Berotek H - instructions for use, doses, side effects, contraindications

Active substanceFenoterolFenoterol

Similar drugsTo uncover

Berotek®

solution d / inhal.

Boehringer Ingelheim International GmbH Germany

Berotek® H

aerosol d / inhal.

Boehringer Ingelheim International GmbH Germany

Fenoterol-aeronaut

aerosol d / inhal.

NATIVA, LLC Russia

Fenoterol-native

solution d / inhal.

NATIVA, LLC Russia

Dosage form: & nbspaerosol for inhalation dosed

Composition:

In 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 into an aerosol canister with a dosing valve and a mouthpiece.

Pharmacotherapeutic group:Bronchodilator - beta2-adrenomimetic selective

ATX: & nbsp

R.03.A.C.04 Fenoterol

Pharmacodynamics:

BEROTEK® N is an effective bronchodilator for preventing and arresting bronchospasm attacks in bronchial asthma and other conditions accompanied by reversible airway obstruction, such as chronic obstructive bronchitis with or without emphysema.

Fenoterol is a selective stimulant of β2adrenoreceptors. When using the drug at higher doses, stimulation of β1- adrenoreceptors (for example, when prescribed for tocolytic therapy). The binding of β2-adrenoceptor activates adenylate cyclase through a stimulant Gsprotein with subsequent increase in the formation of cyclic adenosine monophosphate (cAMP), which activates protein kinase A, the latter deprives myosin of the ability to bind to actin, which prevents the contraction of smooth muscles and promotes bronchodilator action and the elimination of bronchospasm.

Besides, fenoterol inhibits the release of mast cells from inflammatory mediators of inflammation, thereby exerting a protective effect on the influence of such bronchoconstrictors as histamine, methacholine, cold air and allergens. The intake of fenoterol in doses of 0.6 mg increases the activity of the ciliary epithelium of the bronchi and speeds up the mucociliary transport.

Due to the stimulating effect on β-adrenergic receptors, fenoterol can exert an effect on the myocardium (especially in doses exceeding the therapeutic ones), causing an increase and increase in cardiac contractions.

Fenoterol prevents and quickly reduces bronchospasm of various genesis. The onset of action after inhalation - after 5 minutes, a maximum of 30-90 minutes, duration - 3-5 hours.

Pharmacokinetics:

10-30% of the active substance released from the aerosol formulation after inhalation reaches the lower respiratory tract, depending on the inhalation method and the inhalation system used, and the remainder is deposited in the upper respiratory tract and swallowed. This fraction of the active substance undergoes biotransformation due to the effect of a "primary" passage through the liver. Metabolised 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 active substance in the blood plasma, achieved after inhalation.

Fenoterol in humans undergoes intensive metabolism by conjugation to glucuronides and sulfates. If swallowed fenoterol is metabolized, mainly, by sulphation. This metabolic inactivation of the starting material begins already in the wall of the intestine.

Biotransformation, including excretion with bile, is subjected to the bulk - about 85%. The excretion of fenoterol with urine (0.27 L / min) corresponds to approximately 15% of the average total clearance of the systemically available dose. The volume of renal clearance testifies to the tubular secretion of fenoterol in addition to glomerular filtration.

After inhalation, from the dosed aerosol in unchanged form, 2% of the dose is released through the kidneys within 24 hours.

Fenoterol can penetrate unchanged through the placental barrier and enter the breast milk.

Indications:

- Attacks of bronchial asthma or other conditions with reversible airway obstruction, chronic bronchitis, chronic obstructive pulmonary disease;

- prevention of asthma attacks due to physical stress.

Contraindications:

- Hypersensitivity to fenoterol or to other ingredients of the drug;

- hypertrophic obstructive cardiomyopathy;

- Tachyarrhythmia;

- BEROTEK® H in dosage form aerosol for inhalation dosed is not used in children up to 4 years old.

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 disease (including aortic stenosis) , pronounced lesions of cerebral and peripheral arteries, pheochromocytoma.

Since information on the use of the drug in children under the age of 6 is limited, treatment is carried out with caution, only under the supervision of a doctor.

Pregnancy and lactation:

The results of preclinical studies combined with the experience of clinical use of the drug showed no undesirable effects during pregnancy. Nevertheless, caution should be exercised in pregnancy, especially in the first trimester, if the potential benefit to the mother exceeds the potential risk to the fetus.

Consider the possibility of the inhibitory effect of fenoterol on contractile activity of the uterus.

Pre-clinical studies have shown that fenoterol penetrates into breast milk.The safety of the drug in the lactation period has not been studied. During lactation, the drug can be used if the potential benefit to the mother exceeds the potential risk for the child.

Dosing and Administration:

Doses for adults and adolescents over 12 years of age

Attacks of bronchial asthma and other conditions, accompanied by reversible airway obstruction

In most cases, one inhalation dose is sufficient to stop bronchospasm; if no breathing has occurred within 5 minutes, you can repeat the inhalation.

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 asthma physical effort

1-2 inhalation doses to exercise, up to 8 inhalations per day.

Doses for children from 6 to 12 years

Attacks of bronchial asthma and other conditions, accompanied by reversible airway obstruction

In most cases, one inhalation dose is sufficient to stop bronchospasm; if no breathing has occurred within 5 minutes, you can repeat the inhalation.

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 asthma physical effort

1-2 inhalation doses to exercise, up to 8 inhalations per day.

Doses for children from 4 to 6 years

Due to limited experience in children younger than 6 years of age, the drug should be used only as directed by a doctor and under the supervision of adults.

Attacks of bronchial asthma and other conditions, accompanied by reversible airway obstruction

To stop bronchospasm, one inhalation dose is sufficient.

If there is no effect, you should immediately seek medical help from the nearest hospital.

Prevention of asthma physical effort

1 inhalation dose to exercise, up to 4 inhalations per day.

Mode of application

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

Before using the metered aerosol for the first time, double-press the bottom of the can.

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

1. Remove the protective cap.

2. Make a slow, full exhalation.

3. Holding the can, as shown in Fig.1, tightly grasp the tip of the lips. Thus, the arrow and the bottom of the inhaler face upwards.

4. While drawing the deepest breath, simultaneously quickly press the bottom of the canister until the inhalation dose is released. Hold the breath for a few seconds, then take the mouthpiece out of the mouth and exhale slowly.

If repeated inhalation is required, repeat the same procedure (points 2-4).

5. Put the protective cap on.

6. If the aerosol can has not been used for more than three days, the bottle should be pressed once before use.

The cylinder is designed for 200 inhalations. After this, the cylinder should be replaced. Although a certain amount of the drug may remain in the bottle, the amount of drug released by inhalation can be reduced. The balloon is opaque, so the amount of the drug in the bottle can be determined only in the following way: by removing the protective cap, the balloon is immersed in a container, filled with water. The amount of the preparation is determined depending on the position of the cylinder in the water (see Fig. Fig. 2).

The inhaler should be washed at least once a week.

It is important to keep the mouthpiece of your inhaler clean so that the medicine does not accumulate and does not block the spraying.

For cleaning, first remove the dustproof cap and remove the container from the inhaler. Rinse the inhaler with warm water to remove any accumulated medication and / or visible dust. Fig. 3).

After cleaning, shake the inhaler and allow it to air dry without using heaters. When the mouthpiece is dry, return the container and dust cap to their place (see page 15). Fig. 4).

A WARNING: The plastic mouthpiece is designed specifically for Beroteka® H and serves to accurately dispense the drug. The mouthpiece should not be used with other metered aerosols. It is also not possible to use Berotek® H with any other adapters, except the mouthpiece supplied with the preparation.

The contents of the cylinder are under pressure. The cylinder should not be opened and subjected to heating above 50 ° C.

Side effects:

From the immune system: hypersensitivity.

From the side of metabolism and nutrition: hypokalemia.

Co hand nervous system: excitation, nervousness tremor, headache, dizziness.

From the side of the cardiovascular system: myocardial ischemia, arrhythmia, tachycardia, palpitations, increased systolic blood pressure, decreased diastolic blood pressure.

From the respiratory system: paradoxical bronchospasm, coughing, irritation of the larynx and pharynx.

From the digestive system: nausea, vomiting.

Skin and subcutaneous tissue: hyperhidrosis, skin reactions such as a rash, itching, urticaria.

The musculoskeletal system and associated tissue diseases: muscle spasm, myalgia, muscle weakness.

Overdose:

Symptoms

Tachycardia, increased heart rate, tremor, decreased / increased blood pressure, increased pulse pressure, anginal pain, arrhythmias and hyperemia of the face, metabolic acidosis

Treatment

Sedatives, tranquilizers, in severe cases, conduct intensive symptomatic therapy.

As specific antidotes, β-blockers (preferably selective β₁adrenoblockers); at the same time, the possibility of strengthening bronchial obstruction should be considered and the doses of these drugs should be carefully selected in patients with bronchial asthma.

Interaction:

β-Adrenergic drugs, anticholinergics, xanthine derivatives (such as theophylline), cromoglycic acid, glucocorticosteroids and diuretics can enhance the action and side effects of fenoterol.

A significant reduction in bronchodilation with simultaneous use of fenoterol and β-blockers.

Β-Adrenoreceptor agonists should be given with caution to patients receiving monoamine oxidase inhibitors or tricyclic antidepressants that are able to potentiate the action of β-adrenergic agonists.

Inhalation of funds for general anesthesia, such as halothane, trichlorethylene and enflurane, increases the likelihood of β-adrenoreceptor agonists acting on the cardiovascular system. Halothane promotes the development of arrhythmia.

Simultaneous administration of bronchodilators with a similar mechanism of action leads to an additive effect and overdose phenomena.

Special instructions:

At the first use of the metered aerosol of BEROTEC® H, patients can note 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 Berotek® H, containing freon to Beronek® H, which does not contain freon. Patients should be aware that Berotek® H, containing freon and Berotek® H preparation, does not contain freon completely interchangeable and taste changes do not affect the efficacy and safety of the drug.

Other sympathomimetic bronchodilators can be used together with the preparation of BEROTEK® N aerosol for inhalations dosed only under the supervision of a physician.

In acute, rapidly increasing dyspnea (shortness of breath), you should immediately consult a doctor.

Prolonged use:

- relief of attacks of bronchial asthma may be preferable to regular use of the drug (symptomatic treatment);

- Patients should be examined for the need to conduct additional or more intensive anti-inflammatory treatment (for example, glucocorticosteroid inhalations) 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 a risky increase in the rate of adherence of agonists β₂β-adrenoreceptors contained in such preparations as BEROTEK® N aerosol for inhalation dosed, in excess of the recommended doses. In such a situation, the treatment plan and, especially, the adequacy of anti-inflammatory therapy should be reviewed.

In the treatment with agonists β₂-adrenoceptors may develop pronounced hypokalemia.

Particular caution should be exercised in severe bronchial asthma, since this effect can be exacerbated by the concomitant use of xanthine derivatives, glucocorticosteroids and diuretics. With hypoxia, it is possible to increase the effect of hypokalemia on the heart rhythm. In such situations, regular monitoring of serum potassium concentration is recommended.

In rare cases, myocardial ischemia associated with agonists β₂adrenoreceptors. Hypokalemia in patients who receive digoxin, increases the sensitivity to cardiac glycosides and can cause arrhythmia.

The use of the drug BEROTEKA H can lead to positive results of tests for substance misuse due to non-medical indications (due to the presence of fenoterol).

In athletes, the use of BEROTEKA H in connection with the presence of fenoterol in its composition can lead to positive results of doping tests.

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

Studies of the effects of the drug on the ability to drive vehicles and the use of mechanisms were not carried out. However, patients need to be informed that they may experience dizziness during treatment with the drug BEROTEK® N. Therefore, care should be taken when driving vehicles or using mechanisms. If patients experience the above undesirable sensation, one should refrain from such potentially dangerous actions as driving a car or controlling machinery.

Form release / dosage:

Aerosol for inhalation dosed, 0.1 mg / dose.

Packaging:

For 10 ml (200 doses) in a spray canister with a metering valve and a mouthpiece with a protective cap with the company logo. Balloon with instructions for use in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C

Keep out of the reach of children.

Shelf life:

3 years.

Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011310 / 01

Date of registration:06.10.2009

The owner of the registration certificate:Boehringer Ingelheim International GmbHBoehringer Ingelheim International GmbH Germany

Manufacturer: & nbsp

BOEHRINGER INGELHEIM PHARMA, GmbH & Co.KG Germany