Schedule H

Oral

• Capsules: 750 mg

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Mild to Moderate Ulcerative Colitis — Induction of Remission (Adults)

Parameter Recommendation

Starting dose 2.25 g orally twice daily (total 4.5 g/day)

Titration Not typically required

Usual maintenance dose Continue induction dosing for 8–12 weeks based on clinical and endoscopic response

Maximum dose 6.75 g/day

Clinical notes:

• Balsalazide is a prodrug that delivers mesalazine directly to the colonic mucosa following azo bond cleavage by colonic bacteria

• Particularly useful in patients with documented sulfasalazine or mesalazine intolerance

• Assess response at 8 weeks; non-responders may require escalation to immunomodulators or biologics

1. Maintenance of Remission in Ulcerative Colitis (Adults)

Parameter Recommendation

Starting dose 1.5 g/day in divided doses

Titration Adjust based on relapse risk and tolerance; may increase to 3 g/day

Usual maintenance dose 1.5 g twice daily (3 g/day)

Maximum dose 3 g/day for long-term maintenance

Clinical notes:

• Long-term therapy; reassess disease activity and drug tolerance annually

• Suitable alternative to mesalazine in patients with 5-ASA intolerance or suboptimal response

• Duration: Indefinite in patients with relapse history; consider colonoscopic surveillance

Secondary Indications — Adults (Off-label)

Indication Dose Duration Notes

Crohn's Colitis (mild-to-moderate, colonic involvement only) 3–6 g/day in divided doses Up to 12 weeks or as per response Specialist only — OFF-LABEL. Evidence: Limited; mixed efficacy data from RCTs; not effective for small bowel disease

PAEDIATRIC DOSING (Specialist Only)

Primary Indication: Mild to Moderate Ulcerative Colitis

Age Group: 5–17 years

Parameter Recommendation

Starting dose 750 mg three times daily (2.25 g/day) for children weighing <30 kg; 750 mg–1.5 g three times daily for ≥30 kg

Titration Increase gradually based on response and tolerance; adjust per BSA (1.5–2.25 g/m²/day)

Usual maintenance dose 1.5–3 g/day in 2–3 divided doses

Maximum dose 6.75 g/day (not exceeding adult maximum)

Duration 8–12 weeks for induction; maintenance at lowest effective dose

Safety Monitoring:

• Not recommended in children <5 years due to insufficient safety and efficacy data

• Monitor for abdominal pain, diarrhoea, and signs of hypersensitivity

• Periodic CBC, LFTs, and renal function every 3–6 months during long-term use

• Growth monitoring in prolonged therapy

Secondary Indications — Paediatrics (Off-label)

Indication Dose Duration Notes

Crohn's Disease with colonic involvement (≥7 years) 2.25–4.5 g/day in divided doses 8–12 weeks Specialist only — OFF-LABEL. Evidence: Very limited paediatric data; mesalazine preferred; consider only if standard 5-ASA not tolerated (Indian specialist practice)

• Known hypersensitivity to balsalazide, mesalazine, other salicylates, or any excipient

• Severe renal impairment (eGFR <30 mL/min)

• Severe hepatic impairment (Child-Pugh C)

• History of salicylate-induced asthma or bronchospasm

• Complete urinary tract obstruction

• Pre-existing renal disease — monitor serum creatinine and urinalysis regularly

• History of elevated liver enzymes or hepatic dysfunction

• Previous intolerance to sulfasalazine or other 5-ASA compounds (may still cross-react)

• Blood dyscrasias — monitor CBC

• Dehydration or hypovolaemia (increased nephrotoxicity risk)

• Pulmonary disease (rare reports of interstitial lung disease with 5-ASA agents)

• Concurrent use of nephrotoxic agents

• Pregnancy and lactation (see respective sections)

Parameter Details

Overall safety Limited human data; animal studies show no teratogenicity

Risk category No formal FDA/India category; considered relatively safe based on 5-ASA class data

Preferred alternatives Mesalazine generally preferred in Indian obstetric practice due to larger safety database

When may be used If mesalazine not tolerated; benefit must outweigh risk; use lowest effective dose

Monitoring Fetal growth (USS), maternal renal and hepatic function; avoid in third trimester near term if possible

Parameter Details

Compatibility Generally compatible with breastfeeding

Drug levels in milk Low (mesalazine metabolite detected in breast milk at low concentrations)

Preferred alternatives Mesalazine preferred due to established safety data during lactation

Infant monitoring Observe for diarrhoea, feeding difficulties, rash, irritability, and weight gain

Parameter Recommendation

Starting dose Use lower end of dosing range (e.g., 1.5 g twice daily)

Titration Slow upward titration over weeks; renal monitoring essential

Risks Increased susceptibility to renal impairment; GI intolerance; dehydration

Additional monitoring Renal function (baseline and every 2–4 weeks initially), hydration status, LFTs

Interacting Drug Effect & Mechanism Management

Azathioprine / 6-Mercaptopurine Increased risk of myelosuppression (5-ASA inhibits TPMT enzyme) Monitor CBC closely; specialist supervision; dose reduction of thiopurine may be needed

Nephrotoxic drugs (aminoglycosides, NSAIDs, ciclosporin) Additive nephrotoxicity risk Avoid combination if possible; monitor renal function frequently

Methotrexate Increased methotrexate toxicity due to competition for renal tubular secretion Monitor for methotrexate toxicity; check CBC, LFTs, renal function

Interacting Drug Effect Management

Warfarin 5-ASA derivatives may enhance anticoagulant effect Monitor INR closely; dose adjustments may be required

Isoniazid / Anti-TB drugs Additive hepatotoxicity potential Monitor LFTs more frequently

Digoxin Possible reduced digoxin absorption Monitor digoxin levels if used concurrently

Proton pump inhibitors / Antacids Theoretical alteration of colonic pH affecting drug release Clinical significance minimal; no specific action required

• Headache

• Abdominal pain / discomfort

• Diarrhoea

• Nausea

• Flatulence

• Arthralgia

• Nasopharyngitis

Adverse Effect Notes

Hypersensitivity reactions Rash, fever, eosinophilia; may mimic UC flare; discontinue immediately

Acute intolerance syndrome Cramping, bloody diarrhoea, abdominal pain; mimics UC exacerbation; discontinue

Hepatotoxicity Elevated transaminases, cholestatic hepatitis (rare); monitor LFTs

Interstitial nephritis Presents with rising creatinine, proteinuria; requires immediate discontinuation

Acute pancreatitis Rare; discontinue if suspected

Blood dyscrasias Agranulocytosis, aplastic anaemia (rare); monitor CBC

Pericarditis / Myocarditis Very rare; discontinue and refer urgently

Adverse Effect Notes

Hypersensitivity reactions Rash, fever, eosinophilia; may mimic UC flare; discontinue immediately

Acute intolerance syndrome Cramping, bloody diarrhoea, abdominal pain; mimics UC exacerbation; discontinue

Hepatotoxicity Elevated transaminases, cholestatic hepatitis (rare); monitor LFTs

Interstitial nephritis Presents with rising creatinine, proteinuria; requires immediate discontinuation

Acute pancreatitis Rare; discontinue if suspected

Blood dyscrasias Agranulocytosis, aplastic anaemia (rare); monitor CBC

Pericarditis / Myocarditis Very rare; discontinue and refer urgently

• Colazide

• Balsa

• NLEM status: Not listed under NLEM (as of 2023)

• Government supply: Limited availability; mesalazine more commonly stocked in public facilities

1. Colonic targeting advantage: Balsalazide delivers 5-ASA directly to the colon with minimal systemic absorption, making it useful for isolated colonic UC

1. Alternative to mesalazine: Consider in patients with documented mesalazine or sulfasalazine intolerance; not a first-line choice due to cost and availability

1. No small bowel activity: Ineffective for small bowel Crohn's disease — use only for colonic involvement

1. Renal vigilance: Always confirm adequate renal function before initiation, especially in elderly or dehydrated patients

1. Administration tip: Capsules may be opened and contents sprinkled on soft food for patients with swallowing difficulty; do not crush granules

1. Cost consideration: May consider switching to mesalazine for long-term maintenance if tolerance established and cost is a concern

balsalazide; ulcerative colitis; 5-ASA; mesalazine prodrug; anti-inflammatory; GI-targeted; renal-caution; paediatric-use; alternative-to-mesalazine; IBD

RxIndia v1.0 — 02 Apr 2025

• CDSCO product information

• Indian Pharmacopoeia

• API Textbook of Medicine

• ICMR Guidelines for IBD Management

• Indian Society of Gastroenterology recommendations

• AIIMS Adult and Paediatric formulary protocols

• Goodman & Gilman's Pharmacological Basis of Therapeutics