Used for management of ulcerative colitis (as oral delayed-release tablets or extended-release capsules) and to induce (as extended-release capsules and as 1.2-g delayed-release tablets) and maintain (as 400-mg delayed-release tablets) clinical remission in adults with mildly to moderately active disease.
Management of mildly to moderately active distal ulcerative colitis (as rectal suspension) including ulcerative proctosigmoiditis and ulcerative proctitis.
Management of active ulcerative proctitis (as rectal suppositories).
Oral preparations of the drug may be preferable to rectal preparations in patients with extensive inflammatory bowel disease, since efficacy of rectal preparations may be limited to disease distal to the splenic flexure.
Crohn’s Disease
Has been used (as extended-release oral preparations) for the management of active Crohn’s disease† and to induce and maintain clinical remission in adults with mildly to moderately active disease.
Has been used (as rectal preparations) in a limited number of patients for the management of active Crohn’s disease†, but the role of such therapy in this condition is not as well defined as in the management of ulcerative colitis.
Dosage and Administration
Administration
Administer orally or rectally.
Oral Administration
Administer orally as delayed-release tablets (Asacol®, Lialda®) or extended-release capsules (Pentasa®).
Delayed-release tablets should be swallowed whole without breaking the outer coating, since the coating is designed to maintain the integrity of the tablets prior to entering the colon, where the drug is released. Intact or partially intact tablets may be present in stools; if this occurs repeatedly, patients should notify their clinician.
1.2-g delayed-release tablets (Lialda®): Administer orally with food.
Rectal Administration
Administer rectally as a suspension retention enema or suppositories.
Administer rectal suspension preferably at bedtime and retain for about 8 hours. Best results are achieved if the bowel is emptied just prior to enema administration. Administer according to manufacturer’s instructions.
Retain rectal suppositories for ≥1–3 hours, if possible, to achieve maximum benefit.
Dosage
Pediatric Patients
Ulcerative Colitis or Crohn’s Disease
Oral
Delayed-release tablets have been given in an initial dosage of 20–30 mg/kg daily and then increased up to 60 mg/kg daily.†
Adults
Ulcerative Colitis
Management of Mildly to Moderately Active Ulcerative Colitis
Oral
Delayed-release tablets: Usually, 2.4 g daily (given as two 400-mg delayed-release tablets 3 times daily) for 6 weeks.
Induction of Remission of Mildly to Moderately Active Ulcerative Colitis
Oral
Extended-release capsules: Usually, 4 g daily in equally divided doses (given as four 250-mg extended-release capsules or two 500-mg extended-release capsules 4 times daily) for up to 8 weeks. Lower dosages (e.g., 2–4 g daily [in divided doses]) have been used†.
Delayed-release tablets: 2.4 or 4.8 g once daily (given as two or four 1.2-g delayed-release tablets). Safety and efficacy beyond 8 weeks of treatment have not been established.
Maintenance of Remission
Oral
Delayed-release tablets: Usually, 1.6 g daily (four 400-mg delayed-release tablets) given in divided doses for 6 months. Dosages of 800 mg to 4.8 g daily (in divided doses) also have been used.
Extended-release capsules: Dosages of 1.5–3 g daily (in divided doses) have been used.
Advise patients that ulcerative colitis rarely remits completely, and continued use of maintenance dosages of mesalamine may substantially decrease the risk of relapse.
Distal Ulcerative Colitis
Rectal
Suppositories: 1 g (using 1-g suppositories) once daily at bedtime.
Enema suspension: Usually, 4 g once daily (preferably at bedtime).
Although clinical response may be apparent within 3–21 days, therapy with rectal mesalamine usually is continued for 3–6 weeks or until clinical and/or sigmoidoscopic remission is achieved.
Efficacy of rectal therapy (in terms of modification of relapse rates) beyond 6 weeks has not been established, but mesalamine has been used rectally for prolonged periods (e.g., >1 year) in some patients.
Lower dosages or less frequent administration of the rectal drug has been used in some patients†, particularly after initial remission is achieved.
In some patients with distal ulcerative colitis in whom clinical remission occurred following daily administration of 4-g doses of the rectal suspension, dosage was reduced to 4 g every 2 or 3 nights or, occasionally, to less frequent administration. If clinical relapse occurred with such administration, dosage was increased to more frequent use. In some patients with distal ulcerative colitis or ulcerative proctosigmoiditis, the rectal suspension also has been used in dosages of 1–3 g daily.
Crohn’s Disease
Management of Mildly to Moderately Active Crohn’s Disease
Oral
Adults have received dosages of 3.2–4.8 g daily (as delayed-release tablets) or 4 g daily (as extended-release capsules), generally in divided doses. Lower dosages do not appear to be effective.†
Prescribing Limits
Pediatric Patients
Ulcerative Colitis or Crohn’s Disease
Oral
Maximum 60 mg/kg daily.†
Adults
Ulcerative Colitis
Management of Mildly to Moderately Active Ulcerative Colitis
Oral
Delayed-release tablets (400 mg; Asacol®): Maximum 4.8 g daily in divided doses.
Extended-release capsules: Maximum 4 g daily in divided doses.
Induction of Remission of Mildly to Moderately Active Ulcerative Colitis
Oral
Extended-release capsules: Maximum 4 g daily in divided doses.
Delayed-release tablets (1.2 g; Lialda®): Safety and efficacy beyond 8 weeks of therapy not established.
Maintenance of Remission
Oral
Delayed-release tablets (400 mg; Asacol®): Maximum 4.8 g daily, in divided doses.
Extended-release capsules†: Maximum 3 g daily in divided doses.
Distal Ulcerative Colitis
Rectal
Enema suspension: Maximum 4 g once daily.
The drug has been used rectally for >1 year.
Crohn’s Disease
Management of Mildly to Moderately Active Crohn’s Disease
Oral
Delayed-release tablets (400 mg; Asacol®): Maximum 4.8 g daily in divided doses.†
Extended-release capsules: Maximum 4 g daily in divided doses.†
Maintenance of Remission
Oral
Delayed-release tablets (400 mg; Asacol®): Maximum 4.8 g daily in divided doses. †
Extended-release capsules: Maximum 3 g daily in divided doses.†
Special Populations
Geriatric Patients
Careful dosage selection recommended due to possible age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.
Drug Info Tools
