Berotek N aerosol 100 mcg dose 200 doses of 10 ml
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Active ingredients
Fenoterol
Release form
Spray
Composition
Active ingredient: Fenoterol. Concentration of active ingredient (mcg): 100 mcg
Pharmacological effect
Absorption: The therapeutic effect of BEROTEKA H is achieved by its local effect on the airways. 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 mouth. As a result, a certain amount of inhaled fenoterol enters the gastrointestinal tract. The absolute bioavailability of fenoterol after inhalation of a single dose of Berezoteka N is 18.7%. Absorption from the lungs is biphasic: 30% of fenoterol hydrobromide is rapidly absorbed with a half-life of 11 minutes, and 70% is absorbed slowly with a half-life of 120 minutes. After oral administration, the degree of absorption is 60% of the administered dose of fenoterol hydrobromide. This amount is actively exposed to the systemic metabolism, which leads to a bioavailability of about 1.5%. Thus, the swallowed part of the active substance has only a minor effect on plasma concentration after inhalation. Distribution: Fenoterol is distributed throughout the body. The volume of distribution in a stable state after intravenous administration (Vss) is 1.9-2.7 l / kg. Binding to plasma proteins ranges from 40 to 55%. Metabolism: Fenoterol is metabolized in the human body by sulfation and glucuronization. After oral administration, fenoterol is metabolized mainly by sulfation. This metabolic inactivation of the original substance begins in the intestinal walls. Biotransformation, including biliary excretion, is caused mainly (approximately 85%) by an average total clearance of 1.1-1.8 l / min. after intravenous administration. Excretion of fenoterol through the kidneys (0.27 L / min.) Corresponds to approximately 15% of the total clearance of the systemically available dose. Considering the part of the drug that binds to plasma proteins, the value of renal clearance indicates the tubular secretion of fenoterol in addition to glomerular filtration.After oral and intravenous administration, the total radioactivity released into the urine is approximately 39% and 65% of the dose, and the total radioactivity released into the feces is 40.2% and 14.8% of the dose within 48 hours, respectively. After oral administration, 0.38% of the dose is excreted into the urine unchanged, while intravenous administration is 15%. After inhalation using a metered-dose inhaler, 2% of the dose is excreted unchanged in the urine within 24 hours. Fenoterol can pass through the placental barrier unchanged and pass into breast milk. The fetus may develop sympathomimetic effects. After prolonged infusions, the concentration of fenoterol in the blood of the fetus can reach 50% of the concentration of fenoterol in the mother. In premature babies, unlike adults, the elimination of fenoterol is significantly slowed down. The metabolism of fenoterol hydrobromide in diabetes mellitus has not been studied enough.
Pharmacokinetics
Fenoterol hydrobromide is a selective beta-adrenoreceptor stimulant. Activates adenylate cyclase through the stimulatory Gs-protein with a subsequent increase in the formation of cAMP, which in turn activates protein kinase A. The latter phosphorylates target proteins in smooth muscle cells. This in turn leads to the phosphorylation of the light chain kinase of myosin, inhibition of the hydrolysis of phosphoinosine and the discovery of calcium activated fast potassium channels. Thus, fenoterol relaxes the smooth muscles of the bronchi and blood vessels, and also prevents the development of bronchospasm due to exposure to bronchoconstrictive factors such as histamine, methacholine, cold air and allergens (immediate type reaction). After taking the drug, the release of inflammatory mediators from mast cells is inhibited. In addition, after taking fenoterol at a dose of 0.6 mg, there is an increase in mucociliary transport. Higher plasma concentrations of the drug, achieved after oral administration, or more often, after intravenous administration, inhibit the contractility of the uterus. When taking high doses of the drug, effects at the metabolic level are observed: lipolysis, glycogenolysis, hyperglycemia, and hypokalemia (the latter is due to increased absorption of K1 by skeletal muscles).Beta-adrenergic effects of the drug at the level of the heart muscle, such as an increase in heart rate and increased myocardial contractility, are attributed to the action of fenoterol on the vessels, stimulation (Zr-adrenoreceptors of the heart, and when taking the drug in doses that exceed therapeutic (for example, during tocolytic therapy ), stimulation of Pi-adrenoreceptors. Also, as with the use of other beta-adrenergic agents, the prolongation of the QTc interval has been reported. For fenoterol, administered by inhalation a, these phenomena were discrete and were observed at doses higher than recommended. Often, the observed effect of agonists (3-adrenoreceptors is tremor. In contrast to the effect on the smooth muscle of the bronchi, systemic effects of P-adrenoreceptors agonists are associated with the development of tolerance. Fenoterol warns and quickly suppresses bronchospasm of various origins (physical activity, cold air, early response to allergen exposure). The onset of action after inhalation is after 5 minutes, the duration of action is 3-5 hours.
Indications
Attacks of bronchial asthma or other conditions with reversible airway obstruction (including chronic bronchitis, COPD). Prevention of asthma attacks of physical effort.
Contraindications
Tachyarrhythmia, hypertrophic obstructive cardiomyopathy, children under 4 years old, hypersensitivity to fenoterol and other components of the drug. Precautions should be prescribed for hyperthyroidism, arterial hypotension, hypertension, intestinal atony, hypokalemia, diabetes mellitus, recent myocardial infarction (within the last 3 months), diseases of the heart and blood vessels, such as chronic heart failure, CHD, diseases coronary arteries, with heart defects (including aortic stenosis), marked lesions of cerebral and peripheral arteries, 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 physician.
Precautionary measures
BEROTEK should be used only after a thorough assessment of the risk / benefit ratio, especially when used in doses higher than recommended, in the presence of the following diseases: uncontrolled diabetes mellitus, recent myocardial infarction, severe diseases of the cardiovascular system, hyperthyroidism, pheochromocytoma.In case of sudden development and rapid progression of shortness of breath, you should immediately consult a doctor. With the appointment of P2-adrenomimetik possible the development of severe hypokalemia. In this regard, special care is required in severe asthma, since in this case hypokalemia may occur as a result of the simultaneous administration of p2-adrenomimetics, xanthine derivatives, glucocorticoids and diuretics. In addition, during hypoxia, the effect of hypokalemia on the heart rhythm may be enhanced. In patients taking digoxin, hypokalemia may cause an increased susceptibility to arrhythmias. In such cases, it is recommended to control the level of potassium in the blood plasma. The use of sympathomimetic drugs, including BEER, can affect the cardiovascular system. In connection with the reception of β-adrenergic mites, there is a small likelihood of myocardial ischemia. Patients with severe heart disease (for example, coronary heart disease, arrhythmia, or acute heart failure) who are taking BEROTEK should be warned that they should see a doctor if chest pain or other symptoms of worsening heart disease occur. Particular attention should be paid to symptoms such as chest pain and shortness of breath, because they can be caused both by disorders of the respiratory system and by the work of the heart. BEROTEK inhalation solution contains preservative (antimicrobial) benzalkonium chloride and disodium edetate stabilizer. It was found that the above components in some patients may cause bronchoconstriction.
Use during pregnancy and lactation
Existing clinical experience has shown that fenoterol hydrobromide does not have a negative effect on pregnancy. However, it is necessary to observe the usual precautions associated with the use of drugs during pregnancy, especially in the case of this. The inhibitory effect of Berotek H on uterine contractility should be taken into account. Fenoterol hydrobromide can pass into breast milk. The safety of the drug during lactation has not been established.Given the ability of many drugs to penetrate into breast milk, caution should be exercised when prescribing BereTac H for women during breastfeeding. Peculiarities of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms There have been no studies on the effect of the drug on the ability to drive vehicles and drive mechanisms. Nevertheless, it is necessary to inform patients about possible side effects: dizziness, tremor while taking Beer Protect H and recommend caution when driving a vehicle or potentially dangerous machinery. In the case of the occurrence of the above side effects in patients, it is necessary to avoid performing such potentially dangerous operations as driving a vehicle or potentially dangerous mechanisms.
Dosage and administration
Adults and teenagers over 12 years old. Attacks of bronchial asthma and other conditions accompanied by reversible airway obstruction. In most cases, for relief of bronchospasm, 1 inhalation dose is sufficient. if the breathing is not relieved within 5 minutes, you can repeat the inhalation. If the effect is absent after 2 inhalations, and additional inhalations are required, the doctor should be consulted without delay. Preventing asthma physical effort. 1-2 inhalation doses before exercise, up to 8 inhalations per day. Children from 6 to 12 years. Attacks of bronchial asthma and other conditions accompanied by reversible airway obstruction. In most cases, for relief of bronchospasm, 1 inhalation dose is sufficient. if the breathing is not relieved within 5 minutes, you can repeat the inhalation. If there is no effect after 2 inhalations, and additional inhalations are required, you should immediately seek medical attention. Preventing asthma physical effort 1-2 inhalation dose to exercise, up to 8 inhalations per day. Children from 4 to 6 years. Due to the limited experience of use in children under the age of 6 years, the drug should be used only on prescription and under the supervision of adults.Attacks of bronchial asthma and other conditions accompanied by reversible airway obstruction. For relief of bronchospasm, 1 inhalation dose is sufficient. If there is no effect, immediately seek medical attention. Physical effort asthma prevention 1 inhalation dose before exercise, up to 4 inhalations per day. Terms of use of the drug. To achieve the maximum effect, it is necessary to use a 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, you must observe the following rules. 1. Remove the protective cap. 2. Make a slow, deep breath. 3. Holding the spray can, tightly clasp the tip of the lips. In this case, the arrow and the bottom of the cartridge should be directed upwards. 4. Making the maximum deep breath, at the same time quickly press the bottom of the can until the release of 1 inhalation dose. Hold your breath for a few seconds, then take the mouthpiece out of your mouth and exhale slowly. If repeated inhalation is required, repeat the same steps (steps 2-4). 5. Put on the protective cap. 6. If the aerosol canister has not been used for more than 3 days, before applying, press the bottom of the can once. The balloon is designed for 200 inhalations. Then the cylinder should be replaced. Although some contents may remain in the bottle, the amount of drug released during inhalation is reduced. The balloon is opaque, so the amount of the drug in the balloon can be determined as follows: remove the protective cap, immerse the balloon in a container filled with water. The amount of the drug is determined depending on the position of the cylinder in the water. scheme 1. The inhaler should be washed at least 1 time per week. It is important to keep the mouthpiece of the inhaler clean so that the medication does not accumulate and block spraying. To clean, first remove the dust cap and remove the container from the inhaler. Rinse the inhaler with warm water to remove accumulated medication or visible dust. After cleaning, you need to shake the inhaler and allow it to air dry without using heating devices.When the mouthpiece has dried, return the container and dust cap to the place. Plastic mouthpiece for the mouth is designed specifically for the metered aerosol Berotek N and is used for accurate dosing of the drug. The mouthpiece should not be used with other metered aerosols. You can not also use metered aerosol Berotek H with other adapters.
Side effects
On the part of the immune system: hypersensitivity. Metabolism: hypokalemia. On the part of the nervous system: excitement, nervousness, tremor, headache, dizziness. Since the cardiovascular system: myocardial ischemia, arrhythmia, tachycardia, palpitations, increased systolic blood pressure, decreased diastolic blood pressure. On the part of the respiratory system: paradoxical bronchospasm, irritation of the larynx and pharynx. On the part of the digestive system: nausea, vomiting. On the part of the skin and subcutaneous tissues: hyperhidrosis, skin reactions such as rashes, itching, urticaria. On the part of the musculoskeletal system: muscle spasm, myalgia, muscle weakness.
Overdose
Symptoms: possible symptoms associated with excessive stimulation of beta-adrenergic receptors. The most likely occurrence of arrhythmias, tachycardia, palpitations, tremor, hypertension or arterial hypotension, increased pulse pressure, angina pectoris pain, and hot flashes. Treatment: the appointment of sedatives, tranquilizers, in severe cases, intensive symptomatic therapy is indicated. B-adrenoblockers, especially b1-selective (atenolol, etc.), are recommended as specific antidotes. However, it is necessary to take into account the possibility of enhancing bronchial obstruction and carefully select the dose of these drugs to patients suffering from bronchial asthma.
Interaction with other drugs
Beta-adrenergic and anticholinergic agents, xanthine derivatives (for example, theophylline) can enhance the broncho expanding effect of fenoterol. The simultaneous administration of other beta-adrenergic mimetics that enter anticholinergic agents or xanthine derivatives (for example, theophylline) into the systemic circulation can lead to increased side effects. Perhaps a significant weakening of the broncho expanding action of Beer H while the appointment of beta-blockers.Be cautious to prescribe beta-adrenergic agents to patients who received monoamine oxidase inhibitors and tricyclic antidepressants, since these drugs can enhance the effect of beta-adrenergic agents. Inhalation of halogenated hydrocarbon anesthetics, such as halothane, trichlorethylene or enflurane, can increase the adverse effects of beta-adrenergic drugs on the cardiovascular system.
special instructions
Paradoxical bronchospasm. Like other inhalants, Berotec H can cause paradoxical bronchospasm, which can be life threatening. If a paradoxical bronchospasm occurs, the drug should be immediately discontinued and replaced with alternative therapy. Effects of the cardiovascular system. Effects of 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 about rare cases of myocardial ischemia associated with the use of beta-agonists. Patients with background severe heart disease (for example, ischemic heart disease, arrhythmia, or severe heart failure) who are receiving Berotec H should be warned about the need to seek medical attention if they experience chest pain or worsening heart disease. Attention should be paid to assessing symptoms such as shortness of breath and chest pain, as they can be both respiratory and cardiac. Hypokalemia. Potentially severe hypokalemia may develop as a result of beta2-agonist therapy. It is recommended to take special care in severe bronchial asthma, since hypokalemia can be potentiated by concomitant therapy with xanthine derivatives, GCS 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 control the level of potassium in serum. Acute progressive dyspnea. Patients should be advised to immediately consult a doctor in case of acute, rapidly aggravated dyspnea. Regular use.The relief of asthma attacks (symptomatic treatment) is preferable to regular use of the drug. Patients should be examined to identify the need for the appointment or strengthening of anti-inflammatory treatment (for example, inhaled GCS) in order to control airway inflammation and prevent delayed lung damage. In the case of increased bronchial obstruction, it is unacceptable and it may be risky to increase the frequency of intake of β2-adrenoreceptor agonists, including Berotec H, in doses exceeding those recommended and for a long time. Regular use of β2-adrenoreceptor agonists, including the drug Berotec N, to control the symptoms of bronchial obstruction may indicate a worsening of 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. Sharing with sympathomimetic and anticholinergic bronchodilators. Other sympathomimetic bronchodilators should be used in conjunction with the drug Berotek N only under the supervision of a physician. Anticholinergic bronchodilators can be inhaled simultaneously with the drug Berotek N. Effect on the results of laboratory studies. The use of the drug Berotec H may lead to positive results of tests for the presence of fenoterol in studies on the abuse of drugs for non-medical indications, for example, due to increased physical capacity in athletes (doping). Impact on the ability to drive vehicles and control mechanisms Research on the effect of the drug on the ability to drive vehicles and use of mechanisms was not carried out. However, patients need to be informed that during treatment with Berotek H, dizziness may develop. Therefore, caution should be recommended when driving or using machinery.