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Gastroprotective Pregnancy: B — considered safe; dibutyl phthalate excipient in some preparations may be harmful — use Pentasa or Salofalk in pregnancy

Mesalazine (5-Aminosalicylic Acid)

Brand names: Asacol, Mezavant, Octasa, Pentasa

Adult dose

Dose: Induction of remission (UC): 2.4–4.8g/day. Maintenance: 1.2–2.4g/day
Route: Oral / Rectal (suppository or enema)
Frequency: Once or divided doses daily
Max: 4.8g/day (oral induction)
Distal UC: rectal mesalazine (1g suppository OD or enema at night) superior to oral alone. Brand matters — each formulation releases drug at different intestinal sites. Do not switch brands without specialist advice.

Dose adjustments

Renal

Avoid in moderate to severe renal impairment (GFR <30) — mesalazine nephrotoxicity.

Hepatic

Avoid in severe hepatic impairment.

Clinical pearls

  • Renal monitoring: check U&E and creatinine at baseline, 3 months, then annually. Stop if creatinine rises — mesalazine nephritis.
  • Combined oral + rectal therapy is superior to either alone for extensive or left-sided UC.
  • Formulation matters: Pentasa releases from duodenum; Asacol/Octasa releases in distal ileum/colon; Mezavant: pH-dependent MMX release. Do not freely switch.
  • Long-term maintenance reduces colorectal cancer risk in UC — continue indefinitely in most patients.

Contraindications

  • Salicylate hypersensitivity
  • Severe renal impairment
  • Active peptic ulcer disease

Side effects

  • Interstitial nephritis (rare but serious — idiosyncratic)
  • Nausea, diarrhoea (often overlap with UC symptoms)
  • Headache
  • Worsening of colitis (paradoxical — rare)
  • Blood disorders (rare — agranulocytosis)

Interactions

  • Azathioprine: mesalazine inhibits TPMT enzyme — increases azathioprine toxicity risk
  • NSAIDs: additive renal toxicity
  • Warfarin: may enhance anticoagulant effect

Monitoring

  • U&E
  • creatinine (annually)
  • FBC (annually)
  • symptom response
  • stool frequency

Reference: BSG UC Guidelines 2019; NICE NG130 IBD; NICE BNF 84. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.