MESALAMINE

Asacol; Canasa; Lialda; Pentasa; Rowasa

DOSING IN ADULTS

Treatment of ulcerative colitis
  Capsule: 1 g 4 times/day
  Tablet:
    Asacol: 800 mg 3 times/day for 6 weeks
    Lialda: 2.4-4.8 g once daily for up to 8 weeks
Maintenance of remission of ulcerative colitis
  Capsule: 1 g 4 times/day
  Tablet (Asacol): 1.6 g/day in divided doses
Distal ulcerative colitis, proctosigmoiditis, or proctitis: Rectal: Retention enema: 60 mL (4 g) at bedtime, retained overnight, approximately 8 hours
Active ulcerative proctitis: Rectal: Rectal suppository (Canasa): Insert one 1000 mg suppository in rectum daily at bedtime

DOSAGE FORMS 

Capsule, controlled release:
  Pentasa: 250 mg, 500 mg
Suppository, rectal:
  Canasa: 1000 mg [contains saturated vegetable fatty acid esters]
Suspension, rectal: 4 g/60 mL (7s, 28s) Rowasa: 4 g/60 mL (7s, 28s) [contains potassium metabisulfite and sodium benzoate]
Tablet, delayed release [enteric coated]:
  Asacol: 400 mg
  Lialda: 1.2 g

ADMINISTRATION

Oral: Swallow capsules or tablets whole, do not chew or crush. Do not break outer coating of Asacol, Lialda
Lialda and Mezavant should be taken once daily with a meal.
Rectal enema: Shake bottle well. Retain enemas for 8 hours or as long as practical.
Suppository: Remove foil wrapper; avoid excessive handling. Should be retained for at least 1-3 hours to achieve maximum benefit.

SIGNIFICANT ADVERSE REACTIONS 

Headache
Abdominal pain
Chest pain
Rash
Alopecia
Leg swelling 
Cough
Agranulocytosis-more in elderly
Jaundice
Pancreatitis
Renal disease including acute/chronic interstitial nephritis, nephrotic syndrome, and renal failure have been reported. An evaluation of renal function is recommended prior to initiation of therapyand periodically during treatment

Symptomatic worsening of colitis/IBD may occur following initiation of therapy

CONTRAINDICATIONS 

 Hypersensitivity to mesalamine, salicylates, or any component
Canasa suppositories have saturated vegetable fatty acid esters (contraindicated in patients with allergy to these components).
Rowasa enemq contains potassium metabisulfite; may cause severe hypersensitivity reactions (ie, anaphylaxis) in patients with sulfite allergies.

DRUG INTERACTIONS

Digoxin: Mesalamine may decrease absorption, and thus levels/effects, of digoxin.
Thiopurine analogues (azathioprine, mercaptopurine, thioguanine): Mesalamine may increase the levels/effects of thiopurine analogues; risk of myelosuppression may be increased by aminosalicylates (due to inhibition of TPMT).

PREGNANCY RISK FACTOR — B

LACTATION — Enters breast milk/use caution.