Salicylates

Mesalazine

Asacol Suppositories contain 250 or 500 mg mesalazine per suppository.

Opaque, beige suppositories, containing 250 mg or 500 mg mesalazine

For the treatment of mild to moderate acute exacerbations of ulcerative colitis. The suppositories are particularly appropriate in patients with distal disease. For the maintenance of remission of ulcerative colitis.

Suppositories 250 mg: Three to six suppositories a day in divided doses, with the last dose at bedtime.

Suppositories 500 mg: A maximum of three suppositories a day in divided doses, with the last dose at bedtime.

There is no dosage recommendation.

The normal adult dosage may be used unless renal function is impaired (See Special Precautions).

A history of sensitivity to salicylates or renal sensitivity to sulphasalazine. Confirmed severe renal impairment (GFR <20 ml/min). Children under 2 years of age.

Use in the elderly should be cautious and subject to patients having normal renal function.

Renal disorder: Mesalazine is excreted rapidly by the kidney, mainly as its metabolite, N-acetyl-5-aminosalicylic acid. In rats, large doses of mesalazine injected intravenously produce tubular and glomerular toxicity. Asacol should be used with extreme caution in patients with confirmed mild to moderate renal impairment. Treatment with mesalazine should be discontinued if renal function deteriorates. If dehydration develops, normal electrolyte and fluid balance should be restored as soon as possible.

Serious blood dyscrasias have been reported very rarely with mesalazine. Haematological investigations should be performed if the patient develops unexplained bleeding, bruising, purpura, anaemia, fever or sore throat. Treatment should be stopped if there is suspicion or evidence of blood dyscrasia

Concurrent use of other known nephrotoxic agents, such as NSAIDs and azathioprine, may increase the risk of renal reactions.

The side effects are predominantly gastrointestinal, including nausea, diarrhoea and abdominal pain. Headache has also been reported.

There have been rare reports of leucopenia, neutropenia, agranulocytosis, aplastic anaemia and thrombocytopenia, alopecia, peripheral neuropathy, pancreatitis, abnormalities of hepatic function and hepatitis, myocarditis and pericarditis, allergic and fibrotic lung reactions, lupus erythematosus-like reactions and rash (including urticaria), interstitial nephritis and nephrotic syndrome with oral mesalazine treatment, usually reversible on withdrawal. Renal failure has been reported. Mesalazine-induced nephrotoxicity should be suspected in patients developing renal dysfunction during treatment.

Mesalazine may very rarely be associated with an exacerbation of the symptoms of colitis, Stevens Johnson syndrome and erythema multiforme.

Other side effects observed with sulphasalazine such as depression of sperm count and function, have not been reported with Asacol.

Rarely, local irritation may occur after administration of rectal dosage forms containing mesalazine.

Procter & Gamble

(POM)

11 August 2009