Mesalazole suppositories. Medicinal guide geotar Mesalazine dosage

Anti-inflammatory drugs - derivatives salicylic acid.

Compound

The active substance is mesalazine.

Manufacturers

Canonpharma production (Russia)

pharmachologic effect

Pharmacological action - 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 ulcerative colitis in patients with hypersensitivity to sulfasalazine, it 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 effect

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

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.

In distal forms (proctitis, proctosigmoiditis), rectal administration of the drug in the form of suppositories or enemas is preferable.

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 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 antioxidant properties, thanks to which they are able to bind and destroy oxygen free radicals. They also inhibit the activity of some intestinal bacteria, including Escherichia coli.

Pharmacokinetics

When using suppositories, the active substance is released and distributed in the rectum and the 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, due 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, pain behind the sternum, 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.
• Relatively nervous system: asthenia, headache, dizziness, tinnitus, 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 using rectal suppositories, it is necessary to cleanse the intestines.

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 exceeds potential harm for 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.

Gross formula

Pharmacological group of the substance Mesalazine

Nosological classification (ICD-10)

CAS code

Pharmacology

It inhibits the synthesis of PG, inhibits chemotaxis, degranulation and phagocytosis of neutrophils, the secretion of immunoglobulins by lymphocytes, and has antioxidant properties. Has antibacterial action against coli and some cocci (manifested in the large intestine).

Depending on the dosage form and route of administration, the release of mesalazine occurs in a direct and colon(enemas, suppositories) or terminal small intestine and large intestine (tablets). Tablets (enteric) begin to dissolve in the small intestine (at pH> 6) after 110-170 minutes, completely dissolve after 165-225 minutes after ingestion. During the passage through the intestines, mesalazine is released from the tablets gradually, with 15-30% in the ileum, 60-75% in the large intestine, and only 10% enters the bloodstream. Plasma concentration is low - after a single dose of 250 mg Cmax is 0.5-1.5 μg / ml. In the intestinal mucosa and liver forms N-acetyl-5-aminosalicylic acid. The binding of mesalazine to plasma proteins is about 40%, the metabolite is 75-83%. In breast milk penetrates (in the form of a metabolite) 0.1% of the dose. With rectal administration, 10-30% of the dose is found in daily urine. T 1/2 mesalazine 0.5-1.5 hours, N-acetyl-5-aminosalicylic acid - 5-10 hours.

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, it is well tolerated (even at a dose of 4.8 g / day comparable to that of placebo). Reduces the risk of recurrence in Crohn's disease, especially in patients with ileitis and a long duration of the disease.

Application of the substance Mesalazine

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

Contraindications

Hypersensitivity, incl. to other derivatives of salicylic acid (when using enemas, including methyl- and propylparaben), severe violations of the liver and / or kidneys, blood diseases, hemorrhagic diathesis, peptic ulcer of the stomach and duodenum, the last 2-4 weeks of pregnancy, breastfeeding, children's age (up to 2 years).

Application restrictions

Impaired liver and / or kidney function, pregnancy (I trimester), deficiency of glucose-6-phosphate dehydrogenase.

Use during pregnancy and lactation

In the first trimester of pregnancy, the appointment of mesalazine is possible only under strict indications; in the last 2-4 weeks of pregnancy, the drug should be discontinued.

For the duration of treatment, it is recommended to stop breast-feeding due to the lack of sufficient clinical experience during this period. If a breastfed newborn develops diarrhea, breastfeeding should be discontinued.

side effects of mesalazine

From the digestive tract: nausea, vomiting, heartburn, loss of appetite, abdominal pain, diarrhea, flatulence, increased levels of hepatic transaminases, hepatitis, pancreatitis, parotitis.

From the side of cardio-vascular system and blood (hematopoiesis, hemostasis): palpitations, tachycardia, increase or decrease in blood pressure, chest pain, shortness of breath, anemia (hemolytic, megaloblastic, aplastic), leukopenia, agranulocytosis, thrombocytopenia, hypoprothrombinemia.

From the nervous system and sensory organs: headache, dizziness, sleep disturbance, depression, malaise, paresthesia, convulsions, tremor, tinnitus.

From the genitourinary system: proteinuria, hematuria, crystalluria, oliguria, anuria, nephrotic syndrome, oligospermia.

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

Others: fever, photosensitivity, lupus-like syndrome, alopecia, decreased production of lacrimal fluid, possibly increased levels of methemoglobin.

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.

Overdose

Symptoms: nausea, vomiting, gastralgia, weakness, drowsiness.

Treatment: gastric lavage (when taken orally), the appointment of a laxative, symptomatic therapy.

Routes of administration

Inside, rectally.

Mesalazine Substance Precautions

Before starting, during (1-2 times a month), as well as after treatment (every 3 months), 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. However, it should be borne in mind that the syndrome of acute intolerance in some cases can be difficult to differentiate from a severe exacerbation of inflammatory bowel disease.

Interactions with other active substances

Trade names

International name

Group affiliation

Dosage form

pharmachologic effect

It has a local anti-inflammatory (due to inhibition of the activity of neutrophilic lipoxygenase and the synthesis of Pg and leukotrienes). It inhibits migration, degranulation, phagocytosis of neutrophils, as well as the secretion of Ig by lymphocytes. It has an antibacterial effect against Escherichia coli and some cocci (manifested in the large intestine).

It has an antioxidant effect (due to the ability to bind to free oxygen radicals and destroy them). It is well tolerated, reduces the risk of relapse in Crohn's disease, especially in patients with ileitis and a long duration of the disease.

Indications

Contraindications

Side effects

From the side digestive system: nausea, vomiting, heartburn, diarrhea, loss of appetite, abdominal pain, increased activity of "liver" transaminases, hepatitis, pancreatitis.

From the CCC: palpitations, tachycardia, increase or decrease in blood pressure, chest pain, shortness of breath.

From the nervous system: headache, tinnitus, dizziness, polyneuropathy, tremor, depression.

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

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

On the part of the hematopoietic organs: anemia (hemolytic, megaloblastic, aplastic), leukopenia, agranulocytosis, thrombocytopenia, hypoprothrombinemia.

Other: weakness, parotitis, photosensitivity, lupus-like syndrome, oligospermia, alopecia, decreased production of lacrimal fluid.

Application and dosage

The choice of dosage form is determined by the localization and extent of the intestinal lesion.

With common forms, tablets are used, with distal (proctitis, proctosigmoiditis) - rectal forms. With an exacerbation of the disease - 400-800 mg 3 times a day, for 8-12 weeks. For the prevention of relapse - 400-500 mg 3 times a day for ulcerative colitis and 1 g 4 times a day - for Crohn's disease; children over 2 years old - 20-30 mg / kg / day in several doses, for several years. In severe cases of the disease, the daily dose can be increased to 3-4 g, but not more than 8-12 weeks. Tablets should be taken whole, without chewing, after meals, drinking plenty of liquid.

Candles - 500 mg 3 times a day, and a suspension - 60 g of a suspension (4 g of mesalazine) 1 time per day at night, in the form of a medicinal microclyster (it is first recommended to cleanse the intestines).

Candles are prescribed for children at the rate of: during exacerbation - 40-60 mg / kg / day; for maintenance therapy - 20-30 mg / kg / day.

special instructions

Interaction

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pharmachologic effect

Anti-inflammatory intestinal agent. It has a local anti-inflammatory effect due to inhibition of neutrophilic lipoxygenase and the synthesis of prostaglandins and leukotrienes. It slows down the migration, degranulation, phagocytosis of neutrophils, as well as the secretion of immunoglobulins by lymphocytes. It has an antioxidant effect (due to the ability to bind to free oxygen radicals and destroy them). Mesalazine can also scavenge radicals generated from reactive oxygen compounds. Results from in vitro studies point to a possible role for lipoxygenase inhibition. Also shown is the effect on the content of prostaglandins in the intestinal mucosa.

When taken orally, mesalazine has a predominantly local effect in the intestinal mucosa and submucosal layer, acting from the intestinal lumen. Therefore, it is important that mesalasia is available to areas of inflammation. The ratio of systemic bioavailability and plasma concentration of mesalazine is not significant in terms of therapeutic efficacy, but rather serves as a factor affecting safety.

release active substance in the right place, it helps that Salofalk granules are resistant to gastric juice and are characterized by pH-dependent (due to the coating in the form of Eudragit L) and delayed (due to the matrix structure of the granules) the release of mesalazine.

Pharmacokinetics

Suction and distribution

The release of mesalazine occurs in the terminal small and large intestine. Tablets begin to dissolve in the small intestine after 110-170 minutes and completely dissolve after 165-225 minutes after ingestion. The dissolution rate is not affected by changes in the pH of the medium caused by food intake or other drugs.

The release of mesalazine from the granules begins with a delay of 2-3 hours, Cmax in plasma is reached after about 4-5 hours. The systemic bioavailability of mesalazine after oral administration is approximately 15-25%. Eating slows down absorption by 1-2 hours, but does not change the rate and degree of absorption.

Food intake can slow down the transit of the drug by 1-2 hours, while increasing the values ​​of T lag (time gap after which the mesalazine content is first determined in the blood) and T max, however, due to the small size of the granules, this does not change the rate and degree of absorption.

Eating causes a slight increase in Cmax and AUC.

The pharmacokinetic data of granules and tablets are summarized in the following table (granules: 3×500 mg mesalazine/day, tablets: 3×2 (250 mg) mesalazine/day, steady state, 24 healthy volunteers):

The total amount of mesalazine and N-acetyl-5-aminosalicylic acid (N-Ac-5-ASA) excreted by the kidneys within 24 hours is equivalent to approximately 25-32% of the prescribed dose of Salofalk granules and tablets, respectively. Approximately 30% of this amount is absorbed in the ileocecal zone, and approximately 90% in general in the ileocecal zone and the ascending colon. Thus, approximately 80-90% of the prescribed dose of 5-ASA is present in the descending colon, sigmoid colon, and rectum, where their rate of absorption is low.

The distribution of radioactively labeled 153 Sm (samarium) granules and tablets in the gastrointestinal tract was as follows (mean ± SD (confidence interval)):

The values ​​of serum C max 5-ASA and Ac-5-ASA in the equilibrium state were approximately 1.4 and 1.2 times higher after taking 1 time / day compared with the values ​​observed when taking the drug 3 times / day at the same daily dose. C ss in serum at the end of the dosing period when taken 1 time / day was only slightly lower than when taken 3 times / day (by 0.3 and 0.4 times for 5-ASA and Ac-5-ASA, respectively). When taking the drug 1 time / day, there were no signs of systemic cumulation.

Due to the size of the granules (about 1 mm), transit from the stomach to the small intestine is fast. A combined pharmacoscintigraphic and pharmacokinetic study showed that the drug reaches the ileocecal region in about 3 hours, and the ascending colon in about 4 hours. Total time transit through the colon is about 20 hours. Approximately 80% of the accepted oral dose reaches the colon, sigmoid and rectum.

Plasma protein binding of mesalazine and N-Ac-5-ASA is 43% and 78% (75-83%), respectively.

In breast milk penetrates (in the form of a metabolite) 0.1% of the dose.

Metabolism

Mesalazine is metabolized both presystemically in the intestinal mucosa and systemically in the liver, turning into pharmacologically inactive N-Ac-5-ASA. The nature of acetylation does not depend on the acetylating phenotype of the patient. To a small extent, acetylation can be carried out due to the action of the bacterial microflora of the colon.

breeding

When taking mesalazine at a dose of 500 mg 3 times / day, the total elimination of mesalazine and N-Ac-5-ASA by the kidneys under conditions of saturating concentration was about 25%. Excretion of the unmetabolized portion of mesalazine was less than 1% of the oral dose. T 1/2 in this study was 4.4 hours.

Pharmacokinetics in special clinical situations

With a single oral administration of Salofalk granules at a dose of 20 mg / kg to 13 children with active inflammatory disease large intestine (age from 5.9 to 15.8 years), the pharmacokinetics of the systemic exposure of the drug corresponded to that in adults. Salofalk was safe and well tolerated.

There are no data on the pharmacokinetics of Salofalk in the elderly when it is used, both in tablets and in granules.

Indications

Tablets

- nonspecific ulcerative colitis (NUC);

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

Granules

- exacerbation of ulcerative colitis of moderate and mild severity;

- maintenance of remission and or long-term therapy of ulcerative colitis.

Dosing regimen

Tablets

The drug is administered orally adults 500 mg 3 times / day. At severe forms diseases the dose may be increased to 3-4 g/day for 8-12 weeks.

For relapse prevention the drug is prescribed 500 mg 3 times / day, if necessary - for several years.

Children weighing up to 40 kg prescribe 1/2 daily dose for adults - 250 mg 3 times / day (tablets of 250 mg should be used), - 500 mg 3 times / day.

For relapse prevention

Tablets should be taken whole, without chewing, after meals and with plenty of water. With distal forms of UC, it is preferable rectal administration drug in the form of rectal suppositories or rectal suspensions.

Granules

Dosing regimen for treatment of exacerbation of ulcerative colitis depends on the clinical need and in each case is individual. Assign 1 sachet of 500-1000 mg of mesalazine 3 times / day or 3 sachets 1 time / day (corresponding to 1.5-3.0 g of mesalazine per day).

For maintaining remission of ulcerative colitis appoint 500 mg (1 pack.) of mesalazine 3 times / day or 3 sachets of 500 mg 1 time / day (corresponding to 1.5 g of mesalazine per day).

Children over 6 years of age and teenagers at exacerbation of the disease, depending on its severity, mesalazine is prescribed at a dose of 30-50 mg / kg of body weight / day with the distribution of the daily dose into 3 doses or 1 dose. For maintaining remission mesalazine is prescribed at a dose of 15-30 mg/ct of body weight/day, while the daily dose can be divided into 2 doses. Children weighing up to 40 kg it is usually recommended to prescribe half the adult dose, children weighing over 40 kg- adult dose.

Salofalk granules should not be chewed. The prescribed dose of Salofalk granules should be taken in the morning, afternoon and evening, or the entire dose once in the morning. Salofalk granules should be put on the tongue and swallowed without chewing, drinking plenty of liquid.

As in the treatment of an exacerbation inflammatory process, and with long-term use in order to maintain remission, the granules must be taken regularly and consistently, which allows you to achieve the required therapeutic effect. Exacerbation of ulcerative colitis usually subsides after 8-12 weeks, after which the dose of mesalazine in most patients can be reduced to 1.5 g / day.

Side effect

Hypersensitivity reactions: skin rash, itching, erythema, fever, bronchospasm, pericarditis, myocarditis, acute pancreatitis, interstitial nephritis, nephrotic syndrome. Isolated cases of allergic alveolitis and pancolitis have been observed. Under certain conditions, mesalazine and drugs having a similar chemical structure can lead to the development of a syndrome similar to systemic lupus erythematosus syndrome.

From the digestive system: loss of appetite; rarely (<1/1000, но >1/10,000) - diarrhea, nausea, abdominal pain, flatulence, vomiting; very rarely (< 1/10 000) - strong pain in the abdomen due to pancreatitis, severe diarrhea and abdominal pain due to allergic inflammation of the intestine, jaundice and abdominal pain due to impaired bile secretion, increased levels of liver enzymes in the blood, hepatitis.

From the nervous system: rarely (1/10,000) - headache, dizziness; very rarely (< 1/10 000) - периферическая невропатия; возможно - депрессия, нарушения сна, недомогание, парестезии, судороги, тремор, шум в ушах.

From the side of the cardiovascular system: possibly - tachycardia, arterial hypertension or hypotension; very rarely (< 1/10 000) - боли за грудиной, одышка.

From the musculoskeletal system: very rarely (< 1/10 000) - миалгии, артралгии.

From the hematopoietic system: in some cases - anemia, leukopenia, agranulocytosis, thrombocytopenia.

From the blood coagulation system: in some cases - hypoprothrombinemia.

From the urinary system: in some cases - proteinuria, hematuria, crystalluria, oliguria, anuria.

Others: in some cases - a decrease in the production of lacrimal fluid; very rarely (< 1/10 000) - алопеция, лихорадка, ангина, реверсивное уменьшение подвижности сперматозоидов.

Given the chemical structure active substance it is impossible to exclude the possibility of increasing the level of methemoglobin.

If acute signs of intolerance occur, treatment should be stopped immediately.

Contraindications for use

- blood diseases;

- peptic ulcer of the stomach and duodenum;

- hemorrhagic diathesis (with a tendency to bleeding);

- heavy kidney failure;

- severe liver failure;

- deficiency of glucose-6-phosphate dehydrogenase;

- phenylketonuria (for granules);

- children's age up to 3 years (for tablets);

- children's age up to 6 years (for granules);

— hypersensitivity to the components of the drug and other derivatives of salicylic acid.

FROM caution Salofalk should be prescribed for mild renal / hepatic insufficiency and moderate, lung diseases (especially bronchial asthma), in the first trimester of pregnancy.

Use during pregnancy and lactation

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

In the II and III trimesters, Salofalk should be used only in cases where the potential benefit of therapy for the mother outweighs the possible risk to the fetus.

Salofalk in the form of granules can be used during breastfeeding only in cases where the potential effect of its use for the mother outweighs the possible risk of adverse effects for the child. If a breastfed newborn develops diarrhea, breastfeeding should be discontinued.

If it is necessary to prescribe Salfalk in the form of tablets during lactation, breastfeeding should be discontinued.

Use in children

The drug is contraindicated in children under the age of 3 years.

Children weighing up to 40 kg prescribe 1/2 daily dose for adults - 250 mg 3 times / day, children weighing over 40 kg- 500 mg 3 times / day.

For relapse prevention the drug is prescribed 250 mg 3 times / day, if necessary - for several years.

Overdose

Symptoms: nausea, vomiting, gastralgia, weakness, drowsiness.

Treatment: gastric lavage, the appointment of laxatives, symptomatic therapy. In cases of overdose, if necessary, an infusion of electrolyte solutions is performed (forced diuresis).

drug interaction

With simultaneous use, Salofalk causes an increase in the action of indirect anticoagulants (increased risk of gastrointestinal bleeding).

With the simultaneous use of GCS with Salofalk, it is possible to increase undesirable reactions from the gastric mucosa.

With the simultaneous use of Salofalk increases the toxicity of methotrexate.

With the simultaneous use of probenecid and sulfinpyrazone with Salofalk, a decrease in the excretion of uric acid is possible.

With the simultaneous use of Salofalk reduces the diuretic effect of spironolactone and furosemide.

With simultaneous use with Salofalk, the tuberculostatic effect of rifampicin may be weakened.

With simultaneous use, Salofalk enhances the hypoglycemic effect of sulfonylurea derivatives.

When used simultaneously with lactulose or other drugs that reduce the pH of intestinal contents, it is possible to reduce the release of mesalazine from granules due to a decrease in pH due to bacterial metabolism.

In patients who are simultaneously receiving treatment with azathioprine or 6-mercaptopurine, one should be aware of the possible increase in the myelosuppressive effect of azathioprine and 6-mercaptopurine.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

The drug should be stored in a dry, dark place, out of the reach of children, at a temperature not exceeding 25°C. Shelf life of tablets - 3 years, granules - 4 years.

Application for violations of liver function

The drug is contraindicated in severe liver dysfunction.

Application for violations of kidney function

The drug is contraindicated in severe renal impairment.

special instructions

Before starting treatment, during and after treatment, it is necessary to conduct a general analysis of blood and urine.

Before starting treatment and during its implementation, it is necessary to determine the parameters of the functional state of the liver (such as ALT or ACT activity) and monitor urine tests (by immersing test strips). Monitoring is usually recommended 14 days after the start of treatment, then another 2-3 times with an interval of 4 weeks. If test results are normal, follow-up tests should be performed every 3 months. If additional symptoms appear, follow-up studies should be performed immediately.

Use with caution in patients with impaired liver function.

The appointment of Salofalk is not recommended for patients with severe renal impairment. If impaired renal function has developed during treatment, one should think about the nephrotoxic effect of mesalazine. During treatment, kidney function should be monitored.

When prescribing Salofalk to patients with lung diseases, in particular, bronchial asthma should be closely monitored during treatment.

Patients with a history of indications of adverse reactions when prescribing drugs containing sulfasalazine, they should be carefully monitored during the initial period of treatment with Salofalk. If, during treatment with Salofalk, acute intolerance reactions occur, such as convulsions, sharp pains in the abdomen, fever, severe headache and rash, the use of the drug should be stopped immediately.

Patients who are "slow acetylators" have an increased risk of side effects.

There may be staining of urine and tears in a yellow-orange color, staining of soft contact lenses.

If several doses are missed, then without stopping treatment, the patient should consult a doctor.

When prescribing the drug to patients suffering from phenylketonuria, it should be remembered that Salofalk granules contain aspartame in doses equivalent to the following amount of phenylalanine: 0.56 mg (Salofalk granules 500 mg), 1.12 mg (Salofalk granules 1 g).

Pediatric use

Salofalk in granules should not be prescribed children under 6 years old, since the experience of using the drug in patients of this age group is very limited.

Influence on the ability to drive vehicles and control mechanisms

Care must be taken when driving vehicle and potentially dangerous species activities that require increased concentration of attention and speed of psychomotor reaction.