$139.00
Manufacturer: Switzerland
Asacol (mesalazine) is used for nonspecific ulcerative colitis of mild to moderate severity, supportive treatment in the stage of remission. Crohn’s disease.
Description
Ingredients:
active substance: mesalazine;
1 tablet contains mesalazine 400 mg or 800 mg;
excipients: lactose monohydrate, sodium starch glycolate (type A), magnesium stearate, talc, povidone;
shell: methacrylic copolymer (type B), talc, triethyl citrate, iron oxide yellow (E 172), iron oxide red (E 172), macrogol 6000.
Pharmaceutical form. Film-coated tablets are enteric-soluble.
Main physico-chemical properties: oblong tablets, covered with a shell, from reddish to brownish color.
Pharmacotherapeutic group.
Anti-inflammatory agents used in intestinal diseases. ATX code A07E C02.
Pharmacological properties.
Pharmacodynamics.
The mechanism of anti-inflammatory action of mesalazine (5-aminosalicylic acid) is unknown. Research results indicate that mesalazine suppresses the migration of polymorphonuclear leukocytes and inhibits the activity of lipoxygenase, as a result of which the synthesis of anti-inflammatory leukotrienes in macrophages of the intestinal wall is inhibited. There are also data on the effect of mesalazine on the concentration of prostaglandins in the intestinal mucosa. Mesalazine can bind free radicals.
When used orally, mesalazine acts mainly locally on the intestinal mucosa and on the submucosal tissue from the side of the intestinal cavity. Therefore, it is important that mesalazine is available in areas of inflammation. Systemic bioavailability and concentration in blood plasma are not essential for the therapeutic effect, but most likely are a factor of harmlessness.
Pharmacokinetics.
Asakol® tablets, covered with an enteric coating, are resistant to gastric juice. The polymer shell of the tablets ensures the release of the active substance depending on the pH of the environment in the lower part of the ileum and large intestine, which are the main centers of inflammation. The composition of the tablets is selected in such a way as to minimize the absorption of mesalazine in the digestive tract. Absorption of mesalazine is highest in the proximal part of the intestine and lowest in the distal part. Absorption after oral administration is about 24%. Accordingly, 76% of the administered dose remains in the lower ileum and large intestine, as well as in the rectum, showing a local anti-inflammatory effect.
Mesalazine is metabolized in the liver and intestinal mucosa with the formation of an inactive metabolite of N-acetyl-5-aminosalicylic acid. Binding of mesalazine and its metabolite to blood plasma proteins is 43% and 78%, respectively. Excretion occurs mainly with feces and urine in unchanged form and in the form of a metabolite.
Indications.
Nonspecific ulcerative colitis of mild to moderate severity; supportive treatment in the stage of remission. Crohn’s disease.
Contraindications.
Hypersensitivity to the active substance, to any other component of the drug or to salicylates; severe liver and kidney function disorders (creatinine clearance < 30 ml/min); peptic ulcer disease of the stomach and duodenum; hemorrhagic diathesis.
Dosage and Administration.
Adults
Ulcerative colitis.
When treating the disease in the acute phase, the dose is selected individually and is up to 4 g of mesalazine per day, divided into several doses.
With maintenance treatment in the stage of remission, the recommended dose is up to 2 g of mesalazine 1 time per day, selected individually. It is also possible to divide the dose into several doses.
Crohn’s disease.
In the treatment of the disease in the phase of exacerbation and maintenance therapy, the dose is selected individually and is up to 4 g of mesalazine per day, divided into several doses.
Elderly patients do not need dose adjustment, unless renal function is impaired.
Children aged 6 and over
In the treatment of ulcerative colitis and Crohn’s disease in the exacerbation stage, the dose should be selected individually, starting with 30-50 mg/kg of body weight/day, divided into several doses. The maximum dose is
75 mg/kg of body weight/day, divided into several doses. The total daily dose should not exceed 4 g of mesalazine.
For maintenance therapy, the dose should be selected individually, starting with 15-30 mg/kg of body weight/day, divided into several doses. The total daily dose should not exceed 2 g of mesalazine.
As a rule, children with a body weight of up to 40 kg are prescribed half the adult dose, and children with a body weight of more than 40 kg are prescribed a full adult dose.
Tablets should be taken whole, without chewing, with a sufficient amount of liquid, 1 hour before meals. Both during exacerbation of the disease and during maintenance treatment in the stage of remission, in order to achieve the desired therapeutic effect, Asakol® tablets should be taken regularly and continuously. The duration of use is determined by the doctor. Usually, remission in ulcerative colitis and Crohn’s disease occurs after 8-12 weeks of taking Asacol®.
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