Fenoterol-aeronaut - instructions for use, dose, side effects, contraindications

Active substanceFenoterolFenoterol

Similar drugsTo uncover

Berotek®

solution d / inhal.

Boehringer Ingelheim International GmbH Germany

Berotek® H

aerosol d / inhal.

Boehringer Ingelheim International GmbH Germany

Fenoterol-aeronaut

aerosol d / inhal.

NATIVA, LLC Russia

Fenoterol-native

solution d / inhal.

NATIVA, LLC Russia

Dosage form: & nbspaerosol for inhalation dosed

Composition:

Composition per 1 dose:
Active substance:
Fenoterol hydrobromide - 0,100 mg
Excipients:
Ethanol (absolute ethyl alcohol) - 18,000 mg
Triethyl citrate - 0,100 mg
Citric acid monohydrate 0.005 mg
Propellant R 134a of pharmacopoeial quality (1,1,1,2-tetrafluoroethane) is 41.795 mg.

Description:

Colorless or with a faint yellowish tinge, a clear solution that is pressurized in a stainless steel tank with a dosing valve and a spray nozzle; The drug is sprayed out of the balloon as an aerosol spray.

Pharmacotherapeutic group:Bronchodilator - β2-adrenergic selective

ATX: & nbsp

R.03.A.C.04 Fenoterol

Pharmacodynamics:

Fenoterol is an effective bronchodilator for preventing and arresting bronchospasm attacks with bronchial asthma and other conditions accompanied by reversible airway obstruction, such as chronic obstructive bronchitis (with or without emphysema).

Fenoterol is a selective stimulator of β2-adrenergic receptors in the therapeutic dose range. Stimulation β1-adrenoceptors occurs when higher doses are used. Binding to β2-adrenergic receptors activates adenylate cyclase through the stimulatory 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 causes relaxation of smooth muscle.

Fenoterol relaxes the smooth musculature of the bronchi and vessels and protects against bronchoconstrictor stimuli such as histamine, methacholine, cold air and allergens (early response). Besides, fenoterol inhibits the release of mast cells from bronchoconstrictor and proinflammatory mediators. The increase in mucociliary clearance was demonstrated after the use of fenoterol (in a dose of 0.6 mg).

Due to the stimulating effect on β1-adrenoceptors, fenoterol can exert an effect on the myocardium (especially in doses exceeding the therapeutic ones), causing an increase and increase in cardiac contractions.

Fenoterol quickly reduces bronchospasm of various genesis. Bronchodilation develops within a few minutes after inhalation and lasts 3-5 hours. Also fenoterol protects against bronchoconstriction, which occurs under the influence of various stimuli, such as physical activity, cold air and allergens (early response).

Pharmacokinetics:

Suction

After inhalation, 10-30% of the active substance released from the aerosol preparation fenoterola, reaches the lower respiratory tract, depending on the inhalation technique and the inhalation system used. The remainder settles in the upper respiratory tract and mouth, and then swallows.

Absolute bioavailability of fenoterol after inhalation of the metered aerosol is 18.7%. Absorption of fenoterol from the lungs is biphasic: 30% of the dose is absorbed quickly (half-life of 11 min), and 70% - slowly (half-life of 120 min). The maximum plasma concentration after inhalation of 200 μg of fenoterol is 66.9 pg / ml (t_max 15 minutes).

After oral administration, approximately 60% of the dose of fenoterol hydrobromide is absorbed. The absorbed amount undergoes an extensive first phase of metabolism in the liver, as a result, oral bioavailability is approximately 1.5% and its contribution to the concentration of fenoterol in plasma after inhalation is small.

Distribution

The distribution of fenoterol in plasma after intravenous administration adequately describes the 3-component pharmacokinetic model (half-life is t_α = 0.42 min, t_β = 14.3 min and t_γ = 3.2 hours). The volume of distribution of fenoterol at a constant concentration after intravenous administration is 1.9 - 2.7 l / kg, binding to plasma proteins - from 40 to 55%.

Fenoterol hydrobromide in unchanged form can penetrate through the placental barrier and enter the breast milk.

Metabolism

Fenoterol undergoes intensive metabolism in the liver by conjugation to glucuronides and sulfates. The swallowed portion of the dose of fenoterol is metabolized predominantly by sulphation. This metabolic inactivation of the starting material begins already in the wall of the intestine.

Excretion

Fenoterol is excreted by the kidneys and with bile in the form of inactive sulfate conjugates. Biotransformation, including excretion with bile, is subjected to the bulk - about 85%. 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 tubular secretion of fenoterol in addition to glomerular filtration. After inhalation, a 2% dose is released through the kidneys unchanged for 24 hours.

Indications:

- Attacks of bronchial asthma or other conditions with reversible airway obstruction, chronic bronchitis, chronic obstructive pulmonary disease.

- Preventing attacks of bronchial asthma due to physical stress.

Contraindications:

- Hypersensitivity to fenoterol or any of the excipients of the drug.

- Hypertrophic obstructive cardiomyopathy, tachyarrhythmia.

- Fenoterol-aeronaut in a dosage form, aerosol for inhalation dosage is not used in children under 4 years of age.

Carefully:

In the following conditions, the drug Fenoterol-aeronaut should be used only after a thorough assessment of the benefit / risk, especially if the maximum recommended doses are used: hyperthyroidism; hypokalemia; not enough controlled diabetes mellitus; recently suffered myocardial infarction (during the last 3 months); severe organic diseases of the heart and blood vessels,such as chronic heart failure, ischemic heart disease, coronary artery disease, heart disease (including aortic stenosis), severe cerebral and peripheral arterial lesions; pheochromocytoma.

Since information on the use of fenoterol in children under 6 years of age is limited, treatment is carried out with caution, only under the supervision of a doctor.

Pregnancy and lactation:

The results of preclinical studies, combined with the experience of clinical use of fenoterol, did not reveal any undesirable phenomena during pregnancy. Nevertheless, caution should be exercised in pregnancy, especially in the first trimester, 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.

Pre-clinical studies have shown that fenoterol penetrates into breast milk. The safety of fenoterol in the period of breastfeeding has not been studied. Care should be taken when applying the drug during breastfeeding.There are no clinical data on the effects of fenoterol on fertility. Preclinical studies of fenoterol showed no adverse effects on fertility.

Dosing and Administration:

Doses for adults and children over 6 years

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

In most cases, one inhalation dose is sufficient to stop bronchospasm. If no breathing has occurred within 5 minutes, you can repeat the inhalation.

If the effect is absent after two inhalation doses, and additional inhalations are required, medical attention should be sought without delay. The maximum allowable dose during the day is 8 inhalation doses.

Preventing attacks of bronchial asthma due to physical stress 1-2 inhalation doses to exercise, up to 8 inhalation doses per day.

In children aged 6 to 12 years, the drug Fenoterol-Aeronaut should only be used after consultation with a doctor and under the supervision of adults.

Doses for children from 4 to 6 years

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

To stop bronchospasm, one inhalation dose is sufficient.

If there is no effect, you should seek medical help without delay.

Preventing attacks of bronchial asthma due to physical stress

1 inhalation dose to exercise, up to 4 inhalation doses per day.

In children aged 4 to 6 years, the preparation of Fenoterol-Aeronaut should only be used after consultation with a doctor and under the supervision of adults.

Mode of application

To achieve the maximum effect, it is necessary to correctly use the metered aerosol.

Instructions for inhalation

Fenoterol-aeronaut is only for inhalation use.

Before using the inhaler for the first time or if the inhaler has not been used for a week or longer, check its operation. To do this, remove the protective cap from the mouthpiece of the inhaler, shake the inhaler well and press the balloon, releasing one jet of the drug into the air.

Carrying out inhalations

Step 1. Remove the protective cap from the inhaler mouthpiece, as shown in figure 1.

Step 2. Vigorously shake the inhaler.

Step 3. Make a slow, full exhalation. Do not exhale into the inhaler!

Step 4. Holding the balloon as shown in Figure 2, tightly grasp the mouthpiece with your lips.

The balloon must be pointed upside down!

Step 5. Exercise as deep as possible, while simultaneously pushing the bottom of the balloon to release one inhalation dose.

Step 6. Hold the breath for a few seconds, then remove the mouthpiece from the mouth and slowly exhale through the nose.

Step 7. Put the protective cap on the mouthpiece of the inhaler. Repeat steps 2-6 to obtain a second inhalation dose, if necessary.

Cleaning the inhaler

Regularly (once a week) should be washed with water inhaler mouthpiece, as shown in Figure 3.

To do this, remove the metal can from the plastic case and rinse the case and cap with warm water. Do not use hot water. Thoroughly dry, but do not use heating devices. Place the can in the case and put on the cap. Do not immerse the metal can into the water.

The cylinder is designed for 200 inhalations. After this, the cylinder should be replaced.

WARNING: a plastic mouthpiece designed specifically for the preparation Fenoterol-aeronaut and serves for accurate dosing of the drug. The mouthpiece can not be used with other metered aerosols. Also you can not use Fenoterol-aeronaut with any other devices, except the mouthpiece supplied with the drug.

The contents of the cylinder are under pressure. The cylinder should not be opened and subjected to heating above 50 ° C!

Side effects:

Like all other types of inhalation treatment, the drug Fenoterol-aeronaut may cause symptoms of local irritant effect.

From the immune system: hypersensitivity.

From the side of metabolism and nutrition: Hypokalaemia, including severe hypokalemia.

From the nervous system: excitation, nervousness, tremor, headache, dizziness.

From the cardiovascular system: myocardial ischemia, arrhythmia, tachycardia, palpitations, increased systolic blood pressure, reduced diastolic blood pressure.

From the respiratory system: paradoxical bronchospasm, coughing, irritation of the larynx and pharynx.

From the digestive system: nausea, vomiting.

Skin and subcutaneous tissue: hyperhidrosis, skin reactions such as a rash, itching, urticaria.

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

Overdose:

Symptoms

In case of an overdose, the expected symptoms are symptoms caused by excessive beta-adrenergic stimulation. The most pronounced are tachycardia, palpitation, tremor, a decrease or increase in blood pressure, an increase in pulse pressure, angina pectoris, arrhythmia, facial hyperemia. Metabolic acidosis and hypokalemia were also observed with the use of fenoterol in doses exceeding the recommended dose for approved indications.

Treatment

Treatment with drug Fenoterol-aeronaut must be terminated. The acid-base balance and electrolyte balance should be monitored.

For treatment, sedatives are used, in severe cases, intensive symptomatic therapy is performed.

As specific antidotes, β-blockers (preferably selective β1adrenoblockers); at the same time, the possibility of strengthening bronchial obstruction should be considered and the doses of these drugs should be carefully selected in patients with bronchial asthma.

Interaction:

β-Adrenergic drugs, anticholinergics, xanthine derivatives (such as theophylline), cromoglycic acid, glucocorticosteroids and diuretics can enhance the action and side effects of fenoterol.

Hypokalemia caused by β2-agonists can be enhanced by concomitant therapy with xanthine derivatives, corticosteroids and diuretics. This should especially be taken into account in patients with severe airway obstruction (see section "Special instructions").

A significant reduction in bronchodilation with simultaneous use of fenoterol and β-blockers.

Agonists β-adrenoceptor should be carefully administered to patients receiving monoamine oxidase inhibitors or tricyclic antidepressants that are able to potentiate the action of agonists βadrenoreceptors.

Inhalation of funds for general anesthesia, such as halothane, trichlorethylene and enflurane, increases the likelihood of β-adrenoreceptor agonists acting on the cardiovascular system.

Special instructions:

Paradoxical bronchospasm

Like other inhaled drugs Fenoterol-aeronaut can cause a paradoxical bronchospasm, which can endanger life. When a paradoxical bronchospasm occurs, the drug should be immediately withdrawn and replaced with alternative therapy.

Effects of the cardiovascular system

Effects from the cardiovascular system can be observed with the use of sympathomimetic drugs, including the drug Fenoterol-aeronaut. There are data on post-research studies and publications in the literature on rare cases of development of myocardial ischemia associated with the use of beta-agonists.

Patients with background severe heart disease (eg, ischemic heart disease, arrhythmia or severe heart failure) who receive the drug Fenoterol-aeronaut, should be warned about the need to seek medical help if there is chest pain or worsening of heart disease.

Attention should be paid to assessing symptoms such as dyspnoea and chest pain, as they can be both respiratory and cardiac.

Hypokalemia

Potentially severe hypokalemia can develop as a result of β2-agonist therapy.It is recommended to observe special care in severe bronchial asthma, because hypokalemia may be potentiated by concomitant therapy with xanthine derivatives, glucocorticosteroids and diuretics. In addition, hypoxia can increase the effect of hypokalemia on the heart rhythm. Hypokalemia can lead to an increased predisposition to arrhythmias in patients receiving digoxin.

In such situations it is recommended to monitor the level of potassium in the blood plasma.

Acute progressive dyspnoea

Patients should be advised to consult a doctor immediately if there is acute, rapidly increasing dyspnoea.

Regular application

- Coping of asthma attacks (symptomatic treatment) is preferable to regular use of the drug.

- Patients should be screened to identify the need for increased anti-inflammatory treatment (eg, inhalation glucocorticosteroids) for the purpose of controlling inflammation of the respiratory tract and preventing stunted lung damage.

In the case of increased bronchial obstruction is unacceptable and it may be risky to increase the frequency of adherence of β2-adrenergic agonists,such as a drug Fenoterol-aeronaut, in addition to the recommended doses and for a long time. The use of elevated doses of β2-agonists, such as the drug Fenoterol-aeronaut, on a regular basis to control the symptoms of bronchial obstruction may indicate a worsening of disease control. In such a situation, a treatment plan and, especially, the adequacy of anti-inflammatory therapy should be reviewed to prevent a potentially life-threatening deterioration in disease control.

Joint use with sympathomimetic and anticholinergic bronchodilators

Other sympathomimetic bronchodilators should be used together with the drug Fenoterol-aeronaut only under the supervision of a doctor. Anticholinergic bronchodilators can be used concurrently with the drug Fenoterol-aeronaut.

Influence on the results of laboratory studies

Application of the drug Fenoterol-aeronaut can lead to positive results of tests for the presence of fenoterol in studies on drug abuse due to non-medical indications, for example, due to increased physical capabilities in athletes (doping).

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

Studies of the effect of fenoterol on the ability to manage motor vehicles and the use of mechanisms have not been carried out.

However, when using the drug, there may be side effects such as dizziness, etc. Therefore, it is recommended to use caution when driving vehicles or using mechanisms.

Form release / dosage:

Aerosol for inhalation dosed with 100 μg / dose.

Packaging:

For 200 doses of the drug in a stainless steel balloon with a dosing valve and a spray nozzle. Each cylinder is accompanied with instructions for use in a cardboard box.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C, away from heating appliances. Do not freeze.

Keep out of the reach of children.

Shelf life:

2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-004222

Date of registration:30.03.2017

Expiration Date:30.03.2022

The owner of the registration certificate:NATIVA, LLC NATIVA, LLC Russia

Manufacturer: & nbsp