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.
This drug may cause nausea, if affected, do not drive or operate machinery.
Monitoring Parameters
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: Mechanism of 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. 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.
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.