylates: An appealing hypothesis that remains unproven. Am. J. Gastroenterol. 106, 737-740 (2011).
66. Brown JB, Lee G, Managlia E et al. Mesalamine inhibits epithelial b-catenin activation in chronic ulcerative colitis. Gastroenterology 138, 595-605 (2010).
67. Koelink PJ, Mieremet-Ooms MA, Corver WE et al. 5-aminosalicylic acid interferes in the cell cycle of colorectal cancer cells and induces cell death modes. Inflamm. Bowel Dis. 16, 379-389 (2010).
68. Lashner BA, Provencher KS, Seidner DL, Knesebeck A, Brzezinski A. The effect of folic acid supplementation on the risk for cancer or dysplasia in ulcerative colitis. Gastroenterology 112, 29-32 (1997).
69. Pinczowski D, Ekbom A, Baron J, Yuen J, Adami HO. Risk factors for colorectal cancer in patients with ulcerative colitis: A case-control study. Gastroenterology 107, 117-120 (1994).
70. Tang J, Sharif O, Pai C, Silverman AL. Mesalamine protects against colorectal cancer in inflammatory bowel disease. Dig. Dis. Sci. 55, 1696-1703 (2010).
71. Velayos FS, Terdiman JP, Walsh JM. Effect of 5-aminosalicylate use on colorectal cancer and dysplasia risk: A systematic review and metaanalysis of observational studies. Am. J. Gastroenterol. 100, 1345-1353 (2005).
72. Bernstein CN, Nugent Z, Blanchard JF. 5-aminosalicylate is not chemoprophylactic for colorectal cancer in IBD: A population based study. Am. J. Gastroenterol. 106, 731-736 (2011).
73. Terdiman JP, Johnson LK, Kim YS et al. Chemoprevention of colonic polyps with balsalazide: An exploratory, double-blind, placebo-controlled study. Dig. Dis. Sci. 54, 2488-2496 (2009).
74. Kane SV, Cohen RD, Aikens JE, Hanauer SB. Prevalence of nonadherence with maintenance mesalamine in quiescent ulcerative colitis. Am. J. Gastroenterol. 96, 2929-2933 (2001).
75. Moshkovska T, Stone MA, Clatworthy J et al. An investigation of medication adherence to 5-aminosalicylic acid therapy in patients with ulcerative colitis, using self-report and urinary drug excretion measurements. Aliment. Pharmacol. Ther. 30, 1118-1127 (2009).
76. Kane SV. Systematic review: Adherence issues in the treatment of ulcerative colitis. Aliment. Pharmacol. Ther. 23, 577-585 (2006).
77. Kane SV, Robinson A. Review article: understanding adherence to medication in ulcerative colitis - innovative thinking and evolving concepts. Aliment. Pharmacol. Ther. 32, 1051-1058 (2010).
78. Moss AC, Beusterien K, Ahmed A, Cheifetz AS, Devlen J, Yen L. Factors influencing adherence to mesalamine in patients with inflammatory bowel disease: A patient-reported qualitative analysis. Am. J. Gastroenterol. 106(S2), S442 (2011).
79. Higgins PD, Rubin DT, Kaulback K, Schoenfield PS, Kane SV. Systematic review: Impact of non-adherence to 5-aminosalicylic acid products on the frequency and cost of ulcerative colitis flares. Aliment. Pharmacol. Ther. 29, 247-257 (2009).
80. Kane S, Shaya F. Medication non-adherence is associated with increased medical health care costs. Dig. Dis. Sci. 53, 1020-1024 (2008).
81. Moss AC, Chaudhary N, Tukey M et al. Impact of a patient-support program on mesalamine adherence in patients with ulcerative colitis - A prospective study. J. Crohns Colitis 4, 171-175 (2010).
82. Moshkovska T, Stone MA, Smith RM, Bankart J, Baker R, Mayberry JF. Impact of a tailored patient preference intervention in adherence to 5-aminosalicylic acid medication in ulcerative colitis: Results from an exploratory randomized controlled trial. Inflamm. Bowel Dis. 17, 1874-1881 (2011).
83. Sandborn WJ, Korzenik J, Lashner B et al. Once-daily dosing of delayed-release oral mesalamine (400-mg tablet) is as effective as twice-daily dosing for maintenance of remission of ulcerative colitis. Gastroenterology 138, 1286-1296 (2010).
84. Lahiff C, Kane S, Moss AC. Drug development in inflammatory bowel disease: The role of the FDA. Inflamm. Bowel Dis. 17(12), 2585-2593 (2011).
85. Ito H, Iida M, Matsumoto T et al. Direct comparison of two different mesalamine formulations for the maintenance of remission in patients with ulcerative colitis: A double-blind, randomized study. Inflamm. Bowel Dis. 16, 1575-1582 (2010).
86. Pimpo MT, Galletti B, Palumbo G et al. Mesalazine vanishing time from rectal mucosa following its topical administration. J. Crohns Colitis 4, 102-105 (2010).