Usage
Balsalazide is prescribed for the treatment of mildly to moderately active ulcerative colitis in patients 5 years of age and older. Its pharmacological classification is as an anti-inflammatory agent, specifically an aminosalicylate. Balsalazide is a prodrug of mesalamine; it is converted to mesalamine in the colon. The mechanism of action of mesalamine is not fully understood but is thought to involve local inhibition of prostaglandin synthesis and other inflammatory mediators in the colonic mucosa.
Alternate Names
Balsalazide disodium is the chemical name. Brand names include Colazal and Giazo (specifically for adult males).
How It Works
Pharmacodynamics: Balsalazide exerts its therapeutic effect through its active metabolite, mesalamine, which acts locally in the colonic mucosa to reduce inflammation. The exact mechanism of action is not fully elucidated but is believed to involve the inhibition of inflammatory mediators, particularly prostaglandins and leukotrienes.
Pharmacokinetics: Balsalazide is administered orally. It exhibits low and variable absorption in the gastrointestinal tract, delivering a substantial portion of the drug intact to the colon. The drug is then converted by colonic bacteria into mesalamine (5-aminosalicylic acid), the active moiety, and an inactive metabolite. Balsalazide is highly protein-bound (≥99%). Mesalamine is eliminated primarily through fecal excretion, with a small amount undergoing renal excretion. The half-life of mesalamine is approximately 12 hours (range 2-15 hours). Balsalazide itself is not extensively metabolized by CYP enzymes.
Dosage
Standard Dosage
Adults:
- Capsules (Colazal): 2.25 g (three 750 mg capsules) three times daily for 8-12 weeks.
- Tablets (Giazo, for males only): 3.3 g (three 1.1 g tablets) twice daily for up to 8 weeks.
Children (5-17 years):
- Capsules: 2.25 g (three 750 mg capsules) three times daily for up to 8 weeks OR 750 mg (one capsule) three times daily for up to 8 weeks.
Special Cases:
- Elderly Patients: Use with caution; renal function should be monitored.
- Patients with Renal Impairment: Use with caution. Evaluate renal function before and during therapy. Dosage adjustment may be needed.
- Patients with Hepatic Dysfunction: Use with caution. Liver function testing should be considered. Dosage adjustment may be needed.
- Patients with Comorbid Conditions: Consider sodium content in patients on sodium-restricted diets (each gram of balsalazide disodium provides approximately 5 mEq (115 mg) of sodium).
Clinical Use Cases
Balsalazide is specifically indicated for the treatment of mildly to moderately active ulcerative colitis. Its use in other clinical settings, such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations, is not established.
Dosage Adjustments
Dosage adjustments may be necessary in patients with renal or hepatic impairment. Careful monitoring of renal and liver function is advised.
Side Effects
Common Side Effects:
Headache, abdominal pain, diarrhea, nausea, vomiting, respiratory infection, arthralgia, fever, sore throat, insomnia, loss of appetite.
Rare but Serious Side Effects:
Allergic reactions (anaphylaxis, bronchospasm, skin rash), worsening of ulcerative colitis symptoms, renal impairment, liver problems, anemia, pancreatitis, pericarditis, myocarditis.
Long-Term Effects:
Potential long-term effects of balsalazide are not fully established but may include the adverse effects listed above if they persist or worsen with prolonged use.
Adverse Drug Reactions (ADR):
Clinically significant ADRs include severe allergic reactions, worsening colitis symptoms, renal or hepatic dysfunction, and blood dyscrasias. These require prompt medical intervention.
Contraindications
Hypersensitivity to salicylates, aminosalicylates, balsalazide, or any components of the formulation.
Drug Interactions
Although balsalazide and its metabolites are not expected to inhibit major CYP enzymes, clinically significant interactions may occur with other medications, including antibiotics, nonsteroidal anti-inflammatory drugs (NSAIDs), and immunomodulators. Consult a comprehensive drug interaction database for specific interactions.
Pregnancy and Breastfeeding
Pregnancy Safety Category B. While animal studies have not shown fetal harm, there are no adequate and well-controlled studies in pregnant women. Balsalazide should be used during pregnancy only if clearly needed. It is not known whether balsalazide is excreted in human milk, though its metabolite, mesalamine, is. Caution should be exercised when administering balsalazide to nursing women. Monitor infants for diarrhea.
Drug Profile Summary
- Mechanism of Action: Local anti-inflammatory action in the colonic mucosa via inhibition of prostaglandin synthesis and other inflammatory mediators.
- Side Effects: Headache, abdominal pain, diarrhea, nausea, vomiting, respiratory infection, arthralgia. Rarely, allergic reactions, worsening colitis, renal/hepatic dysfunction.
- Contraindications: Hypersensitivity to salicylates, balsalazide, or its components.
- Drug Interactions: Consult a drug interaction database for a complete list of potential interactions.
- Pregnancy & Breastfeeding: Category B; use with caution if clearly needed. Monitor breastfed infants for diarrhea.
- Dosage: Adults: 2.25 g TID (capsules) or 3.3 g BID (tablets, males only); Children (5-17 years): 2.25 g TID or 750 mg TID.
- Monitoring Parameters: Renal and liver function, complete blood count, ulcerative colitis symptoms.
Popular Combinations
Balsalazide is sometimes used in combination with other medications for ulcerative colitis, such as corticosteroids or immunomodulators, but specific recommendations depend on individual patient needs and should be determined by the treating physician.
Precautions
- General Precautions: Evaluate renal and liver function, assess for hypersensitivity to salicylates, monitor for worsening colitis symptoms.
- Specific Populations: Use with caution in pregnant/breastfeeding women and patients with renal/hepatic impairment. Not recommended for children under 5.
- Lifestyle Considerations: Adequate hydration, a fiber-rich diet, and stress management may be beneficial. Avoid alcohol and irritating foods if they exacerbate symptoms. Driving/operating machinery is generally not affected, but individual responses may vary.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Balsalazide?
A: Adults: 2.25 g (three 750 mg capsules) three times daily for 8-12 weeks or 3.3 g (three 1.1 g tablets) twice daily (males only) for up to 8 weeks. Children (5-17): 2.25g TID or 750 mg TID (capsules only) up to 8 weeks.
Q2: What is the primary use of Balsalazide?
A: Treatment of mildly to moderately active ulcerative colitis.
Q3: What are the common side effects of Balsalazide?
A: Headache, abdominal pain, diarrhea, nausea, and vomiting.
Q4: Are there any contraindications to Balsalazide?
A: Hypersensitivity to salicylates, aminosalicylates, balsalazide, or any components of the formulation.
Q5: Can Balsalazide be used during pregnancy?
A: Pregnancy Category B. Use only if clearly needed and under close medical supervision.
Q6: Can Balsalazide be used during breastfeeding?
A: Use with caution. Monitor the infant for diarrhea.
Q7: How does Balsalazide work?
A: It is a prodrug converted to mesalamine in the colon. Mesalamine exerts local anti-inflammatory effects.
Q8: How is Balsalazide administered?
A: Orally, as capsules or tablets. Capsules may be opened and sprinkled on applesauce for easier administration.
Q9: What should be monitored while a patient is on Balsalazide?
A: Monitor renal and liver function, complete blood count, and ulcerative colitis symptoms.
Q10: What is the difference between Colazal and Giazo?
A: Both are brand names for balsalazide. Colazal is available in capsule form, whereas Giazo (tablets) is specifically indicated for adult males.
