The history, pharmacology, pharmacokinetics, clinical uses and efficacy, adverse effects, drug interactions, and dosage and administration of rectal
mesalamine and oral
olsalazine in the treatment of
inflammatory bowel disease (IBD) are reviewed. The high incidence of toxicity associated with
sulfasalazine led to the development of the nonsulfonamide
5-aminosalicylic acid products
mesalamine and
olsalazine. The exact mechanism of action of these agents in the treatment of IBD is unknown. In clinical trials,
mesalamine was shown to be as effective as or more effective than
sulfasalazine or
corticosteroids in treating active
ulcerative colitis,
proctitis, and
proctosigmoiditis.
Mesalamine is effective in the maintenance of remission in patients with
ulcerative colitis. Several studies have demonstrated the effectiveness of
olsalazine in the treatment of active mild to moderate
ulcerative colitis.
Olsalazine is also effective in the maintenance of remission of
ulcerative colitis. The most common adverse effect associated with
mesalamine enemas is perianal irritation or
trauma secondary to insertion. The most common adverse effects associated with
olsalazine are dose-dependent watery
diarrhea and gastrointestinal upset. The recommended dosage of the
mesalamine enema for the treatment of active mild to moderate
ulcerative colitis is one 4-g (60-mL) retention
enema daily for three to six weeks. The dosage of
mesalamine suppositories for the treatment of active ulcerative
proctitis is one 500-mg suppository inserted rectally twice daily for three to six weeks. The dosage of
olsalazine is 1 g daily in divided doses for the maintenance of remission of
ulcerative colitis. Both rectal
mesalamine and oral
olsalazine provide clinicians with an effective therapeutic option for the treatment of
ulcerative colitis,
proctosigmoiditis, and
proctitis in patients unresponsive to or intolerant of the effects of
sulfasalazine or
corticosteroids.