Mesalazine - instructions for use, dose, side effects, contraindications

Inhibition of cyclooxygenase and lipoxygenase, a decrease in the production of prostaglandins, leukotrienes and hydroxyicosatetraenoic acids, has an anti-inflammatory effect. It inhibits migration, degranulation, phagocytosis of neutrophils, as well as secretion of immunoglobulins by lymphocytes,has antioxidant properties, binding to free oxygen radicals.

Pharmacokinetics:

Biotransformation in the intestinal mucosa and liver to N-acetyl-5-aminosalicylic acid. The connection with plasma proteins is ~ 40%. Depending on the dosage form and route of administration, the release of mesalazine occurs in the rectum and colon (enema, suppository) or in the terminal section of the small intestine and large intestine (tablets).

Indications:

Prevention and treatment of exacerbations of Crohn's disease and nonspecific ulcerative colitis.

ICD-10

XI.K50-K52.K50 Crohn's disease [regional enteritis]

XI.K50-K52.K51 Ulcerative colitis

Contraindications:

Individual intolerance, in including other derivatives of salicylic acid.

Pronounced violations of the liver and / or kidney function.

Diseases of the blood.

Hemorrhagic diathesis.

Stomach ulcer and duodenal ulcer.

The last 2-4 weeks pregnancy.

Breast-feeding.

Children up to 2 years.

Carefully:

Impaired liver and / or kidney function.

The first trimester of pregnancy.

Deficiency of glucose-6-phosphate dehydrogenase.

Pregnancy and lactation:

Action category for the fetus by by FDA - B.In the first trimester of pregnancy, the appointment of mesalazine is possible only according to strict indications, in the last 2-4 weeks pregnancy, the drug should be discontinued. When prescribing during breastfeeding, the child should be transferred to the mixture.

Dosing and Administration:

Adults with exacerbation - 400-500 mg 3 times a day, maintenance dose - 500 mg 3 times a day for ulcerative colitis and 1 g 4 times a day for Crohn's disease. Children older than 2 years - 20-30 mg / kg in dayki in several receptions. In severe disease, the daily dose can be increased to 3-4 g, but not more than 8-12 weekspruce. The drug is taken orally with a large amount of water.

Candles are injected after emptying the rectum: with proctitis, proctosigmoid and left-sided ulcerative colitis adults - 1 suppository (500 mg) 3 times a day. Children with a body weight of up to 40 kg - about 250 mg 3 times a day. In the form of drug microclysters, depending on the prevalence of the lesion, 2-4 g of mesalazine (30-60 ml of suspension) 1 time per day, before bedtime.

Side effects:

Digestive system: loss of appetite, nausea, vomiting, heartburn, abdominal pain, diarrhea, bloating, increased liver transaminases, hepatitis, pancreatitis, parotitis.

The cardiovascular system: palpitation, tachycardia, increase or decrease blood pressure, chest pain, shortness of breath.

Blood: anemia (hemolytic, megaloblastic, aplastic), leukopenia, agranulocytosis, thrombocytopenia, hypoprothrombinemia.

Nervous system: headache and tremor, dizziness, sleep disorders, paresthesia, depression, malaise, convulsions, tinnitus.

Genitourinary system: protein and blood in the urine, crystalluria, oliguria, anuria, nephrotic syndrome, oligospermia.

Allergic reactions: skin rash, itching, erythema, bronchospasm.

Others: a decrease in the production of tear fluid, fever, photosensitivity, lupus-like syndrome, alopecia, possibly a rise in the level of methemoglobin.

Overdose:

In case of an overdose, nausea, vomiting, pain in the stomach, weakness and drowsiness are observed. It is necessary to wash the stomach (with ingestion), a laxative and symptomatic therapy.

Interaction:

Omeprazole - increases the absorption of mesalazine.

Azathioprine - increases the risk of leukopenia.

The drug enhances the ulcerogenicity of glucocorticoids, the toxicity of methotrexate, the hypoglycemic effect of sulfonylurea derivatives,hypoprothrombinemic - anticoagulants.

With simultaneous use, the drug slows down the absorption of cyanocobalamin. Weaken the activity of furosemide, spironolactone, rifampicin.

Special instructions:

Before the start of therapy, during treatment (1-2 times per month) and after its completion (every 3 months), the composition of peripheral blood, the level of urea, creatinine, a general urine test should be monitored.

Instructions

Mesalazine (Mesalazinum)