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.

References in periodicals archive ?
Table 3(a) describes the categorical independent variables and Table 3(b) describes continuous independent variables in relation to adherence to immunomodulators, 5-ASA, and biologics as well as blood work adherence.
Treatment with 5-ASA and CHCR prevented this target from modulating the progression of colitis (table 2).
Sh-AA-MBA was tested for the sustained release of a model drug 5-asa in buffer solution (pH = 1.5 [+ or -] 0.5) (similar to artificial gastric juice) for first 3 hours and then at pH 6.8 [+ or -] 0.5, similar to artificial intestinal liquid, for next 8 hour duration at 37[degrees]C.
The loading of 5-ASA into the materials was monitored by using Fourier transform infrared (FTIR) spectroscopy (Nicolet 380 FT-IR, Thermo Scientific, France).
We show here that 5-ASA decreases toxin A-stimulated colonic [LTB.sub.4] levels and SP release and that 5-ASA but not sulfapyridine inhibits toxin A-induced colitis.
The patient was treated by stopping the 5-ASA and adding prednisone (60 mg every day).
According to the company's chief scientific officer Dr Kunwar Shailubhai, in studies with experimental models of colitis in mice, SP-333 at an oral dose as low as 0.05 mg/kg body weight demonstrated superior anti-inflammatory activity compared to 5-aminosalicylic acid (5-ASA) given at a dose of 100 mg/kg.
Among the IBD treatments, oral alpha-4 integrin antagonist, (Development Code: AJM300), once-daily 5-ASA granules (Development code: AJG501) and a budesonide rectal foam are under development.
Treatment is often given in a "step-up" manner starting with drugs like 5- aminosalicylic acid (5-ASA) and antibiotics that have few side effects but also fewer beneficial effects, moving on to steroids, immune modulators and biologic drugs.
Aminosalisilatlar: 5-aminosalisilat (5-ASA) farkli mekanizmalarla antiinflamatuar etki yapmaktadir.
The treatment regimen for AS includes physiotherapy 5-aminosalicylic acid (5-ASA) or immunomodulatory therapy with agents such as 6-mercaptopurine or azathioprine (6MP/AZA), or methotrexate.
Currently, the treatments for ulcerative colitis include a maintenance medication called 5-ASA, which should be taken as many as 12 per day that reduce the risk of flares but that many forget to take, as well as steroids or surgery to remove their colon.

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