Salofalk granules coated 1000mg №50

Dosage form

Granules

Composition

The 1 dose (sachet) of enteric-coated coated granules contains: Mesalazine (5-aminosalicylic acid) 1000 mg

The composition of the core: Microcrystalline cellulose 400.0 mg, hypromellose 36.0 mg, anhydrous colloidal silicon dioxide 0.5 mg, Eudragit NE 40 D (40% dispersion of methyl methacrylate and ethyl acrylate copolymer (2: 1) and 2% of nonoxynol) in terms of dry substance 90.0 mg, Magnesium stearate 15.5 mg, dry substance 33% simethicone emulsion (consists of 92% simethicone 7.7%, methylcellulose, 0.3% sorbic acid) 1.0 mg

The composition of the inner shell: Hypromellose 4.0 mg, methacrylic acid and methyl methacrylate, copolymer (1: 1) (Eudrajit L 100) 150.0 mg, triethyl citrate 15.0 mg, talc 40.0 mg, magnesium stearate 10.0 mg, titanium dioxide 25.0 mg

The composition of the outer shell: Carmellose sodium 30.0 mg, titanium dioxide 10.0 mg, aspartame 2.0 mg, anhydrous citric acid 6.0 mg, vanilla flavoring 4.0 mg, talc 11.0 mg, povidone K-25 10, 0 mg

Packing

In 1 sachet 1000 mg enteric-coated granules. In packing 50 bags.

Mechanism of action

Salofalk has a local anti-inflammatory effect due to inhibition of neutrophilic lipoxygenase and the synthesis of prostaglandins and leukotrienes.

Slows 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 trap radicals formed from reactive oxygen compounds. The results obtained in in vitro studies indicate a possible role for inhibition of lipoxygenase.

Also shown is the effect on 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 mesalazine is available in the area.

The ratio of systemic bioavailability and plasma concentration of mesalazine is not significant in terms of therapeutic efficacy, but rather is a factor affecting safety.

Ensuring the release of the active substance in the right place helps the fact that the Salofalk granules are resistant to gastric juice and are pH-dependent (due to the coating in the form of Eudragit L) and slow (thanks to the matrix structure of the granules) release of mesalazine.

Indications and usage

Exacerbation of moderate to mild ulcerative colitis.
- Maintenance of remission and / or long-term therapy of ulcerative colitis.

Contraindications

Hypersensitivity to the components of the drug and other derivatives of salicylic acid.
- Blood diseases.
- Peptic ulcer of the stomach and duodenum.
- Deficiency of glucose-6-phosphate dehydrogenase.
- Hemorrhagic diathesis.
- Severe renal / hepatic failure.
- Children's age (up to 6 years).
- Phenylketonuria.

Pregnancy (I trimester).
- Mild to moderate renal / hepatic impairment.
- Lung diseases (especially bronchial asthma).

Pregnancy and Breastfeeding

Salofalk granules should be used during pregnancy only in cases where the potential benefits of its use for the mother outweigh the possible risk to the fetus.

Salofalk granules can be used in women during breastfeeding only in those cases if the potential effect of its use for the mother exceeds the possible risk of adverse effects for the child. If a newborn breast-fed has diarrhea, breastfeeding should be stopped.

Dosage and administration

For treatment of acute ulcerative colitis: Depends on the clinical need in each individual case, 1 sachet of 1000 mg mesalazine 3 times a day or 3 sachets 1 time a day (corresponding to 1.5-3.0 g of mesalazine per day).

To maintain remission of ulcerative colitis: 500 mg of mesalazine, 3 times a day or 3 sachets 1 time per day (corresponding to 1.5 g of mesalazine per day).

Children under 6 years old: Salofalk in granules should not be administered to children younger than 6 years old, since the experience of using the drug in patients of this age group is very limited.
Children over 6 years old and adolescents: during exacerbation of the disease, depending on its severity, mesalazine is prescribed in a dose of 30-50 mg / kg of body weight per day with a daily dose distribution of 3 doses or 1 dose. To maintain remission, mesalazine is administered at a dose of 15-30 mg / kg body weight per day: in this case, the daily dose can be divided into 2 doses. Children with a body weight of up to 40 kg are usually recommended to give a half dose of adults, children weighing more than 40 kg should be given a dose of adults.

Salofalk granules should not be chewed. The prescribed dose of Salofalk in granules should be taken in the morning, at lunchtime and in the 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 exacerbations of the inflammatory process, and with prolonged use to maintain remission, the granules should be taken regularly and consistently, which allows to achieve the desired 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 per day.

Adverse reactions

All medications can cause allergic reactions, although serious allergic reactions are very rare.

If you have any of the following symptoms after taking this drug (allergic skin rash, fever, difficulty breathing), you should immediately contact your doctor.

If you feel a serious deterioration in your general health due to fever, and / or inflammation of the pharynx and mouth, please inform your doctor immediately.

Symptoms may have manifested from a decrease in the level of white blood cells in your blood (agranulocytosis). This may increase the risk of serious infection. You must have a blood test to determine changes in your hemogram. Be sure to tell your doctor about your medication.

If you have the following serious side effects, stop taking the drug, and immediately contact your doctor.

The frequency of adverse reactions below is determined by the following gradation:

Rare - which occur in less than 1 in 1,000 patients, but in more than 1 in 10,000 patients).
- Very rare - which occur in less than 1 in 10,000 patients.

Rare - abdominal pain, diarrhea, bloating, nausea and vomiting, headache, dizziness.

Very rare - changes in renal function, sometimes with swelling of the limbs or pain in the abdomen. Chest pain, shortness of breath, or swelling of the limbs due to heart problems. Severe abdominal pain due to acute inflammation of the pancreas. Severe dyspnea due to allergic pneumonia.Severe diarrhea and abdominal pain due to allergic inflammation of the intestines. Skin rash or inflammation. Pain in the muscles and joints. Fever, sore throat, or malaise due to changes in the blood test. Jaundice or abdominal pain due to liver and bile excretion disorders. Hair loss and development of baldness. Numbness and tingling in the hands and feet (peripheral neuropathy). Reversible decrease in sperm motility.

Before starting treatment and during the process of its conduct, it is necessary for the attending physician to determine the parameters of the functional state of the liver (such as the activity of ALT or ACT) and monitor urine tests (by immersing the 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 the test results are normal, control tests should be carried out every 3 months. If additional symptoms are noted, control studies should be performed immediately.

Caution should be exercised in patients with impaired liver function. Appointment Salofalk granules is not recommended for patients with impaired renal function.

If renal impairment has developed during treatment, one should think about the nephrotoxic effect of mesalazine. When administering Salofalk in granules to patients with lung diseases, in particular, bronchial asthma, it is necessary to exercise careful monitoring during treatment.

Patients who had anamnestic indications of adverse reactions when prescribing drugs containing Sulfasalazine, should be carefully monitored in the initial period of treatment with Salofalk in granules. If during the treatment with Salofalk, acute intolerance reactions occur, such as cramps, acute abdominal pain, fever, severe headache and rash, the use of the drug should be stopped immediately.

When administering the drug to patients suffering from phenylketonuria, it should be remembered that Salofalk granules contains aspartame (as a substance that gives a sweet taste) in doses equivalent to the following amount of phenylalanine - 1.12 mg (Salofalk granules 1000 mg).

Salofalk granules should not be used in the treatment of children younger than 6 years. Care should be taken when driving a vehicle and engage in potentially hazardous activities that require increased concentration and psychomotor speed.

During treatment with Salofalk, granules may have interactions with the simultaneous use of the following drugs.

Most of these possible interactions are based on theoretical premises:

Possible increased anticoagulant effect (increased risk of gastrointestinal bleeding): Indirect anti-coagulants.

Possible increased adverse reactions in the stomach: Glucocorticoids.

Possible increase in toxic action of Methotrexate : Methotrexate.

Possible reduction of uric acid excretion: Probenecid / sulfinpyrazon.

Possible weakening of the diuretic effect: spironolactone / Furosemide .

Possible attenuation of tuberculostatic effect: Rimfampicin.

A possible decrease in the release of mesalazine from the granules due to a decrease in pH due to the metabolism of the bacteria Lactulose or other similar drugs that reduce the pH of the intestinal contents.

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

Symptoms: nausea, vomiting, gastralgia, weakness, drowsiness.
Treatment: gastric lavage, the appointment of a laxative, symptomatic therapy. In cases of overdose, if necessary, an infusion of electrolyte solutions (forced diuresis).

Store in a dry place protected from light at a temperature not exceeding 25 ° C.

4 years.