Berotek

Berotek is a preparation that contains in its composition the substance fenoterol, which is the selective stimulator of β-2-adrenoreceptors, which are located mainly inside the respiratory ducts.

[1], [2]

Indications of the beroteka

It is used to eliminate the following diseases:

• obstructive pulmonary pathology of a chronic nature;
• spasms of the bronchi that accompany bronchial asthma;
• curable narrowing of the respiratory tract;
• obstructive form of chronic bronchitis;
• pulmonary emphysema;
• for the prevention of asthma as a result of physical exertion.

Release form

The release occurs in the form of an inhalation solution, which is contained in glass bottles-droppers with a capacity of 20 ml (with 1 ml equal to 20 drops). Inside the box there is one such bottle.

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

Pharmacodynamics

The active element of Berotek helps to relax the smooth muscles of the vessels with bronchial tubes, thereby preventing the development of bronchospastic manifestations that occur, for example, in bronchial asthma.

The narrowing of the bronchial lumen is due to the influence of histamine with methacholine, and in addition to this cold air and various allergens of exogenous nature (reacting to manifestations of immediate hypersensitivity).

Fenotreol, which enters the regional circulatory system, inhibits the release of active inflammatory conductors from mast cells (basophils 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 action of the active element is its interaction with the protein-GS, which stimulates the activity of cell adenylate cyclase. Reaction to this is the strengthening of cAMP binding processes, which is a secondary mediator. The mediator also stimulates the activity of protein kinase type A, which helps phosphorylation of the smooth muscle cells of target proteins located inside cells.

As a result, the inactivation of the light myosin chains (one of the main constituents of the muscle fibers) and the opening of rapid potassium channels result in the relaxation of the smooth muscles within the respiratory ducts and the vascular bed.

It should also be remembered that β-adrenoreceptors are also located inside the heart muscle, so the effect of the active element of the drug is also noted inside the myocardium and the corresponding channel of the vessels. In this case, the level of heart rate and their strength is significantly increased, as a result of which the main and microcirculatory blood circulation within the peripheral tissues is markedly enhanced.

Large portions of medicament have a wider range of activity. Among the effects it provides:

• potentiation of MZ function;
• suppression of contractile uterine 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 demonstrated that its therapeutic effect is almost independent of the level of its active elements inside the serum.

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

Suction from the pulmonary surface is carried out in 2 stages. During the first 11 minutes after inhalation, 30% of the applied dose is absorbed inside the body, and then, in the next 120 minutes, the residue in the form of 70% of the substance overcomes various physiological barriers passing into the soft tissue area.

Peak values of drugs inside the plasma are equal to 45.3 pg / ml. These values are noted already after 15 minutes after the inhalation procedure.

Fenoterol is distributed internally evenly, with a volume of 1.9-2.7 l / kg. This property can best be described using a three-stage pharmacokinetic scheme with half-lives of 0.42 and 14.3 minutes, and 3.2 hours. Inside the blood channel, 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 medicine has passed all the metabolic stages and performed the medicinal action, the active element is excreted in several ways. Its main part is excreted with bile through the lumen of the digestive tube, while developing a rate of about 1.1-1.8 ml / minute. About 15% of the total average clearance level is the elimination of the component by glomerular filtration (approximately 0.27 l / min). Along with this, since the preparation is synthesized with proteins, it is excreted by the way of tubular secretion.

Dosing and administration

Use of an inhalation solution.

The medicine is used topically, affecting the tissues inside the respiratory tract. Before starting to use it is necessary to dissolve the desired portion of medicinal product in saline (distilled water for use is strictly prohibited) until a volume of 3-4 ml is obtained.

Inhalation should be performed with a special otolaryngological device called a nebulizer. In addition, other oxygen-breathing devices may be used. The optimal rates of air flow, containing the therapeutic component, are 6-8 l / min. The sizes of portions correspond to the following volumes: 20 drops are 1 ml of the solution, and in the 1st drop contains approximately 50 μg of the substance fenoterol hydrobromide.

Dimensions of inhalation solution doses:

• for children under 6 years of age, weighing less than 22 kg, the portion is 0.05 ml (corresponds to the 1-st drop) / kg, using three times a day. Single dose of drugs should not be more than 0.5 ml (corresponds to 10 drops);
• for children in the age group of 6-12 years with a weight in the range of 22-36 kg, the portions are 0.25-0.5 ml of the drug, if necessary, urgently remove the signs of urgent bronchial constriction (four times a day is required). The size of the dose may increase if severe forms of bronchial asthma are noted;
• for adults (and the elderly from 75 years of age), and in addition, adolescents from 12 years of age, the dosage is 0.5 ml LS with reception up to 4 times / day. Sometimes it is possible to increase or decrease the dose, if there are appropriate medical data or individual doctor's testimony.

Application of aerosol Berotek N.

Before applying the spray, you need to shake the can, by pressing twice on the bottom to prepare it for the procedures. After this, it is necessary, following the scheme described below, to perform the injection of the drug.

First, it is necessary to exhale slowly and deeply, then grasp the nozzle of the can with the lips so that its axis is directed upwards to the bottom. Next, you need to press the bottom of the cylinder, while taking a deep breath. After this, it takes a short time to hold your breath, so that the drug mixture is absorbed most fully.

If there is a corresponding doctor's prescription, the procedure for obtaining the second dose should be repeated exactly.

The spray can is equipped with a special mouthpiece (the so-called mouthpiece needed to accurately calculate the dose of the inhaled substance). This part must not be used in combination with other aerosol cans. The container contains 200 sprays (inhalations).

[6], [7]

Use of the beroteka during pregnancy

Berotek is allowed to use only on the 2nd and 3rd trimesters of pregnancy.

When breastfeeding, it is advisable to prescribe the medicine only when the probable benefit from it will exceed the possibility of complications in the infant. This is due to the fact that the active substance of the drug can be released together with the mother's milk.

Contraindications

The main contraindications:

• the presence of intolerance in relation to individual elements of the drug;
• hypersensitivity to bioactive components of a drug (hereditary or acquired character);
• 1st trimester of pregnancy;
• Stenosis of the aortic estuary;
• hypertrophic cardiomyopathy of obstructive nature;
• hyperthyroidism;
• tachyarrhythmia;
• presence of various heart defects;
• diabetes mellitus at an uncompensated stage;
• glaucoma;
• children's age is less than 4 years.

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

• increased values of blood pressure that can not be controlled;
• nosological forms of severe type that affect CAS;
• pheochromocytoma;
• thyrotoxicosis;
• period after the transfer of myocardial infarction;
• diabetes mellitus at a compensated stage of development.

Side effects of the beroteka

During the course of conservative treatment with Berotek, the following side-effects may develop:

• disturbances in the work of the central nervous system: dizziness, shallow intentional tremor, accommodation disorder, headaches and changes in the psyche (the latter reaction is only observed singly);
• problems with the function of CAS: palpitations, intense tachycardia, a decrease in blood pressure, an increase in the level of systolic blood pressure, as well as arrhythmia;
• disorders affecting the respiratory tract: local irritation in the mucosa, cough, and in addition spasm bronchus paradoxical character (the last symptom is noted only once);
• lesions that develop in the gastrointestinal tract: the appearance of nausea, after which vomiting usually occurs;
• signs of allergies: urticaria, rash and edema of Quincke in the area of the lips with tongue, and also face;
• other disorders: hypokalemia, in which extremely high rates are observed (especially in people with severe bronchial asthma, taking on drugs based on diuretics, GCS, and besides xanthine), a feeling of weakness, a myalgia of unknown nature, and besides this, hyperhidrosis and delayed urination processes.

[3], [4], [5]

Overdose

With the development of intoxication, the appearance of such negative symptoms is usually noted:

• anginal pain;
• tachycardia and palpitations;
• angina pectoris or arrhythmia;
• increase or decrease in the values of blood pressure (depends on the individual predisposition of the patient);
• increase in pulse pressure;
• dermal hyperemia of an intense nature affecting the face and entire upper body;
• an intentional tremor.

The antideletant of Beroteka is usually β-adrenoblockers of cardioselective type, in particular β1-blockers (antagonistic effect). But the use of these drugs can increase bronchial obstruction, which is why it is necessary to carefully select the required portion of the antidote.

In addition, symptomatic interventions are performed in which tranquilizers and sedatives are prescribed. If there are medical indications, intensive care procedures are used (the most important indicators for life are monitored).

Interactions with other drugs

Substances that potentiate the general medicinal effect of Beroteka:

• beta-adrenoreceptor agonists;
• cholinolytic agents;
• tricyclics;
• substance MAOI.

Combinations with these medicines lead to the emergence of side-effects:

• β-adrenomimetics;
• cholinolytic preparations;
• derivatives of xanthine (among them theophylline).

Other interactions:

• substances that block the activity of β-adrenergic receptors, in the case of combination with the drug, can significantly reduce bronchodilation;
• halogenated hydrocarbon-type antiseptics (such as enflurane, halothane or trichlorethylene) potentiate the action of the active elements of Berotech in relation to the activity of the CCC.

[8], [9]

Storage conditions

Berotek should be kept in a place that is closed from the access of young children. The temperature should not exceed 30 ° C. Also the storage location of the drug should be dark. Keep aerosols away from sources of open flame. Do not freeze the pharmaceutical liquid.

[10], [11], [12]

Shelf life

Berotek is allowed to be used for 5 years from the date of release of the drug.

[13]

Reviews

Berotek receives many positive comments from visitors to the forums dedicated to the treatment of respiratory diseases. The majority of patients thus allocate aerosol form of release of LS, the solution is less popular. Usually in the reviews are noted such advantages of the drug as convenience in use, as well as the duration of its course use. It should also be remembered that such a can is small in size, which allows it to be carried everywhere, and therefore to avoid skipping it.

The opinions of doctors are mostly positive. Yes, it should be remembered that the drug has many side effects, but it is able to eliminate quite a few diseases affecting the respiratory tract.

The drug is used for monotherapy with 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 of the substance regarding its therapeutic interactions, as well as the size of the portions, so that the treatment does not cause any complications.