Mesalazine


Full Prescribing Info
Dosage/Direction for Use

Oral
Ulcerative colitis
Adult: Dose is dependent on product used. Asacol 400 mg tab, Ipocol tab Acute attack: Initially, 2.4 g daily in divided doses. Maintenance of remission: 1.2-2.4 g once daily or in divided doses. Asacol 800 mg tab
Mild acute exacerbations: 2.4 g daily in divided doses. Moderate acute exacerbations: 4.8 g daily in divided doses. Maintenance of remission: Up to 2.4 g daily in divided doses. Mezavant Acute attack: Initially, 2.4-4.8 g once daily. Maintenance of remission: 2.4 g once daily. Pentasa tab Acute attack: Initially, up to 4 g daily in 2 or 3 divided doses. Maintenance of remission: Initially, 2 g once daily, then adjusted individually. Pentasa granule Acute attack: Initially, up to 4 g daily in 2-4 divided doses. Maintenance of remission: 2 g once daily. Salofalk Acute attack: As tab: Initially, 1.5-3 g daily in 3 divided doses. As granule: Initially, 1.5-3 g once daily or in 3 divided doses. Maintenance of remission: 1.5 g daily in 3 divided doses.
Child: Dose is dependent on preparation and brand used. Ipocol tab, Salofalk tab/granules
≥6 yr <40 kg: Acute attack: Initially, 30-50 mg/kg daily in divided doses, then adjusted individually. Max: 75 mg/kg daily. Maintenance of remission: Initially, 15-30 mg/kg daily in divided doses, then adjusted individually; ≥40 kg: Same as adult dose.
Renal impairment: GFR <20 mL/min: Contraindicated.
Hepatic impairment:
Severe: Contraindicated.

Rectal
Ulcerative proctitis
Adult: Dose is dependent on preparation and brand used. Asacol supp 0.75-1.5 g daily in divided doses. Asacol foam enema Rectosigmoid region: 1 g daily for 4-6 wk. Descending colon: 2 g daily for 4-6 wk. Pentasa supp or susp enema Acute treatment: 1 g daily for 2-4 wk. Maintenance: 1 g daily. Salofalk supp 0.5-1 g given 2 or 3 times daily. Salofalk foam/susp enema 2 g once daily at bedtime.
Renal impairment: GFR <20 mL/min: Contraindicated.
Hepatic impairment:
Severe: Contraindicated.
Contraindications
Hypersensitivity to salicylates. Severe hepatic or renal (GFR <20 mL/min) impairment.
Special Precautions
Patient w/ conditions predisposing to myocarditis or pericarditis, active peptic ulceration, history of sulfasalazine hypersensitivity. Mild to moderate renal or hepatic impairment. Pregnancy and lactation. Patient Counselling This drug may cause nausea, if affected, do not drive or operate machinery. Monitoring Parameters Monitor renal and hepatic function (i.e. ALT, CBC).
Adverse Reactions
Headache, dizziness, GI disturbances (e.g. diarrhoea, nausea, vomiting, abdominal pain, flatulence), Rarely, blood dyscrasia (e.g. agranulocytosis, aplastic anaemia, leucopenia, methaemoglobinaemia, neutropenia, thrombocytopenia), myocarditis, pericarditis, pancreatitis, interstitial nephritis, nephritic syndrome, allergic lung reaction, increased liver enzyme values, hepatitis, lupus-like syndrome, skin reactions, alopecia, peripheral neuropathy, arthralgia, myalgia, hypersensitivity reactions, exacerbation of symptoms of colitis.
Potentially Fatal: Induced pericarditis.
Drug Interactions
Drugs that lower colonic pH (e.g. lactulose) may prevent the release of mesalazine. Increased risk of haematologic toxicity w/ azathioprine or mercaptopurine. Increased risk of nephrotoxicity w/ nephrotoxic drugs (e.g. NSAIDs, azathioprine). May decrease GI absorption of digoxin.
Lab Interference
May cause falsely-elevated urinary normetanephrine levels when measured by liq chromatography w/ electrochemical detection.
Action
Mesalazine is considered to be the active moiety of sulfasalazine. The mechanism of action is uncertain, but may be due to its ability to inhibit prostaglandin and leukotriene synthesis in the GI mucosa.
Absorption: Variable, depending on formulation and route of admin.
Distribution: Crosses placenta and enters breast milk (small amounts). Plasma protein-binding: 40-50%.
Metabolism: Undergoes acetylation in the gut wall and liver to acetyl-5-aminosalicylic acid.
Excretion: Via faeces and urine, 10-30%. Plasma half-life: Approx 40 min.
Storage
Oral: Store below 25°C. Protect from light. Rectal: Store below 25°C. Protect from light.
ATC Classification
A07EC02 - mesalazine ; Belongs to the class of aminosalicylic acid and similar antiinflammatory. Used in the treatment of intestinal inflammation.
Disclaimer: This information is independently developed by CIMS based on mesalazine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 CIMS. All rights reserved. Powered by CIMSAsia.com
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