Class: Anti-inflammatory Agents
VA Class: GA900
Chemical Name: 5-[[4-[[(2-carboxyethyl)amino]carbonyl]-phenyl]azo]-2-hydroxybenzoic acid disodium dihydrate
Molecular Formula: C17H13N3Na2O6•2H2O
CAS Number: 150399-21-6
Anti-inflammatory agent with GI tract activity; prodrug of mesalamine.
Uses for Balsalazide
Management of active, mild to moderate ulcerative colitis.
May be beneficial in the management of Crohn's disease† involving the colon.
Balsalazide Dosage and Administration
Administer orally 3 times daily.
Available as balsalazide disodium; dosage expressed in terms of the salt.
Daily dosage of 6.75 g is equivalent to mesalamine 2.4 g.
2.25 g (three 750-mg capsules) 3 times daily for 8 weeks. Some patients may require up to 12 weeks of therapy.
2–6 g daily may be used.
Safety and efficacy not established beyond 12 weeks.
Cautions for Balsalazide
Known hypersensitivity to salicylates, balsalazide or its metabolites, or any ingredient in the formulation.
Exacerbation of preexisting symptoms of ulcerative colitis has been reported rarely.
Potential for prolonged gastric retention of basalazide capsules in patients with pyloric stenosis.
Each g of balsalazide disodium (as commercially available 750-mg capsules) provides approximately 5 mEq (115 mg) of sodium.
Not known whether balsalazide is distributed into milk. Caution if used in nursing women.
Safety and efficacy not established in children <18 years of age.
Insufficient experience in patients >65 years of age to determine whether geriatric patients respond differently than younger adults.
Safety and efficacy not established in patients with hepatic impairment.
Safety and efficacy not established in patients with renal impairment. Use with caution in patients with renal impairment or a history of renal disease, since renal toxicity has been reported in patients receiving other mesalamine preparations.
Common Adverse Effects
Headache, abdominal pain, diarrhea, nausea, vomiting, respiratory infection, arthralgia, flatulence, fatigue.
Interactions for Balsalazide
Potential for interference with bacterial metabolism and release of mesalamine in the colon
Theoretical; no formal interaction studies to date
Immunosuppressive agents (azathioprine, mercaptopurine)
Potential for interference with metabolism of immunosuppressive agents by thiopurine methyltransferase
Absolute bioavailability undetermined in healthy individuals; absorption very limited and variable.
Systemic exposure (based on mean AUC) in ulcerative colitis patients receiving 1.5 g twice daily for 1 year is up to 60 times greater than that in healthy individuals receiving the same dosage.
Plasma Protein Binding
Azo-linkage is cleaved in the colon by intestinal flora to form mesalamine and 4-aminobenzoyl-β-alanine.
In healthy individuals, excreted principally in feces as metabolites (65%) and unchanged drug (<1%); also excreted in urine as N-acetylated metabolites (up to 25%) and unchanged drug (<1%).
In ulcerative colitis patients in remission after 1 year of balsalazide therapy, excreted in urine as N-acetylated metabolites (20–25%), mesalamine (<4%), and unchanged drug (<1%); fecal elimination not studied.
25°C (may be exposed to 15–30°C).
Prodrug with little or no pharmacologic activity until cleaved to form mesalamine (active moiety) and 4-aminobenzoyl-β-alanine.
Exerts local (not systemic) anti-inflammatory effects in the GI tract.
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.
Advice to Patients
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.
Importance of informing 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 2022, Selected Revisions May 1, 2006. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
More about balsalazide
- Side effects
- Drug interactions
- Dosage information
- During pregnancy or Breastfeeding
- Reviews (24)
- Drug images
- Compare alternatives
- Pricing & coupons
- En español
- Drug class: 5-aminosalicylates