5-ASA


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5-ASA

 

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-ASA

mesalamine (5-aminosalicylic acid).

5-ASA

5-aminosalicylic acid.
References in periodicals archive ?
Significant upregulation of IFN-[gamma] mRNA expressions in the DNBS model group, which was attenuated by 5-ASA and CHCR as seen by their levels of their transcripts, seems favorable (table 2).
The loading of 5-ASA into the materials was monitored by using Fourier transform infrared (FTIR) spectroscopy (Nicolet 380 FT-IR, Thermo Scientific, France).
According to the etiologies mentioned for GIN as well as our patient's history, in our case GIN could be an extraintestinal manifestation of CD or induced by a drug, such as 5-ASA or ciprofloxacin.
The data confirm the efficacy and safety of CORTIMENTAMMXA in patients experiencing an active flare of UC despite initial oral 5-ASA therapy, and in a controlled setting that is consistent with clinical practice and the ECCO treatment guidelines,2" said Dr David Rubin, Professor of Medicine at the University of Chicago Medicine and lead CONTRIBUTE author.
A third agent, sulfasalazine (Azulfidine), is metabolized to 5-ASA plus sulfapyridine.
It is the 5-ASA portion that is thought to be responsible for the agents efficacy, whereas the sulfur component allows the drug to be delivered to the colon, its site of action.
The study is expected to evaluate whether there is an incremental benefit when UCERIS 9 mg is added to current oral aminosalicylate (5-ASA) therapy for patients who have mild or moderate active ulcerative colitis who are not controlled on background 5-ASA therapy.
Continued treatment with a salicylate in a patient who isn't responding can be worse than useless, because 5-ASA [5-aminosalicylic acid] can trigger diarrhea in some patients," Dr.
Luminol-enhanced chemiluminescence was used to detect superoxide scavenging by extracts of the herbs, as well as by 5-ASA, and fluorimetry was used to detect peroxyl radical scavenging.
Treatments used by case patients were oral 5-aminosalycilic acid (5-ASA) used by 58 patients, rectal 5-ASA (10 patients), prednisone (47 patients), and azathioprine (9 patients), he noted.

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