Berotec

Berotek is a drug that contains fenoterol, a selective stimulator of β-2-adrenergic receptors, which are located mainly inside the respiratory ducts.

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Indications Beroteka

It is used to eliminate the following diseases:

• chronic obstructive pulmonary pathology;
• bronchial spasms that accompany bronchial asthma;
• treatable narrowing of the airways;
• obstructive form of bronchitis of a chronic nature;
• pulmonary emphysema;
• to prevent the development of asthma as a result of physical activity.

Release form

The product is released as an inhalation solution, which is contained in glass dropper bottles with a capacity of 20 ml (1 ml is equal to 20 drops). There is 1 such bottle inside the box.

It can also be produced as an aerosol for metered inhalations, in canisters with a nozzle, with a volume of 10 ml (approximately 200 sprays). The package contains 1 canister with aerosol.

Pharmacodynamics

The active ingredient of Berotek promotes relaxation of the smooth muscles of the blood vessels with bronchi, thereby preventing the development of bronchospastic manifestations that occur, for example, with bronchial asthma.

Narrowing of the bronchial lumen is achieved due to the influence of histamine with methacholine, and in addition to this, cold air and various exogenous allergens (in response to manifestations of immediate hypersensitivity).

Once inside the regional circulatory system, fenotreol inhibits the process of releasing active inflammatory conductors from mastocytes (basophils that have penetrated into the tissues). It is this effect that determines the medicinal effect of the drug in the treatment of bronchial obstruction.

The biochemical basis of the active element's effect is its interaction with the GS protein, which stimulates the activity of cell adenylate cyclase. The reaction to this is an increase in the processes of binding cAMP, which is a secondary messenger. The messenger stimulates the activity of protein kinase type A, which helps phosphorylate target proteins located inside smooth muscle cells.

As a result, there is inactivation of light myosin chains (one of the main components of muscle fibers) and the opening of fast potassium channels, which results in relaxation of the smooth muscles inside the respiratory ducts, as well as the vascular bed.

It is also necessary to remember that β-adrenoreceptors are also located inside the heart muscle, therefore the effect of the active element of the drug is also noted inside the myocardium and the corresponding vascular bed. At the same time, the level of heart rate and its strength increases significantly, as a result of which the main and microcirculatory blood circulation inside the peripheral tissues is noticeably enhanced.

Large doses of the drug have a wider range of activity. Among the effects it produces are:

• potentiation of the MCC function;
• suppression of uterine contractile activity;
• disorder of glycogenolysis and lipolysis processes;
• decrease in plasma potassium values.

Pharmacokinetics

Berotek is intended for topical use because clinical tests of the drug have demonstrated that its therapeutic effect is almost independent of the level of its active elements within the serum.

After inhalation, approximately 10-30% of the main active component reaches the lower part of the respiratory tract. The remainder of the sprayed substance settles in the upper part of the respiratory system and in the mouth, or is swallowed, thus penetrating into the gastrointestinal tract. The bioavailability of the fenoterol component is approximately 18-19%.

Absorption from the lung surface occurs in 2 stages. During the first 11 minutes after inhalation, 30% of the applied dose is absorbed into the body, and then, over the next 120 minutes, the remainder in the form of 70% of the substance overcomes various physiological barriers, passing into the soft tissue area.

Peak plasma levels of the drug are 45.3 pg/ml. These values are noted after 15 minutes of inhalation.

Fenoterol is distributed evenly within the body, with a volume of 1.9-2.7 l/kg. This property can be best described using a three-stage pharmacokinetic scheme with half-lives of 0.42 and 14.3 minutes, as well as 3.2 hours. Within the bloodstream, the active elements are synthesized with proteins in the amount of 40-55% of the applied dosage.

The active element undergoes metabolic processes occurring inside the liver or intestinal walls by conjugation (or sulfonation), followed by the formation of glucuronides with sulfates.

After the drug has passed all the metabolic stages and performed its medicinal effect, the active element is excreted in several ways. Its main part is excreted with bile through the lumen of the digestive tube, developing a speed of approximately 1.1-1.8 ml/minute. About 15% of the total values of the average clearance level is the elimination of the component by glomerular filtration (approximately 0.27 l/minute). At the same time, since the drug is synthesized with proteins, it is also excreted by tubular secretion.

Dosing and administration

Use of inhalation solution.

The medicine is used locally, affecting the tissues inside the respiratory tract. Before use, it is necessary to dissolve the required portion of the drug in saline (it is strictly forbidden to use distilled water for dilution) until the volume is 3-4 ml.

Inhalation should be performed using a special otolaryngological device called a nebulizer. In addition, other oxygen-breathing devices can be used. Optimal air flow rates containing the medicinal component are 6-8 l/minute. Portion sizes correspond to the following volumes: 20 drops are 1 ml of solution, and 1 drop contains approximately 50 mcg of fenoterol hydrobromide.

Dose sizes of inhalation solution:

• for children under 6 years of age weighing less than 22 kg, the dose is 0.05 ml (equivalent to 1 drop)/kg, taken three times a day. The single volume of the medicine should not exceed 0.5 ml (equivalent to 10 drops);
• for children aged 6-12 years weighing 22-36 kg, the dose is 0.25-0.5 ml of the drug if it is necessary to urgently eliminate signs of urgent bronchial constriction (four doses per day are required). The dose may be increased if severe forms of bronchial asthma are observed;
• for adults (and the elderly from 75 years old), and also teenagers from 12 years old, the dosage size is 0.5 ml of the drug with intake up to 4 times a day. Sometimes it is possible to increase or decrease the portion if there are appropriate medical data or individual indications of the doctor.

Application of Berotek N aerosol.

Before using the spray, shake the can by pressing the bottom twice to prepare it for the procedure. After that, follow the procedure described below to inject the medicine.

First, you need to exhale slowly and deeply, then grasp the nozzle of the can with your lips so that its axis is directed upside down. Next, you need to press on the bottom of the can, while simultaneously inhaling deeply. After this, you need to hold your breath for a short time so that the medicinal mixture is absorbed as completely as possible.

If there is a corresponding prescription from a doctor, the procedure for obtaining a second dose must be exactly repeated.

The spray can is equipped with a special mouthpiece (the so-called mouthpiece, necessary to accurately calculate the dose of the inhaled substance). This part is prohibited to be used in combination with other aerosol cans. The container with the drug contains 200 sprays (inhalations).

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Use Beroteka during pregnancy

Berotek is allowed to be used only in the 2nd and 3rd trimesters of pregnancy.

When breastfeeding, it will be advisable to prescribe the drug only when the probable benefit from it exceeds the possibility of complications in the baby. This is due to the fact that the active substance of the drug can be excreted along with the mother's milk.

Contraindications

Main contraindications:

• the presence of intolerance to individual elements of the drug;
• hypersensitivity to the bioactive components of the drug (hereditary or acquired);
• 1st trimester of pregnancy;
• Aortic stenosis;
• hypertrophic cardiomyopathy of obstructive nature;
• hyperthyroidism;
• tachyarrhythmia;
• the presence of various heart defects;
• diabetes mellitus at an uncompensated stage;
• glaucoma;
• children under 4 years of age.

Conservative therapy using drugs should be carried out under constant supervision of doctors and with regular diagnostic tests for the following diseases:

• elevated blood pressure values that cannot be controlled;
• severe nosological forms that affect the cardiovascular system;
• pheochromocytoma;
• thyrotoxicosis;
• period after myocardial infarction;
• diabetes mellitus at the compensated stage of development.

Side effects Beroteka

During the conservative treatment course using Berotek, the following side effects may develop:

• disorders of the central nervous system: dizziness, fine intentional tremors, accommodation disorders, headaches and mental changes (the last reaction is observed only occasionally);
• problems with the cardiovascular system: palpitations, intense tachycardia, decreased blood pressure, increased systolic blood pressure, and arrhythmia;
• disorders affecting the respiratory tract: local irritation in the mucous membranes, cough, and also paradoxical bronchospasm (the latter symptom is observed only occasionally);
• lesions developing in the gastrointestinal tract: the appearance of nausea, usually followed by vomiting;
• signs of allergy: urticaria, rash and Quincke's edema in the area of the lips with tongue, as well as the face;
• other disorders: hypokalemia, in which extremely high values are observed (especially in people with severe bronchial asthma, taking diuretic-based drugs, GCS, and also xanthine for treatment), a feeling of weakness, myalgia of unknown origin, and also hyperhidrosis and delays in urination.

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Overdose

When intoxication develops, the following negative symptoms are usually observed:

• anginal pain;
• tachycardia and palpitations;
• angina attacks or arrhythmia;
• increase or decrease in blood pressure values (depending on the individual predisposition of the patient);
• increase in pulse pressure indicators;
• intense skin hyperemia affecting the face and the entire upper body;
• intentional tremor.

The antidote to Berotek is usually β-adrenoblockers of the cardioselective type, especially β1-blockers (antagonist effect). But the use of these drugs can increase bronchial obstruction, which is why it is necessary to very carefully select the required dose of the antidote.

In addition, symptomatic measures are taken, in which tranquilizers and sedatives are prescribed. If there are medical indications, intensive care procedures are used (the most vital indicators are monitored).

Interactions with other drugs

Substances that potentiate the general medicinal effect of Berotek:

• beta-adrenergic receptor agonist drugs;
• anticholinergic agents;
• tricyclics;
• MAOI substances.

Combinations with these medications lead to the occurrence of side effects:

• β-adrenergic agonists;
• anticholinergic drugs;
• xanthine derivatives (including theophylline).

Other interactions:

• substances that block the activity of β-adrenergic receptors, when combined with the drug, are capable of significantly reducing bronchodilation;
• Halogenated hydrocarbon antiseptics (such as enflurane, halothane or trichloroethylene) potentiate the effect of the active elements of Berotek on the activity of the cardiovascular system.

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Storage conditions

Berotek should be kept in a place that is out of the reach of small children. Temperature indicators should not exceed 30°C. Also, the storage place of the drug should be dark. Aerosols should be kept away from open fire. It is prohibited to freeze the pharmaceutical liquid.

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Shelf life

Berotek can be used for 5 years from the date of manufacture of the drug.

Reviews

Berotek receives many positive comments from visitors to forums dedicated to the treatment of respiratory diseases. Most patients highlight the aerosol form of the drug, while the solution is less popular. Usually, reviews note such advantages of the drug as ease of use, as well as the duration of its course use. It is also necessary to remember that such a can is small in size, which allows you to carry it with you everywhere, and therefore avoid missing its use.

Doctors' reviews are mostly positive. Yes, it should be remembered that the drug has many side effects, but at the same time it is able to eliminate quite a few diseases affecting the respiratory tract.

The drug is used for monotherapy in some nosological forms, and in addition, it is used in combination with other drugs and for preventive health improvement. But it is necessary to strictly follow the instructions for the substance regarding its therapeutic interactions, as well as portion sizes, so that the treatment does not cause any complications.