5-aminosalicylic acid


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mesalamine

 [mĕ-sal´ah-mēn]
an active metabolite of sulfasalazine, used in prophylaxis and treatment of inflammatory bowel disease; administered orally or rectally. Called also 5-aminosalicylic acid.

mesalamine (5-aminosalicylic acid, 5-ASA, mesalazine, mesalazine (UK))

Apriso, Asacol, Asacol HD, Canasa, Ipocol (UK), Lialda, Mesasal (CA), Mesren (UK), Mezavant (CA), Novo-5-ASA-Ect (CA), Pentasa, Rowasa, Salofalk (CA) (UK)

Pharmacologic class: 5-amino-2-hydroxybenzoic acid

Therapeutic class: GI anti-inflammatory drug

Pregnancy risk category B

Action

Unknown. Thought to act in colon, where it blocks cyclooxygenase and inhibits prostaglandin synthesis.

Availability

Capsules (extended-release): 250 mg, 500 mg, 0.375 g (Apriso)

Rectal suspension: 4 g/60 ml

Suppositories: 1,000 mg

Tablets (delayed-release): 400 mg (Pentasa), 800 mg (Asacol HD), 1.2 g (Lialda)

Indications and dosages

Active ulcerative colitis

Adults: 800 mg P.O. (Asacol delayed-release tablets) t.i.d. for 6 weeks

To induce remission in mildly to moderately active ulcerative colitis

Adults: 1 g P.O. (Pentasa extended-release capsules) q.i.d. for a total dosage of 4 g daily for up to 8 weeks. Or, two to four 1.2 g (Lialda) extended-release tablets P.O. once daily for total daily dose of 2.4 or 4.8 g for up to 8 weeks.

Active distal ulcerative colitis, proctosigmoiditis, or proctitis

Adults: 4-g enema (Rowasa 60 ml) P.R. daily at bedtime, retained for 8 hours. Continue for 3 to 6 weeks.

Active ulcerative proctitis

Adults: 500 mg (Canasa suppository) P.R. b.i.d., increased to t.i.d. if response inadequate after 2 weeks. Or 1,000 mg (suppository) P.R. at bedtime, continued for 3 to 6 weeks.

To maintain remission of ulcerative colitis

Adults: 1.6 g (Asacol) P.O. daily in divided doses. Or, 1.5 g (Apriso) P.O. daily in the morning.

Contraindications

• Hypersensitivity to drug, its components, or salicylates

Precautions

Use cautiously in:
• severe hepatic or renal impairment
• allergy to sulfasalazine
• pyloric stenosis (delayed-release tablets)
• conditions predisposing to development of myocarditis or pericarditis
• pregnant or breastfeeding patients
• children younger than age 18 (safety and efficacy not established).

Administration

• Give Apriso capsules with or without food. Don't give concurrently with antacids.
• Give Lialda tablets with meal.
• Make sure patient swallows tablets whole without crushing or chewing.
• For best effect, have patient retain suppository for 1 to 3 hours.

Adverse reactions

CNS: headache, dizziness, malaise, weakness

CV: chest pain, mesalamine-induced cardiac hypersensitivity reactions (myocarditis and pericarditis)

EENT: rhinitis, pharyngitis

GI: nausea, vomiting, diarrhea, eructation, flatulence, anal irritation (with rectal use), pancreatitis

GU: interstitial nephritis, renal failure

Musculoskeletal: back pain

Skin: alopecia, rash

Other: fever, acute intolerance syndrome, anaphylaxis, acute intolerance syndrome

Interactions

Drug-drug.Antacids: increased risk of dissolution of coating of Apriso granules

Azathioprine, 6-mercaptopurine: increased potential for blood disorders

Nephrotoxic drugs (including nonsteroidal anti-inflammatory agents): increased risk of renal adverse reactions

Patient monitoring

Monitor carefully for mesalamine-induced cardiac hypersensitivity reactions (myocarditis and pericarditis).

Closely monitor patients with history of allergic reactions to sulfasalazine or sulfite sensitivity (if using enema).
• Assess kidney and liver function before and periodically during therapy.
• Monitor for suppository efficacy, which should appear in 3 to 21 days. However, know that treatment usually continues for 3 to 6 weeks.

Watch for signs and symptoms of intolerance syndrome, such as cramping, acute abdominal pain, bloody diarrhea, fever, headache, and rash. If these occur, discontinue drug and notify prescriber.

Watch for signs and symptoms of intolerance syndrome, such as cramping, acute abdominal pain, bloody diarrhea, fever, headache, and rash. If these occur, discontinue drug. Drug may be restarted later only if clearly needed, under close medical supervision and at reduced dosage.

Patient teaching

• Instruct patient to swallow tablets or capsules whole.
• Tell patient to contact prescriber if partially intact tablets repeatedly appear in stools.
• Advise patient using suppository to avoid excessive handling and to retain suppository for 1 to 3 hours or longer for maximum benefit.
• Teach patient about proper enema administration. Tell him to stay in position for at least 30 minutes and, if possible, retain medication overnight.

Advise patient to immediately report breathing difficulties, allergic symptoms, cramping, acute abdominal pain, bloody diarrhea, fever, headache, or rash.
• As appropriate, review all other significant and life-threatening adverse reactions, especially those related to the drugs mentioned above.

5-aminosalicylic acid

/5-ami·no·sal·i·cyl·ic ac·id/ (5-ASA) mesalamine.

5-aminosalicylic acid

[ah-mē′nō-sal′əsil′ik]

mesalamine

A delayed-release anti-inflammatory salicylate developed for delivery to synovial tissue in arthritics; it is used to maintain remission in Crohn’s disease, and to treat ulcerative colitis. Mesalamine’s anti-inflammatory activity in the intestine is similar to (and better tolerated than) sulfasalazine, but it is more expensive.
References in periodicals archive ?
All patients were receiving concomitant therapy with 5-aminosalicylic acid derivatives (5-ASA) and/or immunomodulator medications.
Patients were allowed to continue using 5-aminosalicylic acid, steroids, and immunosuppressants, but not anti-TNF therapy.
PARIS -- Almost half (46%) of 1,013 children treated with 5-aminosalicylic acid only for 4 weeks after diagnosis with Crohn's disease had no disease flare within the same year, according to a study sponsored in part by Procter & Gamble Pharmaceuticals and the Crohn's & Colitis Foundation of America.
SYNTHESIS OF A NOVEL AROMATIC POLY(ANHYDRIDE-ESTER) OF 5-AMINOSALICYLIC ACID FOR ENHANCED DRUG DELIVERY
Sulfasalazine revisited: A meta-analysis of 5-aminosalicylic acid in the treatment of ulcerative colitis.
mesalamine--a 5-aminosalicylic acid (5-ASA) drug, relatively nontoxic and well tolerated, used in an enema and suppository preparation to treat inflamed intestine.
3,Phno 3076, 5-Aminosalicylic Acid 400 Mg Tab- Note:-At The Time Of Supply Manufacturing Date Should Be Earlier Than Six Months, And Expiry Date Should Not Be Earlier Than One Year.
5-aminosalicylic acid is not protective against colorectal cancer in inflammatory bowel disease: A meta-analysis of non-referral populations.
There was significant benefit in favor of probiotics and lower relapse rates for these patients, which as well was similar to conventional treatment with 5-aminosalicylic acid (5-ASA).
Some patients' symptoms will resolve spontaneously, whereas others may require over-the-counter antidiarrheal medications such as bismuth subsalicylate, or in other cases, 5-aminosalicylic acid compounds or immunosuppressants.
It is formed by sulphapyridine, which is readily absorbed, and 5-aminosalicylic acid (5-ASA), of which only 25% is absorbed and then excreted in urine as acetyl-5-ASA (9,17).

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