No

5-Aminosalicylic Acid Derivative

Oral: Remission and treatment of mildly to moderately active ulcerative colitis

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

B

Known hypersensitivity to mesalamine, sulfasalazine, sulfites, or salicylates

Pericarditis should be considered in patients with chest pain; pancreatitis should be considered in any patient with new abdominal complaints. Elderly may have difficulty administering and retaining rectal suppositories. Given renal function decline with aging, monitor serum creatinine often during therapy. Use caution in patients with impaired hepatic function.

>10%:

Central nervous system: Headache, malaise

Gastrointestinal: Abdominal pain, cramps, flatulence, gas

1% to 10%: Dermatologic: Alopecia, rash

<1%: Anal irritation, acute intolerance syndrome (bloody diarrhea, severe abdominal cramps, severe headache), pericarditis, fatal myocarditis, hypersensitivity pneumonitis, allergic reactions, pancreatitis, nephrotic syndrome, interstitial nephritis, hepatitis, aplastic anemia, pancytopenia, leukopenia, agranulocytosis, anemia, elevated transaminases, LDH, alkaline phosphatase, or bilirubin, jaundice, cholestatic jaundice, liver necrosis/failure, Kawasaki-like syndrome

Symptoms of overdose include decreased motor activity, diarrhea, vomiting, renal function impairment

Treatment is supportive; emesis, gastric lavage, and follow with activated charcoal slurry

Decreased effect: Decreased digoxin bioavailability

Unstable in presence of water or light; once foil has been removed, unopened bottles have an expiration of 1 year following the date of manufacture

Mesalamine (5-aminosalicylic acid) is the active component of sulfasalazine; the specific mechanism of action of mesalamine is unknown; however, it is thought that it modulates local chemical mediators of the inflammatory response, especially leukotrienes; action appears topical rather than systemic

Absorption: Rectal: ~15%; variable and dependent upon retention time, underlying GI disease, and colonic pH

Metabolism: In the liver by acetylation to acetyl-5-aminosalicylic acid (active) and to glucuronide conjugates; intestinal metabolism may also occur

Half-life: 5-ASA: 0.5-1.5 hours; Acetyl 5-ASA: 5-10 hours

Time to peak serum concentration: Within 4-7 hours

Elimination: Most metabolites are excreted in urine with <2% appearing in feces

Adults (usual course of therapy is 3-6 weeks):

Capsule: 1 g 4 times/day

Tablet: 800 mg 3 times/day

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

Rectal suppository: Insert 1 suppository in rectum twice daily

Some patients may require rectal and oral therapy concurrently

Malaise is common

None reported

No information available to require special precautions

No effects or complications reported

Take as directed. Oral: Do not chew or break tablets. Enemas: Shake well before using, retain for 8 hours or as long as possible. Suppository: After removing foil wrapper, insert high in rectum without excessive handling (warmth will melt suppository). You may experience flatulence, headache, or hair loss (reversible). Report abdominal pain, unresolved diarrhea, severe headache, or chest pain. Breast-feeding precautions: Consult prescriber if breast-feeding.

Provide patient with copy of mesalamine administration instructions

Capsule, controlled release (Pentasa®): 250 mg

Suppository, rectal (Rowasa®): 500 mg

Suspension, rectal (Rowasa®): 4 g/60 mL (7s)

Tablet, 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.