Mesalazine - instructions for use. Mesalazine: help to the intestines in case of serious diseases Sign up for a consultation with Andrey Gennadievich

Latin name: Mesalazine
ATX code: A07EC02
Active substance:
Manufacturer: Canonpharma Production,
Russia and others
Pharmacy leave condition: On prescription
Price: from 350 to 700 rubles.

Mesalazine is an anti-inflammatory drug. At present, it is impossible to purchase it in the country's pharmacies, only Mesalazine analogues with an identical active substance.

Indications for use

"Mesalazine" is only suitable for a fairly narrow range of diseases: Crohn's disease and ulcerative colitis. Diseases can be in stages of any type, "Mesalazine" is applicable to all.

Composition

One Mesalazine tablet contains:

• Active ingredient: 500 mg mesalazine
• Other ingredients: copovidone, silicon dioxide, sodium alginate, magnesium stearate, calcium hydrogen phosphate dihydrate, cellulose.

Medicinal properties

Impact medicinal product on the body - a purely anti-inflammatory, localized for the most part in the intestines, at the epicenter of inflammation. Mesalazine is capable of:

• Inhibit the synthesis and activity of inflammatory mediators - metabolites of arachidonic acid and neutrophilic lipoxygenase
• Inhibit degranulation, migration, phagocytosis and also suspend the secretion of immunoglobulins
• Contact with free oxygen radicals (the substance has antioxidant qualities).

When a person takes the tablets of this drug, mesalazine is released from the shell in the colon or thin department intestines, and then begins to act. The entire volume of Mesalazine is excreted in the urine.

The average price is from 350 to 700 rubles.

Release form

The drug can be found in the form of a cardboard pack. Inside it are cell packs containing 15 pieces of tablets. In total, there can be 2, 4, 6 and 10 packs in a pack.

Tablets are white-grayish, almost white in color, and small blotches are possible on their surface. The shape of the tablets is biconvex, round.

Mode of application

"Mesalazine" treats two diseases - Crohn's disease and ulcerative colitis, and for each of them it must be used in accordance with a separate instruction. Below are the doses that are most often prescribed to patients, but it is up to the specialist to determine the personal rate of the drug for a particular patient.

For Crohn's disease

With an exacerbation of the disease and during maintenance therapy:

• Adults: up to about 4 g of medicine per day, divided into several doses
• Children: most commonly 20-30 mg per kg of body weight per day, divided into two doses.

For ulcerative colitis

When the disease is exacerbated:

• Adults: most often up to 4 g of medicine per day, divided into several doses
• Children: usually 20-30 mg per kg of body weight per day, divided into two doses.

With maintenance therapy:

• Adults: about 2 g of medicine per day, divided into several doses
• Children: most often - 20-30 mg per kg of weight per day, divided into several doses.

During pregnancy and breastfeeding

The active substance of the drug - mesalazine - is able to penetrate the placental barrier, but all the permissible consequences of this phenomenon have not yet been evaluated and investigated. So in any case, it is possible to use the drug for pregnant women only under emergency circumstances, if the expected benefit will prevail over the predicted harm to the unborn child. In addition, it is completely forbidden to drink pills in the ninth month of pregnancy.

"Mesalazine" is also able to penetrate into breast milk therefore, when using the drug during lactation, it is necessary to stop breastfeeding.

Contraindications

There are some contraindications to the use of Mesalazine tablets:

• Blood diseases
• Peptic ulcer of the duodenum or stomach
• Renal, liver failure
• Hemorrhagic diathesis
• Hypersensitivity
• Patient's age up to 12 years
• Weight up to 50 kg.

Precautionary measures

The main thing to do is to check and monitor the level of urea, creatinine, blood composition every month for three months before starting the course of treatment and after it every month for three months. It is also necessary to do general analysis urine.

During treatment, it is necessary to monitor the patient's condition, and in case of symptoms of hypersensitivity or allergy, the drug should be discontinued immediately. You need to know that sometimes it is difficult to distinguish hypersensitivity syndrome from severe inflammation of the intestine.

Patients who are "slow acetylators" experience symptoms of side effects more often than others.

Cross-drug interactions

Tablets "Mesalazine" interact:

• With methotreskate - exacerbate toxicity
• With furosemide, spironolactone, sulfanilamide, rifampicin - reduce activity
• With anticoagulants - increase the effect
• With sulfonylurea derivatives - improve hypoglycemic effect
• With blockers of tubular secretion - enhance the effect
• With cyanocobalamin - inhibit absorption.

Side effects

Certain symptoms, conditions and illnesses are likely to occur when using pills, and here are some of them:

• Hypersensitivity and allergic reactions: itching, skin rash, bronchospasm, erythema
• Gastrointestinal organs: vomiting, nausea, heartburn, flatulence, diarrhea, hepatitis, parotitis, pancreatitis
• Circulatory system: palpitations, tachycardia, blood pressure disorders, shortness of breath, anemia, leukopenia, agranulocytosis, thrombocytopenia
• Nervous system: headache, dizziness, sleep disturbance, depression, paresthesia, convulsions, tremor
• Genitourinary system: proteinuria, hematuria, crystalluria, oliguria, anuria, nephrotic syndrome, oligospermia.

Sometimes patients experienced fever, alopecia, lupus-like syndrome, photosensitivity. A decrease in the production of lacrimal fluid and an increase in the level of methemoglobin are also likely.

Overdose

When the dose of Mesalazine tablets is exceeded, an overdose often occurs. Its signs are:

• Weakness
• Drowsiness
• Nausea
• Vomit
• Gastralgia (cramping pains in the stomach associated with its diseases).

To eliminate these symptoms and prevent their complications, a special treatment is carried out: first, the patient's stomach is washed, and then the doctor prescribes a laxative and symptomatic therapy.

Terms and conditions of storage

Analogues

Dr. Falk Pharma GmbH, Germany
Price from 1200 to 7400 rubles.

The drug "Salofalk" has the same active ingredient as "Mesalazin." "Salofalk" can be found in the form of tablets, and in the form of granules, and in the form of suppositories, and in the form of a suspension.

Tablets "Salofalk" have a light yellow, and sometimes yellow-brown color. And Salofalk granules are also able to treat exacerbations of mild and moderate colitis and maintain remission.

pros

• Ability to treat exacerbations of colitis with granules and maintain its remission
• Suitable for children from three years of age.

Minuses

• higher price
• More side effects.

Krka, Slovenia
Price from 250 to 440 rubles.

The drug "Sulfasalazine" has sulfasalazine as an active ingredient and is available only in the form of tablets.

pros

• Can be used by children over 6 years old
• Treatment of arthritis
• Long lasting effect

Minuses

• More contraindications
• Long term treatment.

Ferring, Denmark
Price from 3000 to 9700 rubles

Pentasa is another analogue of Mesalazine, which has a similar active ingredient. Its main plus is that it can be given to children from two years old. It is also available in the form of tablets, suppositories, suspensions and granules.

pros

• Can be given to children from two years
• Many release forms: tablets, granules, suppositories, suspension

Minuses

• TO side effects allergic dermatosis, myocarditis, etc.
• higher price.

Anti-inflammatory drugs - derivatives of salicylic acid.

Composition Mesalazine

The active substance is mesalazine.

Manufacturers

Canonpharma production (Russia)

pharmachologic effect

pharmachologic effect- anti-inflammatory.

It inhibits the synthesis of PG, inhibits chemotaxis, degranulation and phagocytosis of neutrophils, the secretion of immunoglobulins by lymphocytes, and has antioxidant properties.

Plasma concentration is low.

In the intestinal mucosa and liver forms N-acetyl-5-aminosalicylic acid.

Effective in the treatment of colitis, ileitis in Crohn's disease, for the prevention of exacerbations of ulcerative colitis in patients with hypersensitivity to sulfasalazine, is well tolerated.

Reduces the risk of recurrence in Crohn's disease, especially in patients with ileitis and a long duration of the disease.

Side effects of mesalazine

Feeling of discomfort, pain in the abdomen, nausea, flatulence, frequent urge to defecate, exacerbation of hemorrhoids, hyperthermia, flu-like syndrome and acute intolerance syndrome (colic, bloody diarrhea, fever, headache, rash), asthenia, drug-induced lupus-like syndrome, arthralgia, alopecia, methemoglobinemia, increased levels of transaminases, alkaline phosphatase, creatinine, urea nitrogen, allergic skin rashes.

Indications for use

Inflammatory bowel disease (ulcerative colitis, Crohn's disease), in the acute stage and prevention of their recurrence.

Contraindications Mesalazine

Hypersensitivity (including to other derivatives of salicylic acid), severe violations of the liver and kidneys, blood diseases, hemorrhagic diathesis, peptic ulcer stomach and duodenum, pregnancy, breastfeeding (stop for the duration of treatment), childhood(up to 2 years).

Overdose

No information.

Interaction

It enhances the ulcerogenicity of glucocorticoids, the toxicity of methotrexate, the hypoglycemic effect of sulfonylurea derivatives, the hypoprothrombinemic effect of anticoagulants.

Slows down the absorption of cyanocobalamin.

Weakens the activity of furosemide, spironolactone, rifampicin.

special instructions

Choice dosage form depends on the location of the intestinal lesion and its prevalence.

With common forms of ulcerative colitis (total and subtotal), as well as with Crohn's disease with lesions small intestine tablets are used.

With distal forms (proctitis, proctosigmoiditis), it is preferable rectal application drug in the form of suppositories or enemas.

With a left-sided lesion of the colon, both therapy using only suppositories or enemas is possible, as well as their combination with tablets.

Before, during, and after treatment, the composition of peripheral blood, the level of urea, creatinine, and urinalysis should be monitored.

If acute intolerance syndrome is suspected, mesalazine should be discontinued.

In 1 tablet mesalazine 500 mg.

Calcium hydrogen phosphate, copovidone, colloidal silicon dioxide, magnesium stearate, sodium alginate, microcrystalline cellulose - as excipients.

Release form

Tablets with prolonged action number 50.

pharmachologic effect

Anti-inflammatory, antimicrobial.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

An anti-inflammatory agent that local action in the intestinal mucosa. It is active against Escherichia coli and cocci. Suppresses the synthesis of inflammatory mediators - prostaglandins and leukotrienes. It has antioxidant properties due to the ability to destroy free oxygen radicals. Reduces the risk of relapses Crohn's disease .

Pharmacokinetics

About 50% of the dose is absorbed in the small intestine. It undergoes acetylation in the intestines and in the liver. Contacts proteins for 43%. Metabolites are excreted by the kidneys and intestines. T1 / 2 0.5-2 hours Accumulates in individuals with chronic .

Indications for use

Treatment and prevention non-specific , proctitis , Crohn's disease .

IN I trimester of pregnancy it is possible to appoint according to strict indications.

Contraindications

• dysfunction of the liver and kidneys;
• hemorrhagic diathesis ;
• hypersensitivity;
• last month of pregnancy;
• lactation;
• age up to 2 years;
• children weighing less than 50 kg.

Side effects

• headache, sleep disturbance, seizures, depression , , noise in ears;
• abdominal pain, loss of appetite, heartburn, nausea, vomiting, , , hepatitis, ;
• heartbeat, increase in blood pressure, , shortness of breath;
• hemolytic or aplastic anemia , leukopenia, thrombocytopenia, agranulocytosis, hypoprothrombinemia;
• oliguria or , hematuria, nephrotic syndrome;
• rash, , itching, bronchospasm;
• fever, lupus-like syndrome.

Mesalazine, instructions for use (Method and dosage)

Mesalazine tablets are taken orally, whole, after meals, drinking plenty of water.

At ulcerative colitis in the acute stage, adults are prescribed 4 g per day (in several doses). The maximum SD is 6-8 g. The dose for children is 20-30 mg per 1 kg of body weight per day, divided into several doses. When switching to maintenance therapy, adults take 2 g per day.

At distal proctitis prescribe drugs in the form of candles. Since there is no form of release of Mesalazine candles, candles are used or 1 g 2 times a day. The duration of treatment is 2-3 months.

Peripheral blood picture, liver and kidney function are monitored monthly during treatment. In individuals with a reduced rate of acetylation in the liver, the risk of adverse reactions increases.

Overdose

A mild degree of overdose is manifested by dizziness, malaise, nausea, vomiting, visual impairment and fever (poor prognostic sign). In severe cases, it develops , drowsiness, collapse , , convulsions and bleeding.

In order to detect an overdose, which is not always clinically manifested, the concentration of salicylates in the blood is determined (above 70 mg% - severe poisoning, above 100 mg% - extremely severe).

Treatment: taking a laxative, gastric lavage, prescribing sorbents, symptomatic therapy, control of acid-base composition. Depending on this introduction or sodium citrate . Alkalinization of urine (if the level of salicylates is more than 40 mg%) is carried out by infusion of sodium bicarbonate. With pulmonary edema - mechanical ventilation with a mixture of oxygen.

Clinical and pharmacological group

pharmachologic effect

Anti-inflammatory drug with a 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 colon. 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 acetylated form.

Dosage

Inside apply 400-800 mg 3 times / day for 8-12 weeks.

drug interaction

With the simultaneous use of mesalazine with azathioprine, mercaptopurine, the toxicity of azathioprine and mercaptopurine increases; with warfarin - a case of a decrease in the effectiveness of warfarin is described.

Use during pregnancy and lactation

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

If necessary, use during lactation should decide on the termination breastfeeding, due to the lack of sufficient clinical experience with the use of mesalazine in this category of patients.

Side effects

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

From the CNS and peripheral nervous system: headache, depression, dizziness, sleep disturbances, paresthesia, tremor, 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 hemopoietic system: anemia, leukopenia, agranulocytosis, thrombocytopenia; hypoprothrombinemia.

Others: alopecia, decreased production of lacrimal fluid.

Indications

NUC, Crohn's disease (prevention and treatment of exacerbations).

Contraindications

Blood diseases, pronounced disorders of the liver and / or kidneys, peptic ulcer of the stomach or duodenum in the acute phase, blood clotting disorders, children under 2 years of age, hypersensitivity to salicylates.

special instructions

It is used with caution in diseases of the liver and kidneys, insufficiency of glucose-6-phosphate dehydrogenase, allergic diseases and predisposition to them. Before starting treatment, and then monthly during the first 3 months of treatment, the picture of peripheral blood, liver function, as well as the determination of the concentration of urea and creatinine in the blood should be monitored. Patients who are "slow acetylators" have an increased risk of side effects.

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

Preparations containing MESALAZINE (MESALAZINE)

In the treatment of diseases of the rectum is prescribed complex therapy, which will necessarily include rectal suppositories. Mesalazine suppositories remain the most effective. They quickly relieve the inflammatory process and contribute to a speedy recovery.

Composition and action

The drug is released in the form rectal suppositories in the amount of 7 pcs. in one blister. The active substance is mesalazine. Depending on the dosage of the active ingredient, the drug is released in 250 mg and 500 mg.

Additional components:

• cetyl alcohol;
• docusate sodium;
• semi-synthetic glycerides.

Trade names

There are the following trade names drug:

• Salofalk;
• Pentasa;
• Akasol;
• 5 ASA.

Pharmacological properties of suppositories with mesalazine

It is an antimicrobial and anti-inflammatory agent.

Pharmacodynamics

Mesalazine refers to antibacterial and anti-inflammatory drugs with localization of action in the intestine.

The active substance inhibits the activity of neutrophilic lipoxygenase and the production of arachidonic acid metabolites.

When using the drug, it is possible to slow down the formation of cytokines in the intestinal mucosa, stop the migration, degranulation, phagocytosis of neutrophils, and the production of immunoglobulins by lymphocytes.

In addition, rectal suppositories have an antioxidant property, due to which they are able to bind and destroy free radicals oxygen. They also inhibit the activity of some intestinal bacteria, including Escherichia coli.

Pharmacokinetics

When using candles active substance released and distributed in the rectum and distal third of the colon. The absorption of the drug into the systemic circulation is low and amounts to 10%. The substance is metabolized in the intestinal mucosa and in the liver as an inactive metabolite. Mesalazine and its metabolites are excreted by the kidneys with urine and through the intestines with feces.

Indications for use

The agent under consideration is used in the treatment of inflammatory pathologies of the rectum and distal large intestine:

• Crohn's disease;
• ulcerative colitis;
• proctitis;
• prosigmoiditis.

The drug is effective in the acute stage and for prevention.

With hemorrhoids

Candles Salofalk are used as part of complex treatment hemorrhoids, when the pathological process proceeds in a severe form, with frequent relapses, severe pain and bleeding. The medication has a healing effect, thanks to which it quickly eliminates anal fissures.

The use of suppositories with mesalazine for hemorrhoids

The drug is designed for rectal use. The dosage is prescribed taking into account the age of the patient:

• Adults. For mild and moderate forms of diseases in the acute stage, 1 suppository (500 mg) per day is used. Limiting daily rate- 1.5 g. For prophylactic purposes, 1 suppository (250 mg) is prescribed 3 times a day. Severe forms of the disease are treated using 2 suppositories (500 mg) 3 times a day. The maximum daily allowance should not exceed 3-4 g. The course of therapy lasts 8-12 weeks.
• Children. In the acute stage, 40-60 mg / kg of body weight per day is prescribed. In order to prevent relapses - 20-30 mg / kg per day. Apply candles 3 times a day. The duration of the therapeutic course is determined on an individual basis.

Contraindications to the use of suppositories with mesalazine

It is prohibited to use the drug in the following cases:

• allergy to the components of the drug;
• kidney or liver failure;
• blood diseases;
• stomach and duodenal ulcer;
• children's age up to 2 years;
• lactation.

Side effects

When using rectal suppositories, the development of negative symptoms is possible:

• Regarding the digestive system: discomfort and soreness in the abdomen, nausea, vomiting, bloating, diarrhea, anorexia, hepatitis and pancreatitis.
• Regarding CCC: palpitations, tachycardia, arterial hypertension, chest pain, shortness of breath, pericarditis, myocarditis.
• Regarding the urinary system: oliguria, anuria, proteinuria, hematuria, nephrotic syndrome.
• Regarding the hematopoietic organs: anemia, increased concentration of leukocytes and platelets, crystallurgy.
• Regarding the nervous system: asthenia, headache, dizziness, ringing in the ears, tremor, depression.
• Allergy: skin rash, itching, urticaria, dermatosis, bronchospasm.

Overdose

In case of an overdose, the following symptoms may develop:

• nausea;
• vomit;
• abdominal pain;
• weakness;
• drowsiness.

The doctor prescribes gastric lavage, laxative and symptomatic treatment.

special instructions

Before use rectal suppositories bowels need to be cleansed.

During pregnancy and lactation

It is possible to use the drug during the period of bearing a child only if the possible benefit to the mother's body outweighs the potential harm to the fetus. The medication is contraindicated in the 3rd trimester and during lactation.

Application in childhood

The drug is approved for use in patients from 2 years of age.

drug interaction

Simultaneous administration of Mesalazole with other drugs has the following features:

• The therapeutic effect of anticoagulants increases, resulting in a possible risk of bleeding in the gastrointestinal tract.
• The ulcerogenic effect of glucocorticoids on the gastric mucosa is enhanced.
• Increases ulcerogenic action.
• Enhances the toxic effect of methotrexate.
• Weakens the effect of Rifampicin.
• Weakens the action of Furosemide.
• Increases the hypoglycemic effect of sulfonylurea.
• Inhibits the absorption of cyanocobolamin.

Terms and conditions of storage

To store rectal suppositories, you must choose a dry and protected from sunlight place where there is no access for children. The storage temperature should be +15...+25°C. The drug can be used within 2 years from the date of manufacture.

Terms of dispensing from pharmacies

On prescription.

Price

The cost of the medication is 350-700 rubles.

Analogues

The tool in question has the following substitutes:

• Mekasol;
• Pentasa;
• Kansalizin;
• Mezavant.