Balsalazide

Balsalazide disodium is delivered intact to the colon where it is cleaved by bacterial azoreduction to release equimolar quantities of mesalamine, which is the therapeutically active portion of the molecule, and the 4-aminobenzoyl-β-alanine carrier moiety. The carrier moiety released when balsalazide disodium is cleaved is only minimally absorbed and is largely inert.

• Balsalazide disodium capsules are indicated for the treatment of mildly to moderately active ulcerative colitis in patients 5 years of age and older. Limitations of Use: Safety and effectiveness of balsalazide disodium capsules beyond 8 weeks in pediatric patients 5 years to 17 years of age and 12 weeks in adults have not been established.ICD-10: K51.90

• Balsalazide disodium capsules are contraindicated in patients with known or suspected hypersensitivity to salicylates, aminosalicylates, or to any of the components of balsalazide disodium capsules or balsalazide metabolites [see Warnings and Precautions ( 5.3 ), Adverse Reactions ( 6.2 ), Description ( 11 )] . Known or suspected hypersensitivity to salicylates, aminosalicylates, or any of the components of balsalazide disodium capsules or balsalazide metabolites.contraindicated

Administration Instructions: Evaluate renal function before initiating therapy with balsalazide disodium capsules. ( 2.1 ) Swallow capsules whole. Do not cut, break, crush or chew. ( 2.1 ) For patients who cannot swallow intact capsules, the capsules may be opened and sprinkled on applesauce, then chewed and swallowed immediately. ( 2.1 ) Teeth and/or tongue staining may occur when administered sprinkled on applesauce. ( 2.1 ) Drink an adequate amount of fluids. ( 2.1 , 5.8 ) Take balsalazide disodium capsules with or without food. ( 2.1 ) Dosage: Adults: The recommended dosage is 2.25 g (three 750 mg capsules) three times daily for 8 weeks. Some adult patients required treatment for up to 12 weeks in clinical trials. ( 2.2 ) Pediatric Patients 5 Years to 17 Years of Age: The recommended dosage is either : 2.25 g (three 750 mg capsules) three times for up to 8 weeks. OR: 750 mg (one capsule) three times daily for up to 8 weeks. ( 2.2 ) 2.1 Important Preparation and Administration Instructions Evaluate renal function before initiating therapy with balsalazide disodium capsules [see Warnings and Precaution ( 5.1 )] . Swallow balsalazide disodium capsules whole. Do not cut, break, crush or chew the capsules. For patients who cannot swallow intact capsules, balsalazide disodium capsules may also be administered by opening the capsule and sprinkling the capsule contents on applesauce.

Renal Impairment: Assess renal function at the beginning of treatment and periodically during treatment. Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function. Discontinue if renal function deteriorates. ( 5.1 , 7.1 , 8.6 ) Mesalamine-Induced Acute Intolerance Syndrome: Symptoms may be difficult to distinguish from an exacerbation of ulcerative colitis; monitor for worsening symptoms; discontinue treatment if acute intolerance syndrome is suspected. ( 5.2 ) Hypersensitivity Reactions, including Myocarditis and Pericarditis : Evaluate patients immediately and discontinue if a hypersensitivity reaction is suspected. ( 5.3 ) Hepatic Failure : Evaluate the risks and benefits in patients with known liver impairment. ( 5.4 ) Severe Cutaneous Adverse Reactions : Discontinue at the first signs or symptoms of severe cutaneous adverse reactions or other signs of hypersensitivity and consider further evaluation ( 5.5 ) Upper Gastrointestinal Tract Obstruction : Avoid in patients with pyloric stenosis or other organic or functional obstruction. ( 5.6 ) Photosensitivity : Advise patients with pre-existing skin conditions to avoid sun exposure, wear protective clothing, and use a broad-spectrum sunscreen when outdoors. ( 5.7 ) Nephrolithiasis : Stones containing mesalamine, the active moiety in balsalazide disodium capsules, are undetectable by standard radiography or computed tomography (CT). Ensure adequate fluid intake during treatment with balsalazide disodium capsules.

The following clinically significant adverse reactions are described elsewhere in labeling: Renal Impairment [see Warnings and Precautions ( 5.1 )] Mesalamine-Induced Acute Intolerance Syndrome [see Warnings and Precautions ( 5.2 )] Hypersensitivity Reactions [see Warnings and Precautions ( 5.3 )] Hepatic Failure [see Warnings and Precautions ( 5.4 )] Severe Cutaneous Adverse Reactions [see Warnings and Precautions ( 5.5 )] Upper Gastrointestinal Tract Obstruction [see Warnings and Precautions ( 5.6 )] Photosensitivity [see Warnings and Precautions ( 5.7 )] Nephrolithiasis [see Warnings and Precautions ( 5.8 )] Most common adverse reactions (≥3%) are: headache, abdominal pain, diarrhea, nausea, vomiting, respiratory infection, and arthralgia. Adverse reactions in pediatric patients were similar. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Hikma Pharmaceuticals USA Inc. at 1-800-962-8364 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adult Ulcerative Colitis: During clinical development, 259 adult patients with active ulcerative colitis were exposed to 6.75 g/day balsalazide in 4 controlled trials.

Geriatric Patients : Increased risk of blood dyscrasias; monitor blood cell counts and platelet counts. ( 8.5 ) 8.1 Pregnancy Risk Summary: Published data from meta-analyses, cohort studies and case series on the use of mesalamine, the active moiety of balsalazide, during pregnancy have not reliably informed an association with mesalamine and major birth defects, miscarriage, or adverse maternal or fetal outcomes (see Data) . There are adverse effects on maternal and fetal outcomes associated with ulcerative colitis in pregnancy (see Clinical Considerations) . In animal reproduction studies, there were no adverse developmental effects observed after oral administration of balsalazide disodium in pregnant rats and rabbits during organogenesis at doses up to 2.4 and 4.7 times, respectively, the maximum recommended human dose (MRHD) (see Data) . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Metabolism

Balsalazide disodium capsules contain a powder of balsalazide disodium that is insoluble in acid and designed to be delivered to the colon as the intact prodrug. Upon reaching the colon, bacterial azoreductases cleave the compound to release 5-ASA, the therapeutically active portion of the molecule, and 4-aminobenzoyl-β-alanine.

Balsalazide disodium is an aminosalicylate, and symptoms of salicylate toxicity include: nausea, vomiting and abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe salicylate intoxication may lead to electrolyte and blood pH imbalance and potentially to other organ (e.g., renal and liver) damage. There is no specific antidote for balsalazide overdose; however, conventional therapy for salicylate toxicity may be beneficial in the event of acute overdosage and may include gastrointestinal tract decontamination to prevent further absorption. Proper medical care should be sought immediately with appropriate supportive care, including the possible use of emesis, cathartics, and activated charcoal to prevent further absorption. Correct fluid and electrolyte imbalance by the administration of appropriate intravenous therapy and maintain adequate renal function.

• Dec 28, 2007ANDAANDA077883Apotex
• Dec 28, 2007ANDAANDA077806Hikma
• Jun 8, 2023ANDAANDA217592Zydus Lifesciences
• Apr 3, 2025ANDAANDA219422Carnegie

1. 1Diarrhoea438.6%
2. 2Drug Ineffective438.6%
3. 3Injection Site Pain397.8%
4. 4Colitis Ulcerative326.4%
5. 5Fatigue316.2%
6. 6Arthralgia306.0%
7. 7Off Label Use295.8%
8. 8Nausea285.6%
9. 9Rash234.6%
10. 10Headache214.2%
11. 11Pain193.8%
12. 12Asthenia183.6%
13. 13Dyspnoea183.6%
14. 14Incorrect Dose Administered183.6%
15. 15Insomnia173.4%

The 9 most recently updated of 9 ClinicalTrials.gov registrations naming Balsalazide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Fasting Study of Balsalazide Disodium Capsules 750 mg and Colazal® Capsules 750 mg
  Completed · Phase 1 · Interventional · 80 enrolled · Mylan Pharmaceuticals Inc
  NCT00648531updated 2024-04-24
• Fed Study of Balsalazide Disodium Capsules 750 mg and Colazal® Capsules 750 mg
  Completed · Phase 1 · Interventional · 60 enrolled · Mylan Pharmaceuticals Inc
  NCT00649480updated 2024-04-24
• Assessment of 5-Aminosalicylic Acid Prescription Patterns and Treatment Outcomes in Patients With Ulcerative Colitis in Korea
  Completed · Observational · 11,385 enrolled · Ferring Pharmaceuticals
  NCT04499495updated 2022-09-10
• New Tablet Formulation and Dosing Regimen of Balsalazide Disodium in Mildly to Moderately Active Ulcerative Colitis
  Completed · Phase 3 · Interventional · 225 enrolled · Bausch Health Americas, Inc.
  NCT00269438updated 2019-11-25
• Balsalazide Disodium vs. Mesalamine in Mildly to Moderately Active Ulcerative Colitis
  Completed · Phase 3 · Interventional · 400 enrolled · Bausch Health Americas, Inc.
  NCT00408174updated 2019-11-25
• Randomized Placebo-Controlled Trial of Budesonide Multi-Matrix System (MMX®) 9 Milligrams (mg) in Participants With Ulcerative Colitis Currently on a 5-Aminosalicylic Acid (5-ASA)
  Completed · Phase 3 · Interventional · 510 enrolled · Bausch Health Americas, Inc.
  NCT01532648updated 2019-09-06
• Open-Label, Long-term Balsalziade Disodium Tablet Ulcerative Colitis Study
  Completed · Phase 3 · Interventional · 443 enrolled · Bausch Health Americas, Inc.
  NCT00486031updated 2019-08-15
• A Single Dose, 2-Period, 2-Treatment, 2-Way Crossover Bioequivalency Study of Balsalazide Disodium 750 mg Capsules Under Fasting Conditions
  Completed · Interventional · 52 enrolled · Roxane Laboratories
  NCT00618202updated 2018-01-23
• Bioequivalency Study of Balsalazide Capsules Under Fasting Conditions
  Completed · Interventional · 52 enrolled · Roxane Laboratories
  NCT00618228updated 2018-01-23

Frequently asked questions

How does Balsalazide work?

Balsalazide disodium is delivered intact to the colon where it is cleaved by bacterial azoreduction to release equimolar quantities of mesalamine, which is the therapeutically active portion of the molecule, and the 4-aminobenzoyl-β-alanine carrier moiety. The carrier moiety released when balsalazide disodium is cleaved is only minimally absorbed and is largely inert.

What is Balsalazide used for?

According to FDA labeling, Balsalazide carries indications including: Balsalazide disodium capsules are indicated for the treatment of mildly to moderately active ulcerative colitis in patients 5 years of age and older. Limitations of Use: Safety and effectiveness of balsalazide disodium capsules beyond 8 weeks in pediatric patients 5 years to 17 years of age and 12 weeks in adults have not been established.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Balsalazide?

Balsalazide is classified as Aminosalicylic acid and similar agents, Aminosalicylate, Cyclooxygenase Inhibitors, Lipoxygenase Inhibitors, Decreased Platelet Aggregation, Decreased Prostaglandin Production, Decreased Thromboxane Production.

What are the brand names for Balsalazide?

Balsalazide is marketed under brand names including Colazal.

What are the contraindications for Balsalazide?

Balsalazide labeling lists contraindications including: Balsalazide disodium capsules are contraindicated in patients with known or suspected hypersensitivity to salicylates, aminosalicylates, or to any of the components of balsalazide disodium capsules or balsalazide metabolites [see Warnings and Precautions ( 5.3 ), Adverse Reactions ( 6.2 ), Description ( 11 )] . Known or suspected hypersensitivity to salicylates, aminosalicylates, or any of the components of balsalazide disodium capsules or balsalazide metabolites.. Always consult the full prescribing information and a clinician.