Oral: Treatment and maintenance of remission of mildly to moderately active ulcerative colitis

Rectal: Treatment of active mild to moderate distal ulcerative colitis, proctosigmoiditis, or proctitis

Rowasa® enema: Contains potassium metabisulfite; may cause severe hypersensitivity reactions (ie, anaphylaxis) in patients with sulfite allergies.

>10%:

Central nervous system: Headache (suppository 14%), pain (14%)

Gastrointestinal: Abdominal pain (18%; enema 8%)

Genitourinary: Eructation (16%)

Respiratory: Pharyngitis (11%)

1% to 10%:

Cardiovascular: Chest pain (3%), peripheral edema (3%)

Central nervous system: Chills (3%), dizziness (suppository 3%), fever (enema 3%; suppository 1%), insomnia (2%), malaise (2%)

Dermatologic: Rash (6%; suppository 1%), pruritus (3%; enema 1%), acne (2%; suppository 1%)

Gastrointestinal: Abdominal pain (enema 8%; suppository 5%), colitis exacerbation (3%; suppository 1%), constipation (5%), diarrhea (suppository 3%), dyspepsia (6%), flatulence (enema 6%; suppository 5%), hemorrhoids (enema 1%), nausea (capsule/suppository 3%), nausea and vomiting (capsule 1%), rectal pain (enema 1%; suppository 2%), vomiting (5%)

Local: Pain on insertion of enema tip (enema 1%)

Neuromuscular & skeletal: Back pain (7%; enema 1%), arthralgia (5%), hypertonia (5%), myalgia (3%), arthritis (2%), leg/joint pain (enema 2%),

Ocular: Conjunctivitis (2%)

Respiratory: Flu-like syndrome (3%; enema 5%), cough increased (2%)

Miscellaneous: Diaphoresis (3%)

<1%: Alopecia

Postmarketing and/or case reports: Agranulocytosis, alkaline phosphatase increased, ALT/AST increased, anemia, anorexia, aplastic anemia, appetite increased, asthma exacerbation, bilirubin increased, bloody diarrhea, blurred vision, BUN increased, chest pain, cholestatic jaundice, cholecystitis, confusion, depression, dry mouth, dry skin, dysuria, edema, emotional lability, eosinophilia, eosinophilic pneumonia, epididymitis, erythema nodosum, eye pain, facial edema, fibrosing alveolitis, gastritis, GGT increased, gout, Guillain-Barré syndrome, hematuria, hepatitis, hepatocellular damage, hepatotoxicity, hyperesthesia, hypersensitivity pneumonitis, interstitial nephritis, interstitial pneumonia, jaundice, Kawasaki-like syndrome, LDH increased, leukopenia, liver failure, liver necrosis, lupus-like syndrome, lymphadenopathy, menorrhagia, minimal change nephrotic syndrome, myocarditis, neck pain, nephropathy, nephrotoxicity, oral ulcers, pancreatitis, pancytopenia, perforated peptic ulcer, pericarditis, peripheral neuropathy, pleuritis, psoriasis, pyoderma gangrenosum, serum creatinine increased, somnolence, taste perversion, thrombocytopenia, transverse myelitis, tinnitus, tremor, T-wave abnormalities, urinary urgency, urticaria, vertigo

Azathioprine, mercaptopurine, thioguanine: Risk of myelosuppression may be increased by aminosalicylates (due to inhibition of TPMT).

Digoxin: Mesalamine may decrease digoxin bioavailability.

Enema: Store at controlled room temperature. Use promptly once foil wrap is removed; contents may darken with time (do not use if dark brown)

Suppository: Store at controlled room temperature away from direct heat, light, and humidity; do not refrigerate

Tablet: Store at controlled room temperature

Absorption: Rectal: Variable and dependent upon retention time, underlying GI disease, and colonic pH; Oral: Tablet: ~28%, Capsule: ~20% to 30%

Metabolism: Hepatic and via GI tract to acetyl-5-aminosalicylic acid

Half-life elimination: 5-ASA: 0.5-1.5 hours; acetyl-5-ASA: 5-10 hours

Time to peak, serum: 4-7 hours

Excretion: Urine (as metabolites); feces (<2%)

Oral:

Treatment of ulcerative colitis:

Capsule: 1 g 4 times/day

Tablet: Initial: 800 mg (2 tablets) 3 times/day for 6 weeks

Maintenance of remission of ulcerative colitis:

Capsule: 1 g 4 times/day

Tablet: 1.6 g/day in divided doses

Rectal:

Retention enema: 60 mL (4 g) at bedtime, retained overnight, approximately 8 hours

Rectal suppository (Canasa™):

500 mg: Insert 1 suppository in rectum twice daily; may increase to 3 times/day if inadequate response is seen after 2 weeks

1000 mg: Insert 1 suppository in rectum daily at bedtime

Note: Suppositories should be retained for at least 1-3 hours to achieve maximum benefit.

Note: Some patients may require rectal and oral therapy concurrently.

Elderly: See adult dosing; use with caution

Oral: Swallow capsules or tablets whole, do not chew or crush.

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.

Oral: Do not chew or break tablets or capsules. Notify prescriber if whole or partial tablets are repeatedly found in stool.

Enemas: Shake well before using, retain for 8 hours or as long as possible. May cause staining of clothing, undergarments.

Suppository: Do not refrigerate. After removing foil wrapper, insert high in rectum without excessive handling (warmth will melt suppository). Retain suppositories for at least 1-3 hours to achieve maximum benefit. Report severe abdominal pain, unresolved diarrhea, jaundice, severe headache, any unusual pain (back, joint, muscle, swelling of extremities, or chest pain). May cause staining of clothing, undergarments; lubricating gel may be used if needed to assist insertion.

Enema and suppository: May cause staining of clothing, undergarments; lubricating gel may be used if needed to assist insertion.

Breast-feeding precaution: Consult prescriber if breast-feeding.

Capsule, controlled release (Pentasa®): 250 mg

Suppository, rectal (Canasa™): 500 mg, 1000 mg [contains saturated vegetable fatty acid esters]

Suspension, rectal: 4 g/60 mL (7s) [contains potassium metabisulfite and sodium benzoate]

Rowasa®: 4 g/60 mL (7s, 28s) [contains potassium metabisulfite and sodium benzoate]

Tablet, delayed release [enteric coated] (Asacol®): 400 mg

Grand RJ, Ramakrishna J, and Calenda KA, "Inflammatory Bowel Disease in the Pediatric Patient,"Gastroenterol Clin North Am, 1995, 24(3):613-32.