Mesalazine


Generic Medicine Info
Indications and Dosage
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.

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.
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.
Patient Counseling Information
This drug may cause nausea, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor renal and hepatic function, CBC.
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
Description: 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.
Pharmacokinetics:
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.
Chemical Structure

Chemical Structure Image
Mesalazine

Source: National Center for Biotechnology Information. PubChem Database. Mesalamine, CID=4075, https://pubchem.ncbi.nlm.nih.gov/compound/Mesalamine (accessed on Jan. 22, 2020)

Storage
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.
References
Anon. Mesalamine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 11/02/2016.

Anon. Mesalamine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 11/02/2016.

Buckingham R (ed). Mesalazine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/02/2016.

Disclaimer: This information is independently developed by MIMS 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 MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS 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 © 2021 MIMS. All rights reserved. Powered by MIMS.com
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