Salofalk, enteric soluble prolonged-acting granules 1000mg 50pcs

Composition

In 1 dose (sachet) of granules coated with an enteric coating contains:

Mesalazine (5 – aminosalicylic acid) 1000 mg

Core composition:

Cellulose microcrystalline 400,0 mg,

hypromellose 36,0 mg,

silicon dioxide colloidal anhydrous 0.5 mg,

Eudragit NE 40 D (40% dispersion of methyl methacrylate and ethylacrylate copolymer (2: 1) and 2% Nonoxynol-9) in terms of dry substance of 90.0 mg, magnesium stearate 15,5 mg

dry matter 33% simethicone emulsion (consisting of 92% of simethicone to 7.7%, methylcellulose,0.3% of sorbic acid) 1.0 mg

Composition of the inner shell:

Hypromellose 4.0 mg,

methacrylic acid and methyl methacrylate, copolymer (1: 1) (Eudragite L 100) 150.0 mg,

Triethyl citrate 15.0 mg,

talc 40.0 mg,

magnesium stearate 10.0 mg,

titanium dioxide 25.0 mg

Composition of the outer shell:

Carmellose sodium 30.0 mg,

Titanium dioxide 10.0 mg,

Aspartame 2.0 mg,

Citric acid anhydrous 6.0 mg,

Vanilla flavor 4.0 mg,

talc 11.0 mg,

Povidone K-25 10.0 mg

Pharmacological action

Salofalk has a local anti-inflammatory effect due to the 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 its ability to bind to free oxygen radicals and destroy them). Mesalazine can also trap radicals formed from reactive oxygen species.

The results obtained in vitro studies indicate a possible role of lipoxygenase inhibition.

The effect on the content of prostaglandins in the intestinal mucosa is also shown.

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 to mesalazine plasma concentrations is not significant in terms of therapeutic efficacy, but rather serves as a factor affecting safety.

Ensuring the release of the Active ingredient in the right place helps that Salofalk granules are resistant to gastric juice and are characterized by pH-dependent (due to the coating in the form of Eudrajit L) and delayed (due to the matrix structure of the granules) release of mesalazine.

Indications

Exacerbation of ulcerative colitis of moderate and mild severity.

– Maintenance of remission and / or long-term treatment of ulcerative colitis.

Use during pregnancy and lactation

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

Salofalk granules can be used in women during breast-feeding only if the potential effect of its use for the mother exceeds the possible risk of adverse effects for the child.

If a breastfed newborn develops diarrhea, breastfeeding should be discontinued.

Contraindications

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

With caution:

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

Side effects

Hypersensitivity reactions: skin rash, pruritus, erythema, fever, bronchospasm, pericarditis, myocarditis, acute pancreatitis, interstitial nephritis, nephrotic syndrome.

There were isolated cases of allergic alveolitis and pancolitis.

Under certain conditions, mesalazine and drugs with a similar chemical structure can lead to the development of a syndrome similar to that of systemic lupus erythematosus.

From the digestive system: loss of appetite; rarely (<1/1000, but > 1/10 000) – diarrhea, nausea, abdominal pain, flatulence, vomiting; very rarely (<1/1000, but >

Nervous system disorders: rare (1/10 000) – headache, dizziness; very rare (

From the cardiovascular system: possibly-tachycardia, arterial hypertension or hypotension; very rarely ( Musculoskeletal disorders: very rare (

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

From the side of the blood coagulation system: in some cases – hypoprothrombinemia.

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

Other: in some cases-a decrease in the production of tear fluid; very rarely (

Taking into account the chemical structure of the Active ingredient, it is impossible to exclude the possibility of increasing the level of methemoglobin. If acute signs of intolerance occur, treatment should be stopped immediately.

Interaction

During treatment with Salofalk granules, interactions may occur with the simultaneous use of the following medications.

Most of these possible interactions are based on theoretical assumptions:

Possible increase in the anticoagulant effect (increased risk of gastrointestinal bleeding): Indirect anticoagulants.

Possible increase in adverse reactions from the stomach: Glucocorticoids.

Possible increase in the toxic effect of methotrexate: Methotrexate.

Possible reduction of uric acid excretion: Probenecid/ sulfinpyrazone.

Possible weakening of the diuretic effect: Spironolactone / furosemide.

Possible weakening of the tuberculostatic effect: Rimfampicin.

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

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

How to take, course of use and dosage

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

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

Salofalk pellets should not be chewed. The prescribed dose of Salofalk granules should be taken in the morning, at lunchtime and in the evening, or the entire dose once in the morning. Salofalk pellets should be placed on the tongue and swallowed without chewing, washed down with plenty of liquid.

Both in the treatment of exacerbations of the inflammatory process, and with prolonged use in order to maintain remission, granules should be taken regularly and consistently, which allows achieving 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 per day.

Overdose

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

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

Special instructions

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

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

If renal dysfunction develops during treatment, you should think about the nephrotoxic effect of mesalazine. When prescribing Salofalk in granules to patients with lung diseases, in particular, bronchial asthma, it is necessary to carry out careful monitoring during treatment.

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

When prescribing the drug to patients suffering from phenylketonuria, it should be remembered that Salofalk granules contain 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 under 6 years of age. You should be careful when driving a vehicle and engage in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reaction.

Form of production

Pellets

Storage conditions

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

Shelf life

4 years

Active ingredient

Mesalazine

Conditions of release from pharmacies

By prescription

Dosage form

granules