Budenofalk granules 9mg, No. 20

• Induction of remission in patients with exacerbation of mild to moderate Crohn's disease with lesions of the ileum and / or ascending colon;

• Induction of remission in patients with active collagenous colitis.

Inside.

Recommended daily dose: 1 pack. (corresponds to 9 mg of budesonide) 1 time per day in the morning half an hour before meals.

The granules should be placed on the tongue and swallowed without chewing with plenty of liquid.

The duration of the course of treatment should be no more than 8 weeks. At the end of the course of treatment, the drug should be taken at extended intervals between doses, for example, every other day for 2 weeks, after which the treatment can be discontinued.

active substance: budesonide - 9 mg

Excipients:

core of granules : sugar grits (sucrose, corn starch) - 900 mg; lactose monohydrate - 36 mg; povidone K25 - 2.7 mg

granule shell: methacrylic acid and methyl methacrylate copolymer 1: 1 (Eudragit L 100) - 54.9 mg; methacrylic acid and methyl methacrylate copolymer 1: 2 (Eudragit S 100) - 54.9 mg; methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer 2: 0.1: 1 (ammonio-methacrylate copolymer, type B, Eudragit RS) - 9 mg; methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer 2: 0.2: 1 (ammonio-methacrylate copolymer, type B, Eudragit RL) - 6.3 mg; triethyl citrate - 12.6 mg; talc - 134.1 mg

aromatic mixture: xanthan gum - 25 mg; sorbitol - 899.5 mg; anhydrous citric acid - 35 mg; sucralose - 3 mg; lemon flavoring - 10 mg; talc - 20 mg; magnesium stearate - 3 mg

• Hypersensitivity to budesonide or other components of the drug;

• intestinal infectious diseases (bacterial, fungal, amoebic, viral infection);

• cirrhosis of the liver;

• intolerance to lactose, fructose, galactose, lactase deficiency, sucrase / isomaltase deficiency, glucose-galactose malabsorption.

• children's age (up to 18 years old).

With care: tuberculosis; arterial hypertension; diabetes; osteoporosis; peptic ulcer; glaucoma; cataract; a family history of diabetes or glaucoma.

Trade name: BudenofalkЃ

Description:

Enteric granules

A mixture of powder and granules of a round shape or granules of a round shape from white to almost white, with a lemon scent.

Composition:

1 pack.

active substance: budesonide - 9 mg

Excipients:

core of granules : sugar grits (sucrose, corn starch) - 900 mg; lactose monohydrate - 36 mg; povidone K25 - 2.7 mg

granule shell: methacrylic acid and methyl methacrylate copolymer 1: 1 (Eudragit L 100) - 54.9 mg; methacrylic acid and methyl methacrylate copolymer 1: 2 (Eudragit S 100) - 54.9 mg; methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer 2: 0.1: 1 (ammonio-methacrylate copolymer, type B, Eudragit RS) - 9 mg; methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer 2: 0.2: 1 (ammonio-methacrylate copolymer, type B, Eudragit RL) - 6.3 mg; triethyl citrate - 12.6 mg; talc - 134.1 mg

aromatic mixture: xanthan gum - 25 mg; sorbitol - 899.5 mg; anhydrous citric acid - 35 mg; sucralose - 3 mg; lemon flavoring - 10 mg; talc - 20 mg; magnesium stearate - 3 mg

pharmachologic effect

Pharmacological action - glucocorticoid .

Pharmacodynamics

Budesonide is a non-halogen-containing GCS with anti-inflammatory, anti-allergic, anti-exudative and decongestant properties.

These properties are based on a decrease in the release of mediators from mast cells, basophils and macrophages; redistribution and suppression of the migration of inflammatory cells, inhibition of inflammatory reactions; membrane stabilizing action.

The induction of certain proteins (eg, macrocortin) is possibly one of the specific mechanisms of action of budesonide. By inhibiting phospholipase A2, these proteins are involved in the metabolism of arachidonic acid and thus prevent the formation of inflammatory mediators LT and PG. Since the process of induction of protein synthesis takes a certain period of time, the full therapeutic effect of budesonide develops gradually.

Pharmacokinetics

Suction. The release of budesonide from the granules begins after 2-3 hours. After a single fasting intake of 9 mg of budesonide Cmax in blood plasma is 2.2 ng / ml and is achieved after about 6 hours. Systemic bioavailability when taken on an empty stomach is 9-13%.

Distribution. Budesonide has a high Vd (approximately 3 L / kg). Plasma protein binding is 85Ц90%.

Metabolism. Approximately 90% of budesonide is metabolized by the liver to form metabolites with low GCS activity. The resulting metabolites (6-hydroxybudesonide and 16-hydroxyprednisolone) have low biological activity (no more than 1% of the activity of budesonide).

Excretion. Average T1 / 2 is approximately 3-4 hours. Simultaneous food intake slows down excretion by 2-3 hours, but does not change the rate of absorption. The average value of budesonide clearance is 10-15 l / min. Budesonide is excreted by the kidneys in small amounts.

Patients with impaired liver function. Depending on the type and severity of liver disease, the metabolism of budesonide in the cytochrome CYP3A system in these patients may be reduced.

Indications

• Induction of remission in patients with exacerbation of mild to moderate Crohn's disease with lesions of the ileum and / or ascending colon;

• Induction of remission in patients with active collagenous colitis.

Contraindications

• Hypersensitivity to budesonide or other components of the drug;

• intestinal infectious diseases (bacterial, fungal, amoebic, viral infection);

• cirrhosis of the liver;

• intolerance to lactose, fructose, galactose, lactase deficiency, sucrase / isomaltase deficiency, glucose-galactose malabsorption.

• children's age (up to 18 years old).

With care: tuberculosis; arterial hypertension; diabetes; osteoporosis; peptic ulcer; glaucoma; cataract; a family history of diabetes or glaucoma.

Application during pregnancy and lactation

During pregnancy, the use of the drug Budenofalk is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

In women of childbearing age, before starting therapy with Budenofalk, a possible pregnancy should be excluded, and reliable methods of contraception should be used during treatment.

Until now, it is not known whether budesonide is able to penetrate into breast milk, therefore, during the period of treatment, it is necessary to stop breastfeeding.

Side effects

The adverse events listed below, noted during the use of the drug, are distributed according to the frequency of occurrence in accordance with the following gradation: very often (? 1/10); often (from? 1/100 to <1/10); infrequently (from? 1/1000 to <1/100); rarely (from? 1/10000 to <1/1000); very rare (<1/10000).

From the side of metabolism and nutrition: often - Cushing's syndrome, for example, moon face, abdominal obesity, decreased glucose tolerance, diabetes mellitus, hypertension, sodium retention with the development of edema, increased potassium excretion, decreased function or atrophy of the adrenal cortex, red striae, steroid acne, a disorder of the secretion of sex hormones (eg amenorrhea, hirsutism, impotence); very rarely - growth retardation in children.

From the side of the organ of vision: very rarely - glaucoma, cataract.

From the gastrointestinal tract: very rarely - stomach complaints, gastroduodenal ulcers, pancreatitis, constipation.

On the part of the immune system: often - an increased risk of infectious diseases.

From the musculoskeletal system and connective tissue: often - muscle and joint pain, muscle weakness and muscle twitching (contraction), osteoporosis; very rarely - aseptic bone necrosis (femur and head of the humerus).

From the nervous system: often - headache; very rarely - benign intracranial hypertension ( pseudotumor cerebri ), incl. edema of the optic nerve head in adolescents.

Mental disorders: often - depression, irritability, euphoria; very rarely - multiple psychic effects and behavior changes.

Skin and subcutaneous tissue disorders: often - allergic exanthema, petechiae, ecchymosis, delayed wound healing, contact dermatitis.

From the side of the vessels: very rarely - an increased risk of thrombosis, vasculitis (withdrawal syndrome after prolonged therapy).

General disorders: very rarely - fatigue (fatigue), general malaise.

When using the drug Budenofalk, side effects may also occur that are characteristic of all systemic corticosteroids. Such side effects depend on the dose, duration of therapy, concomitant or previous treatment with other glucocorticoid drugs, and individual sensitivity.

When transferring patients from taking systemic corticosteroids to budesonide, extraintestinal symptoms may increase or reappear (especially damage to the skin and joints).

In clinical trials, it was shown that the incidence of GCS-related adverse events with the use of the drug Budenofalk 3 mg was less (approximately half) compared with oral therapy with equivalent dosages of prednisolone.

Interaction

Pharmacodynamic interactions

Cardiac glycosides. The action of cardiac glycosides can be enhanced by potassium deficiency.

Diuretics Potassium excretion may increase.

Pharmacokinetic interactions

Inhibitors of cytochrome CYP3A (P450) , for example, ketoconazole, itraconazole, ritonavir, troleandomycin, erythromycin, clarithromycin, cyclosporin, grapefruit juice can enhance the effect of GCS.

Inducers of cytochrome CYP3A (P450) , such as carbamazepine and rifampicin, can reduce the systemic and local effects of budesonide on the intestinal mucosa. In this case, a dose adjustment of budesonide is necessary.

CYP3A substrates (P450) can compete with budesonide. Compounds and drugs that are metabolized with the participation of CYP3A can lead to an increase in the concentration of budesonide in the blood plasma, if a competing substance has a high affinity for CYP3A or budesonide has a high affinity for CYP3A, then an increase in the concentration of a competing substance in the blood plasma is possible.

An increase in the effects of corticosteroids associated with an increase in their concentration in blood plasma was observed in women taking estrogens or high doses of combined oral contraceptives. This fact was not observed when using low-dose COCs.

The simultaneous appointment of cimetidine and budesonide can lead to a clinically insignificant increase in the level of budesonide in blood plasma.

Theoretically, interaction with ion-exchange resins capable of binding steroids (for example, cholestyramine), as well as antacids, cannot be ruled out. With the simultaneous administration of these drugs with the drug Budenofalk, as a result of the interaction, the therapeutic effect of budesonide may decrease. Simultaneous administration of budesonide with these drugs is possible with an interval of at least 2 hours.

Method of administration and dosage

Inside.

Recommended daily dose: 1 pack. (corresponds to 9 mg of budesonide) 1 time per day in the morning half an hour before meals.

The granules should be placed on the tongue and swallowed without chewing with plenty of liquid.

The duration of the course of treatment should be no more than 8 weeks. At the end of the course of treatment, the drug should be taken at extended intervals between doses, for example, every other day for 2 weeks, after which the treatment can be discontinued.

Overdose

No cases of overdose have been identified.

Treatment: symptomatic.

special instructions

The drug Budenofalk can suppress the function of the hypothalamic-pituitary-adrenal system. Before surgery or exposure to another stress factor, the additional appointment of systemic glucocorticosteroids is recommended.

The drug Budenofalk contains lactose, sucrose and sorbitol. The drug should not be taken in patients with rare hereditary conditions of galactose or fructose intolerance, sucrose-isomaltase deficiency or glucose-galactose malabsorption, as well as lactase deficiency.

Suppression of the inflammatory response and immune function when taking the drug increases the propensity for severe infections. The risk of worsening the course of bacterial, fungal, amoebic and viral infections during treatment with Budenofalk should be taken into account.

Patients who have not previously tolerated chickenpox should refrain from contact with patients with chickenpox or shingles. In case of contact or risk of contracting chickenpox, these patients should receive passive immunization with varicella-zoster Ig. Immunization should be carried out within 10 days after contact with the patient. You should not stop taking budesonide, you may need to increase the dose.

Immunocompromised patients who come into contact with a sick measles should be treated with normal Ig as soon as possible.

Patients taking budesonide on a daily basis should not be given live vaccines, due to the possible suppression of antibody responses to such vaccines. With the appointment of high doses and long-term treatment, systemic effects of corticosteroids can occur, including Cushing's syndrome, suppression of adrenal function, decreased bone mineralization, cataracts, glaucoma, and various mental disorders (see 'Side Effects').

The drug has a predominantly local effect, as a result of which a beneficial effect of the drug cannot be expected in patients with extraintestinal symptoms.

Treatment with Budenofalk is not indicated in patients with Crohn's disease with lesions of the upper gastrointestinal tract.

Treatment with Budenofalk results in a greater reduction in steroid hormone levels in the body than conventional oral steroid therapy. When switching from other treatment regimens with steroid drugs, symptoms may appear associated with a change in the level of steroid hormones in the body.

When taking the drug Budenofalk in patients with severely impaired liver function, an increase in the systemic bioavailability of budesonide can be expected. In patients with liver disease without cirrhosis, daily doses of Budenofalk are safe, there is no need for dose adjustment in such patients.

Taking the drug Budenofalk can give a positive result in doping tests.

In patients with autoimmune hepatitis, the level of transaminases (ALT, AST) in serum should be regularly monitored (every 2 weeks during the first month of treatment and at least every 3 months thereafter) in order to possibly adjust the dosage of budesonide.

Influence on the ability to drive vehicles, mechanisms. Due to the possible development of side effects (increased blood pressure, headache), care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Release form

Enteric granules 9 mg. 2215 mg (9 mg budesonide) in a polyester / aluminum / PE bag. 20 or 50 packs. in a cardboard box.

Conditions of dispensing from pharmacies

On prescription.

Storage conditions

At a temperature not exceeding 25 ? C.

Keep out of the reach of children.

Shelf life is 4 years.

Do not use after the expiration date printed on the package.