Budesonid-nativ

General characteristics. Structure:

Active ingredient: 0,25 mg/ml or 0,5 mg/ml of a budesonid.

Excipients: methylparahydroxybenzoate (нипагин), succinic acid, dinatrium эдетат (Trilonum of B), a macrogoal 400 (poly(ethylene oxide)-400), propylene glycol, water cleared.

Pharmacological properties:

Pharmacodynamics. The glucocorticosteroid synthetic (GKS) for topical administration, has an antiinflammatory, antiallergic and immunodepressive effect. Raises products of the lipomodulin which is inhibitor of a phospholipase And, slows down release of arachidonic acid, synthesis of products of metabolism of arachidonic acid - cyclic endoperoxides and prostaglandins (Pg) oppresses. Prevents regional accumulation of neutrophils, reduces inflammatory exudation and products of cytokines, slows down migration of macrophages, reduces intensity of processes of infiltration, formation of substance of a chemotaxis, slows down release from mast cells of mediators of an inflammation.

Increases quantity of "active" beta adrenoceptors, recovers reaction of bronchial tubes to bronchodilators, allowing to reduce the frequency of their use, reduces hypostasis of a mucous membrane of bronchial tubes, products of slime, formation of a phlegm and reduces hyperreactivity of respiratory tracts. Improves mukotsiliarny transport. It is well transferred at prolonged treatment, has no mineralokortikosteroidny activity, in the recommended doses practically does not make system impact.

The therapeutic effect begins in several hours after inhalation. The maximum therapeutic effect develops only in several days after introduction of therapeutic doses of an inhalation budesonid, on average in 5-7 days.

Inhalation of a budesonid is capable to prevent an attack of bronchial asthma, but does not stop an acute bronchospasm.

Pharmacokinetics. Absorption - low. After inhalation of 20-25% reaches small bronchial tubes, the part of a dose which came to the digestive tract (DT) is absorbed and almost completely (90%) is exposed to biotransformation in a liver to inactive metabolites. System bioavailability of a budesonid makes 38% of the accepted dose, and 1/6 these sizes are formed at the expense of a proglatyvaniye of a part of drug.

Time of approach of the maximum concentration in a blood plasma - 15-45 min. after inhalation introduction. Communication with proteins of plasma - 88%. The volume of distribution of a budesonid makes about 3 l/kg. Has high system clearance - 84 l/h. An elimination half-life ~ 2,8 h, the maximum concentration in a blood plasma - 0,01 mmol/l. It is removed through intestines in the form of metabolites - 10%, kidneys - 70%.

Indications to use:

The Bronchial Asthma (BA) demanding a maintenance therapy of GKS; chronic obstructive pulmonary disease (COPD).

Route of administration and doses:

The dosage of the drug "Budesonid-nativ" has to be individual. The initial dose at adults for treatment of BA and HOBL makes - 1 - 2 mg a day. The dose at the supporting treatment makes 0,5 - 4 mg days. After obtaining effect the dose is reduced to the minimal effective dose necessary for preservation of a stable state. In certain cases at patients at whose treatment achievement of bystry therapeutic effect is necessary doses of drug can be increased.

If the patient accepted GKS orally, transfer into treatment of Budesonidom-nativ needs to be carried out at the stable state of health of the patient, for 10 - 14 days combine inhalations and reception of GKS inside. Within 10 days it is recommended to accept high doses of Budesonida-nativ against the background of reception of peroral glucocorticosteroids in the picked-up dose. Further it is necessary to reduce a dose of peroral glucocorticosteroids gradually (for example, on 2,5 mg of Prednisolonum) to minimum possible level. In many cases it is possible to refuse reception of peroral glucocorticosteroids completely. There are no data on use of a budesonid for patients with a renal failure or an abnormal liver function. As removal of a budesonid happens at the expense of biotransformation in a liver, it is possible to expect increase in duration of effect of drug at patients with the expressed cirrhosis.

Children, are more senior than 16 years: initial dose of 0,25-0,5 mg/days. If necessary the dose can be increased to 1 mg/days. The maintenance dose makes 0,25-2 mg/days.

At appointment patients with cirrhosis need more careful observation. Drug is used by means of the nebulizer. The bottle contains 1 single dose.

Instruction for use. Open a bottle with drug. Fill the nebulizer through an upper opening with necessary amount of drug. You make Nebulirovaniye according to the instruction for used like the nebulizer.

The volume of solution of a budesonid delivered in the patient's lungs by means of the nebulizer is a variable and depends on several factors, including the following:

• Inhalation time
• Level of filling of the camera
• Technical characteristics of the nebulizer
• The volume relations at a breath/exhalation and the respiratory volume of the patient
• Uses of a mouthpiece or mask

Note:
1. After each inhalation rinse a mouth water.
2. If you use a mask, be convinced that at inhalation the mask densely adjoins to the person. After inhalation wash up a face.

Cleaning.

- The camera of the nebulizer should be cleared after each use.
- The camera of the nebulizer and a mouthpiece or a mask are washed with warm water, using soft detergent or according to instructions of the producer.

Features of use:

Use at pregnancy and during breastfeeding. During the periods of pregnancy and a lactation it is necessary to be careful. Purpose of drug is rational if the advantage of its use for mother exceeds potential risk for a fruit or the child. Data on allocation of a budesonid with breast milk are absent.

Budesonid-nativ it is not intended for stopping of acute symptoms of BA and HOBL. It is necessary to observe the application instruction of an inhaler strictly. Avoid hit of drug in eyes. After use of drug it is recommended to rinse a mouth water for decrease in risk of developing of candidosis stomatitis.

Upon transition from therapy by peroral glucocorticosteroids to the drug "Budesonid-nativ" it is necessary to carry out decrease in a dosage of system GKS very slowly and small doses (for example, on 2,5 mg of Prednisolonum). At the patients who were on long therapy by system GKS the pseudorheumatism syndrome is possible. In these cases sometimes it is necessary to increase a dose of peroral GKS temporarily. Such symptoms as fatigue, headaches, nausea, vomiting are in rare instances observed.

After full cancellation long observation of the patient (risk of development of insufficiency of adrenal glands), and also assessment of function of external respiration is recommended. The drug "Budesonid-nativ", can be appointed to patients who cannot apply other dosage forms of inhalation GKS (patients of advanced and senile age).

Drug does not influence ability to occupations potentially dangerous types of activity requiring special attention and bystry reactions (driving and other vehicles, work with moving mechanisms, work of the dispatcher and operator, etc.).

To apply only in nebulizers!

Side effects:

Often (> 1/100): cough, dryness in a mouth, hoarseness of a voice, a dysphonia, irritation of a mucous membrane of an oral cavity and throat, candidosis stomatitis, dryness of a mucous membrane of a throat, a headache, nausea.

Seldom (<1/1000): formation of bruises or thinning of skin, unpleasant flavoring feelings, a paradoxical bronchospasm (for prevention - a combination of inhalations to beta2-adrenomimetika), ezofagealny candidiasis.

Exhaustion of bark of adrenal glands, hyperglycemia, arterial hypertension can lead high doses of drug to development of system side effects.

Interaction with other medicines:

At treatment of bronchial asthma of Budesonid-nativ it is well combined with beta2-adrenomimetika, kromoglitsiyevy acid or nedokromily, methylxanthines and an ipratropiya bromide. Phenobarbital, Phenytoinum, rifampicin reduce efficiency (induction of microsomal enzymes of a liver).

Metandiyenon, estrogen increases concentration of a budesonid in a blood plasma.

Reception of 200 mg of a ketokonazol increases concentration in plasma of orally accepted budesonid in a dose of 3 mg on average by 6 times once a day. At purpose of a ketokonazol in 12 h after reception of a budesonid concentration in plasma of the last increases by 3 times. Information on similar interaction with inhalation dosage forms of a budesonid is absent, however it is necessary to expect noticeable increase in concentration of drug in plasma.

Other potential inhibitors of the ISOENZYME CYP3A4, for example итраконазол, also considerably increases plasma concentration of a budesonid. Drug it is possible to dilute 0,9% with chloride sodium solution.

Contraindications:

Hypersensitivity to drug components, children's age up to 16 years.

With care. Active and inactive forms of tuberculosis, fungal, bacterial and viral infections of a respiratory organs, pregnancy, lactation period.

Overdose:

At acute overdose of clinical manifestations does not arise. At long use of drug in the doses considerably exceeding recommended the system glucocorticosteroid effect in the form of a hypercorticoidism and suppression of function of adrenal glands can develop.

Storage conditions:

In dry protected from light, the place, unavailable to children, at a temperature not above 25 °C. A period of validity - 3 years. Not to use after the date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for inhalations of 0,25 mg/ml, 0,5 mg/ml. On 2 ml in bottles from a drot for medicines or the bottles of orange glass corked by rubber bungs, which are pressed out by caps aluminum. On 10 bottles together with the application instruction in a pack from a cardboard bandbox.