Budenofalk - instructions for use, dose, side effects, contraindications

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

Auxiliary substances (aromatic mixture): gum xanthan 25 mg, sorbitol 899.5 mg, citric acid anhydrous 35 mg, sucralose 3 mg, flavoring lemon 10 mg, talc 20 mg, magnesium stearate 3 mg.

Description:

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

Pharmacotherapeutic group:Glucocorticosteroid for topical application

ATX: & nbsp

R.03.B.A.02 Budesonide

Pharmacodynamics:The action of the drug Budenofalk is based mainly on local action in the intestine. Budesonide is a non-halogenated glucocorticosteroid with anti-inflammatory effect, based on the inhibition of the release of mediators from mast cells,basophils and macrophages, redistribution and inhibition of migration of inflammatory cells. One possible mechanism of action of budesonide is the induction of the synthesis of specific proteins, such as macrocortin. Inhibiting phospholipase A2, macrocortin reduces the formation of arachidonic acid from the phospholipids of cell membranes and indirectly prevents the synthesis of inflammatory mediators - leukotrienes and prostaglandins.

Pharmacokinetics:

Suction

The release of budesonide from the granules begins in 2-3 hours. After a single dose of 9 mg of budesonide on an empty stomach, the maximum concentration in the blood plasma (C_m_Oh) is 2.2 ng / ml and is reached after about 6 hours. Systemic bioavailability when taken on an empty stomach is 9-13%.

Distribution

Budesonide has a large volume of distribution (approximately 3 l / kg). Binding to plasma proteins is 85-90%.

Metabolism

Approx. 90 % Budesonide is metabolized by the liver with formation of metabolites with low glucocorticosteroid activity. The resulting metabolites (6β-hydroxybuddesonide and 16α-hydroxyprednisolone) have low biological activity (not more than 1% of budesonide activity).

Excretion

The average half-life is approximately 3-4 hours.Simultaneous food intake slows the excretion for 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.

Special groups of patients (patients with impaired liver function)

Depending on the type and severity of liver disease, budesonide metabolism in the cytochrome system CYP3A in such patients can be reduced.

Indications:

- Induction of remission in patients with exacerbation of mild and moderate forms of Crohn's disease with ileum and / or ascending colon damage;

- Induction of remission in patients with active collagenous colitis.

Contraindications:

Hypersensitivity to budesonide or other components of the drug, cirrhosis, children's age (up to 18 years), lactose intolerance, fructose, galactose, glucose-galactose malabsorption, sucrose isomaltase deficiency, lactase deficiency.

Carefully:

Tuberculosis, arterial hypertension, diabetes, osteoporosis, gastric and duodenal ulcer, glaucoma, cataracts, a burdened family history of diabetes or glaucoma, and some other conditions in which the use of glucocorticosteroids can lead to undesirable effects.

Pregnancy and lactation:

During pregnancy, the use of Budenofalk is only possible if the expected benefit to the mother exceeds the potential risk to the fetus. Budesonide in small amounts excreted in breast milk, so the period of treatment should stop breastfeeding or decide to stop treatment with budesonide considering the benefits of breast-feeding the child and the benefit of therapy for the woman.

Dosing and Administration:

For oral administration.

Recommended daily dose: 1 package (corresponding to 9 mg of budesonide) 1 time per day in the morning for half an hour before a meal.

Granules should be placed on the tongue and swallowed, without chewing, with plenty of liquid.

The duration of treatment should not be more than 8 weeks. At the end of the course of treatment, the drug should be taken with extended intervals between doses, for example every other day for 2 weeks, after which the treatment may be discontinued.

Side effects:

The following undesirable phenomena noted with 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 rarely (<1/10000).

Organs and Systems	Frequency, according to classification MedDRA	Adverse events
Disorders from the metabolism and nutrition	Often	Cushing's syndrome, for example, lunar face, abdominal obesity, decreased glucose tolerance, diabetes mellitus, hypertension, sodium retention with edema development, increased potassium excretion, decreased adrenocortical function or atrophy, red striae, steroid acne, sex hormone secretion disorder , amenorrhea, hirsutism, impotence)
Disorders from the metabolism and nutrition	Rarely	Growth retardation in children
Disturbances on the part of the organ of sight	Rarely	Glaucoma, cataract
Disorders from the gastrointestinal tract	Rarely	Complaints from the stomach, gastroduodenal ulcers, pancreatitis, constipation
Immune system disorders	Often	Increased risk of infectious diseases
Disturbances from musculoskeletal system and connective tissue	Often	Muscle and joint pain, muscle weakness and muscle twitching (contractions), osteoporosis
	Rarely	Aseptic necrosis of bones (thigh and head of humerus)
Disturbances from the nervous system	Often	Headache
Disturbances from the nervous system	Rarely	Benign intracranial hypertension (pseudotumor cerebri), including edema of the optic nerve disc in adolescents
Disorders of the psyche	Often	Depression, irritability, euphoria
Disorders of the psyche	Rarely	Multiple psychiatric effects and behavioral changes
Disturbances from the skin and subcutaneous tissues	Often	Allergic exanthema, petechiae, ecchymosis, delayed wound healing, contact dermatitis
Vascular disorders	Rarely	Increased risk of thrombosis, vasculitis (withdrawal syndrome after prolonged therapy)
Are common disorders	Rarely	Fatigue (fatigue), general malaise

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

When transferring patients from receiving systemic glucocorticosteroids to budesonide, extraintestinal symptoms may increase or re-emerge (especially skin and joint damage).

Overdose:There have been no cases of overdose to date.

Interaction:

Pharmacodynamic interactions

Cardiac glycosides:

The action of cardiac glycosides can be intensified because of potassium deficiency.

Diuretics:

The excretion of potassium can increase.

Pharmacokinetic interactions

Inhibitors of cytochrome CYP3A (P450), eg, ketoconazole, itraconazole, ritonavir, troleandomycin, erythromycin, clarithromycin, ciclosporin, grapefruit juice can enhance the effect of glucocorticosteroids.

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

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

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

Simultaneous administration 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) and antacids can not be ruled out. With the simultaneous administration of these drugs with 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 two hours.

Special instructions:

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

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

Suppression of the inflammatory response and immune function when taking the drug increases the tendency to severe infection. It should take into account the risk of deterioration of the course of bacterial, fungal, amoebic and viral infections during treatment with the drug Budenofalk.

Patients who did not tolerate varicella before, should refrain from contact with patients with chicken pox or shingles. In case of contact or risk of chickenpox infection, such patients need passive immunization with immunoglobulin against chicken pox. Immunization should be performed within 10 days after contact with the patient. You should not stop taking budesonide, you may need to increase the dose.

Patients with weakened immunity in contact with measles patients should be treated as soon as possible with normal immunoglobulins.

Patients who receive budesonide, live vaccines should not be given because of the possible suppression of the antibody response to such vaccines.

With the administration of high doses and long-term treatment, systemic effects of corticosteroids, including Cushing's syndrome, suppression of adrenal function, decreased bone mineralization, cataracts, glaucoma, and various mental disorders can occur (see "Side effect").

The drug has a predominantly local effect, so you can not expect a beneficial effect of the drug in patients with extraintestinal symptoms.

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

Treatment with the drug Budenofalk leads to a greater decrease in levels of steroid hormones in the body than conventional therapy with steroid preparations for oral administration. When switching from other treatment regimens to steroid drugs, there may be symptoms associated with a change in the level of steroid hormones in the body.

When taking Budenofalk in patients with severe impairment of liver function, one can expect an increase in the systemic bioavailability of budesonide. In patients with liver disease without cirrhosis, daily doses of Budenfalk are safe, there is no need for dose correction in such patients.

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

Effect on the ability to drive transp. cf. and fur:

In connection with the possible development of side effects (increased blood pressure, headache), care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Granules intestine-soluble 9 mg.

Packaging:

At 2215 mg (9 mg budesonide) in a package of polyester / aluminum / polyethylene, 20 or 50 packs together with instructions for use in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 30 ° C. Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-004274

Date of registration:28.04.2017

Expiration Date:28.04.2022

The owner of the registration certificate:DOCTOR FALK PHARMA GmbH DOCTOR FALK PHARMA GmbH Germany

Manufacturer: & nbsp

LOSAN PHARMA, GmbH Germany

Representation: & nbspDOCTOR FALK PHARMA GmbH DOCTOR FALK PHARMA GmbH Germany

Information update date: & nbsp05.06.2017

Illustrated instructions

Instructions

Budenofalk (Budenofalk)