Class: Anti-inflammatory Agents
VA Class: GA900
Chemical Name: 3,3′-azobis[6-hydroxybenzoic acid disodium salt
Molecular Formula: C14H8N2Na2O6
CAS Number: 6054-98-4
Anti-inflammatory agent with GI tract activity; a 5-aminosalicylic acid derivative and a prodrug of mesalamine.1 2 4
Uses for Olsalazine Sodium
Used to maintain clinical remission in patients who are intolerant of sulfasalazine.1 2 3 4 5 6
May be beneficial in the management of Crohn’s disease† involving the colon.4 40 41 42
Olsalazine Sodium Dosage and Administration
Administer orally1 2 3 4 twice daily1 2 with food.1 4
Dosage of olsalazine sodium, which is commercially available as the disodium salt, is expressed in terms of olsalazine sodium.1
Daily dosage of 1g usually provides >0.9 g of mesalamine in the colon.1
500 mg twice daily.1 2 3 4
Cautions for Olsalazine Sodium
Known hypersensitivity to salicylates, olsalazine or its metabolites, or any ingredient in the formulation.1 43
Diarrhea (reported in about 17% of patients) 1 2 3 4 6 has required discontinuance in about 6% of patients.1 2 4
Diarrhea/loose stools, possibly dose-related,1 3 tend to occur within 1 week of initiating the drug or a dosage increase.2 4
Occasionally bloody2 and difficult to distinguish from underlying disease symptoms1 or may be distinguishable by its high water content and absence of blood.4 Possibly more severe and frequent in patients with extensive ulcerative colitis.2 4 5
Usually transient and dosage reduction or increased frequency of dosing of the drug and concomitant administration of food or an antidiarrhea agent (e.g., loperamide) may reduce severity.3 4
May resolve without dosage reduction3 and once it has resolved, may not recur.4
Exacerbation of preexisting symptoms of ulcerative colitis has been reported with other 5-aminosalicylic acid derivatives (e.g., mesalamine, sulfasalazine).1
Each g of olsalazine sodium, which contains the disodium salt, provides approximately 5.78 mEq (133 mg) of sodium.1 43
Distributed into milk in rats; not known whether distributed into human milk.1 Use caution.1
Safety and efficacy not established.1 43
Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.1
Use with caution in patients with renal impairment, since renal tubular damage has been reported in animals and rarely in postmarketing surveillance;1 perform urinalysis, monitor serum creatinine and BUN concentrations in such patients.1
Common Adverse Effects
Diarrhea/loose stools,1 2 3 4 6 abdominal pain or cramps,1 4 nausea,1 4 dyspepsia,1 heartburn,1 bloating,1 anorexia,1 vomiting,1 stomatitis,1 rectal bleeding,1 headache,1 2 4 fatigue,1 2 drowsiness,1 lethargy,1 depression,1 insomnia,1 vertigo,1 dizziness or lightheadedness,1 4 rash,1 2 4 pruritus,1 arthralgia or joint pain,1 4 upper respiratory infection.1
Interactions for Olsalazine Sodium
Potential interaction (increased prothrombin time).1
Olsalazine Sodium Pharmacokinetics
Olsalazine (prodrug) has limited systemic bioavailability; about 2.4% of an oral dose may be absorbed.1 4
Most (98–99%) of an oral dose reaches the colon intact1 2 3 4 resulting in very high local concentrations of the active metabolite mesalamine.1
Plasma Protein Binding
Olsalazine: >99%;1 Mesalamine: 74%;1 N-acetyl-5-acetylsalicylic acid (a metabolite): 81%.1
Crosses placenta in animals.1
Distributed into milk in rats; not known whether distributed into human milk.1
Azo-linkage is cleaved in the colon by intestinal flora to form 2 molecules of mesalamine.1 2 3 4
Mesalamine is rapidly acetylated in colonic epithelium and liver to N-acetyl-5-acetylsalicylic acid.1 4 6
0.1% of olsalazine is metabolized in the liver to olsalazine-O-sulfate.1 4
Mesalamine is excreted principally in feces as N-acetyl-5-acetylsalicylic acid,1 4 6 and to a lesser extent in urine (about 20%) mostly as N-acetyl-5-acetylsalicylic acid;7 9 25 <1% of olsalazine excreted in urine unchanged.1
Olsalazine: approximately 0.9 hours.1 Olsalazine-O-sulfate: 7 days.1
25°C (may be exposed to 15–30°C).1
Prodrug with little or no anti-inflammatory activity until cleaved to form mesalamine (active moiety).1 2 3 4 6
Exerts local (not systemic) anti-inflammatory effects in the GI tract.1 2 3 4 7 8 9 10 11 12 13 14 15 17 18 19 21 23 24 26 27 28 29 30 31 32 35 33 34 36 38
May reduce inflammation in the colon by inhibiting cyclooxygenase and lipoxygenase, which catalyze the formation of prostaglandin precursors (endoperoxides) and of leukotrienes and hydroxyeicosatetraenoic acids, respectively, from arachidonic acid and/or its metabolites.1 4 7 8 9 11 12 13 14 15 16 18 19 20 21 23 32 35 38 39
Advice to Patients
Importance of taking with food.1
Importance of taking in equally divided doses.1
Importance of informing clinicians if diarrhea occurs.1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.1
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1
Importance of advising patients of other important precautionary information. (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
AHFS DI Essentials. © Copyright 2017, Selected Revisions September 1, 2005. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
1. Celltech. Dipentum (olsalazine) capsules prescribing information. Rochester, NY; 2002 Sep.
2. Sandberg-Gertzen H, Jarnerot G, Kraaz W. Azodisal sodium in the treatment of ulcerative colitis. A study of tolerance and relapse prevention properties. Gastroenterol. 1986:90:1024-30. (IDIS 214428)
3. Ireland A, Mason CH, Jewell DP. Controlled trial comparing olsalazine and sulphasalazine for the maintenance treatment of ulcerative colitis. Gut. 1988; 29:835-7. [PubMed 2898422]
4. Wadworth AN, Fitton A. Olsalazine. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in inflammatory bowel disease. Drugs. 19911; 41:647-64.
5. Kornbluth A, Sachar DB. Ulcerative colitis practice guidelines in adults. Am J Gastroenterol. 1997; 92:204-11. [PubMed 9040192]
6. Sandborn WJ. Rational selection of oral 5-aminosalicylate formulations and prodrugs for the treatment of ulcerative colitis. Am J Gastroenterol. 2002; 97:2939-41. (IDIS 492059)
7. Salix Pharmaceuticals. Colazal (balsalazide disodium) capsules prescribing information. Raleigh, NC; 2000 Jul.
8. Prakash A, Spencer CM. Balsalazide. Drugs. 1998; 56:83-9. [PubMed 9664201]
9. Novartis, East Hanover, NJ: Personal communication.
10. Anon. Oral balsalazide (Colazal) for ulcerative colitis. Med Lett Drugs Ther. 2001; 43:62-3. [PubMed 11468602]
11. Reid-Rowell. Rowasa (mesalamine) prescribing information. Marietta, GA; (5EKI0, 1990).
12. Reid-Rowell. Rowasa (mesalamine): a product profile. Marietta, GA; 1988 Mar.
13. Bondesen S, Rasmussen SN, Rask-Madsen J et al. 5-Aminosalicylic acid in the treatment of inflammatory bowel disease. Acta Med Scand. 1987; 221:227-42. [PubMed 3296672]
14. Weintraub M, Evans P. 5-Aminosalicylic acid: an old, ‘new’ treatment for inflammatory bowel disease. Hosp Formul. 1987; 22:528-33.
15. Peppercorn MA. Sulfasalazine and related new drugs. J Clin Pharmacol. 1987; 260-5. (IDIS 228622)
16. Reid-Rowell. Rowasa (mesalamine) product information form for the American Hospital Formulary Service. Marietta, GA; 1988 Apr. 17.
17. Anon. Mesalamine for ulcerative colitis. Med Lett Drugs Ther. 1988; 30:53-6. [PubMed 3283508]
18. Ligumsky M, Karmeli F, Sharon P et al. Enhanced thromboxane A2 and prostacyclin production by cultured rectal mucosa in ulcerative colitis and its inhibition by steroids and sulfasalazine. Gastroenterology. 1981; 81:444-9. [PubMed 6114012]
19. Sharon P, Ligumsky M, Rachmilewitz D et al. Role of prostaglandins in ulcerative colitis. Gastroenterology. 1978; 75:638-40. [PubMed 30669]
20. Lauritsen K, Laursen LS, Bukhave K et al. Effects of topical 5- aminosalicylic acid and prednisolone on prostaglandin E2 and leukotriene B4 levels determined by equilibrium in vivo dialysis of rectum in relapsing ulcerative colitis. Gastroenterology. 1986; 91:837-44. [PubMed 3017804]
21. Donowitz M. Arachidonic acid metabolites and their role in inflammatory bowel disease: update requiring addition of a pathway. Gastroenterology. 1985; 88:580-7. [PubMed 2856909]
22. Sharon P, Stenson WF. Enhanced synthesis of leukotriene B4 by colonic mucosa in inflammatory bowel disease. Gastroenterology. 1984; 86:453-60. [PubMed 6319219]
23. Kirsner JB, Shorter RG. Recent developments in ‘nonspecific’ inflammatory bowel disease: first of two parts. N Engl J Med. 1982; 306:775-85. [PubMed 7038488]
24. Campieri M, Lanfranchi GA, Boschi S et al. Topical administration of 5- aminosalicylic acid enemas in patients with ulcerative colitis: studies on rectal absorption and excretion. Gut. 1985; 26:400-5. [PubMed 3979912]
25. Dew MJ, Ebden P, Kidwai NS et al. Comparison of the absorption and metabolism of sulphasalazine and acrylic-coated 5-amino salicylic acid in normal subjects and patients with colitis. Br J Clin Pharmacol. 1984; 17:474-6. [PubMed 6144318]
26. Klotz U. Clinical pharmacokinetics of sulphasalazine, its metabolites and other prodrugs of 5-aminosalicylic acid. Clin Pharmacokinet. 1985; 10:285-302. [PubMed 2864155]
27. Campieri M, Lanfranchi GA, Brignola C et al. 5-ASA blood levels in topical treatment of ulcerative colitis: preliminary observations. Scand J Gastroenterol. 1982; 17:(Suppl)500.
28. Fischer C, Maier K, Stumpf E et al. al. Disposition of 5-aminosalicylic acid, the active metabolite of sulphasalazine, in man. Eur J Clin Pharmacol. 1983; 25:511-5. [PubMed 6140167]
29. Dew MJ, Cardwell M, Kidwai NS. et. al. 5-Aminosalicylic acid in serum and urine after administration by enema to patients with colitis. J Pharm Pharmacol. 1983; 35:323-4. [PubMed 6134804]
30. Pieniaszek HJ Jr, Bates TR. Capacity-limited gut wall metabolism of 5- aminosalicylic acid, a therapeutically active metabolite of sulfasalazine, in rats. J Pharm Sci. 1979; 68:1323-5. [PubMed 41931]
31. Klotz U, Maier K, Fischer C et al. Therapeutic efficacy of sulfasalazine and its metabolites in patients with ulcerative colitis and Crohn’s disease. N Engl J Med. 1980; 303:1499-1502. [PubMed 6107853]
32. Cooper BT. Sulphasalazine in inflammatory bowel disease: recent advances. N Z Med J. 1986; 99:757-9. [PubMed 2877428]
33. Campieri M, Lanfranchi GA, Brignola C et al. 5-Aminosalicylic acid for the treatment of inflammatory bowel diseases. Gastroenterology. 1985; 89:701-2. [PubMed 4018510]
34. Schroeder KW, Tremaine WJ, Ilstrup DM. Coated oral 5-aminosalicylic acid therapy for mildly to moderatel active ulcerative colitis. N Engl J Med. 1987; 317:1625-9. [PubMed 3317057]
35. Peskar BM, Dreyling KW, May B, et. al. Possible mode of action of 5-aminosalicylic acid. Dig Dis Sci. 1987; 32(Suppl)51-6S. (PubMed 2891468)
36. McPhee MS, Swan JT, Biddle WL et al. al. Proctocolitis unresponsive to conventional therapy. Dig Dis Sci. 1987; 32:(Suppl)76-81S. [PubMed 3319462]
37. Kirsner JB. Observations on the medical treatment of inflammatory bowel disease. JAMA. 1980; 243:557-64. [PubMed 6101350]
38. Allgayer H, Stenson WF. A comparison of effects of sulfasalazine and its metabolites on the metabolism of endogenous vs. exogenous arachidonic acid. Immunopharmacology. 1988; 15:39-46. [PubMed 2896181]
39. Hoult JRS, Page H. 5-Aminosalicylic acid, a co-factor for colonic prostacyclin synthesis? Lancet. 1981; 2:255. Letter.
40. Blomqvist P, Feltelius N, Lofberg R et al. A 10-year survey of inflammatory bowel diseases-drug therapy, costs and adverse reactions. Aliment Pharmacol Ther. 2001; 15:475-81. [PubMed 11284775]
41. Podolsky DK. Inflammatory Bowel Disease. N Engl J Med. 2002; 347:417-29. [PubMed 12167685]
42. Hanauer SB. Inflammatory bowel disease. N Engl J Med. 1996; 334:841-8 [PubMed 8596552]
43. Celltech, Rochester, NY: Personal communication.
More about olsalazine
- Side Effects
- During Pregnancy or Breastfeeding
- Dosage Information
- Drug Interactions
- Support Group
- En Español
- 0 Reviews – Add your own review/rating
- Drug class: 5-aminosalicylates
Other brands: Dipentum