Composition, form of production and packaging
The solution for inhalations is clear, colorless or with a slight yellowish tinge.
fenoterola hydrobromide 1 mg
Auxiliary substances: sodium benzoate - 0.5 mg, disodium edetate dihydrate - 0.554 mg (corresponds to disodium edetate - 0.5 mg), citric acid monohydrate - 1.64 mg (corresponds to citric acid anhydrous - 1.5 mg), water d / u - up to 1 ml.
20 ml - bottles of dark glass (1) with a dropper - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2015.
Fenoterol-native is an effective bronchodilator for preventing and arresting 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? 2- adrenoreceptors. When using the drug in higher doses, is there stimulation? 1- adrenoreceptors (for example, when prescribed for tocolytic therapy). The mechanism of action is associated with the activation of adenylate cyclase through the stimulatory G s protein, followed by an increase in the formation of cyclic adenosine monophosphate (cAMP), which activates protein kinase A, which deprives myosin of the ability to bind to actin, which inhibits smooth muscle contraction and promotes bronchodilator action and elimination of bronchospasm.
In addition, fenoterol inhibits the release of mast cells from inflammatory mediators of inflammation, thereby exerting a protective effect on the influence of such bronchoconstrictors as histamine, methacholine, cold air and allergens. The use of fenoterol in a dose of 0.6 mg increases the activity of the ciliary epithelium of the bronchi and accelerates mucociliary transport.
Due to the stimulating effect on ОІ-adrenergic receptors, fenoterol can exert an effect on the myocardium (especially at doses exceeding the therapeutic ones), causing an increase and increase in cardiac contractions.
Fenoterol prevents and quickly reduces bronchospasm of various genesis. The onset of action after inhalation - after 5 minutes, a maximum of 30-90 minutes, the duration of the action is 3-5 hours.
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, a certain amount of inhaled fenoterol enters the digestive tract. After inhalation of a single dose of the drug, the degree of absorption is 17% of the administered dose. Absorption is biphasic: 30% fenoterol hydrobromide is rapidly absorbed from T 1/2 11 min, 70% - absorbed slowly from T 1/2 120 min. There is no correlation between plasma concentrations of fenoterol achieved after inhalation and the time-effect pharmacodynamic curve. The prolonged (3-5 h) bronchodilatory 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.
Binding to plasma proteins - 40-55%. Unchanged, fenoterol can penetrate the placental barrier and enter the breast milk.
If swallowed, the active substance undergoes biotransformation due to the effect of "first passage" 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.
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.
- bouts of bronchial asthma or other conditions with reversible airway obstruction, such as chronic obstructive pulmonary disease, obstructive bronchitis, emphysema;
- prevention of attacks of bronchial asthma due to physical stress;
- as a bronchodilator before inhalation of other drugs (antibiotics, mucolytic agents, GCS);
- carrying out bronchodilation tests while examining the function of external respiration.
The preparation Fenoterol-native is intended only for inhalation.
20 drops = 1 ml.
1 drop = 50 Ојg 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 fenoterol hydrobromide) in most cases is sufficient for immediate arrest of the attack.
If you need to re-prescribe the drug inhaled by 0.5 ml (10 drops = 0.5 mg fenoterol hydrobromide) up to 4 times / 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 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 fenoterol hydrobromide) to 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 intake of the dilution is complete.
Fenoterol-native should not be diluted with distilled water. The solution is diluted every time before use; the remnants of the diluted solution are poured.
Fenoterol-native is recommended to be used with an 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, the preparations of ipratropium bromide and ambroxol in the form of solutions for inhalation.
Frequency determination: very often (> 1/10), often (from 1/100 to 1/10), infrequently (from 1/1000 to 1/100), rarely (from 1/10000 to 1/1000), very rarely (<1/10000).
From the nervous system: very often - nervousness, anxiety, tremor, headache, dizziness; very rarely - arousal.
From the cardiovascular system: often - tachycardia, a feeling of heartbeat; very rarely - arrhythmia, an increase in systolic blood pressure, a decrease in diastolic blood pressure, ischemia of the myocardium.
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.
From the skin and subcutaneous tissues: infrequently - allergic skin reactions, such as rash, itching, urticaria; rarely hyperhidrosis.
From the musculoskeletal system: infrequently - muscle weakness, muscle spasm, myalgia.
From the immune system: rarely - hypersensitivity.
- hypersensitivity to fenoterol or any component of the drug;
- hypertrophic obstructive cardiomyopathy;
- age to 18 years.
With caution: hyperthyroidism; arterial hypotension; arterial hypertension; intestinal atony; hypokalemia; diabetes; recently suffered myocardial infarction (within the last 3 months); heart and vascular disease, such as chronic heart failure, coronary artery disease, coronary artery disease, heart disease (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. However, in pregnant women (especially in the first trimester), the drug is prescribed only if the intended 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 intended use for the mother exceeds the potential risk for the child.
APPLICATION FOR CHILDREN
Contraindicated use of the drug in children and adolescents under the age of 18 years.
Other sympathomimetic bronchodilators can be used concomitantly with Fenoterol-native only under the supervision of a physician.
In case of acute, rapidly increasing dyspnea, the patient should consult a doctor immediately.
With prolonged use of the drug:
- relief of attacks of bronchial asthma 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 (eg, inhaled GCS) to control inflammation of the airways and prevent prolonged exacerbations of bronchial asthma.
In the case of increased bronchial obstruction, it is considered unacceptable and it may even be risky to increase the multiplicity of beta- 2 -agonists in preparations such 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 beta 2 -agonists, the development of severe hypokalemia is possible. Particular care should be exercised in severe bronchial asthma, t. this effect can be enhanced by the concomitant use of xanthine derivatives, GCS 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 potassium concentration in blood serum.
In rare cases, myocardial ischemia associated with beta 2 -agonists was observed.
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.
Impact on the ability to drive vehicles and manage mechanisms
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.
Symptoms: tachycardia, increased heart rate, decreased or increased blood pressure, increased pulse pressure, chest pain, arrhythmias, sensation of flushing to the face, tremor, metabolic acidosis, headache, dizziness, anxiety, agitation, hypokalemia.
Treatment: sedatives, tranquilizers, in severe cases, conduct intensive symptomatic therapy. As specific antidotes, it is possible to prescribe beta-blockers (preferably selective beta 1- adrenoblockers); 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.
SCS, anticholinergic agents, xanthine derivatives (eg, theophylline), cromoglycic acid can enhance the effect of fenoterol.
Beta-adrenergic agents, GCS 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 beta-blockers.
Caution should be used to administer beta-agonists to patients receiving MAO inhibitors or tricyclic aptidepressants, these drugs can enhance the effect 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.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, protected from light at a temperature of no higher than 25 В° C. Do not freeze. Shelf life - 3 years.