SUMMARY OF PRODUCT CHARACTERISTICS

1 NAME OF THE MEDICINAL PRODUCT

Asacol 500mg Suppositories

2 QUALITATIVE AND QUANTITATIVE COMPOSITION

Asacol Suppositories contain 500mg mesalazine per suppository.

3 PHARMACEUTICAL FORM

Opaque, beige suppositories, containing 500mg mesalazine.

4 CLINICAL PARTICULARS

4.1 Therapeutic indications

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.

4.2 Posology and method of administration

ADULTS:

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.

ELDERLY: The normal adult dosage may be used unless renal function is impaired (see section 4.4).

CHILDREN: There is no dosage recommendation.

4.3 Contraindications

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.

4.4 Special warnings and precautions for use

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 (see section 4.3). 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.

4.5 Interaction with other medicinal products and other forms of interaction

Concurrent use of other known nephrotoxic agents, such as NSAIDs and azathioprine, may increase the risk of renal reactions (see section 4.4)

4.6 Pregnancy and lactation

No information is available with regard to teratogenicity; however, negligible quantities of mesalazine are transferred across the placenta and are excreted in breast milk following sulphasalazine therapy. Use of Asacol during pregnancy should be with caution, and only if the potential benefits are greater than the possible hazards. Asacol should, unless essential, be avoided by nursing mothers.

4.7 Effects on ability to drive and use machines

Not applicable.

4.8    Undesirable effects

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.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme; website: www.mhra.gov.uk/yellowcard

4.9    Overdose

There is no specific antidote.

Pharmacodynamic properties

Mesalazine is one of the two components of sulphasalazine, the other being sulphapyridine. It is the latter which is responsible for the majority of the side effects associated with sulphasalazine therapy whilst mesalazine is known to be the active moiety in the treatment of ulcerative colitis. Asacol consists only of this active component which is delivered directly by the suppositories.

5.2 Pharmacokinetic properties

The suppository is designed to deliver mesalazine directly to the proposed site of action in the distal bowel.

5.3 Preclinical safety data

There are no preclinical data of relevance to the prescriber which are additional to that already included in other sections of the SPC.

6 PHARMACEUTICAL PARTICULARS

6.1 List of excipients

Witepsol W45 (Hard Fat).

6.2 Incompatibilities

Not applicable.

Shelf life

3 years.