Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Anti-inflammatory drug with a predominant localization of the action in the intestine. Mesalazine (5-aminosalicylic acid) inhibits the activity of neutrophilic lipoxygenase and the synthesis of arachidonic acid metabolites (prostaglandins and leukotrienes) that mediate inflammation. It inhibits migration, degranulation, phagocytosis of neutrophils, as well as secretion of immunoglobulins by lymphocytes. Mesalazine has antioxidant properties, 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. The binding with plasma proteins is 43%. Metabolized in the intestinal mucosa and in the liver with the formation of N-acetyl-5-ASA. T 1/2 is 0.5-2 hours. Mesalazine is excreted in urine, mostly in acetylated form.
INDICATIONS
NNC, Crohn's disease (prevention and treatment of exacerbations).
DOSING MODE
Inside, apply 400-800 mg 3 times / day for 8-12 weeks.
SIDE EFFECT
On the part of the digestive system: diarrhea, nausea, vomiting, heartburn, abdominal pain, loss of appetite, dry mouth, stomatitis, increased activity of hepatic enzymes.
From the nervous system: headache, depression, dizziness, sleep disorders, paresthesia, tremor, tinnitus.
Allergic reactions: skin rash, itching, erythema.
From the cardiovascular system: a feeling of palpitations, tachycardia, hypertension or hypotension, chest pain, shortness of breath.
From the urinary system: proteinuria, hematuria, crystalluria, oliguria, anuria.
On the part of the hematopoiesis system: anemia, leukopenia, agranulocytosis, thrombocytopenia; hypoprothrombinemia.
Other: alopecia, a decrease in the production of tear fluid.
CONTRAINDICATIONS
Diseases of the blood, expressed violations of the liver and / or kidney, peptic ulcer of the stomach or duodenum in the phase of exacerbation, blood clotting disorders, children under 2 years old, hypersensitivity to salicylates.
PREGNANCY AND LACTATION
In the first trimester of pregnancy, use is only possible on strict indications. If individual course of the disease allows, in the last 2-4 weeks of pregnancy, the use of mesalazine should be discontinued.
If it is necessary to use during the lactation period, 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 FUNCTIONS OF THE LIVER
Contraindicated in severe impairment of kidney function.
Use with caution in diseases of the kidneys.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function.
Use with caution in diseases of the liver.
APPLICATION FOR CHILDREN
Contraindicated in children under 2 years. Use in children younger than 2 years is possible only if the intended benefit of therapy exceeds the potential risk to the child.
SPECIAL INSTRUCTIONS
With caution apply for diseases of the liver and kidneys, insufficiency of glucose-6-phosphate dehydrogenase, allergic diseases and predisposition to them. Before the start of treatment, and then monthly for the first 3 months of treatment should monitor the pattern of peripheral blood, liver function, as well as determining the concentration of urea and creatinine in the blood. In patients who are "slow acetylators", the risk of side effects is increased.
Use in children under 2 years of age is possible only if the intended benefit of therapy exceeds the potential risk for 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 is described.
