Asacol

Mesalazine.

Each gastro-resistant tablet contains 400 mg mesalzine.
Each suppository contains 500 mg mesalazine.
Excipients/Inactive Ingredients: The tablets contain a small amount of lactose (400mg: 76 mg).

The tablets are used for the induction of remission of mild to moderate ulcerative colitis and the maintenance of remission of ulcerative colitis. The tablets are also used for the maintenance of remission of Crohn's disease.
The suppositories are used for the induction of remission of proctitis and proctosigmoiditis.
The suppositories can be used in combination with tablets in more serious generalized disease and in cases slow respond to oral therapy alone.

Tablets: Ulcerative colitis: Adult dose for the induction of remission 2.4 to 4.8g daily in divided doses. For maintenance of remission 1.2 to 2.4g daily in divided doses.
Crohn's disease: Adult dose for the maintenance of remission 2.4g daily in divided doses.
The tablets are for oral administration and must be swallowed whole and not chewed or broken. Ideally the tablets should be taken with a glass of water before meals.
Use in the elderly should be handled with caution and only for patients having a normal renal function.
There is no specific dose recommendation for children.
Suppositories: Adult dose for the induction of remission of proctitis and proctosigmoiditis one 500mg suppository three times a day, after defecation. To be inserted in the morning, at noon and in the evening. 1 suppository each time. There is no specific dose recommendation for children. The suppositories are for rectal use and must not be swallowed.

In principle, the signs and symptoms would be expected to be similar to those observed in cases of salicylate intoxication: mixed acidosis-alkalosis, hyperventilation, pulmonary edema, dehydration as a result of sweating and vomiting, and hypoglycemia.
Treatment: For mixed acidosis-alkalosis: restoration of the acid-base balance in line with the specific situation and replacement of electrolytes.
For dehydration due to sweating and vomiting: administration of fluids.
For hypoglycemia: glucose administration.
In addition gastric lavage and intravenous transfusion of electrolyte to promote diuresis. There is no known antidote.

Contra-indicated in patients with a history of allergy to salicylates, in patients with a hypersensitivity to an ingredient, and in patients with severe liver and renal impairment (GFR less than 20 ml per minute). Other contra-indications include gastric or duodenal ulcers, hemorrhagic tendency. Children under two years of age.

Not recommended for use in patients with renal impairment and caution should be exercised in patients with raised blood urea or proteinuria. The possibility of mesalazine-induced nephrotoxicity should be considered in patients developing impairment of renal function during treatment. It is recommended that all patients have an evaluation of their renal function prior to initiation of Asacol therapy and periodically while on Asacol therapy. Such a test is generally recommended within 14 days of initiation of therapy with 2-3 repeat evaluations each after another 4 weeks. If the results are normal, tests are recommended quarterly. In case additional signs of illness appear, further control tests are necessary.
In case of lung function impairment, especially asthma, patients need to be very closely monitored.
In patients with history of sensitivity to sulphasalazine, therapy should be initiated only under close medical supervision. Treatment must be stopped immediately if acute symptoms of intolerance such as cramps, abdominal pain, fever, severe headache, or rash.
Very rarely serious blood dyscrasia has been reported. Hematological investigations, including a complete blood count, should be performed prior to initiation and whilst on therapy according to the physician's judgment. Such tests are generally recommended within 14 days of initiation of therapy with 2-3 repeat tests each after another 4 weeks.
If the results are normal, tests are recommended quarterly. In case additional signs of illness appear, further control tests are necessary.
This procedure is to be followed especially, if a patient develops signs or symptoms pointing to blood dyscrasia during treatment, such as unexplained bleeding, hematoma, purpura, anemia. continuous fever, or a sore throat. Treatment with Asacol should be stopped immediately if there is a suspicion or evidence of blood dyscrasia and patients should seek immediate medical advice.
Safety and effectiveness of Asacol tablets and suppositories have not been fully established in pediatric patients.
Use in the elderly should be handled with caution and only for patients having a normal renal function.

Animal studies have revealed no evidence of teratogenic effects or fetal toxicity due to mesalazine. Limited clinical studies on the use of mesalazine in pregnancy have shown no detrimental effect on gestation and fetal outcome.
Low concentrations of mesalazine and its N-acetyl metabolite have been detected in human breast milk. Whilst the clinical significance of this has not been determined, caution should be exercised when mesalazine is administered to a nursing mother.
The use of mesalazine during pregnancy and lactation should be restricted to those cases where in the physician's opinion potential benefits from this therapy outweigh potential risks.

Dose-dependent hypersensitivity reactions such as fever¹, bronchospasm¹ or alopecia¹ can occur rarely¹. Alopecia can also be a rare extra-intestinal manifestation of chronic inflammatory bowel disease. Other rare¹ adverse reactions are predominantly gastrointestinal, including diarrhoea and abdominal pain.
Adverse reactions which occur rarely very rarely² are listed by system organ class.
Blood and lymphatic: Blood dyscrasia, bone marrow depression with leukopenia, neutropenia, thrombocytopenia, pancytopenia up to aplastic anemia.
Nervous system: Headache, vertigo, arthralgia.
Cardiac: Myocarditis, pericarditis.
Muscles: Myalgia.
Respiratory: Allergic lung reactions, bronchospasm, eosinophilic penumonia.
Digestive: Nausea, vomiting, pancreatitis, hepatitis, exacerbation of the symptoms of colitis.
Skin and appendages: Mesalazine-induced lupus-erythematodes-like symptoms with pericarditis and pleuroperi-carditis as prominent symptoms as well as rash and arthralgia.
Renal & urinary: Interstitial nephritis, nephrotic syndrome. Renal failure, which may be reversible on withdrawal.
Patients should immediately inform their physician if they experience any of these changes or other signs of illness.
¹rare: one adverse reaction in 1000 to 10,000 treatment years.
²very rare: less than one adverse reaction per 10,000 treatment years.

Mesalazine decreases the absorption of digoxin.
Mesalazine can increase the immunosuppresive effects of azathioprine and 6-mercaptopurine. A blood count, especially the leukocyte cell count should be monitored repeatedly, especially at initiation of such combination therapy.
The uricosuric activity of probenecid and sulfinpyrazone, the diuretic effect of furosemide and the activity of spironolactone can be reduced.
Gastrointestinal side-effects of glucocorticoids can be increased.

The products should not be stored above 25°C. They should stored in a dry place.

GIT Regulators, Antiflatulents & Anti-Inflammatories

A07EC02 - mesalazine ; Belongs to the class of aminosalicylic acid and similar antiinflammatory. Used in the treatment of intestinal inflammation.

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