Mesalazine (oral)

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[edit] BRAND NAMES

[edit] STRUCTURE

Mesalazine.jpg

[edit] MECHANISM OF ACTION

The mechanism of action of mesalazine (5-ASA) appears to be local to the colonic mucosa rather than systemic. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with chronic inflammatory bowel disease, and it is possible that 5-ASA diminishes inflammation by blocking production of arachidonic acid metabolites in the colon.

[edit] INDICATIONS

Treatment of mildly to moderately active ulcerative colitis, a disease of the colon and rectum in which the lining of the bowel becomes inflamed. Symptoms can include rectal bleeding, frequent diarrhea and abdominal pain

[edit] DOSAGE

Adults:

  • Initial Daily Dose is 800 mg, three times a day for a total daily dose of 2.400 mg for a duration of 6 weeks.
  • Maintenance of remission of ulcerative colitis: The recommended dosage is 1500-1600 mg daily. Treatment duration in the prospective, well-controlled trial was 6 months.


  • Asacol HD (U.S.): Initial Daily Dose is Two 800 mg tablets three times daily for 6 week

[edit] CONTRAINDICATIONS

  • Hypersensitivity to salicylates

[edit] WARNINGS AND PRECAUTIONS

  • Acute exacerbation of colitis symptoms can occur
  • Renal impairment may occur. Monitor renal function at the beginning of treatment and periodically during therapy

[edit] INTERACTIONS

  • Do not co-administer with antacids

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category B (US). Mesalazine should be used during pregnancy only if clearly needed.
  • Nursing Mothers: Low concentrations of mesalamine and higher concentrations of its N-acetyl metabolite have been detected in human breast milk. While the clinical significance of this has not been determined, caution should be exercised when mesalamine is administered to a nursing woman.

[edit] SIDE EFFECTS

The most common adverse reactions (incidence ≥3%) are headache, diarrhea, upper abdominal pain, nausea, nasopharyngitis, flu or flu-like illness, sinusitis

[edit] RELATED LINKS

Mechanism of action of mesalazine (5-ASA), Sulfasalazine and Balsalazide, used for the treatment of inflammatory bowel

[edit] BIBLIOGRAPHY

[edit] REFERENCES