Berotek n instructions for use. Berotek for inhalation: instructions for use

Registration number: P N015273 / 01-020316

Trade name of the drug: BEROTEC

International non-proprietary name:
Fenoterol
Chemical name:
1- (3,5-Dihydroxyphenyl) -2- [amino] ethanol hydrobromide

Dosage form: solution for inhalation
Composition:
1 ml of solution for inhalation (\u003d 20 drops) contains fenoterol hydrobromide 1 mg
Excipients benzalkonium chloride 0.1 mg, disodium edetate dihydrate 0.5 mg, sodium chloride 8.60 mg, hydrochloric acid 1N (to adjust pH 3.2) 0.946 mg, purified water to 1.00 ml

Description: Clear, colorless or nearly colorless liquid, free of particles. The smell is almost imperceptible.

Pharmacotherapeutic group: bronchodilating agent - selective β2-adrenergic agonist
ATX: R03AC04

Pharmacological properties:

Pharmacodynamics
BEROTEC is an effective bronchodilator for the prevention and relief of bronchospasm attacks in bronchial asthma and other conditions accompanied by reversible airway obstruction, such as chronic obstructive bronchitis (with or without pulmonary emphysema).
Fenoterol is a selective β2-adrenergic receptor stimulant in the therapeutic dose range. Stimulation of β1-adrenergic receptors occurs when using higher doses of the drug. Binding to β2-adrenergic receptors activates adenylate cyclase through the stimulatory Gs protein, followed by an increase in the formation of cyclic adenosine monophosphate (cAMP), which activates protein kinase A, the latter depriving myosin of the ability to bind with actin, which causes relaxation of smooth muscles.
Fenoterol relaxes the smooth muscles of the bronchi and blood vessels and protects against bronchoconstrictor stimuli such as histamine, methacholine, cold air and allergens (early response). In addition, fenoterol inhibits the release of bronchoconstrictor and pro-inflammatory mediators from mast cells. An increase in mucociliary clearance was demonstrated after the use of fenoterol (at a dose of 0.6 mg).
Due to the stimulating effect on β1-adrenergic receptors, fenoterol can have an effect on the myocardium (especially at doses exceeding therapeutic ones), causing an increase in heart rate and increase.
Fenoterol quickly relieves bronchospasm of various origins. Bronchodilation develops within minutes after inhalation and lasts 3-5 hours.
Also, pre-inhalation of fenoterol prevents bronchoconstriction, which occurs under the influence of various stimuli such as exercise, cold air and allergens (early response).

Pharmacokinetics
After inhalation, 10-30% of the active substance released from the aerosol preparation reaches the lower respiratory tract, depending on the inhalation technique and the inhalation system used. The remainder is deposited in the upper respiratory tract and in the mouth and is then swallowed.
The absolute bioavailability of fenoterol after inhalation of a metered aerosol is 18.7%. The absorption of fenoterol from the lungs is two-phase: 30% of the dose is absorbed quickly (half-life 11 minutes), and 70% - slowly (half-life 120 minutes). The maximum plasma concentration after inhalation of 200 μg fenoterol is 66.9 pg / ml (the time to reach the maximum plasma concentration tmax 15 min).
After oral administration, approximately 60% of the dose of fenoterol hydrobromide is absorbed. The absorbed amount undergoes an extensive first phase of metabolism in the liver, resulting in an oral bioavailability of approximately 1.5%, and its contribution to plasma fenoterol concentration after inhalation is small.
The distribution of fenoterol in plasma after intravenous administration is adequately described by the 3-component pharmacokinetic model (the half-life is tα \u003d 0.42 min, tβ \u003d 14.3 min and tγ \u003d 3.2 h). The volume of distribution of fenoterol at a constant concentration after intravenous administration is 1.9-2.7 l / kg, binding to plasma proteins is from 40 to 55%.
Fenoterol undergoes intensive metabolism in the liver by conjugation to glucuronides and sulfates. The swallowed portion of the fenoterol dose is metabolized primarily by sulfation. This metabolic inactivation of the parent substance begins already in the intestinal wall.
Fenoterol is excreted by the kidneys and bile in the form of inactive sulfate conjugates. Biotransformation, including excretion with bile, undergoes the main part of approximately 85%. Excretion of fenoterol in the urine (0.27 L / min) corresponds to approximately 15% of the mean total clearance of the systemically available dose. The volume of renal clearance is indicative of tubular secretion of fenoterol in addition to glomerular filtration. After inhalation, 2% of the dose is excreted through the kidneys unchanged within 24 hours.
Fenoterol hydrobromide in unchanged form can cross the placental barrier and pass into breast milk.

Indications for use

Bronchial asthma attacks or other conditions with reversible airway obstruction, chronic bronchitis? chronic obstructive pulmonary disease.
- Prevention of attacks of bronchial asthma due to physical exertion.
- As a bronchodilator before inhalation of other drugs (antibiotics, mucolytics, glucocorticosteroids)
- Conducting bronchodilation tests in the study of the function of external respiration.

Contraindications

Hypersensitivity to fenoterol or to any of the excipients of the drug.
Hypertrophic obstructive cardiomyopathy, tachyarrhythmia.

Carefully

In the following conditions, BEROTEC should be used only after careful assessment of the benefits / risks of treatment, especially if the maximum recommended doses are applied:
arterial hypotension, arterial hypertension, hyperthyroidism, hypokalemia, insufficiently controlled diabetes mellitus, recent myocardial infarction (within the last 3 months), severe organic diseases of the heart and blood vessels, such as chronic heart failure, ischemic heart disease, coronary artery disease, heart defects (including aortic stenosis), pronounced lesions of the cerebral and peripheral arteries, pheochromocytoma, children under 6 years of age.

Pregnancy and the period of breastfeeding

The results of preclinical studies in combination with the existing experience of the clinical use of the drug did not reveal any adverse events during pregnancy. However, the drug should be used with caution during pregnancy, especially in the first trimester, if the potential benefit to the mother outweighs the potential risk to the fetus.
Consideration should be given to the possibility of an inhibitory effect of fenoterol on the contractile activity of the uterus.
Preclinical studies have shown that fenoterol passes into breast milk. The safety of the drug during breastfeeding has not been studied. During the period of breastfeeding, the use of the drug is possible if the potential benefit to the mother outweighs the potential risk to the child.

Method of administration and dosage

Treatment with BEROTEC is carried out by inhalation using commercially available nebulizers. Pulmonary deposition and systemic bioavailability of the drug depend on the nebulizer used and may be higher than when using metered-dose BEROTEC N aerosol. When using a stationary oxygen source, the solution is best inhaled at a flow rate of 6-8 l / min.
When dosing, it should be borne in mind that 20 drops are 1 ml, with 1 drop containing 50 μg of fenoterol hydrobromide. The recommended dose of BEROTEC is diluted in a nebulizer chamber with 0.9% sodium chloride solution to a final volume of 3-4 ml and inhaled until sufficient relief of symptoms is achieved. BEROTEC must not be diluted with distilled water. The solution is diluted each time immediately before use; the remains of the prepared solution are poured out.
BEROTEC solution can be inhaled simultaneously with anticholinergic and mucolytic drugs for which compatibility with it has been proven - solutions for inhalation Atrovent (ipratropium bromide) and Lazolvan (ambroxol).
Treatment with BEROTEC should be started and carried out under the supervision of medical personnel, for example, in a clinic. Home treatment may be recommended to patients after consulting a doctor in cases where the use of a low-dose metered-dose aerosol of a fast-acting beta-agonist bronchodilator (such as BEROTEC N) was insufficient to relieve the condition. It can also be recommended for patients who need nebulizer therapy for other reasons, for example, in case of problems with the use of metered aerosols or when it is necessary to prescribe higher doses.
Treatment usually should be started at the lowest recommended doses. The dose should be individually tailored to the needs of the patient and adjusted according to the severity of the acute episode. The drug should be discontinued when sufficient symptom relief is achieved.
If necessary, the dose can be reapplied after at least 4 hours.
The dose may depend on the route of inhalation and the characteristics of the nebulizer used. The duration of inhalation can be controlled by the dilution volume of the drug.

The following dosing regimens are recommended.
Adults (including patients over 75 years old) and adolescents over 12 years old:
a) Attacks of bronchial asthma and other conditions with reversible airway obstruction
Inhalation 0.5 ml (10 drops \u003d 500 mcg fenoterol hydrobromide) is sufficient in most cases for immediate relief of symptoms; if it is necessary to re-prescribe the drug up to 4 times a day, consider reducing individual doses depending on the effectiveness of the nebulizer;
in severe cases (for example, for most patients admitted to the intensive care unit), higher doses may be required - 1-1.25 ml (20-25 drops \u003d 1000-1250 mcg fenoterol hydrobromide);
in extremely severe cases, under the supervision of a physician, doses of up to 2 ml (40 drops \u003d 2000 μg fenoterol hydrobromide) can be administered;
b) Prevention of bronchial asthma attacks due to physical exertion
Inhalation 0.5 ml (10 drops \u003d 500 μg fenoterol hydrobromide) before exercise.
Children from 6 to 12 years old (weighing about 22-36 kg):
a) Attacks of bronchial asthma and other conditions with reversible airway obstruction:
Inhalation 0.25-0.5 ml (5-10 drops \u003d 250-500 mcg fenoterol hydrobromide) is sufficient in most cases for immediate relief of symptoms;
if it is necessary to re-prescribe the drug up to 4 times a day, consider reducing individual doses depending on the effectiveness of the nebulizer;
in severe cases (for example, in most cases of hospital treatment), higher doses of up to 1 ml (20 drops \u003d 1000 μg fenoterol hydrobromide) may be required;
in extremely severe cases, under the supervision of a physician, doses of up to 1.5 ml (30 drops \u003d 1500 μg fenoterol hydrobromide) can be administered;
b) Prevention of bronchial asthma attacks due to physical exertion:
Inhalation 0.5 ml (10 drops \u003d 500 mcg fenoterol hydrobromide) before exercise;
Children under 6 years of age (weighing less than 22 kg):
Due to the limited information on the use of the drug in this age group, treatment is carried out only under the supervision of a doctor, prescribing the drug in the following dose:
Inhalation About 50 μg of fenoterol hydrobromide per dose (\u003d 0.05 ml or 1 drop) per 1 kg of body weight, but not more than 0.5 ml (10 drops) per dose up to 3 times a day.

Side effect

Like all other inhalation treatments, BEROTEC can cause local irritant symptoms.
From the immune system
hypersensitivity
On the part of metabolism and nutrition
Hypokalemia, including severe hypokalemia
From the nervous system
agitation, nervousness, tremor, headache, dizziness
On the part of the cardiovascular system
myocardial ischemia, arrhythmia, tachycardia, palpitations, increased systolic blood pressure, decreased diastolic blood pressure
From the respiratory system
paradoxical bronchospasm, cough, irritation of the larynx and pharynx
From the digestive system:
nausea, vomiting
Skin and subcutaneous tissue
hyperhidrosis, skin reactions such as rash, pruritus, urticaria
The musculoskeletal system and related tissue diseases
muscle spasm, myalgia, muscle weakness

Overdose

Symptoms
In overdose, the expected symptoms are those caused by excessive beta-adrenergic stimulation. The most pronounced are tachycardia, palpitations, tremors, a decrease or increase in blood pressure, an increase in pulse pressure, angina pectoris, arrhythmias, and facial flushing. Metabolic acidosis and hypokalemia have also been observed with the use of fenoterol in doses in excess of the recommended doses for the approved indications.
Treatment
Treatment with BEROTEC should be discontinued. The acid-base balance and electrolyte balance should be monitored.
For treatment, sedatives are used: in severe cases, intensive symptomatic therapy is carried out.
As specific antidotes, β-blockers (preferably selective β1-blockers) can be prescribed; at the same time, the possibility of increased bronchial obstruction should be taken into account and the doses of these drugs should be carefully selected in patients with bronchial asthma.

Interaction with other medicinal products

β-adrenergic drugs, anticholinergics, xanthine derivatives (such as theophylline), cromoglycic acid, glucocorticosteroids and diuretics can increase the action and side effects of fenoterol.
Β2-agonist-induced hypokalemia may be exacerbated by concomitant therapy with xanthine derivatives, corticosteroids, and diuretics. This should be especially taken into account in patients with severe airway obstruction (see section "Special instructions").
A significant decrease in bronchodilation with the simultaneous use of fenoterol and β-blockers.
Β-adrenergic receptor agonists should be used with caution in patients receiving monoamine oxidase inhibitors or tricyclic antidepressants that can enhance the action of β-adrenergic receptor agonists.
Inhalation of general anesthetic agents such as halothane, trichlorethylene, and enflurane increases the likelihood of cardiovascular effects of β-adrenergic receptor agonists.

special instructions

In patients with diabetes mellitus, regular monitoring of plasma glucose should be carried out during treatment.
Paradoxical bronchospasm
Like other inhaled drugs, BEROTEC can cause paradoxical bronchospasm, which can be life threatening. If paradoxical bronchospasm occurs, the drug should be immediately discontinued and replaced with alternative therapy.
Effects on the cardiovascular system
Effects on the part of the cardiovascular system can be observed with the use of sympathomimetic drugs, including BEROTEC. There are data from post-registration studies and publications in the literature on rare cases of myocardial ischemia associated with the use of beta-agonists.
Patients with underlying severe heart disease (for example, ischemic heart disease, arrhythmias, or severe heart failure) receiving BEROTEC should be warned to seek medical attention if they experience chest pain or worsening heart disease.
Consideration should be given to assessing symptoms such as dyspnea and chest pain, as they can be both respiratory and cardiac.
Hypokalemia
Potentially severe hypokalemia can develop with beta2-agonist therapy. It is recommended to be especially careful in severe bronchial asthma, since hypokalemia can be potentiated by concomitant therapy with xanthine derivatives, glucocorticosteroids and diuretics. In addition, hypoxia can increase the effect of hypokalemia on heart rate. Hypokalemia can lead to an increased susceptibility to arrhythmias in patients receiving digoxin.
In such situations, it is recommended to monitor serum potassium levels.
Acute progressive dyspnea
Patients should be advised to seek immediate medical attention in case of acute, rapidly worsening dyspnea.
Regular use
Relief of attacks of bronchial asthma (symptomatic treatment) is preferable to regular use of the drug;
Patients should be evaluated to determine the need for the appointment or intensification of anti-inflammatory treatment (for example, inhaled glucocorticosteroids) in order to control airway inflammation and prevent delayed lung damage.
In the case of increased bronchial obstruction, it is unacceptable and may be risky to increase the frequency of administration of β2-adrenergic receptor agonists, such as BEROTEC, in excess of the recommended doses and for a long time. The use of increased doses of β2-agonists, such as BEROTEC, on a regular basis to control symptoms of bronchial obstruction may indicate a deterioration in disease control. In such a situation, the treatment plan, and especially the adequacy of anti-inflammatory therapy, should be reviewed to prevent a potentially life-threatening deterioration in disease control.
Concurrent use with sympathomimetic and anticholinergic bronchodilators
Other sympathomimetic bronchodilators should be used in conjunction with BEROTEC only under medical supervision. Anticholinergic bronchodilators can be inhaled simultaneously with BEROTEC.
Influence on the results of laboratory tests
The use of BEROTEC may lead to positive test results for the presence of fenoterol in studies of drug abuse for non-medical indications, for example, due to the enhancement of physical capabilities in athletes (doping).
The preparation contains a preservative - benzalkonium chloride and a stabilizer - disodium edetate. It has been shown that these components can cause bronchospasm in some sensitive patients with airway hyperresponsiveness.

The effect of the drug on the ability to drive vehicles and work with mechanisms

Studies of the effects of the drug on the ability to drive vehicles and use mechanisms have not been conducted.
However, patients should be advised that symptoms such as dizziness have been observed during clinical trials. Therefore, it is recommended to be careful when driving or using machinery.

Release form
Solution for inhalation 0.1%. 20, 40 and 100 ml in amber glass vials with a polyethylene dropper and a polypropylene screw cap with first opening control. One bottle with instructions for use in a cardboard box.

It is a highly effective dosage agent with bronchodilator properties. Berotek acts very quickly: aerosol (according to the instructions) is able to relieve and prevent bronchial spasms. Persons suffering from bronchospasm are advised to always have it with them as an emergency aid in case of choking.

Mechanism of action, dosage forms

The active ingredient of Berotek aerosol - fenoterol hydrobromide belongs to the group of beta2 - adrenergic agonists that have a selective effect on the bronchi.

Patients are often interested in whether it is a hormonal drug or not. This is a non-hormonal agent, this group of drugs acts on the beta2 nerve receptors located in the bronchi and responding to the effects of adrenaline. Adrenaline dilates the bronchi and all beta2-adrenomimetics do the same.

At the same time, the drug (if used in the recommended dosages) has almost no effect typical of adrenaline on other organs, including the heart and kidneys. If you exceed the dosage or use the medicine too often, then this will manifest itself in the form of side effects: palpitations, heart rhythm disturbances, etc.

A feature of the drug is that it acts quickly, selectively (selectively) on the bronchi and for a rather long time: up to 5 hours.

Manufacturer Beroteka N german company Boehringer Ingelheim Pharma... Available in cans of 10 ml (200 doses of 100 mcg).

Italian firm Boehringer Ingelheim produces 0.1% solution for inhalation. Dropper bottles of 20, 40 and 100 ml (1 ml \u003d 20 drops, 1 drop contains 50 mcg of fenoterol).

Who is appointed

The use of a drug is determined by its mechanism of action.

Berotek is best used on an emergency basis to relieve bronchospasm or in some situations when their development is expected.

Indications:

• the onset of bronchospasm in a patient suffering from any acute or chronic diseases of the respiratory system, accompanied by spasms of the bronchi; the attack is removed after a few minutes, the action lasts up to 5 hours;
• possible onset of an attack of bronchospasm in a certain situation, for example, with physical exertion, a smoky room, etc.; inhalation of a bronchodilator will cause persistent expansion of the bronchi and prevent their spasm;
• sometimes the attending physician prescribes inhalation of the drug before inhalation of other drugs with antibacterial, anti-inflammatory and other properties to pre-expand the bronchi and facilitate the absorption of the main substance; very often the agent is used together - a glucocorticosteroid with pronounced anti-inflammatory and antiallergic properties; it can also be combined with expectorant and phlegm-thinning agents (eg, c).
• the agent is also used to study the function of external respiration.

Who should not use Berotec

The drug is contraindicated in the following diseases and conditions:

• heart rhythm disturbances (arrhythmias) and bouts of increased heart rate (tachycardia);
• hypertrophic obstructive cardiomyopathy - thickening of the myocardium and the muscles of the interventricular septum, which impede blood flow;
• individual drug intolerance;
• under the age of four (for aerosol).

• increased thyroid function (thyrotoxicosis);
• low blood potassium (hypokalemia);
• progressive course of diabetes mellitus;
• transferred 3 months or earlier before the appointment of myocardial infarction;
• angina pectoris, impaired cerebral circulation, heart defects, etc.;
• pheochromacytoma - a tumor of the adrenal glands, accompanied by sharp rises in blood pressure (BP);
• child's age up to 6 years;
• lactation.

Side effect

• angina attacks (spasm of the coronary arteries), heart rhythm disturbances, palpitations, increased upper blood pressure, lowering lower blood pressure, increased pulse pressure;
• aggressiveness, irritability, tearfulness, headache and dizziness;
• dry cough, bouts of bronchospasm, acute growing shortness of breath; if such side effects appear, you should immediately consult a doctor;
• hypokalemia;

A lack of potassium can lead to severe complications from the heart: arrhythmias and even cardiac arrest;

• nausea and vomiting;
• spasm or vice versa, muscle relaxation, muscle pain;
• various kinds of skin rashes (including allergic ones), increased sweating.

Is an overdose possible?

In case of an overdose, intensified symptoms of side effects appear: paroxysmal acute pain in the heart, an increase or a sharp decrease in blood pressure, heart rhythm disturbances, tachycardia attacks, shortness of breath, etc. Face flushed, frightened.

Emergency help:

• cessation of drug use;
• fresh air (open a window, a window);
• release from tight clothing;
• taking any sedative (Valokardin, Validol, Seduxen);
• potassium intake (Asparkam, Panangin);
• calling an ambulance; if the condition does not improve, hospitalization.

As an antidote, drugs from the group of beta-blockers are sometimes prescribed, which block the action of adrenaline and drugs with similar properties. These drugs include Atenolol, Betaxolol, Bisoprolol. But it is not worth using them independently without medical supervision as antidotes: they can cause bronchospasm. Sometimes an overdose requires intensive therapy and even resuscitation measures.

Instructions for use

The dosage is selected individually. It is usually minimal. Medicinal substances in this group are more suitable for emergency use than for routine use. Scheduled appointments are made in combination with other bronchodilator, anti-inflammatory and antibacterial agents as preparation for the action of the main drug.

Standard dosages of Berotek aerosol for adults and children over 6 years old:

• to relieve bronchospasm - one dose; if the bronchospasm has not disappeared, after five minutes you can inhale one more time, no more; in the absence of effect, you need to call an ambulance; maximum 8 injections per day can be made; children should only be inhaled under adult supervision;
• to prevent bronchospasm - before a dangerous situation (for example, before physical activity, which can cause bronchospasm), inhale 1 - 2 times with an interval of 5 minutes; maximum per day - 8 times.

At the age of 4 to 6 years, aerosol should be used with caution and only under adult supervision, as this the dosage form can cause broncho- and laryngospasm in young children, accompanied by suffocation... It is better to prescribe a bronchodilator to such children as. But sometimes the drug is still prescribed to babies in a standard dose of 1 injection (no more than 4 injections per day) both for the removal and for the prevention of bronchospasm.

0.1% solution for inhalation.The minimum effective dosage is used to relieve bronchospasm in this patient. She is selected by the doctor individually in the hospital, after which the procedures can be continued at home using an inhaler nebulizer. Inhalation administration is more effective, so you can choose the right dosage, therefore, solutions are prescribed to patients with severe disease.

Standard doses of solution for inhalation:

• for adults and children over 12 years old; initial dose - 10 drops (500 mcg); inhalations can be carried out 4 times a day at intervals of at least 4 hours; if necessary, under the supervision of a doctor in a hospital, the dosage can be increased, focusing on the patient's condition up to 20 drops; in severe conditions, it is possible to use 40 drops.

When using a nebulizer, the solution must be diluted with saline (water cannot be used!) Until a total volume of 3-4 ml is obtained.

Features of the appointment of inhalation to children

Children are usually prescribed Berotek for inhalation:

• 6 - 12 years old: 5-10 drops (250-500 mcg) 4 times a day; the dose can be increased to 20-30 drops only in a hospital setting;
• up to 6 years old: the dosage is selected strictly individually, depending on body weight and general condition, at the rate of 50 μg (1 drop) per kg of weight per 1 inhalation; the dose should not exceed 10 drops (500 mcg) 3 times a day.

For babies, drugs of this group are prescribed only in extreme cases, so there is no great clinical experience in their use at this age.

Important: in no case can you use it without a doctor's prescription!

Appointment during pregnancy and lactation

According to the instructions, pregnancy is not a contraindication for use. During pregnancy, this drug is prescribed with caution, only as prescribed by a doctor and in the minimum effective dosage. In the course of research, the negative effect of this substance on the fetus has not been identified, but experience with its use during pregnancy is limited, so caution should be exercised.

Important: during lactation, the active substance is excreted in breast milk, as far as it is dangerous for the baby, there are no data. Therefore, appointments are made only if absolutely necessary, in minimal doses and as prescribed by a doctor.

According to the instructions, Berotek for inhalation relieves the condition of patients after the first procedures. It has been proven that the treatment has a protective effect on the respiratory tract from allergic agents, methacholine, temperature changes, and a histamine agent.

Berotek belongs to the modern drugs of the bronchodilator group. Such means are successfully used in pulmonology. They are indicated for many ailments of the respiratory tract, including asthma, bronchitis and bronchiectasis. Mainly Berotek is used as the basis for inhalation procedures.

This synthetic substance was created in laboratory conditions, therefore, it can only be used according to a special scheme, after a medical consultation. At the heart of Berotek is a highly active substance that deliberately relieves spasms in the bronchial tree. In this way, an almost instant bronchodilator effect is achieved. The drug effectively blocks mast cells, preventing the release of a huge amount of inflammatory mediators.

Inhalation use of Beroteka requires a preliminary study of the instructions for use. The medicine is based on fenoterol. Therefore, the drug exhibits pronounced pharmaceutical properties and belongs to selective stimulants of beta-2-blockers. It has a tropism for the elements of the human respiratory tract. Due to this, it is possible to quickly relax the elements of the smooth muscles of the bronchi and blood vessels, to resist bronchospastic reactions.

Release forms

There are two forms in which Berotec is produced:

1. Berotek is a liquid without color, which is available in containers of 20, 40 and 100 ml.
2. You can often find Berotek N - metered aerosol. These are metal vials, each of which contains 10 ml of the drug.

Composition

Fenoterol is the active ingredient in Berotek. Excipients depend on the form:

• solution for inhalation: sodium chloride, hydrochloric acid, benzalkonium chloride, disodium edetate dihydrate, water;
• aerosol: propellant - tetrafluoroethane, ethanol, citric acid anhydride, water.

Indications for use

The instructions for use clearly indicate that Berotek is used for inhalation for medical purposes to relieve asthmatic attacks, which mainly proceed as bronchial lesions. In some cases, the drug can be used as an additional component of the complex therapy of obstructive ailments.

An important point in the successful use of the drug is the complete reversibility of the obstruction.

The list of indications for the use of Berotek also includes:

1. Planned expansion of the bronchi before inhalation procedures using mucolytics, hormones, or antibiotics.
2. Berotek is often used before testing the function of external respiration. It has been proven that the drug has a quick and necessary expanding effect on the bronchi.
3. An effective preventive tool against new asthma attacks of the bronchial type, which usually occur during intense physical exertion.

Method of administration and dosage

The dose of the medication is always selected individually by the attending physician. The number of drops for inhalation, the frequency of carrying out depends on many factors:

• patient weight;
• age;
• the severity of the condition;
• the presence of concomitant pathology.

Be sure to take into account the presence of intolerance or allergic reactions to any substances. When choosing a dosage, the concentration of the drug is taken into account. Each drop of Berotek contains 50 mcg of fenoterol, 1 ml - 20 drops.

The medication has been used successfully in a variety of ways. This does not reduce the effectiveness of the medication. Berotek can act as one of the components of the nebulizer mixture. Often, the solution is simply used to irrigate the oral cavity. In the latter case, an aerosol form of release is used.

In the case of inhalation, it is preferable to choose the liquid form of the medication. The required amount of the substance before the procedure must be diluted in saline. If necessary, the doctor, at his discretion, may additionally prescribe some mucolytic drugs for bronchitis.

Instructions for use

Each aerosol can contains no more than 200 doses of medication. After using them, you cannot use a spray can, even if Berotek remains in it. The fact is that after the 200th dose, the drug is released poorly, so the patient will not receive full treatment during inhalation. After the end of operation, the cartridge should be thrown away and a new one should be bought.

A huge role in the effectiveness of inhalation is played by the patient's awareness and ability to correctly perform this procedure. Carrying out inhalations with the drug has its own characteristics. After the appointment of Berotek, the doctor should familiarize the patient with the correct technique for using the aerosol. The main subtleties of the procedure include:

1. Free the cartridge from the protective membrane first.
2. Closely grip the tip of the balloon with your lips so that there are no gaps. Thus, the entire dose can easily enter the oral cavity.
3. Simultaneously with pressing the bottom of the can, you need to take deep breaths, holding your breath. At the end of the procedure, the end of the balloon is pulled out of the mouth, exhaled slowly. Each repeated inhalation should be carried out in the same way.

It is important to remember that if the balloon has not been used for more than 3 days, before the therapy, you must first press the bottom of the balloon into the air.

The mouthpiece must be kept clean. It is important to flush the device at least once a month. Otherwise, Berotek will accumulate, preventing the next dose from advancing. You only need to rinse the inhaler with plain, warm water.
The type of therapy largely depends on the purpose of the appointment. To stop an attack of asthmatic genesis, one injection is enough. Repeated inhalation is indicated if relief does not occur within 5 minutes.

The medication cannot be used uncontrollably. There are certain rules and regulations for the use of aerosols:

1. For emergency care, inhalation starts from a single injection (this is equivalent to 10 drops of medicine).
2. For the purpose of prophylaxis, up to 8 doses of the drug can be used per day, but each dose includes no more than 2 injections.
3. With severe spasm in the bronchial structures, a double dose of the drug is injected once at once.

Inhalation with Berotek has its own characteristics:

1. With an asthmatic attack of bronchial genesis, the use of 0.5 ml of the drug is shown - this is 10 drops of Berotek.
2. In severe cases, the dosage is always increased. As a rule, a single use of the drug is enough to stop the attack.
3. About 10 drops of Berotek are enough for adequate and effective prevention of new asthma attacks.
4. The duration of drug use for an adult or a child after 12 years old is selected individually. Such a decision is always made only by the attending physician. The patient's condition and response to therapy are taken into account.

Contraindications

Berotek for inhalation is a highly effective pulmonary drug. But this does not make it completely harmless. There is a certain list of conditions and situations in which it is absolutely impossible to use the medicine.

First of all, we are talking about individual intolerance to fenoterol - the main component of the drug. You can not use the medicine for episodes of tachyarrhythmias, the presence of severe cardiomyopathy.

Use the medicine with caution if you have:

• heart defects;
• hyperthyroidism;
• hypo or hypertension;
• pheochromocytomas.

In pediatrics, it is forbidden to use the medicine until the child is 6 years old. But this is a relative contraindication. In extreme, severe cases, the medicine is prescribed to babies of any age under the direct supervision of specialists.

Side effects

Infrequently, but in some cases, Berotek is capable of provoking disturbances in the work of many organs and body systems. Often, adverse reactions include:

• intense arousal;
• soreness in the head;
• tremor;
• hypokalemia;
• pressure surges;
• dyspeptic disorders;
• paradoxical bronchospasm;
• spasm of muscle elements;
• hyperhidrosis.

In the presence of severe diabetes during therapy with Berotek, it is necessary to carefully monitor blood glucose levels.

Any combination of Berotek with other medicines must be agreed with the doctor. Self-medication can lead to dire consequences and complications.

Treatment with Berotek

It is enough to carry out one inhalation in order to relieve spasm in the bronchi. The manipulation is repeated if breathing does not ease within five minutes. To prevent asthma, use 1-2 inhalation doses of the agent in question. The maximum number of procedures performed is 8 per day.

The prescribed single dose of Beroteka is diluted to 3-4 ml. Then the drug is sprayed and inhaled. It is diluted with 0.9% sodium chloride solution. Manipulation is performed before each inhalation.

Berotek for children

The decision to prescribe the drug to children is made exclusively by a specialist. Best in pediatric practice, the inhaled version of the drug for nebulizer therapy through a mask has proven itself.

The dosage is selected individually, taking into account the age, weight, constitution of the child and the severity of his condition. During a period of severe exacerbation, no more than 4 inhalations are allowed per day.

Dosage of Beroteka for children

For adolescents after 12 years of age, the drug is indicated for asthma attacks and all conditions that are accompanied by reversible obstruction. Inhalation starts with 10 drops.

Berotek during pregnancy and lactation

There is no evidence regarding the undesirable effect of Berotek on the fetus after the first trimester. But it is used with caution. During lactation, inhalation is prescribed when the benefits for the mother outweigh the risk.

Use only as directed by a physician!

Interaction of Beroteka with other medicinal products

Inhalation with antidepressants is not recommended. An increase in undesirable effects is possible with the appointment of hormones. It is forbidden to practice joint use with bronchodilators, since an overdose is possible, a strong additive effect.

Analogs

Berotek has not many analogues, there are many more substitutes. Analogs:

• Partusisten;
• Aerum;
• Fenoterol;
• Aruterol;
• Fenoterol hydrobromide
• Dosberotek;
• Segamol.

A good substitute is.

Only the attending physician can replace the drug or prescribe analogues!

Price

The price for Berotek depends on the form of release.

Price for Berotek in Russia - Moscow, St. Petersburg and other cities:

• Berotek solution for inhalation 0.1%, 20 ml - 340-380 rubles;
• Berotek aerosol 100 mcg / dose, 200 doses, 10 ml - 430-490 rubles;

Price for Atrovent in Ukraine:

• Berotek solution for inhalation 0.1%, 20 ml - 280-300 hryvnia;
• Berotek N aerosol 100 mcg / dose, 200 doses, 10 ml - 260-280 hryvnia;

Dosage form

Dosed aerosol for inhalation, 100 mcg / dose

Composition

1 inhalation dose contains

active substance - fenoterol hydrobromide 100 mcg,

excipients: citric acid anhydrous, ethanol absolute, purified water

propellant: 1,1,1,2 - tetrafluoroethane (HFA 134a),

Description

Transparent, colorless, slightly yellowish or slightly brownish liquid, with an ethanol odor, free of suspended particles.

Pharmacotherapeutic group

Drugs for the treatment of obstructive airway diseases. Inhalation sympathomimetics. Beta2-selective adrenostimulants. Fenoterol

ATX code R03AC04

Pharmacological properties

Pharmacokinetics

The therapeutic effect of BEROTEC N is due to its local effect in the respiratory tract. As a consequence, the concentration of the drug in the blood plasma is not necessarily associated with bronchodilator action.

Suction.After inhalation, about 10-30% of the active substance reaches the lower respiratory tract, the rest of the sprayed drug settles in the upper respiratory tract, in the oral cavity and is subsequently swallowed.

The absolute bioavailability of fenoterol after inhalation of the drug is 18.7%. It was found that the rate of absorption is 13% of the dose after inhalation. Further absorption becomes biphasic, in which 30% of a single dose of fenoterol hydrobromide is rapidly absorbed with a half-life of 11 minutes, the remaining 70% is absorbed slowly and the half-life is 120 minutes.

With oral administration of the drug, about 60% of fenoterol is absorbed. The absorbed amount of the drug undergoes intensive metabolism during the first phase of absorption of the drug, which is reflected in the oral bioavailability of about 1.5%. Therefore, the part of the active active substance of the drug received by ingestion has practically no effect on the concentration of the active substance in the plasma after inhalation. Maximum plasma concentrations are reached after about 60 to 120 minutes.

Distribution... The distribution of fenoterol in the body is uniform. The connection with plasma proteins is 40-55%.

Biotransformation... The ingested part of the drug is mostly metabolized to form sulfate conjugates, mainly in the intestinal walls.

Withdrawal... After passing through all the stages of exchange and providing a therapeutic effect, the active component is excreted through several paths. Excretion with bile is about 85% of the total average clearance, 15% of the total average clearance is the elimination of fenoterol (0.27 L / min) through the mechanisms of tubular and glomerular filtration. The drug is excreted unchanged through the kidneys within 24 hours.

In unchanged form, fenoterol can penetrate in small amounts through the blood-brain barrier and enter breast milk.

There are insufficient data on the effect of fenoterol hydrobromide on metabolic status in diabetes mellitus.

Pharmacodynamics

BEROTEC N is a bronchodilator used to relieve attacks of bronchial asthma and other conditions accompanied by reversible airway obstruction, such as chronic obstructive bronchitis, complicated or uncomplicated by emphysema.

After inhalation of fenoterol hydrobromide, bronchodilation occurs within a few minutes, and the bronchodilatic effect lasts from 3 to 5 hours.

Fenoterol hydrobromide has a direct adrenomimetic effect, selectively stimulating beta2-adrenergic receptors of the bronchi in therapeutic doses. At higher doses, it has the ability to stimulate beta1-adrenergic receptors.

Fenoterol hydrobromide causes relaxation of the smooth muscles of the bronchi and blood vessels. The effect of relaxing smooth muscles is dose-dependent, and is due to the effect on the adenylate cyclase system due to the binding of beta-agonists to their receptors, via guanosine-binding protein, leading to the activation of adenylate cyclase. By phosphorylation of a protein (protein kinase A), the intracellular level of cAMP increases, which causes relaxation of smooth muscles. In high doses, fenoterol also acts on striated muscles (tremors). In addition, fenoterol blocks the release of inflammatory mediators from mast cells. After taking fenoterol (0.6 mg), an increase in mucociliary clearance was revealed.

Fenoterol has a positive inotropic and chronotropic (direct and / or reflex) effect on the heart. The effects on lipid and carbohydrate metabolism (lipolysis, glycogenolysis and hyperglycemia) and relative hypokalemia due to increased K + uptake in skeletal muscle are pharmacological effects that occur only at higher doses. As with other beta-adrenergic agents, prolongation of the QT interval has been reported. For fenoterol in a metered-dose inhaler, the above events were discrete and were observed at doses higher than recommended. Clinical significance has not been established.

Due to the high density of beta2 receptors in the myometrium, fenoterol can also relax the muscles of the uterus. This effect is especially noticeable during pregnancy. The dose to achieve the tocolytic effect of fenoterol is significantly higher than that required to relieve bronchospasm. Hence, there is a high risk of unwanted effects.

Indications for use

Symptomatic treatment of acute asthma attacks

Prevention of exercise-induced bronchial asthma attacks

Symptomatic treatment of bronchial asthma of allergic or non-allergic origin and / or other pathological conditions associated with reversible airway obstruction, such as chronic obstructive bronchitis, complicated or uncomplicated by emphysema

Note

If long-term treatment is required, concomitant anti-inflammatory therapy should be considered.

Method of administration and dosage

Doses

The dose depends on the nature and severity of the disease.

Unless otherwise noted, the following doses are recommended for adults and children over 6 years of age:

For relief of sudden bronchial spasm and dyspnea attacks, one inhalation dose of fenoterol hydrobromide 100 mcg is required. As a rule, in an acute attack of shortness of breath, one inhalation is sufficient to quickly facilitate breathing. If after 5 minutes after the first inhalation there is no noticeable improvement in breathing, you can repeat the inhalation. Severe asthma and second dose failure may mean additional doses are needed. Such patients should seek immediate medical attention.

If long-term treatment with beta2-sympathomimetics is required, the dose should be 1 - 2 inhalation doses of BEROTEC N 3 - 4 times a day. The time and dose of each application of BEROTEC N should be selected depending on the frequency and severity of shortness of breath (symptomatically). It is also necessary to carry out long-term anti-inflammatory therapy, especially in the case of bronchial asthma. The interval between inhalations should be at least 3 hours. The total daily dose should not exceed 8 inhalations per day, and the maximum single dose should not exceed 4 inhalations, since a higher dose, as a rule, has no additional therapeutic effect, but may increase the likelihood of side effects, including the development of serious side effects ...

For specific prophylaxis of bronchial asthma attacks of physical exertion or in case of predicted contact with an allergen, 1 - 2 inhalation doses of BEROTEC N should be administered, if possible, 10 - 15 minutes before the expected physical activity / contact with the allergen.

Unless otherwise noted, the following doses are recommended for children aged 4-6 years:

To relieve a sudden bronchial spasm and asthma attacks, it is necessary to administer a single dose of fenoterol hydrobromide 100 μg (1 inhalation)

If long-term treatment is required, inhalation of 100 μg of fenoterol hydrobromide (1 inhalation) 4 times a day is necessary. The time and dose of each application of BEROTEC N should be selected depending on the frequency and severity of shortness of breath (symptomatically). It is also necessary to carry out long-term anti-inflammatory therapy, especially in the case of bronchial asthma. The interval between inhalations should be at least 3 hours. The total daily dose should not exceed 4 inhalations, and the maximum single dose should not exceed 2 inhalation doses, since a higher dose, as a rule, has no additional therapeutic effect, but may increase the likelihood of side effects, including the development of serious side effects.

For specific prophylaxis of bronchial asthma attacks of physical exertion or in case of predicted contact with an allergen, inhalation of 100 μg of fenoterol hydrobromide (1 press) is required, if possible, 10-15 minutes before the expected physical activity / contact with the allergen.

The drug is not suitable for use in children under 4 years of age.

Special instructions for treatment

Treatment of bronchial asthma should be phased, taking into account the severity of the condition. The response to therapy should be monitored with regular medical evaluation.

Taking high doses of beta2-sympathomimetics such as BEROTEC N without specialist advice can be life-threatening.

In order to assess the course of the disease and the adequacy of bronchodilator and anti-inflammatory treatment, it is important that the patient independently performs a daily check-up in accordance with the doctor's instructions. This check is done, for example, by recording the forced expiratory volume, which is measured with a pneumotachometer.

Mode of application

Inhalation is carried out in accordance with the instructions for use!

Correct use of the inhalation device is essential for successful therapy. During inhalation, the arrow on the balloon must always point straight up and the tip down, regardless of the position in which the inhalation is carried out. It is preferred that the patient administers the drug while sitting or standing.

Before using the metered aerosol for the first time, press twice on the bottom of the can.

Each time you use a metered aerosol, the following rules must be observed:

1. Remove the protective cap

2. Take a deep breath.

3. While holding the can, grasp the tip tightly with your lips. The arrow on the cylinder must point up and the tip down.

4. Making the deepest possible inhalation, simultaneously quickly press the bottom of the balloon until one inhalation dose is released. Hold your breath for a few seconds, then remove the tip from your mouth and exhale slowly.

If you are unable to take a deep breath due to severe shortness of breath, first inject one inhalation dose into your mouth; this will make breathing easier and allow you to use the device correctly.

If repeated inhalation is required, repeat steps 2 - 4

5. Put on the protective cap after use.

To prepare ("open the lungs") and support aerosol therapy with corticosteroids, saline and disodium cromoglycate (DNAG), inhalation of BEROTEC N should be done first.

The duration of treatment depends on the nature, severity and progression of the disease; The attending physician must determine the duration of therapy on a case-by-case basis.

If the aerosol can has not been used for more than 3 days, press the bottom of the can once before use.

The inhaler tip should be cleaned at least once a week.

The tip should be kept clean to avoid drug buildup and blockage of spray.

To clean, remove the protective cap and remove the tip can.

Rinse handpiece thoroughly with clean warm water to remove accumulated drug and / or contamination.

After cleaning, shake the inhaler and leave to dry at room temperature without heating. After the tip is dry, put the solution bottle back in and put on the protective cap.

The tip is specially designed for use with metered-dose aerosol BEROTEC N. This tip cannot be used with other metered-dose inhalers. BEROTEC N should only be used with the supplied tip.

The cylinder is under pressure and must not be opened!

Side effects

Side effects are identified with the following frequency: very often: ≥ 1/10; often: ≥ 1/100< 1/10; нечасто: ≥ 1/1,000 < 1/100; редко: ≥ 1/10,000 < 1/1,000; очень редко: < 1/10,000; неизвестно: невозможно оценить на основании доступных данных.

From the immune system:

Not known: hypersensitivity (eg, pruritus, exanthema, purpura, thrombocytopenia, facial edema)

Metabolic and nutritional disorders

Uncommon: hypokalemia

Rare: hyperglycemia

Hypokalemia may occur more often in patients with severe bronchial asthma who are prescribed combination therapy with xanthine derivatives (eg, theophylline), corticosteroids and / or diuretics. In addition, hypoxia can enhance the arrhythmogenic effect of hypokalemia. In such cases, it is recommended to monitor serum potassium levels. There is an increase in blood levels of insulin, free fatty acids, glycerol and ketone bodies.

Mental disorders:

Uncommon: mental changes, agitation

Unknown: nervousness

Mental changes are manifested by increased excitability, hyperactive behavior, sleep disorders and hallucinations. They are mainly seen in children under 12 years of age.

Nervous system disorders:

Often: tremors, dizziness

Unknown: headache

Cardiovascular disorders:

Uncommon: arrhythmia, angina pectoris, ventricular premature beats

Unknown: tachycardia, palpitations, myocardial ischemia

Respiratory system disorders:

Often: cough

Uncommon: paradoxical bronchospasm

Unknown: local irritation

In the case of paradoxical bronchospasm, therapy should be discontinued immediately.

Gastrointestinal disorders:

Often: nausea

Uncommon: vomiting, heartburn

Skin disorders:

Often: sweating

Uncommon: itching

Not known: urticaria, skin reactions such as rash

Musculoskeletal and connective tissue disorders:

Uncommon: muscle cramps

Not known: muscle weakness, myalgia

Kidney and urinary tract disorders:

Uncommon: urination disorder

Other violations

Uncommon: increase or decrease in blood pressure

Contraindications

Hypersensitivity to fenoterol hydrobromide or any other components of the drug

Hypertrophic obstructive cardiomyopathy, tachyarrhythmia

Drug interactions

The combined use of the drug with other beta2-adrenergic agonists, methylxanthines (for example, theophylline), anticholinergics and corticosteroids may lead to an increase in the effect of the drug BEROTEC N. (for example, drugs containing pirenzepine), may increase side effects (for example, tachycardia, arrhythmias).

Hypokalemia caused by beta2-adrenergic agonists may be exacerbated by concomitant therapy with xanthine derivatives, corticosteroids and diuretics. This should be considered especially in patients with severe airway obstruction. In such cases, it is necessary to monitor the level of electrolytes. This is especially important with the simultaneous use of diuretics and digitalis glycosides.

The simultaneous use of BEROTEC N and beta-blockers can cause mutual weakening of the action with the risk of developing severe bronchospasm in patients with bronchial asthma.

In addition, treatment with BEROTEC N can reduce the hypoglycemic effect of antidiabetic drugs. However, as a rule, this effect occurs when using high doses, usually used for systemic administration (for example, tablets or injection / infusion).

The combined use of BEROTEC N and monoamine oxidase inhibitors or tricyclic antidepressants can enhance the effect of fenoterol on the cardiovascular system.

With the use of halogenated anesthetics such as halothane, methoxyflurane or enflurane, there is an increased risk of serious cardiac arrhythmias and lowering blood pressure in patients treated with BEROTEC N.

Note:

If the use of halogenated anesthetics is necessary, it should be borne in mind that fenoterol should be discontinued at least 6 hours before the onset of anesthesia.

special instructions

BEROTEC N should be used with caution and only after a careful assessment of the risk-benefit ratio in case of: severe diseases of the cardiovascular system, especially after a recent heart attack and with ischemic heart disease; patients taking cardiac glycosides; severe and untreated hypertension; aneurysms; hyperthyroidism; poorly controlled diabetes; pheochromocytomas.

Paradoxical bronchospasm

Like other inhaled drugs, BEROTEC can lead to the development of a life-threatening condition: paradoxical bronchospasm. If paradoxical bronchospasm develops, BEROTEC N should be discontinued immediately and replaced with alternative treatment.

Effects on the cardiovascular system

The use of sympathomimetics, including BEROTEC N, may have effects on the cardiovascular system. In the published literature and data from post-registration experience of use, rare cases of myocardial ischemia associated with the intake of beta-adrenergic agonists are described. Patients with severe underlying cardiovascular disease (for example, ischemic heart disease, arrhythmias or severe heart failure) taking BEROTEC N should be informed about immediate medical attention if they develop chest pain or other symptoms of worsening heart disease. Particular attention should be paid to the assessment of symptoms such as shortness of breath and chest pain, as they can be from the respiratory and cardiovascular systems.

Hypokalemia

Potentially severe hypokalemia may result from beta2-agonist therapy. Particular care should be taken in severe asthma, since this effect can be enhanced by concomitant treatment with xanthine derivatives, glucocorticosteroids and diuretics. In addition, hypoxia can increase the effect of hypokalemia on heart rate.

Hypokalemia may lead to an increased susceptibility to arrhythmias in patients receiving digoxin.

Acute progressive dyspnea

In the event of acute, rapidly progressive dyspnea, patients should be advised to seek immediate medical advice.

Special warnings for regular use

An increased need for beta2-sympathomimetics such as BEROTEC N is a sign of worsening condition. In such a situation, the doctor should revise the patient's treatment plan and consider the option of starting or intensifying anti-inflammatory therapy, or prescribing additional drugs.

In the absence of satisfactory positive dynamics or even if it worsens, despite the prescribed treatment, it is necessary to seek medical help to reconsider the treatment. It may be advisable to combine it with other drugs (anti-inflammatory drugs such as corticosteroids or bronchodilators such as theophylline) or change the dose. Taking the drug in an amount significantly in excess of the prescribed dose can be dangerous.

It was repeatedly reported that the risk of developing severe complications of the underlying disease and even death was increased if bronchial asthma was treated for a long period with inhalation of beta2-sympathomimetics in high or excessive doses, and anti-inflammatory treatment was not effective enough. The reasons for the development of complications of the underlying disease still require further study.

Simultaneous use with sympathomimetic or anticholinergic bronchodilators

Other sympathomimetic bronchodilators should be used together with BEROTEC N only under medical supervision. Anticholinergic bronchodilators can be used in conjunction with BEROTEC N.

Children should only use this medication under adult supervision and as directed by a physician.

When taking high doses of the drug in patients with diabetes mellitus, the level of glucose in the blood may increase and in this regard, it is necessary to carefully monitor the level of glucose in the blood.

Since there are no data on the pharmacokinetics of fenoterol in the case of hepatic or renal failure, the advisability of taking the drug in such patients should be very carefully weighed.

This medicinal product contains 99% ethanol (alcohol, less than 100 mg per dose).

Laboratory research

The use of BEROTEC N can cause a positive reaction to doping control.

Fertility, pregnancy and lactation

Fenoterol crosses the placental barrier. Despite the fact that animal studies have not revealed a negative effect on the embryo, inhalation use of fenoterol during pregnancy, especially during the first three months, is possible only after a careful assessment of the risk-benefit ratio.

It is unlikely that the active substance will have a tocolytic effect after inhalation, although this effect cannot be completely ruled out.

The safety of using the drug during lactation has not been established. Fenoterol hydrobromide can pass into breast milk; therefore, caution should be exercised when prescribing BEROTEC N to women during breastfeeding.

Studies on the effect of fenoterol hydrobromide on human fertility have not been conducted. Preclinical studies of fenoterol hydrobromide did not reveal any adverse effects on reproductive performance.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

Studies on the effect of the drug on the ability to drive vehicles and control mechanisms have not been conducted.

However, it is necessary to inform patients about possible side effects such as dizziness while taking BEROTEC N and recommend caution when driving or operating machinery.

Overdose

Symptoms: depending on the degree of overdose, the following side effects typical for beta2-adrenergic agonists are possible: facial flushing, light-headedness, headache, tachycardia, palpitations, arrhythmia, arterial hypotension up to shock, increased blood pressure, anxiety, chest pain, agitation , extrasystoles and severe tremors are possible, especially in the fingers, but also throughout the body, hyperglycemia, gastrointestinal disturbances, including nausea and vomiting, especially with oral overdose, an increase in the level of potassium in the extracellular space, leading to hypokalemia. Hyperglycemia, hyperlipidemia and hyperketonemia, metabolic acidosis may develop.

Treatment: symptomatic. Treatment with BEROTEC N should be discontinued. Consideration should be given to monitoring acid-base balance and electrolytes. The action of fenoterol can be reduced by beta-blockers. However, one should bear in mind the possibility of the risk of developing severe bronchospasm in patients with bronchial asthma, which requires careful selection of the dose of the drug. This also applies to cardioselective beta-blockers.

Release form and packaging

10 ml of the drug are placed in stainless steel cylinders with a dosing device, an inhaler for oral use and a safety cap.

1 bottle, together with an inhaler and instructions for medical use in the state and Russian languages, are placed in a cardboard box.

Registration number: P N011310 / 01-111212
Trade name: Berotek® N
International non-proprietary name: fenoterol
Dosage form: metered dose inhalation aerosol

Composition:
1 inhalation dose contains:
fenoterol hydrobromide 100 μg (0.100 mg)
Excipients:
citric acid anhydrous 0.001 mg,
purified water 1,040 mg,
ethanol absolute 15.597 mg,
tetrafluoroethane (HFA 134a, propellant (tetrafluoroethane)) 35.252 mg

Description:
A clear, colorless or light yellow or light brownish liquid, free from suspended particles, placed under pressure in a metal aerosol can with a dosing valve and a mouthpiece.

Pharmacotherapeutic group: bronchodilator-β2-selective adrenergic agonist
ATX: R03AC04

Pharmacological properties

BEROTEC® N is an effective bronchodilator for the prevention and relief of bronchospasm attacks in bronchial asthma and other conditions accompanied by reversible airway obstruction, such as chronic obstructive bronchitis with or without pulmonary emphysema.
Fenoterol is a selective β2-adrenergic receptor stimulant. When using the drug in higher doses, β1-adrenergic receptors are stimulated (for example, when prescribed for tocolytic therapy). The binding of β2-adrenergic receptors activates adenylate cyclase through the stimulatory Gs-protein with a subsequent increase in the formation of cyclic adenosine monophosphate (cAMP), which activates protein kinase A, the latter deprives myosin of the ability to bind with actin, which prevents smooth muscle contraction and promotes bronchodilator action and elimination.
In addition, fenoterol inhibits the release of inflammatory mediators from mast cells, thereby providing a protective effect against the effects of bronchoconstrictors such as histamine, methacholine, cold air and allergens. Taking fenoterol in doses of 0.6 mg increases the activity of the ciliated epithelium of the bronchi and accelerates mucociliary transport.
Due to the stimulating effect on β-adrenergic receptors, fenoterol can have an effect on the myocardium (especially at doses exceeding therapeutic ones), causing an increase in heart rate and intensification.
Fenoterol prevents and quickly relieves bronchospasm of various origins. The onset of action after inhalation is 5 minutes, maximum - 30-90 minutes, duration - 3-5 hours.

10-30% of the active substance released from the aerosol preparation after inhalation reaches the lower respiratory tract, depending on the inhalation method and the inhalation system used, and the rest is deposited in the upper respiratory tract and is swallowed. This proportion of the active substance undergoes biotransformation due to the effect of "primary" passage through the liver. Metabolized in the liver. It is excreted by the kidneys and with bile in the form of inactive sulfate conjugates. Thus, the swallowed amount of the drug has no effect on the concentration of the active substance in the blood plasma achieved after inhalation.
Fenoterol in humans undergoes intensive metabolism by conjugation to glucuronides and sulfates. When swallowed, fenoterol is metabolized mainly by sulfation. This metabolic inactivation of the parent substance begins already in the intestinal wall.
Biotransformation, including excretion with bile, undergoes the main part - approximately 85%. Excretion of fenoterol in the urine (0.27 L / min) corresponds to approximately 15% of the average total clearance of the systemically available dose. The volume of renal clearance is indicative of tubular secretion of fenoterol in addition to glomerular filtration.
After inhalation, 2% of the dose is excreted unchanged from the metered aerosol through the kidneys within 24 hours.
Fenoterol can pass unchanged through the placental barrier and pass into breast milk.

Indications for use

Bronchial asthma attacks or other conditions with reversible airway obstruction, chronic bronchitis, chronic obstructive pulmonary disease.
- Prevention of attacks of bronchial asthma due to physical exertion.

Contraindications

Hypersensitivity to fenoterol or other ingredients of the drug.
Hypertrophic obstructive cardiomyopathy, tachyarrhythmia.
Berotek N in dosage form, metered dose inhalation aerosol is not used in children under 4 years of age.

Carefully: hyperthyroidism, arterial hypotension, arterial hypertension, intestinal atony, hypokalemia, diabetes mellitus, recent myocardial infarction (within the last 3 months), heart and vascular diseases such as
chronic heart failure, ischemic heart disease, coronary artery disease, heart defects (including aortic stenosis), severe cerebral and peripheral arterial lesions, pheochromocytoma. Since information on the use of the drug in children under 6 years of age is limited, treatment is carried out with caution, only under the supervision of a doctor.

Pregnancy and lactation

The results of preclinical studies in combination with the existing experience of the clinical use of the drug did not reveal any adverse events during pregnancy. However, the drug should be used with caution during pregnancy, especially in the first trimester, if the potential benefit to the mother outweighs the potential risk to the fetus.
Consideration should be given to the possibility of an inhibitory effect of fenoterol on the contractile activity of the uterus.
Preclinical studies have shown that fenoterol passes into breast milk. The safety of the drug during lactation has not been studied. During lactation, the use of the drug is possible if the potential benefit to the mother exceeds
potential risk to the child.

Method of administration and dosage

Bronchial asthma attacks and other conditions accompanied by reversible airway obstruction
In most cases, a single inhalation dose is sufficient to copy bronchospasm; if there is no relief of breathing within 5 minutes, inhalation can be repeated.
If the effect is absent after two inhalations, and additional inhalations are required, you should immediately seek medical help at the nearest hospital.
Prevention of exercise asthma
1-2 inhalation doses before exercise, up to 8 inhalations per day.

Due to limited experience in children under 6 years of age, the drug should only be used as directed by a physician and under adult supervision.
Bronchial asthma attacks and other conditions accompanied by reversible airway obstruction
One inhalation dose is sufficient to copy bronchospasm.
If there is no effect, you should immediately seek medical attention at the nearest hospital.
Prevention of exercise asthma
1 inhalation dose before exercise, up to 4 inhalations per day.

To achieve the maximum effect, it is necessary to use the metered aerosol correctly.

Before using the metered aerosol for the first time, double-click on the bottom of the can.
Each time you use a metered aerosol, the following rules must be observed:
1. Remove the protective cap.
2. Make a slow full exhalation.
3. While holding the can as shown in Fig. 1, tightly wrap your lips around the tip. In this case, the arrow and the bottom of the inhaler are facing up.

Fig. 1
4. Making the deepest possible inhalation, simultaneously quickly press the bottom of the can until the inhalation dose is released. Hold your breath for a few seconds, then remove the mouthpiece from your mouth and exhale slowly.
If repeated inhalation is required, repeat the same steps (points 2-4).
5. Put on the protective cap.
6. If the aerosol can has not been used for more than three days, press the bottom of the can once before use.
The balloon is designed for 200 inhalations. After that, the cylinder should be replaced. Although some drug may remain in the balloon, the amount of drug released by inhalation may be reduced. The balloon is opaque, so the amount of the drug in the balloon can only be determined in the following way: after removing the protective cap, the balloon is immersed in a container filled with water. The amount of the drug is determined depending on the position of the balloon in the water (see Fig. 2).

fig 2.
The inhaler should be flushed at least once a week.
It is important to keep the mouthpiece of your inhaler clean to prevent medication from accumulating and blocking the spray.
To clean, first remove the dust cap and remove the container from the inhaler. Flush the inhaler with warm water to remove accumulated medication and / or visible dust.

(fig. 3)
After cleaning, shake the inhaler and let it air dry without using heating devices. When the mouthpiece is dry, replace the container and dust cap.

(fig. 4)
WARNING: the plastic mouthpiece for the mouth is specially designed for Berotek N and serves for accurate dosing of the drug. The mouthpiece should not be used with other metered aerosols. Also, you can not use Berotec N with any other adapters, except for the mouthpiece supplied with the drug.
The contents of the cylinder are under pressure. The cylinder must not be opened and heated above 50 ° C.

Side effects

Hypersensitivity

Hypokalemia

Excitement, nervousness
tremor, headache, dizziness

Myocardial ischemia, arrhythmia, tachycardia, palpitations, increased systolic blood pressure, decreased diastolic blood pressure

Paradoxical bronchospasm, cough, irritation of the larynx and pharynx

Nausea, vomiting

Hyperhidrosis, skin reactions such as rash, pruritus, urticaria
The musculoskeletal system and related tissue diseases.
muscle spasm, myalgia, muscle weakness

Overdose

Tachycardia, increased heart rate, tremor, decrease / increase in blood pressure, increase in pulse pressure, anginal pain, arrhythmias and facial flushing, metabolic acidosis

Sedatives, tranquilizers, in severe cases, intensive symptomatic therapy
As specific antidotes, β-blockers (preferably selective β1-blockers) can be prescribed; at the same time, the possibility of increasing bronchial obstruction should be taken into account and the doses of these drugs should be carefully selected in patients with bronchial asthma

Drug interactions

β-adrenergic drugs, anticholinergics, xanthine derivatives (such as theophylline), cromoglycic acid, glucocorticosteroids and diuretics can increase the action and side effects of fenoterol.
A significant decrease in bronchodilation with the simultaneous use of fenoterol and β-blockers.
Β-adrenergic receptor agonists should be used with caution in patients receiving monoamine oxidase inhibitors or tricyclic antidepressants that can enhance the action of β-adrenergic receptor agonists.
Inhalation of general anesthetic agents such as halothane, trichlorethylene, and enflurane increases the likelihood of cardiovascular effects of β-adrenergic agonists. Halothane contributes to the development of arrhythmias. The simultaneous appointment of bronchodilators with a similar mechanism of action leads to an additive effect and overdose phenomena.

special instructions

When using the metered-dose aerosol BEROTEC N for the first time, patients may notice that the new aerosol has a slightly different taste compared to the previous aerosol containing freon. Patients should be warned about this when switching from BEROTEC N, containing freon to BEROTEC N, which does not contain freon. efficacy and safety of the drug.
Other sympathomimetic bronchodilators can be used together with BEROTEC N inhalation aerosol dosed only under medical supervision.
Acute, rapidly worsening shortness of breath (shortness of breath) should see a doctor immediately.
Long-term use:
relief of attacks of bronchial asthma may be preferable to regular use of the drug (symptomatic treatment);
patients should be examined to identify the need for additional or more intensive anti-inflammatory treatment (for example, inhalation of glucocorticosteroids) in order to control inflammation of the airways and prevent prolonged exacerbations of bronchial asthma.
In the case of increased bronchial obstruction, it is considered unacceptable and may even be risky to increase the frequency of administration of β2-adrenergic receptor agonists contained in drugs such as BEROTEC N metered dose inhalation aerosol in excess of the recommended doses. In such a situation, the treatment plan should be revised and especially the adequacy of anti-inflammatory therapy. When treated with β2-adrenergic receptor agonists, severe hypokalemia may develop. Particular care should be taken in severe bronchial asthma, since this effect can be enhanced by the concomitant use of xanthine derivatives, glucocorticosteroids and diuretics. With hypoxia, the effect of hypokalemia on the heart rate may increase. In such situations, regular monitoring of serum potassium concentration is recommended.
In rare cases, myocardial ischemia associated with β2-adrenergic receptor agonists was observed. Hypokalemia in patients receiving digoxin increases sensitivity to cardiac glycosides and can cause arrhythmias.
The use of BEROTECA N can lead to positive drug abuse tests for non-medical reasons (due to the presence of fenoterol).
In athletes, the use of BEROTECA N, due to the presence of fenoterol in its composition, can lead to positive results of doping tests.

Effects on ability to drive vehicles and use machinery

Studies of the effects of the drug on the ability to drive vehicles and use mechanisms have not been conducted.
However, patients should be advised that they may feel dizzy during treatment with BEROTEC N. Therefore, caution should be advised when driving or using machinery. If patients experience the above undesirable sensation, they should refrain from such potentially dangerous activities as driving a car or operating machinery.

Release form
Aerosol for inhalation dosed 0.1 mg / dose. 10 ml (200 doses) in a metal aerosol can with a dosing valve and a mouthpiece with a protective cap with the company logo. A can with instructions for use in a cardboard box.

Storage conditions
At a temperature not higher than 25 ° С
Keep out of the reach of children.

Shelf life
3 years.
Do not use the drug after the expiration date printed on the package.

Terms of dispensing from pharmacies
Dispensed by prescription

Marketing Authorization Holder
Boehringer Ingelheim International GmbH, Germany,

Manufacturer
Boehringer Ingelheim Pharma GmbH & Co.KG, Germany
Germany, 55216, Ingelheim am Rhein, Bingerstrasse 173

You can get additional information about the drug, as well as send your claims and information about adverse events to the following address in Russia
OOO Boehringer Ingelheim
125171, Moscow, Leningradskoe shosse, 16A, building 3
Tel / Fax: 8 800 700 99 93