Schedule H

Oral, Rectal (suppository, enema)

Formulation Strengths Available

Tablets (delayed-release/enteric-coated) 400 mg, 800 mg, 1200 mg

Extended-release tablets 400 mg, 800 mg, 1200 mg

Granules/Sachets (modified-release) 1 g, 1.5 g, 2 g

Rectal suppository 250 mg, 500 mg, 1 g

Rectal enema suspension 4 g/60 mL

Note: Different oral formulations have varying release mechanisms (pH-dependent, time-dependent, MMX technology) — they are not interchangeable.

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

✦ Ulcerative Colitis — Induction of Remission (Active Disease)

A. Distal Disease (Proctitis / Proctosigmoiditis):

Parameter Details

Starting dose Rectal suppository: 1 g at bedtime; OR Rectal enema: 4 g at bedtime

Titration Not applicable

Usual maintenance dose Continue until remission achieved (typically 4–8 weeks)

Maximum dose Suppository: 1 g/day; Enema: 4 g/day

Clinical Notes:

• Rectal therapy is first-line for distal disease (disease limited to rectum or rectosigmoid)

• Suppositories preferred for proctitis (reach up to 15–20 cm); enemas preferred for left-sided disease (reach up to 40–60 cm)

• Retain enema overnight for best efficacy

B. Extensive/Pancolitis (Mild to Moderate):

Parameter Details

Starting dose 2.4–4.8 g/day orally in 2–3 divided doses

Titration Not applicable for induction

Usual maintenance dose 2.4 g/day (once remission achieved)

Maximum dose 4.8 g/day

Clinical Notes:

• Higher doses (4.8 g/day) more effective for moderate disease

• Once-daily dosing with extended-release formulations is as effective as divided dosing and improves adherence

• Swallow tablets whole; do not crush or chew enteric-coated formulations

C. Combined Oral + Rectal Therapy (Left-sided or Extensive UC):

Parameter Details

Starting dose Oral: 2.4–4.8 g/day + Rectal: suppository 1 g or enema 4 g at bedtime

Titration Not applicable

Usual maintenance dose Individualised based on response

Maximum dose Oral: 4.8 g/day + Rectal: 4 g/day

Clinical Notes:

• Combined therapy superior to oral alone for left-sided/extensive disease

• Consider in patients with inadequate response to oral monotherapy

✦ Ulcerative Colitis — Maintenance of Remission

Parameter Details

Starting dose 1.6–2.4 g/day orally

Titration Not applicable

Usual maintenance dose 2–2.4 g/day orally as single dose or in 2 divided doses

Maximum dose 4.8 g/day (if higher dose required for remission maintenance)

For Distal Disease Maintenance:

Parameter Details

Starting dose Suppository: 500 mg–1 g at bedtime 2–3 times weekly; OR Enema: 4 g 2–3 times weekly

Titration Not applicable

Usual maintenance dose As above

Maximum dose As per acute dosing

Clinical Notes:

• Long-term maintenance therapy reduces relapse risk and colorectal cancer risk

• Once-daily oral dosing improves adherence

• Continue indefinitely in most patients with UC

✦ Crohn's Disease — Mild to Moderate Colonic Disease

Parameter Details

Starting dose 2–4 g/day orally in 2–3 divided doses

Titration Not applicable

Usual maintenance dose 2–2.4 g/day

Maximum dose 4 g/day

Clinical Notes:

• Efficacy limited to mild colonic Crohn's disease

• NOT effective for isolated small bowel (ileal) disease

• NOT recommended as monotherapy for moderate-severe Crohn's disease

• Consider alternative immunomodulators for maintenance

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

✦ Ulcerative Colitis — Induction and Maintenance

Eligibility: Age ≥5 years (oral formulations); rectal use under specialist supervision in younger children

Weight-based Dosing (Oral):

Body Weight (kg) Induction Dose Maintenance Dose Maximum Dose

17–32 30–50 mg/kg/day in 2 divided doses 15–30 mg/kg/day 2.4 g/day

33–53 37.5–61 mg/kg/day in 2 divided doses 20–37.5 mg/kg/day 2.4 g/day

54 2.4–4.8 g/day in 2 divided doses 1.2–2.4 g/day 4.8 g/day

Rectal Therapy (Distal Disease):

Age Group Suppository Enema

5–10 years 250–500 mg at bedtime 1–2 g at bedtime (reduced volume)

10–17 years 500 mg–1 g at bedtime 2–4 g at bedtime

Monitoring Requirements:

• CBC with differential at baseline and periodically

• Renal function (serum creatinine) at baseline, 3 months, then every 6–12 months

• Growth monitoring in children on long-term therapy

• LFTs annually

Clinical Notes:

• Granule/sachet formulations preferred in children who cannot swallow tablets

• Extended-release forms may be used in adolescents who can swallow tablets whole

• Paediatric gastroenterology supervision mandatory

Secondary Indications — Paediatric Doses (Off-label, if any)

Indication Dose Duration Notes

Crohn's Colitis (Mild) 30–50 mg/kg/day orally in divided doses Long-term maintenance OFF-LABEL — Specialist only; limited efficacy data in paediatric Crohn's disease

Age Restriction Statement:

• Oral formulations: Not recommended below 5 years of age except under specialist paediatric gastroenterology supervision

• Rectal formulations: May be used in children <5 years under specialist supervision with appropriate dose adjustment

Important Notes:

• Mesalamine can cause nephrotoxicity (interstitial nephritis) even in patients with normal baseline renal function

• Baseline renal function mandatory before initiation

• Pre-existing renal disease significantly increases nephrotoxicity risk

• Known hypersensitivity to mesalamine, other salicylates (including aspirin), or any excipient

• Severe renal impairment (eGFR <30 mL/min/1.73 m²)

• Severe hepatic impairment

• Pre-existing severe blood dyscrasias

• History of mesalamine-induced acute intolerance syndrome (cramping, bloody diarrhoea, fever)

• Pre-existing renal impairment (even mild) — enhanced nephrotoxicity risk

• History of sulphasalazine intolerance — potential cross-reactivity (though mesalamine lacks sulpha moiety)

• Elderly patients — reduced renal reserve; more susceptible to adverse effects

• Pre-existing hepatic disease — monitor LFTs

• History of myocarditis or pericarditis — rare association with mesalamine

• Pyloric stenosis or other upper GI obstruction — may affect delayed-release formulation transit

• Concurrent use of nephrotoxic drugs

Parameter Details

Safety Category Generally considered safe; compatible with pregnancy (extensive experience)

Preferred Alternative Mesalamine is the preferred 5-ASA agent in pregnancy (over sulphasalazine due to folate interference)

When to Use Use to maintain disease remission; uncontrolled IBD poses greater risk to pregnancy than mesalamine

Monitoring Maternal renal function; fetal growth monitoring

Note: High-dose folic acid supplementation (5 mg/day) recommended if using any 5-ASA agent during pregnancy.

Parameter Details

Compatibility Compatible with breastfeeding

Drug Levels in Milk Low (minimal transfer)

Preferred Alternative Mesalamine is preferred over sulphasalazine in lactating women

Infant Monitoring Monitor for diarrhoea (rare); observe feeding pattern and weight gain

Note: Rare case reports of diarrhoea in breastfed infants — usually resolves without intervention.

Parameter Recommendation

Starting Dose Lower end of dose range (1.6–2.4 g/day for oral therapy)

Titration Slower titration; extended intervals between dose increases

Special Risks Increased risk of nephrotoxicity due to age-related decline in renal function; dehydration risk; polypharmacy interactions

Monitoring Baseline and regular renal function monitoring essential (every 3–6 months); monitor for volume depletion

Interacting Drug Mechanism/Effect Recommendation

Azathioprine / 6-Mercaptopurine Mesalamine inhibits TPMT enzyme; increased risk of myelosuppression Monitor CBC closely; consider TPMT genotyping or phenotyping before initiation; dose reduction of thiopurine may be needed

NSAIDs Additive nephrotoxicity Avoid concurrent use if possible; if unavoidable, monitor renal function frequently

Nephrotoxic drugs (aminoglycosides, ciclosporin, tacrolimus) Increased nephrotoxicity risk Avoid combination or use with enhanced renal monitoring

Interacting Drug Mechanism/Effect Recommendation

Warfarin Rare reports of enhanced anticoagulant effect Monitor INR more frequently when initiating or changing mesalamine dose

Antacids / PPIs May alter pH-dependent release of some enteric-coated formulations Clinical significance uncertain; monitor for efficacy

Lactulose May lower colonic pH; may affect release of pH-dependent formulations Monitor clinical response

Digoxin Possible reduced digoxin absorption Monitor digoxin levels if used concurrently

Live vaccines (oral typhoid) Theoretical concern of reduced vaccine efficacy in immunocompromised IBD patients Consider timing; use inactivated vaccines when possible

• Headache

• Nausea, vomiting

• Abdominal pain, bloating, flatulence

• Diarrhoea (may mimic disease flare)

• Dyspepsia

• Rash

• Rectal discomfort, irritation (with rectal formulations)

• Anal pruritus (with suppositories)

Adverse Effect Clinical Notes

Nephrotoxicity (Interstitial nephritis) Can occur at any time; often reversible if detected early; requires immediate discontinuation; monitor renal function regularly

Acute Intolerance Syndrome Paradoxical worsening with cramping, bloody diarrhoea, fever — resembles acute UC flare; discontinue immediately

Hepatotoxicity Elevated transaminases; rare cholestatic hepatitis; discontinue if significant elevation

Myocarditis / Pericarditis Rare; presents with chest pain, dyspnoea, fever; reversible on discontinuation

Blood Dyscrasias Agranulocytosis, aplastic anaemia, thrombocytopenia — rare; monitor CBC

Stevens-Johnson Syndrome / TEN Very rare; discontinue immediately

Pancreatitis Rare; consider if unexplained abdominal pain

Pulmonary toxicity Eosinophilic pneumonia, interstitial pneumonitis — rare

Phase Parameters

Baseline Serum creatinine / eGFR; CBC with differential; LFTs; urinalysis

After Initiation (3 months) Repeat renal function tests

Long-term (Chronic Use) Renal function every 6 months; CBC and LFTs annually; urinalysis annually

If Renal Impairment at Baseline More frequent monitoring (every 3 months)

Concurrent Thiopurine Use CBC every 1–2 weeks initially, then monthly

Brand Name Manufacturer Formulations

Mesacol Sun Pharma Tablets, Suppository, Enema

Mesacol OD Sun Pharma Extended-release tablets

Pentasa Ferring Granules/Sachets

Asacol Zydus Delayed-release tablets

Mesagard Aristo Tablets

Mesar Intas Tablets

Mesaflam Mankind Tablets

Notes:

• Included in NLEM 2022; select strengths under NPPA price control

• Generic formulations significantly more affordable than branded equivalents

• Rectal therapy is first-line for distal UC: Suppositories for proctitis, enemas for left-sided disease — more effective than oral therapy alone for distal disease

• Combine oral + rectal for enhanced efficacy: Combined therapy is superior to oral alone in left-sided and extensive UC; particularly useful in patients with inadequate response to oral monotherapy

• Once-daily dosing is non-inferior to divided dosing: Extended-release formulations allow once-daily dosing with equivalent efficacy and improved adherence

• Monitor renal function in ALL patients: Nephrotoxicity can occur even in patients with normal baseline renal function; check creatinine at baseline, 3 months, then every 6 months

• Not interchangeable with sulphasalazine: Mesalamine lacks the sulpha moiety and is generally better tolerated; preferred in sulphasalazine-intolerant patients; however, some cross-reactivity possible

• Acute intolerance syndrome mimics UC flare: If symptoms worsen paradoxically after starting mesalamine, consider drug-induced intolerance rather than treatment failure

• Long-term use reduces colorectal cancer risk: Regular mesalamine use in UC patients associated with reduced colorectal cancer risk — reinforce importance of adherence

mesalamine; mesalazine; 5-ASA; ulcerative colitis; inflammatory bowel disease; IBD; Crohn's disease; proctitis; renal-monitoring; pregnancy-safe; NLEM India

RxIndia v1.1 — 27 Jan 2026

• CDSCO Approved Product Information

• Indian Pharmacopoeia / National Formulary of India (NFI)

• NLEM 2022 (National List of Essential Medicines)

• API Textbook of Medicine

• ICMR Guidelines on Inflammatory Bowel Disease Management

• AIIMS Gastroenterology Clinical Protocols

• Indian Society of Gastroenterology — IBD Task Force Recommendations

• IAP Guidelines (Paediatric IBD)

• WHO Essential Medicines List (supportive reference for paediatrics)