Pharmacological action of Asacol

Antiinflammatory agent with predominant localization of action in the intestine. Mesalazine (5-aminosalicylic acid) inhibits the activity of neutrophilic lipoxygenase and the synthesis of arachidonic acid metabolites (prostaglandins and leukotrienes), which are inflammatory mediators. It inhibits migration, degranulation, phagocytosis of neutrophils, as well as the secretion of immunoglobulins by lymphocytes. Mesalazine has antioxidant properties by binding to free oxygen radicals.

Pharmacokinetics

After oral administration, mesalazine is slowly released from the dosage form in the distal small intestine and in the large intestine. Plasma protein binding is 43%. It is metabolized in the intestinal mucosa and in the liver to form N-acetyl-5-ASA. T1/2 is 0.5-2 hours. Mesalazine is excreted in the urine, mainly in the acetylated form.

Indications of the active substances of the drug Asacol

Nonspecific ulcerative colitis, Crohn's disease (prevention and treatment of exacerbations).

Contraindications to use

Blood diseases, severe liver and / or kidney dysfunction, gastric ulcer or duodenal ulcer in the acute phase, blood coagulation disorders, children under 2 years of age, hypersensitivity to salicylates.

Application during pregnancy and lactation

In the first trimester of pregnancy, use is possible only under strict indications. If the individual course of the disease allows, then in the last 2-4 weeks of pregnancy, the use of mesalazine should be discontinued.

If it is necessary to use it during lactation, the issue of stopping breastfeeding should be resolved, due to the lack of sufficient clinical experience with the use of mesalazine in this category of patients.

Application for violations of liver function

Contraindicated in severe violations of liver function.

Use with caution in liver diseases.

Application for impaired renal function

Contraindicated in severe renal impairment.

Use with caution in kidney disease.

Use in children

Contraindicated in children under 2 years of age. Use in children under 2 years of age is possible only if the intended benefit of therapy outweighs the potential risk to the child.

Special instructions

Use with caution in diseases of the liver and kidneys, deficiency of glucose-6-phosphate dehydrogenase, allergic diseases and predisposition to them. Before starting treatment, and then monthly during the first 3 months of treatment, monitoring of the picture of peripheral blood, liver function, as well as determination of the concentration of urea and creatinine in the blood should be carried out. Patients who are "slow acetylators" are at increased risk of side effects.

Use in children under 2 years of age is possible only if the intended benefit of therapy outweighs the potential risk to the child.

Drug interaction

With the simultaneous use of mesalazine with azathioprine, mercaptopurine, the toxicity of azathioprine and mercaptopurine increases; with warfarin - a case of decreasing the effectiveness of warfarin has been described.

Side effect

From the digestive system: diarrhea, nausea, vomiting, heartburn, abdominal pain, loss of appetite, dry mouth, stomatitis, increased activity of liver enzymes.

From the nervous system: headache, depression, dizziness, sleep disturbances, paresthesia, tremors, tinnitus.

Allergic reactions: skin rash, itching, erythema.

From the side of the cardiovascular system: palpitations, tachycardia, arterial hypertension or hypotension, chest pain, shortness of breath.

From the urinary system: proteinuria, hematuria, crystalluria, oliguria, anuria.

From the hematopoietic system: anemia, leukopenia, agranulocytosis, thrombocytopenia; hypoprothrombinemia.

Others: alopecia, decreased production of tear fluid.