Berotec N
Active material: Fenoterol
When ATH: R03AC04
CCF: Bronchodilators – beta2-adrenomimetik
ICD-10 codes (testimony): J43, J44, J45
When CSF: 12.01.01.02.01
Manufacturer: BOEHRINGER INGELHEIM PHARMA GmbH & Co. KG (Germany)
Pharmaceutical form, composition and packaging
Aerosol for inhalation dose in the form of a transparent, colourless or slightly yellowish or slightly brownish color liquid, free from suspended particles.
| 1 dose | |
| Fenoterol gidrobromid | 100 g |
Excipients: Citric acid anhydrous, Ethanol absolute, Purified water, 1,1,1,2-tetrafluoroethane (HFA 134a, propellant).
10 ml (200 doses) – stainless steel cartridge with dispensing valve action (1) – packs cardboard.
Pharmacological action
Bronchodilators, selective beta2-adrenomimetik.
Activates adenilatziklazu via stimuljatornyj (G)s-protein with a consequent increase in education camp, which in turn activates a protein kinase. Latest phosphorylate target proteins in the cells of smooth muscles, that in turn leads to fosforilirovaniju myosin light chain kinase, inhibition of the hydrolysis of fosfoinozina and the opening of calcium-activated potassium channels fast.
Thus, fenoterol relaxes smooth muscles bronchus and vessels, and also prevents the development of bronchospasm, resulting from exposure to such bronhokonstriktornyh factors, kak histamine, metaholin, cold air and allergens (reaction immediate type). After taking the drug inhibited the release of mast cell mediators of inflammation. Besides, After taking fenoterola in high doses, there is an increasing mukociliarnogo of transport.
Beta-adrenergic effect of the drug on cardiac function, such as an increase in the frequency and strength of heart contractions, due to the action of vascular fenoterol, стимуляцией b2-adrenoreceptors of the heart, and with doses, exceeding therapeutic, стимуляцией b1-adrenoreceptorov.
When admission preparation in high doses observed effects at the level of metabolism: lipolysis, Glycogenolysis, hyperglycemia and hypokalemia (the latter happens due to increased potassium uptake skeletal muscles). Fenoterol (in high concentrations) oppressing oxytocics activity of the uterus.
Fenoterol warns and quickly eliminates bronhospazm different Genesis (physical effort, cold air, early response to allergen exposure).
Home of the drug after inhalation – through 5 m, duration – 3-5 no.
Pharmacokinetics
Absorption
Depending on the inhalation system about 10-30% fenoterola hydrobromide reaches the lower divisions of the respiratory tract, and the rest deposited in the upper divisions respiratory tract and swallowed. As a result, a number of ingaliruemogo fenoterola hydrobromide enters the DIGESTIVE TRACT. After inhalation single dose absorption is 17% dose. Suction is two-phase nature: 30% fenoterola hydrobromide absorbed with a period of poluabsorbcii 11 m; 70% absorbed slowly with a period of poluabsorbcii 120 m.
There is no correlation between the values of concentrations fenoterola in plasma, achieved after inhalation, and pharmacodynamic curve “time-effect”. Long bronhorasshirjajushhij the effect of the drug (3-5 no) after inhalation, compared with the corresponding effect, achieved after in/introductions, not supported by high concentrations of the active substance in the system bloodstream. After ingestion absorbed about 60% an oral dose. This part of the active substance is biotransformation due to the effects of “first pass” through the liver. As a result, bioavailability after intake is lowered to 1.5%. This explains the fact, that proglochennoe amount of the drug has little effect on the concentration of the active substance in plasma, attainable after inhalation.
Distribution
Fenoterola hydrobromide penetrates through the placental barrier and is excreted in breast milk.
Metabolism
Biotransformiroetsa by conjugation with sulphates, predominately in the bowel wall.
Deduction
Return with urine and bile in the form of inactive conjugates of sulfate.
Testimony
— severe asthma;
-Prevention of asthma physical effort;
-symptomatic treatment of bronchial asthma or other conditions, accompanied by reversible airway narrowing (incl. obstructive bronchitis). In patients with bronchial asthma and chronic obstructive pulmonary disease, respond to SCS therapy, should consider the need for concomitant anti-inflammatory therapy.
Dosage regimen
To acute asthma adults and children over 6 years appointed 1 dose, if necessary through 5 min inhalation can be repeated (the patient must be informed, What if there is no effect after 2-x doses, it is necessary to consult a doctor); children aged 4 to 6 years appointed 1 dose.
To Prevention of asthma physical effort adults and children over 6 years appointed 1-2 dose 1 inhalation, to 8 doses/day; children aged 4 to 6 years appointed 1 dose.
To symptomatic treatment of bronchial asthma and other conditions, accompanied by reversible airway narrowing, adults and children over 6 years appointed 1-2 dose 1 inhalation, If you require repeated inhalation, then no more 8 doses/day. Children aged 4 to 6 years appointed 1 dose 4 times / day (no more 2 inhalation at 1 reception, tk. increasing the dose increases the risk of side effects). The interval between inhalation – no less 3 no. The maximum daily dose – 4 inhalation.
Terms of use of the drug
Before using the measured aerosol for the first time, you should double click on the bottom of the cylinder.
Every time you use a metered aerosol should do the following.
1. Remove the protective cap.
2. Make slow, deep breath.
3. Hold the bottle, clasp lips mouthpiece. The container should be sent upside down.
4. Making the most deep breath, both quickly push the bottom of the bottle before release 1 dose inhalation. For a few seconds, hold your breath, then remove the mouthpiece from the mouth and breathe out slowly. Repeat steps for the 2nd dose inhalation.
5. Wear protective cap.
6. If an aerosol can is not used more than 3 days, Prior to use, single click on the bottom of the container until the aerosol cloud.
The cylinder is designed for 200 inhalations. Then, the cylinder must be replaced. Despite, that the cylinder can be some content, the amount of drug, released during inhalation, decreases.
The container is opaque, Therefore, the amount of the drug in the container can be defined as follows:: remove the protective cap, container ship in container, filled with water. The amount of drug is determined depending on the position of the balloon in water.
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The mouthpiece should be kept clean, If necessary, it can be washed in warm water. After using soap or detergent mouthpiece should be thoroughly washed with water.
Plastic mouthpiece for mouth designed specifically for dosed aerosol Berotek® N and serves for precise dosing of the drug. Mouthpiece should not be used with other dosage aerosols. Also, you cannot use metered aerosol Berotek® N with other adapters.
Side effect
CNS: often – minor tremor; possible (especially in patients with risk factors) dizziness, headache, nervousness; in some cases – mental changes.
Cardio-vascular system: often – tachycardia, palpitations; rarely (when used in high doses) – lowering diastolic pressure, increased systolic pressure, Arrhythmia, angina.
Metabolism: There may be increasing the concentration of glucose in the blood, severe hypokalemia.
Co respiratory system: possible coughing, Local irritation; rarely - paradoxical bronchospasm.
From the digestive system: nausea, vomiting.
Other: There may be increased sweating, weakness, muscle aches, convulsions; rarely – local inflammatory and allergic reactions (especially in patients with a heightened sensitivity).
Contraindications
- Dryness;
- Gipertroficheskaya obstruktivnaya cardiomyopathy;
- Children up to age 4 years;
-hypersensitivity to fenoterola gidrobromidu and other components of the drug.
FROM caution should designate product in decompencirovannom diabetes, recent myocardial infarction, heavy cardiovascular diseases, uncontrolled hypertension, gipertireoze, pheochromocytoma.
Pregnancy and lactation
We found no adverse effects of the drug on the course of pregnancy. Nonetheless, Pregnancy (especially in the I trimester) the drug is indicated only in cases, the expected benefit to the mother outweighs the potential risk to the fetus.
Remember about depressing effects on uterine activity oxytocics fenoterola.
Known, What is the breast milk fenoterol. The safety of the drug in lactation has not been established. Use of the drug during breast-feeding is possible only in cases, When the expected benefits for a mother than the potential risk to the child.
Cautions
The simultaneous application Beroteka® H and anticholinergic bronchodilators.
In case of a sudden occurrence and rapid progression of the shortness of the patient also should immediately consult your doctor.
Regular use of Beroteka® N in increasing doses for relief of bronchial obstruction can cause an uncontrolled deterioration of the disease. In the case of reinforcement of bronchial obstruction simply increasing doses of Beroteka® N longer recommended for a long time not only justified, but also dangerous. To prevent life-threatening deterioration of disease should consider reviewing the patient's treatment plan and an adequate anti-inflammatory therapy with inhaled corticosteroids.
Other sympathomimetic bronchodilators should be appointed at the same time with Berotekom® H only under medical supervision.
When you assign a beta2-adrenomimetikov may develop hypokalemia. In this regard, particular caution is required in severe asthma, tk. in this case, hypokalemia can occur as a result of the simultaneous appointment beta2-adrenomimetikov, xanthine derivatives, glucocorticoids and diuretics. Besides, When hypoxia may increase the impact of gipokaliemii on cardiac rhythm. It is recommended to monitor the level of potassium in the blood plasma.
Diabetic patients need to conduct regular monitoring of glucose in plasma.
It should be taken into account, that symptomatic treatment is preferable to regular use of the drug. You must conduct a regular survey of patients to determine whether additional or more intensive anti-inflammatory treatment (eg, inhaled CORTICOSTEROIDS).
Use in Pediatrics
Experience of clinical application of the drug in children aged 4 years missing.
Overdose
Symptoms: may cause symptoms, associated with excessive Beta-Adrenergic stimulation, – tachycardia, palpitations, tremor, arterial hypertension, hypotension, an increase in pulse pressure, angina, Arrhythmia, flushing of the face.
Treatment: use of sedatives, trankvilizatorov, in severe cases, shows the intensive therapy.
As specific antidotes recommended appointment cardioselective β1-adrenoblokatorov. However, you should consider the possibility of strengthening the bronchial obstruction and carefully pick up the dose of these drugs in patients with bronchial asthma.
Drug Interactions
Beta-agonists and anticholinergics, xanthine derivatives (incl. theophylline), cromoglicic acid, GKS can exacerbate the effects of fenoterola.
With simultaneous use of other beta-agonists, anticholinergics, xanthine derivatives (eg, teofillina), GCS, diuretics, Enter the bloodstream, may increase the side effects.
Possibly significant weakening of bronchodilator action fenoterola while applying beta-adrenoblokatorov.
Against the backdrop of Beroteka® H may develop hypokalemia, which may be increased with concomitant administration with xanthine derivatives, steroids and diuretics.
Should be cautious appoint Berotek® H patients, receiving MAO inhibitors and tricyclic antidepressants, tk. These medications can exacerbate the effects of fenoterola.
Means for inhalation anesthesia, containing halogenated hydrocarbons (incl. halothane, trichlorethylene, enfluran) may increase the effect of fenoterola on cardiovascular system (may develop arrhythmias).
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.
The balloon is pressurized. You cannot open the container and heated to temperatures above 50° c.
