Berotec® N
Paradoxical bronchospasm
Like other inhaled drugs, BEROTEK N can cause paradoxical bronchospasm, which can be life-threatening. If paradoxical bronchospasm occurs, the drug should be immediately discontinued and replaced with alternative therapy.
Cardiovascular effects
Effects on the cardiovascular system can be observed with the use of sympathomimetic drugs, including the drug BEROTEK N. 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 (eg, coronary artery disease, arrhythmia, or severe heart failure) receiving BEROTEK N should be warned to seek medical attention if chest pain or worsening of heart disease occurs.
Care should be taken to evaluate symptoms such as shortness of breath and chest pain, as they may be either respiratory or cardiac in nature.
Hypokalemia
Potentially serious hypokalemia may occur due to beta 2-agonist therapy. Particular caution is recommended in severe bronchial asthma, since hypokalemia can be potentiated by concomitant therapy with xanthine derivatives, glucocorticosteroids and diuretics. In addition, hypoxia can enhance the effect of hypokalemia on heart rate. Hypokalemia may 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 the event of acute, rapidly worsening shortness of breath.
Regular use
— Relief of attacks of bronchial asthma (symptomatic treatment) is preferable to regular use of the drug;
— Patients should be assessed for the need for initiation or intensification of anti-inflammatory treatment (eg, inhaled corticosteroids) to control airway inflammation and prevent delayed lung injury.
In case of increased bronchial obstruction, it is unacceptable and may be risky to increase the dosage of β2-adrenergic agonists. such as the drug BEROTEK N, in excess of recommended doses and for a long time. The use of increased doses of beta 2-agonists, such as BEROTEK N, on a regular basis to control symptoms of bronchial obstruction may indicate deterioration of disease control. In such a situation, the treatment plan and especially the adequacy of anti-inflammatory therapy should be reconsidered to prevent potentially life-threatening deterioration of disease control. Concomitant use with sympathomimetic and anticholinergic bronchodilators
Other sympathomimetic bronchodilators should be used in conjunction with BEROTEK N only under medical supervision. Anticholinergic bronchodilators can be inhaled simultaneously with BEROTEK N. Effect on laboratory results
The use of BEROTEK N may result in positive test results for fenoterol in drug abuse studies for non-medical indications, such as performance enhancement in athletes (doping).
Please note that the drug contains a small amount of ethanol (15.597 mg per dose).
Instructions for use BEROTEK N (BEROTEC N)
Suction
Depending on the method of inhalation and the inhalation system used, about 10-30% of the active substance released from the aerosol preparation after inhalation reaches the lower respiratory tract, and the rest is deposited in the upper respiratory tract and in the mouth. As a result, some amount of inhaled fenoterol enters the gastrointestinal tract. The absolute bioavailability of fenoterol after inhalation of one dose of BEROTEKA® N is 18.%. Absorption from the lungs is two-phase:
- 30% of fenoterol hydrobromide is rapidly absorbed with a T1/2 of 11 minutes, and 70% is absorbed slowly with a T1/2 of 120 minutes.
Cmax of the drug in blood plasma (Cmax 45.3 pg/ml) was observed 15 minutes after a single inhalation of 100 mcg of fenoterol using a metered-dose inhaler with freon in patients with bronchial asthma. However, in studies involving healthy volunteers, in which blood tests were taken more frequently, it was found that serum Cmax of the drug was achieved earlier: 2 and 3.5 minutes after dosing. Cmax of the drug in serum after inhalation of a single dose of fenoterol 200 mcg using an HFA metered dose inhaler:
- Cmax 66.9 pg/ml, tmax15 minutes.
The therapeutic effect of BEROTEK N is achieved by its local action on the airways. Thus, Cmax in blood plasma is not necessarily related to the bronchodilator effect.
After oral administration, the degree of absorption is 60% of the administered dose of fenoterol hydrobromide. This amount undergoes extensive first-pass metabolism, resulting in a bioavailability of approximately 1.5%. Thus, the ingested portion of the active substance has only a minor effect on Cmax in blood plasma after inhalation.
Distribution
Fenoterol is distributed throughout the body. The volume of distribution at steady state after intravenous administration (Vss) is 1.9-2.7 l/kg. Vd of fenoterol in blood plasma after intravenous administration occurs according to a three-phase pharmacokinetic model. T1/2 are tα= 0.2 minutes, tβ= 14.3 minutes and tγ= 3.2 hours. Plasma protein binding ranges from 40 to 55%.
Metabolism
The biotransformation of fenoterol hydrobromide in humans occurs through conjugation with sulfates. Following oral administration, fentorerol is metabolized primarily through sulfation. This metabolic inactivation of the parent substance begins already in the intestinal walls.
Removal
Biotransformation, including biliary excretion, is due mainly (approximately 85%) to the average total clearance of 1.1-1.8 l/min. after intravenous administration. Renal excretion of fenoterol (0.27 L/min) corresponds to approximately 15% of the average total clearance of the systemically available dose. Considering the part of the drug that binds to plasma proteins, the renal clearance value indicates tubular secretion of fenoterol in addition to glomerular filtration.
After oral and IV administration, the total radioactivity excreted in urine is approximately 39% and 65% of the dose, and the total radioactivity excreted in feces is 40.2% and 14.8% of the dose over 48 hours, respectively. After oral administration, 0.38% of the dose is excreted unchanged into the urine, while with intravenous administration - 15%. After inhalation using a metered dose inhaler, 2% of the dose is excreted unchanged in the urine within 24 hours.
In unchanged form, fenoterol hydrobromide can cross the placental barrier and enter breast milk.
The metabolism of fenoterol hydrobromide in diabetes has not been sufficiently studied.
Buy Berotec solution for inhalation 1mg/1ml 20ml in pharmacies
Berotec Buy Berotec in pharmacies DOSAGE FORMS solution for inhalation 0.1% solution for inhalation 1 mg/ml
MANUFACTURERS Boehringer Ingelheim (Italy) Instituto de' Angeli S.r.L. (Italy)
GROUP Drugs that stimulate beta-adrenergic receptors
COMPOSITION Active ingredient: fenoterol.
INTERNATIONAL NON-PROPENTED NAME Fenoterol
SYNONYMS Berotek N, Fenoterol, Ftagirol
PHARMACOLOGICAL ACTION Bronchodilating, tocolytic. Excites beta2-adrenergic receptors, activates adenylate cyclase and causes the accumulation of cAMP. Relaxes the smooth muscles of the bronchi, stabilizes the membranes of mast cells and basophils (the release of biologically active substances is reduced), improves mucociliary clearance. Increases the frequency and strength of heart contractions. Has a tocolytic effect.
INDICATIONS FOR USE Bronchial asthma, asthmatic bronchitis, emphysema, pneumosclerosis, threat of premature birth.
CONTRAINDICATIONS Hypersensitivity, heart defects, arrhythmia, ischemic heart disease, decompensated diabetes mellitus, thyrotoxicosis, glaucoma, status asthmaticus, pregnancy (first trimester). Restrictions on use: Pregnancy (II and III trimester) and breastfeeding is possible if the expected effect of therapy exceeds the potential risk to the fetus or child, children's age (up to 6 years).
SIDE EFFECTS From the nervous system and sensory organs: hand tremors, dizziness, headache, nervousness, weakness. From the cardiovascular system and blood (hematopoiesis, hemostasis): tachycardia, palpitations; when using high doses - a decrease in dBP and an increase in sBP, arrhythmia. From the respiratory system: cough, paradoxical bronchospasm. From the gastrointestinal tract: nausea, vomiting. Other: sweating, myalgia and muscle spasms, hypokalemia, allergic reactions.
INTERACTION MAO inhibitors, tricyclic antidepressants, anticholinergics, xanthines (theophylline), corticosteroids, diuretics, other beta-agonists may enhance the effects, incl. side effects (especially with hypokalemia). Halogenated hydrocarbon anesthetics (halothane, trichlorethylene, enflurane) potentiate the effect on the cardiovascular system. Beta blockers significantly reduce activity.
METHOD OF APPLICATION AND DOSAGE Inhalation: adults, 0.2 mg 1-3 times a day, children 6-12 years old - 0.1 mg 1-3 times a day.
OVERDOSE Symptoms: tachycardia, palpitations, arterial hyper- or hypotension, increased pulse pressure, anginal pain, arrhythmia, flushing, tremor. Treatment: prescription of sedatives, tranquilizers, and in severe cases, intensive care. Cardioselective beta-blockers (atenolol, etc.) are recommended as antidotes.
SPECIAL INSTRUCTIONS No data available.
STORAGE CONDITIONS List B. At a temperature not exceeding 30 °C (do not freeze).
Berotec®
Treatment with BEROTEK® 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 Berotec® N metered 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 taken into account that 20 drops equal 1 ml, with 1 drop containing 50 mcg of fenoterol hydrobromide.
The recommended dose of BEROTEK® is diluted in the 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. BEROTEK® must not be diluted with distilled water. The solution is diluted each time immediately before use; the remainder of the prepared solution is poured out.
BEROTEK® solution can be inhaled simultaneously with anticholinergic and mucolytic drugs for which compatibility has been proven - Atrovent (ipratropium bromide) and Lazolvan (ambroxol) inhalation solutions.
Treatment with BEROTEK® should be initiated and carried out under the supervision of medical personnel, for example, in a clinic setting.
Treatment at home may be recommended to patients after consultation with a physician in cases where the use of a low-dose metered-dose aerosol of a fast-acting beta-agonist bronchodilator (such as Berotec® N) has not been sufficient to relieve the condition. It may also be recommended for patients who require nebulizer therapy for other reasons, such as problems with the use of metered-dose aerosols or the need for higher doses.
Treatment should usually begin with the minimum recommended doses. The dose should be individualized based on the patient's needs and adjusted based on the severity of the acute episode. The drug should be discontinued when sufficient relief of symptoms is achieved.
If necessary, the dose can be reapplied after at least 4 hours.
The dose may depend on the method of inhalation and the characteristics of the nebulizer used. The duration of inhalation can be controlled by the volume of drug dilution.
The following dosage regimens are recommended:
Adults (including patients over 75 years of age) and adolescents over 12 years of age:
a) Attacks of bronchial asthma and other conditions with reversible airway obstruction
Inhalation.
- 0.5 ml (10 drops = 500 mcg fenoterol hydrobromide) is in most cases sufficient for immediate relief of symptoms; if it is necessary to re-prescribe the drug up to 4 times a day, a reduction in individual doses should be considered 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 = 1000-1250 mcg of fenoterol hydrobromide);
- in extremely severe cases, under the supervision of a physician, doses of up to 2 ml (40 drops = 2000 mcg of fenoterol hydrobromide) can be administered;
b) Prevention of attacks of bronchial asthma due to physical stress
Inhalation.
0.5 ml (10 drops = 500 mcg fenoterol hydrobromide) before physical activity.
Children from 6 to 12 years old (with a body weight of 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 = 250-500 mcg fenoterol hydrobromide) is in most cases sufficient for immediate relief of symptoms;
- if it is necessary to re-prescribe the drug up to 4 times a day, a reduction in individual doses should be considered depending on the effectiveness of the nebulizer; in severe cases (for example, in most cases of treatment in a hospital setting) higher doses of up to 1 ml (20 drops = 1000 mcg fenoterol hydrobromide) may be required;
- in extremely severe cases, under the supervision of a physician, doses of up to 1.5 ml (30 drops = 1500 mcg of fenoterol hydrobromide) can be administered;
b) Prevention of attacks of bronchial asthma due to physical stress:
Inhalation.
0.5 ml (10 drops = 500 mcg fenoterol hydrobromide) before physical activity;
Children under 6 years of age (weight 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 physician, prescribing the drug in the following dose: inhalation of about 50 mcg of fenoterol hydrobromide per dose (= 0.05 ml or 1 drop) per 1 kg of body weight, but no more than 0.5 ml (10 drops) per dose up to 3 times a day.
Publications in the media
Pharmaceutical group - bronchodilator - selective beta2-adrenergic agonist.
Pharmaceutical action. A selective stimulator of beta2-adrenergic receptors, it activates adenylate cyclase with a subsequent increase in the formation of cAMP, which stimulates the Ca2+ pump, which redistributes Ca2+ ions in myocytes, resulting in a decrease in the concentration of the latter in myofibrils. It has a fairly pronounced, quickly-onset bronchodilator effect with an average duration of action. Prevents and quickly eliminates bronchospasm of various origins. Increases the activity of the ciliated epithelium of the bronchi. The onset of action after inhalation is 5 minutes, maximum 30-90 minutes, duration 3-6 hours.
Pharmacokinetics. Quickly absorbed. Intensively metabolized during the “first pass” through the liver. Metabolized in the liver and not destroyed by COMT. It is excreted by the kidneys and bile in the form of inactive sulfate conjugates. Does not cumulate, does not cross the placenta and does not accumulate in mother's milk.
Indications. Broncho-obstructive syndrome: bronchospasm during physical activity, croup, COPD (including bronchial asthma); silicosis, bronchiectasis, tuberculosis. As a bronchodilator before inhalation of other drugs (antibiotics, mucolytic drugs, corticosteroids). Carrying out bronchodilation tests to study the function of external respiration.
Contraindications. Hypersensitivity.
Carefully. IHD, uncontrolled arterial hypertension, mitral disease (insufficiency and/or stenosis), myocarditis, tachyarrhythmias, ventricular flutter, HOCM, myocardial infarction (acute stage), hypokalemia, thyrotoxicosis, WPW syndrome, glaucoma.
Dosing. Inhalation: to relieve an acute attack of suffocation for adults and children over 6 years old - 0.2 mg; for the prevention of asthma attacks - 0.2 mg, adults - 3 times a day, school-age children - 2 times a day, children 4-6 years old - 0.1 mg, 4 times a day. If 1 inhalation does not relieve an attack of suffocation, then after 5 minutes it can be repeated. The next appointment is possible no earlier than 3 hours later.
Side effect. From the nervous system: slight tremor, dizziness, headache, nervousness, anxiety. From the cardiovascular system: tachycardia, palpitations, angina pectoris, rarely (when using high doses) - decreased blood pressure, especially diastolic. From the respiratory system: cough, rarely - paradoxical bronchospasm, dryness or irritation in the mouth or throat. From the digestive system: nausea, vomiting. Other: changes in taste, motor restlessness, sleep disturbances, weakness, muscle spasms or twitching, hypokalemia, hyperglycemia, rarely - allergic reactions.
Overdose. Symptoms: tachycardia, palpitations, decreased or increased blood pressure, increased pulse pressure, anginal pain, blood flow to the face, tremor. Treatment: prescription of sedative or anxiolytic drugs (tranquilizers), in severe cases - symptomatic therapy. Cardioselective beta-blockers (atenolol, etc.) are recommended as antidotes.
Interaction. Xanthine derivatives (theophylline), cromoglycic acid, corticosteroids, beta-agonists, MAO inhibitors, tricyclic antidepressants, anticholinergics, diuretics may enhance the effects, incl. side effects (especially with hypokalemia). Halogen-containing hydrocarbon drugs for general anesthesia (halothane, trichlorethylene, enflurane) enhance the effect on the cardiovascular system. Beta blockers significantly reduce activity. The simultaneous administration of bronchodilators with a similar mechanism of action leads to an additive effect and overdose phenomena. Halothane sensitizes the myocardium to the action of fenoterol and promotes the development of arrhythmia.
Special instructions. Increasing the total daily dose of the drug by more than 12 breaths of the aerosol does not cause an additional therapeutic effect. In patients with diabetes mellitus, during treatment it is necessary to regularly monitor plasma glucose concentrations.
