for medical use
of Berotek® medicine H
БЕРОТЕК® of N
the International unlicensed
name Fenoterolum Dosage Form Aerosol
the Structure dosed for inhalations, 100 mkg / a dose
1 inhalation dose contains
active agent – Fenoterolum hydrobromide of 100 mkg,
excipients: anhydrous citric acid, absolute ethanol, the water purified.
propellant: 1,1,1,2 – tetraftoretan (HFA 134a),
Transparent colourless, slightly yellowish or slightly brownish color liquid, with an ethanol smell, free from the suspended particles.
Drugs for treatment of obstructive respiratory diseases. Inhalation sympathomimetics. Beta2-adrenostimulyatora selection.
ATH Fenoterolum R03AC04 code
Pharmacokinetics Therapeutic Effect properties of drug BEROTEK H is created by local impact on airways. There is no correlation between the concentration of Fenoterolum in blood plasma reached after inhalation with effect of a bronkhodilatation.
After inhalation of 10-30% of active ingredient from aerosol drug pass into the lower airways, the rest is postponed in upper airways and in an oral cavity. As a result a part of Fenoterolum comes to digestive tract subsequently.
Absolute bioavailability – 18.7%. Further absorption becomes two-phase at which 30% of Fenoterolum of hydrobromide are quickly absorbed with elimination half-life of 11 minutes, 70% – are absorbed slowly and time of semi-removal is 120 minutes.
The maximum plasma concentration after inhalation of 200 mkg make Cmax of 66.9 pg/ml, tmax is 15 min. old. About 60% of Fenoterolum of hydrobromide are absorbed. The absorbed amount of drug is exposed to deep metabolism for the first circulation, as a result the oral biocomprehensibility decreases approximately to 1.5%. Therefore the swallowed part of active ingredient practically does not increase its level in plasma after inhalation.
Distribution of Fenoterolum happens on all organism. Communication with proteins of plasma – 40-55%. The part of drug which got inside mostly is metabolized with education sulfate conjugates, mainly in intestines walls. Biotransformation, including mostly excretion with bile, – about 85%. The renal clearance of Fenoterolum (0.27 l/min) corresponds to about 15% of the general dose which came to a system blood stream. Taking the fraction of drug connected with proteins of plasma into consideration, the value of renal clearance corresponds to canalicular secretion of Fenoterolum in addition to glomerular filtration.
The general excretion with urine in 24 hours – 2% of a dose, steadily after inhalation.
In not changed look Fenoterolum can get in insignificant quantity through a blood-brain barrier and get to maternal milk.
Data on effect of Fenoterolum of hydrobromide on the metabolic status in diabetes are not enough.
of BEROTEK of N – the effective bronchodilator used for the stopping of attacks of bronchial asthma and chronic obstructive bronchitis complicated or uncomplicated by emphysema.
After hydrobromide Fenoterolum inhalation in lungs the bronkhodilatation comes within several minutes, and the bronkhodilatichesky effect lasts from 3 to 5 hours.
Fenoterolum hydrobromide has direct sympathomimetic effect, selectively stimulating beta2-adrenoceptors of bronchial tubes in therapeutic doses. In higher doses it has ability to stimulate beta1-adrenoceptors. Linking with beta2-adrenoceptors activates adenylatecyclase with the participation of the stimulating Gs-protein. The increased level of cyclic AMF activates a protein kinase And which then phosphorylates proteins target in smooth muscle cells. It, in turn, leads to phosphorylation of a light chain of a miozinkinaza, inhibition of hydrolysis of a fosfoinozitid and opening of the potassium channels activated by calcium.
Fenoterolum hydrobromide relaxes smooth muscles of bronchial tubes and vessels and counteracts development of the bronkhospastichesky reactions caused by influence of a histamine, metasincaline, cold air and allergens (reactions of immediate hypersensitivity). Right after introduction Fenoterolum blocks release of bronkho-konstriktorny mediators of inflammation from mast cells. Use of higher doses of Fenoterolum increases mukotsiliarny clearance.
At higher concentrations of Fenoterolum in plasma which are reached most often at intake the contractility of a uterus is inhibited and also metabolic effects are observed: lipolysis, glycogenolysis, hyperglycemia and hypopotassemia. The hypopotassemia is caused, mainly, by the increased consumption of potassium ions skeletal muscles. Beta and adrenergic impact on heart, such as increase in frequency and force of warm reductions, is a consequence of influence of Fenoterolum on vessels, stimulations of beta2-adrenoceptors of a myocardium and when using the doses exceeding therapeutic, beta1-adrenoceptors. As well as when using other beta and adrenergic drugs, lengthening an interval of QTs at use high dosed by the Most often observed effect of beta2-agonists was noted the tremor is. Unlike impact on unstriated muscles of bronchial tubes to system influences of beta2-agonists the tolerance can develop.
– prevention and symptomatic treatment of bad attacks of asthma and other respiratory diseases with a reversible bronchospasm: a chronic obstructive pulmonary disease, the chronic obstructive bronchitis complicated or uncomplicated emphysema.
– prevention of attacks of asthma of physical tension
the Route of administration and doses
the Bad attack of asthma and other respiratory diseases with a reversible bronchospasm
In most cases for stopping of a bronchospasm is enough 1 inhalation dose if within 5 minutes of simplification of breath did not come, it is possible to repeat inhalation, as much as possible to 8 inhalations a day.
If after 2 inhalation doses the simplification did not come, additional inhalations can be required.
Prevention of attacks of asthma of physical tension
1-2 inhalation doses before loading, up to 8 inhalations a day.
The dosed BEROTEK aerosol H at children should be applied only on doctor’s orders and under control of adults.
It is necessary to use a route of administration For achievement of the maximum effect correctly dosed aerosol.
Before use of the dosed aerosol for the first time press a barrel bottom twice.
Every time when using of the dosed aerosol it is necessary to follow the following rules:
1. To remove a protective cap.
2. To make a slow, full exhalation.
3. Holding a cylinder (as shown in fig. 1), to densely clasp with lips a mouthpiece. The cylinder has to be directed by a bottom up.
4. Making the deepest breath, to press at the same time quickly a cylinder bottom before release of one inhalation dose. To hold the breath for several seconds, then to take out a mouthpiece from a mouth and to exhale slowly.
To repeat the same actions (steps 2-3) for receiving the second inhalation dose.
5. To put on a protective cap.
6. If the aerosol barrel was not used more than three days, before use it is necessary to press once a barrel bottom before emergence of a cloud of aerosol.
As a container opaque, it is impossible to define as far as the cylinder is empty. The cylinder is counted on 200 inhalations. After use of this quantity of doses in a container there can be a small amount of solution. Nevertheless, it is necessary to replace a container as differently it is possible not to receive a necessary medical dose.
The amount of the drug which remained in a container can be checked as follows.
Remove a plastic mouthpiece from a container and place a container in a vessel with water. Contents of a container can be determined by its situation in water (see fig. 2).
you Clean an inhaler at least once a week.
It is important to keep an inhaler mouthpiece clean to prevent the drug accumulation interfering dispersion.
For cleaning of an inhaler at first remove a dustproof cover, and then a barrel from an inhaler. Wash out an inhaler under a stream of warm water, so far all residues of medicine and/or dirt will not be removed.
After cleaning stir up an inhaler and leave it to be dried up on air without use of any heating device.
After the mouthpiece is dried up, replace a barrel and a dustproof cover.
PREVENTION: the plastic mouthpiece is developed especially for the dosed BEROTEK aerosol H and serves for exact drug dosing. The mouthpiece should not be used with other dosed aerosols. Also it is impossible to use BEROTEK aerosol H with any other adapters, except the mouthpiece delivered together with a cylinder.
Contents of a cylinder are under pressure. The cylinder cannot be opened and subjected to heating above 50 °C.
– cough, irritation in a throat
– a bronchospasm, including a paradoxical bronchospasm
– nausea, vomiting
– a hypopotassemia
– a hyperhidrosis, urticaria, rash, an itching
– myocardium ischemia, arrhythmia, tachycardia, heartbeat
– the increased systolic arterial blood pressure
– the lowered diastolic arterial blood pressure
– a tremor, a headache, dizziness
– muscle weakness, spasms, myalgia
– disturbing excitement, nervousness
– anaphylactic reactions, hypersensitivity
– positive reaction to Fenoterolum when passing doping tests (increase in effectiveness of sports preparation)
As well as at any means of inhalation therapy, at use of drug can arise symptoms of local irritation.
– hypersensitivity to Fenoterolum to hydrobromide or any other components of drug
– the hypertrophic subaortic stenosis, a tachyarrhythmia
Beta and adrenergic and anticholinergics, ksantinovy derivatives (for example, theophylline) can strengthen bronchodilatory effect of Fenoterolum. Co-administration of other beta-adrenergic agonists getting to a system blood stream of anticholinergics or ksantinovy derivatives (for example, theophylline), can lead to strengthening of side effects.
Perhaps considerable weakening of bronchodilatory action BEROTEKA of N at co-administration of beta blockers.
With care to appoint beta and adrenergic means to the patients receiving inhibitors of a monoaminooxidase or tricyclic antidepressants as these drugs are capable to strengthen action of beta and adrenergic means.
Inhalations of the halogenated hydrocarbon anesthetics, for example a halothane, trichloroethylene or an enfluran, can strengthen adverse influence of beta and adrenergic funds for a cardiovascular system.
Patients can note special instructions At the first use of the dosed BEROTEK aerosol H that new aerosol has other taste in comparison with the former aerosol containing freon. It is necessary to warn patients about it upon transition from one formula of drug to another. Patients need to know that both formulas of drug are completely interchanged, and change of taste does not influence efficiency and safety of a new formula of aerosol.
Other sympathomimetic bronchodilators it is necessary to appoint along with BEROTEKOM N only under medical observation.
Anticholinergic bronkholidilatator can be appointed at the same time.
With care (after carrying out the careful analysis of a ratio of risk – the expected advantage) apply at: dekompensirovanny diabetes, recently postponed myocardial infarction, a serious illness of a cardiovascular system, a hyperthyroidism, a pheochromocytoma.
In case of sudden emergence and fast progressing of an asthma (the complicated breath) it is necessary to see a doctor immediately.
– as necessary symptomatic treatment (stopping of attacks) is more preferable than regular use.
– it is necessary to estimate a condition of patients at addition or strengthening of anti-inflammatory therapy (inhalation corticosteroids) for control of inflammatory process in airways and courses of the disease and also for prevention of chronic damage of lungs.
Regular use of the increasing doses of the drugs containing beta2-agonists such as BEROTEK of N, for stopping of bronchial obstruction can cause uncontrollable deterioration in a course of the disease. In case of strengthening of bronchial obstruction simple increase in a dose of beta2-agonists, including BEROTEKA the N, is more recommended for a long time, not only is not justified, but also it is dangerous. For prevention of life-threatening deterioration in a course of the disease it is necessary to consider a question of revision of the treatment plan of the patient and adequate anti-inflammatory therapy by inhalation glucocorticosteroids.
Development of the expressed hypopotassemia when assigning therapy by beta2-agonists is possible. The extra care is recommended to be shown in heavy asthma as the effect of a gipokalemiya can be enhanced by the accompanying treatment by xanthine derivatives, glucocorticosteroids and diuretics. Besides, the hypoxia can strengthen impact of a hypopotassemia on a warm rhythm and also result in the increased susceptibility to arrhythmia at the patients receiving digoxin. In such situations the control of level of potassium in blood serum is recommended.
Sympathomimetic means, including BEROTEK of N, can influence a cardiovascular system. There are data confirming the exceptional cases of myocardial ischemia connected with reception of beta-agonists. The patients with the basic serious illness of heart (e.g. coronary heart disease, arrhythmia or heavy heart failure) accepting BEROTEK of N have to be warned about need of the request for medical care in case of appearance at them of a stethalgia or other symptoms of the aggravation of symptoms connected with a heart disease. It is necessary to pay attention to assessment of such symptoms as difficulty of breath and a stethalgia as they can be either respiratory, or warm origin.
Use of BEROTEKA of N can lead to positive test for Fenoterolum in tests for not clinical abuse of psychoactive substances, for example for improvement of effectiveness of sports preparation (doping).
The fertility, pregnancy and the period of a lactation
of Researches of influence of Fenoterolum of hydrobromide on fertility of the person were not carried out. However data of clinical trials showed lack of negative influence of Fenoterolum of hydrobromide on fertility of the person.
The existing clinical experience showed that Fenoterolum hydrobromide has no negative effect on pregnancy. Nevertheless, it is necessary to observe the usual precautionary measures connected with use of medicines during pregnancy, especially in the I trimester.
It is necessary to take the inhibiting influence BEROTEKA of N on contractility of a uterus into account.
Fenoterolum hydrobromide can get into breast milk. Safety of use of drug in the period of a lactation is not established. Nevertheless, considering ability of many medicines to get into breast milk, it is necessary to be careful when assigning BEROTEKA of N to women during breastfeeding.
Features of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms
of Researches of influence of drug on ability to driving of motor transport and to control of mechanisms it was not carried out.
Nevertheless, it is necessary to inform patients on possible side effects: dizziness, a tremor during reception BEROTEKA of N and to recommend to be careful during the driving of the car or control of mechanisms. In case of emergence in patients of the above-stated side effects, it is necessary to avoid performance of such operations, potentially dangerous to them, as driving or control of mechanisms.
Symptoms: emergence of the symptoms connected with excess stimulation of beta adrenoceptors is possible. Appearance of tachycardia, serdtsebiyeniy, a tremor, arterial hypertension or arterial hypotension, increase in pulse pressure, stenokardichesky pains, arrhythmia and inflows is the most probable.
Development of a metabolic acidosis in cases when the dose of the applied Fenoterolum considerably exceeds most recommended daily dose of N. BEROTEK is also possible.
Treatment: prescribing of sedatives, tranquilizers, in hard cases the intensive symptomatic care is shown.
As specific antidotes b-adrenoblockers, especially b1-selection are recommended (atenolol, etc.). However it is necessary to consider a possibility of strengthening of bronchial obstruction and to carefully select a dose of these drugs to the patients having bronchial asthma.
The form of release and packing
On 10 ml of drug place in cylinders from stainless steel with the portioning device, an inhaler for oral use and a protective cap.
On 1 cylinder together with an inhaler and the instruction for medical use in the state and Russian languages place in a cardboard box.
To Store storage conditions at a temperature not above 25 °C.
Not to open and not to heat a cylinder.
To store out of children’s reach!
A period of storage
not to use drug after expiry date.
According to the prescription
of Proiswoditel Boehringer Ingelcheim Pharm GmbH and To. KG, Germany
the Owner of the registration certificate
of Boehringer Ingelcheim Pharm GmbH and To. KG, Germany
the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality a produktsiipredstavitelstvo “Boehringer Ingelcheim of Pharm Hess mbkh” to the RKYuridicheskiy address: Almaty, 050010, Kairbekov St. 38 the Actual address: Almaty, 050008, the ave of Abay the Innova Tower 52business-center, the 7th etazhtet: +7 (727) 250 00 77 fax: +7 (727) 244 51 77 e-mail-mail