Fenoterol-native (Fenoterol-nativ)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceFenoterolFenoterol
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    • Dosage form: & nbspinhalation solution
    Composition:

    1 ml of solution for inhalation contains:

    Active substance:

    Fenoterol hydrobromide

    1.0 mg

    Excipients:

    Sodium benzoate

    0.5 mg

    Disodium edetate dihydrate

    0.554 mg

    (corresponds to the disodium edetate)

    0.5 mg

    Citric acid monohydrate

    1.64 mg

    (corresponding to citric acid anhydrous)

    1.5 mg

    Water for injections

    up to 1.0 ml
    Description:

    Transparent colorless or with a weak yellowish tinge solution.

    Pharmacotherapeutic group:bronchodilator - beta2-adrenergic selective
    ATX: & nbsp

    R.03.A.C.04   Fenoterol

    Pharmacodynamics:

    Fenoterol-native is an effective bronchodilator for the prevention and relief of bronchospasm attacks in bronchial asthma and other diseases accompanied by reversible airway obstruction, such as chronic obstructive pulmonary disease, chronic bronchitis, emphysema.

    Fenoterol is a selective stimulant β2receptors. When using the drug in higher vines, stimulation of β1-adrenoreceptors (for example, when prescribed for tocolytic therapy). The mechanism of action is associated with the activation of 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 inflammatory mediators from mast cells, thereby exerting a protective effect against the influence of bronchoconstrictors such 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 β2-adrenoceptors, fenoterol can exert an effect on the myocardium (especially in doses exceeding therapeutic), causing an increase and intensification of cardiac contractions.

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

    Pharmacokinetics:

    Suction

    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 rest is deposited in the upper respiratory tract and swallowed. As a result, some amount of inhaled fenoterol enters the gastrointestinal tract. After inhalation of a single dose of the drug, the degree of absorption is 17% of the administered dose. Absorption is biphasic in nature - 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. There is no correlation between plasma concentrations of fenoterol achieved after inhalation and the pharmacodynamic "time-effect" curve. The prolonged (3-5 hours) bronchodilator effect of the drug after inhalation, comparable to the corresponding effect achieved after intravenous administration, is not supported by high concentrations of active substance in the systemic circulation.

    Distribution

    Binding to plasma proteins - 40-55%. Unchanged fenoterol can penetrate the placental barrier and enter the breast milk.

    Metabolism

    If swallowed, the active substance undergoes biotransformation due to the effect of "primary transmission" through the liver. Metabolised in the liver. Thus, the swallowed amount of the drug does not affect the concentration of active substance in the blood plasma, achieved after inhalation. Biotransformation of fenoterol in humans occurs solely by conjugation with sulfates mainly in the intestinal wall.

    Excretion

    It is excreted by the kidneys and with bile in the form of inactive sulfate conjugates. 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.

    Indications:

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

    - prevention of asthma attacks due to physical stress;

    - as a bronchodilator before inhalation of other drugs (antibiotics, mucolytic agents, glucocorticosteroids);

    - conducting bronchodilation tests in the study of the function of external respiration.

    Contraindications:

    - Hypersensitivity to fenoterol or any component of the drug;

    - hypertrophic obstructive cardiomyopathy;

    - tachyarrhythmia;

    - age to 18 years.

    Carefully:

    Hyperthyroidism, arterial hypotension, arterial hypertension, intestinal atony, hypokalemia, diabetes mellitus, recent myocardial infarction (within the last 3 months), heart disease, vascular diseases such as chronic heart failure, coronary artery disease, coronary artery disease, malformations heart (including aortic stenosis), marked lesions of cerebral and peripheral arteries, pheochromocytoma, glaucoma.

    Pregnancy and lactation:

    There was no adverse effect of the drug on the course of pregnancy. Nevertheless, pregnant women (especially in the first trimester) drug is prescribed only in those cases,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.

    Fenoterol penetrates into breast milk. The safety of the drug during lactation is not known. The use of the drug during lactation is possible only in cases where the potential benefit to the mother exceeds the potential risk for the child.

    Dosing and Administration:

    The preparation Fenoterol-native is intended only for inhalation.

    20 drops = 1 ml.

    1 drop = 50 μg of fenoterol hydrobromide.

    Doses should be selected according to the individual needs of the patient; In addition, during treatment the patient should be under the supervision of a doctor.

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

    Inhalation.

    - 0.5 ml (10 drops = 0.5 mg of fenoterol hydrobromide) in most cases is sufficient for immediate arrest of the attack;

    - if necessary, the reappointment of the drug is inhaled by 0.5 ml (10 drops = 0.5 mg fenoterol hydrobromide) up to 4 times a day, but it is possible to reduce the individual dose depending on the effectiveness of treatment;

    - In severe cases, if a dose of 1 ml (20 drops) is ineffective, higher doses of 1 to 1.25 ml (20-25 drops = 1-1.25 mg fenoterol hydrobromide) may be required;

    - in extremely severe cases, if the dose to 2.0 ml (40 drops) is ineffective, 2 ml (40 drops = 2 mg fenoterol hydrobromide) are inhaled under the supervision of the doctor.

    Preventing attacks of bronchial asthma due to physical stress

    Inhalation.

    - 0.5 ml (10 drops = 0.5 mg of fenoterol hydrobromide) before exercise.

    Treatment is usually started with the lowest recommended dose.

    The recommended dose is diluted with 0.9% sodium chloride solution to a final volume of 3-4 ml, sprayed and inhaled until the total dilution is consumed.

    Fenoterol-native can not be distilled with distilled water. Solution diluted every time before applying; the remnants of the diluted solution are poured.

    Fenoterol-native It is recommended to use with the inhalation device - nebulizer. In the presence of oxygen breathing apparatus, the solution is best inhaled at a flow rate of 6-8 l / min.

    Fenoterol-native can be inhaled simultaneously with cholino- and mucolytic agents. This concerns, first of all, drugs ipratropium bromide and ambroxol in the form of solutions for inhalation.

    Side effects:

    Determination of the frequency: very often (> 1/10), often (1/100 to 1/10) infrequently (from 1/1000 to 1/100), rare (from 1/1000 to 1/10000), very seldom (<1/10000).

    From the nervous system: very often - nervousness, anxiety, tremor, headache, dizziness; very rarely - arousal.

    From the cardiovascular system: often tachycardia, palpitation; very rarely - arrhythmia, increased systolic blood pressure, reduced diastolic blood pressure, myocardial ischemia.

    From the side of metabolism and nutrition: often - hypokalemia, hyperglycemia.

    From the respiratory system: infrequently - cough, irritation of the larynx and pharynx; rarely - a paradoxical bronchospasm.

    From the digestive system: infrequently - nausea, vomiting.

    Skin and subcutaneous tissue: infrequently - allergic skin reactions, such as a rash, itching, urticaria; rarely hyperhidrosis.

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

    From the immune system: rarely - hypersensitivity.

    Overdose:

    Symptoms: tachycardia, increased heart rate, decrease or increase arterial pressure, increased pulse pressure, chest pain, arrhythmias, sensation of a flush of blood to the face, tremor, metabolic acidosis, headache, dizziness, anxiety, agitation, hypokalemia.

    Treatment: sedatives, tranquilizers, in severe cases intensive symptomatic therapy. As specific antidotes, β-blockers (preferably selective β1adrenoblockers); it is necessary to consider the possibility of strengthening bronchial obstruction and carefully select the doses of these drugs in patients suffering from bronchial asthma.

    Interaction:

    Glucocorticosteroids, anticholinergics, xanthine derivatives (for example, theophylline), cromoglycic acid can enhance the action of fenoterol.

    β-adrenergic agents, glucocorticosteroids and diuretics can enhance the side effects of fenoterol.

    It is possible to significantly reduce the bronchodilator action of Fenoterol-native while concomitant administration of β-adrenoblockers.

    Caution should be used to administer β-agonists to patients receiving monoamine oxidase inhibitors or tricyclic antidepressants,since these drugs can enhance the action of fenoterol.

    Inhalations of halogenated hydrocarbon anesthetics (halothane, trichlorethylene, enflurane) can enhance the effect of fenoterol 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:

    Other sympathomimetic bronchodilators can be used concomitantly with Fenoterol-native only under the supervision of a doctor.

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

    With prolonged use of the drug:

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

    - it is necessary to conduct regular examination of patients to identify the need for 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 obstruction of the bronchi is considered unacceptable and it may even be risky to increase the frequency of reception of β2-agonists contained in such preparations as Fenoterol-native, in excess of the recommended doses. In such a situation, a treatment plan and, especially, the adequacy of anti-inflammatory therapy should be reviewed. In the treatment of β2agonists 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 it is recommended to conduct regular monitoring of the potassium concentration in the serum of the crope.

    In rare cases, myocardial ischemia associated with β2agonists.

    The use of fenoterol in patients with hypokalemia who receive cardiac glycosides can cause arrhythmia.

    In patients with diabetes mellitus during treatment, regular monitoring of glucose in the plasma should be carried out.

    The drug contains a disodium edetate stabilizer, which in some patients can cause bronchospasm.

    The use of fenoterol can lead to positive results of tests for the abuse of psychoactive drugs for non-medical indications, as well as for doping in athletes.

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

    Studies to study the effect of the drug on the ability to drive vehicles and control mechanisms have not been conducted. In the case of side effects when using the drug should refrain from driving vehicles and controlling mechanisms.

    Form release / dosage:

    Solution for inhalation, 1 mg / ml.

    Packaging:

    For 20 ml of the drug in bottles of dark glass with a polyethylene dropper and a screwed polypropylene lid or polyethylene lid.

    One bottle with instructions for use is placed in a cardboard box.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Do not freeze.

    Keep out of the reach of children.

    Shelf life:

    3 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002943
    Date of registration:02.04.2015
    The owner of the registration certificate:NATIVA, LLC NATIVA, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp20.09.2015
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