Budenit Steri-Neb

General characteristics. Structure:

Active agent: будесонид 0,25 mg and 0,5 mg
Excipients: polysorbate 80, sodium chloride, citrate sodium a dihydrate, citric acid monohydrate, dinatrium эдетат, water for injections.

Description:
Finely divided suspension of almost white color, almost inodorous.

Pharmacological properties:

The glucocorticosteroid (GKS) with the expressed local antiinflammatory and antiallergic action, будесонид raises products of the lipokartin which is A2 phospholipase inhibitor, slows down release of arachidonic acid, synthesis of leukotrienes and prostaglandins oppresses, reduces inflammatory exudation and products of cytokines, slows down migration of macrophages, reduces expressiveness of processes of infiltration of granulation, formation of substance of a chemotaxis (that explains efficiency at reactions of hypersensitivity of the slowed-down type), slows down release from mast cells of mediators of an inflammation (reaction of immediate hypersensitivity).

Budesonid recovers sensitivity of the patient 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. Raises mukotsiliarny transport. It is well transferred at prolonged treatment, has no mineralokortikoidny activity.

Time of the beginning of therapeutic effect after inhalation of one dose of drug makes several hours. The maximum therapeutic effect is reached in 1-2 weeks after treatment. Budesonid effectively prevents attacks of bronchial asthma of physical tension, but does not stop a bad attack of a bronchospasm.

Pharmacokinetics.
After inhalation будесонид it is quickly adsorbed, at adults system bioavailability after inhalation of a budesonid via the nebulizer makes about 15% of the general appointed dose.

The maximum concentration (Cmax) in plasma makes 3,5nmol/litre and is reached in 30 minutes after the beginning of inhalation.

Linkng with proteins of plasma – 85-90%.

The volume of distribution makes 3 l/kg.

Budesonid is exposed to transformation with participation of microsomal enzymes of a liver, first of all CYP3A4 isoenzyme. The main metabolites – 6-β-гидроксибудесонид and 16-ά-гидроксипреднизолон are almost deprived biological activity (100 times less, than будесонид).

It is removed by kidneys in the form of metabolites – 70%, through intestines – 10%. System clearance it is inhalation the administered drug – 0,5l/min. System clearance of metabolites – 1,4 l/min.

Elimination half-life (T1/2) – about 2-2,8 hours.

Indications to use:

• Treatment of bronchial asthma (as basic therapy; at insufficient efficiency (b2-adrenomimetik; for a dose decline of peroral GKS) in case of inefficiency or impossibility of use of a budesonid in the inhaler forcing drug in respiratory tracts or the inhaler containing drug in the form of powder.
• Treatment of the chronic obstructive pulmonary disease (COPD).
• The stenosing laryngotracheitis (false croup).

Route of administration and doses:

Budenit Steri-Neb apply it is inhalation by means of inhalers - nebulizers (see the section "Technology of Use" of the present instruction).

The recommended drug doses in case of the beginning of inhalation glucocorticosteroid therapy at the heavy course of bronchial asthma, and also against the background of a dose decline or cancellation of reception of peroral glucocorticosteroids, the following:
Adults (including elderly) and children are more senior than 12 years: usually 1-2 mg two times a day.
The maintenance dose makes 0,5-4 mg/days.

Children from 6 months to 12 years: 0,25-0,5 mg two times a day.

The maintenance dose makes 0,25-2 mg/days. If the recommended dose does not exceed 1 mg/days, all dose of drug can be accepted for once (once).

The maintenance dose needs to be selected individually. At achievement of therapeutic effect, the maintenance dose needs to be lowered to the smallest dose at which the patient has no disease symptoms.

Adults (including poeyuily) and children of 12 years: 0,5-1 mg two times a day.

Children from 6 months to 12 years: 0,25-0,5 mg two times a day.

The table of recalculation of doses for the patients receiving peroral glucocorticosteroids in terms of будесонид

Dose (mg) of a budesonid,    Budenit Steri-Neb        Budenit Steri-Neb
accepted inside    0,5mg/2ml (0,25 mg/ml)    1 mg / 2 ml (0,5 mg/ml)
                                        Volume (ml)                     Volume (ml)

                                            0,25 1                                       -

                                              0,5 2                                      1

                                            0,75 3                                       -

                                             1,0 4                                       2

                                             1,5 6                                       3

                                             2,0 8                                       4

 
In need of achievement of additional therapeutic effect, it is possible to recommend increase in a dose of drug of Budenit Steri-Neb instead of a combination with peroral GKS (for reduction of risk of development of system effects).

The stenosing laryngotracheitis (false croup)

Children of 6 months are also more senior: the recommended dose of 2 mg/days once or in 2 receptions on 1 mg with an interval of 30 min.

Features of use:

Drug Budenit Steri-Neb is not intended for bystry removal of attacks of bronchial asthma, for stopping of an acute bronchospasm it is recommended to use inhalation bronchodilatory means of short action.

The patients who are not receiving GKS:
Usually therapeutic effect occurs within 10 days. At patients with excessive secretion of slime in bronchial tubes additional treatment can be originally carried out by peroral GKS short (about 2 weeks). After a course of peroral therapy in many cases it is possible to refuse completely reception of GKS inside.

The patients who are on therapy of GKS:
Before transfer of the patient, from treatment by peroral GKS on treatment by drug Budenit Steri-Neb, condition of the patient it has to be rather stable then drug Budenit Steri-Neb is used in a combination with earlier applied GKS dose for intake within about 10 days. In the subsequent the dose of peroral GKS needs to be lowered gradually (for example, by 2,5 mg of Prednisolonum or its equivalent every month) as far as it is possible to the lowest level. In most cases peroral GKS can be completely replaced drugs of Budenit Steri-not B.

Sometimes, during transfer from treatment of GKS for intake on treatment of Budenit Steri-Neb symptoms which were stopped by reception of system drugs earlier, for example – rhinitis, eczema and muscular and joint pain are observed. Such in as fatigue, a headache, nausea and vomiting can indicate emergence by a symptom development of system insufficiency of GKS. In such cases there can even be a need to temporarily increase a dose of peroral GKS.

Systemic side effect of inhalation GKS can be shown first of all at introduction of high doses during a long span. The probability of emergence of this effect is much less, than at treatment by peroral GKS. Oppression of adrenal glands, a growth inhibition at children and teenagers, decrease in mineral density of a bone, a cataract and glaucoma belongs to possible system effects. Therefore it is very important to titrate IGKS dose to the smallest dose at which effective control of a disease remains. It is regularly recommended to control growth at the children receiving IGKS during a long span. In case of a growth inhibition it is necessary to carry out correction of treatment for the purpose of reduction of a dose of GKS for inhalation to the smallest dose at which effective control of bronchial asthma remains.

Oral administration of a ketokonazol and itrakonazol or other inhibitors of an isoenzyme CYP3A4 causes increase in system influence of a budesonid. Therefore in case of need combined use it is necessary to accept them with the maximum interval. It is necessary to consider the possibility of a dose decline of a budesonid also.

For minimizing of risk of fungal stomatitis it is necessary to inform the patient and/or the child's parents on need to rinse a mouth water after each inhalation of drug.

Influence on ability to manage the vehicle and to work with the equipment
Drug Budenit Steri-Neb does not exert negative impact on ability to manage the vehicle and to work with the equipment. In case of development of rare side reactions from a nervous system it is necessary to avoid the activity demanding speed, psychomotor reactions.

Technology of use
Ultrasonic nebulizers are not suitable for use with drug Budenit Steri-Neb, the dose necessary for the patient can change depending on the used nebulizer. Time of inhalation and a dose of drug depend on the speed of an air flow, volume of the camera of the nebulizer and volume of filling. Therefore for inhalation of drug Budenit Steri-Neb it is necessary to use corresponding the nebulizer, and also a mouthpiece and a special face pack. The nebulizer has to be connected to the air compressor for creation of the corresponding air flow.

Before use of medicine it is necessary to read the instruction of the producer of nebulizers.
• To prepare the nebulizer according to the instruction of his producer.
• To separate Steri-Neb (an ampoule with sterile solution) from the block, for this purpose to turn and pull its (fig. 1).
• Holding the Ampoule vertically up a cap, to break off a cap (Fig. 2).
• To squeeze out solution in a tank of the nebulizer (Fig. 3)
• To use the nebulizer according to the instruction of his producer.
• It is necessary to rinse a mouth after the end of inhalation.
• If the mask was used, it is necessary to wash out face skin.
• The solution which remained unused in the nebulizer camera should be poured out.
• To carefully wash up the nebulizer.

 

When using drug it is necessary to avoid hit of solution in eyes.

Side effects:

Often (≥1/100> 1/10): irritation and dryness of a mucous membrane of a throat, candidosis stomatitis, hoarseness of a voice, cough, dryness of a mucous membrane of an oral cavity, unpleasant flavoring feelings.

Seldom (≥1/10 000> 1/1 000): nervousness, excitability, a depression, a behavior disorder, reactions of hypersensitivity of the immediate and slowed-down action (including rash, contact dermatitis, a small tortoiseshell, a Quincke's disease and a bronchospasm), emergence of skin bruises or thinning of skin, a headache, nausea, ezofagialny candidiasis.

At inhalation treatment of GKS there can be system effects, first of all at prolonged treatment by high doses. The probability of emergence of such effects is much less, than at treatment of GKS for intake. Oppression of adrenal glands, a growth inhibition at children and teenagers, decrease in mineral density of a bone, a cataract, and glaucoma belongs to possible system effects.

Drug Budenit Steri-Neb contains 0,1 mg/ml of dinatrium of an edetat. Which can cause a bronchospasm at concentration higher than 0,2 mg/ml.

As well as in case of other inhalation therapy there can be a paradoxical bronchospasm with bystry strengthening of an asthma after introduction of a dose. In case of heavy reaction it is necessary to appoint alternative therapy.

In certain cases there is an irritation of face skin when using the nebulizer with a mask. For the prevention of irritation after use of a mask face skin needs to be washed out water.

Interaction with other medicines:

Pharmaceutical: drug Budenit Steri-Neb can be mixed from 0,9% solution of sodium of chloride and with other solutions intended for use by means of nebulizers, for example, sterbutaliny, salbutamol, Fenoterolum, Acetylcysteinum. Sodium kromoglikaty or ipratropiya bromide.

Pharmacological: Metabolism of a budesonid is generally carried out with the participation of CYP3A4 isoenzyme. Reception of 100 mg of a ketokonazol 2 times a day increases concentration in plasma of orally applied budesonid of 10 mg once on average by 7,8 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, therefore, such inhibitors of an isoenzyme CYP3A4 as кетоконазол and итраконазол, can system influence of a budesonid. Other powerful CYP3A4 inhibitors possibly can also increase considerably concentration of a budesonid in plasma.

Preliminary inhalation βадреномиметиков expands bronchial tubes, improves receipt of a budesonid in respiratory tracts and strengthens its therapeutic effect.

Phenobarbital, Phenytoinum, rifampicin reduce efficiency (induction of microsomal enzymes of a liver).

Metandiyenon, estragenes strengthen action of a budesonid.

Contraindications:

• Hypersensitivity to a budesonid or to any other component of drug; age up to 6 months.

With care: pulmonary tuberculosis, fungal, bacterial, parasitic and viral infections of a respiratory organs, cirrhosis, pregnancy, lactation period.

Use at pregnancy and during breastfeeding
Use of a budesonid during pregnancy is possible only if the advantage for mother exceeds possible risk for a fruit. In need of use drug is used in a minimal effective dose. Data on allocation of a budesonid with breast milk are absent. Appointment drug in the period of a lactation perhaps only under observation of the doctor in case the expected advantage for mother exceeds possible risk for the child.

Overdose:

At acute overdose budesonidy clinical manifestations usually do not arise. Treatment – drug withdrawal, inhalation of short-range bronchodilatory means.

At long use in the doses exceeding recommended the system GKS-effect in the form of a hypercorticoidism and suppression of function of adrenal glands can develop.

Storage conditions:

At a temperature not above 25ºС. To store in the place, unavailable to children. Period of validity 2 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Suspensions for inhalation 0,25mg/ml; 0,5 mg/ml.
On 2 ml of drug in an ampoule from polyethylene of low density. Ampoules are soldered with each other in the form of the block. Each block is placed in the laminated foil. On 4 blocks together with the instruction on uses place in a cardboard pack. On 6 blocks together with the application instruction place in a cardboard pack and on 2 cardboard packs place in a cardboard box.