BEROTEK

Active material: Fenoterol
When ATH: R03AC04
CCF: Bronchodilators – beta₂-adrenomimetik
ICD-10 codes (testimony): J43, J44, J45, Z51.4
When CSF: 12.01.01.02.01
Manufacturer: BOEHRINGER Ingelheim International GmbH (Germany)

Pharmaceutical form, composition and packaging

The solution for inhalations clear, colorless or near colorless, free from particles, with an almost imperceptible odor.

Excipients: benzalkonium chloride, disodium эdetata digidrat, sodium chloride, hydrochloric acid, water distillirovannaya.

20 ml – amber glass vials (1) with dropper – packs cardboard.
40 ml – amber glass vials (1) with dropper – packs cardboard.
100 ml – amber glass vials (1) with dropper – packs cardboard.

Pharmacological action

Bronchodilators, selective beta₂-adrenomimetik. Contacting the β₂-adrenoreceptor, 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 the influence of such factors as bronhokonstriktornyh 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, an increase of mukociliarnogo clearance. Fenoterol has also shown respiratory stimulant properties.

Beta-adrenergic effect of the drug on cardiac function, such as increased heart rate and force of heart contractions, due to the action of vascular fenoterol, стимуляцией b₂-adrenoreceptors of the heart, and when used in doses, exceeding therapeutic, стимуляцией b₁-adrenoreceptorov. Tremor is the most common undesirable effect when using beta-agonist.

There is insufficient data on the impact of fenoterola hydrobromide on metabolism in diabetes mellitus.

The most commonly observed effect of stimulants β₂-adrenoceptor is tremor. In contrast to the effects on bronchial smooth muscle stimulators for systemic effects β₂-adrenergic receptors may develop tolerance.

Fenoterol warns and quickly eliminates bronhospazm different Genesis. Home of the drug after inhalation – through 5 m, maximum action – through 30-90 m, duration – 3-6 no.

Pharmacokinetics

Absorption

Depending on the method of inhalation and inhalation system used around 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.

The time to reach C_max – 2 no.

Distribution

Plasma protein binding – 40-55%.

Fenoterola hydrobromide penetrates through the placental barrier and is excreted in breast milk.

Metabolism

Metabolised in the liver by conjugation with sulphates mainly in 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;

as a basic means of ingalaciei other medications (antibiotics, mukolitikov, GCS);

-for undertaking tests expanding study of respiratory function.

Dosage regimen

The drug is prescribed inhalation. It should be taken into account, what 20 drops = 1 ml, 1 drop contains 50 mcg fenoterola hydrobromide. Treatment out under the supervision of a physician.

To cupping attacks of bronchial asthma adult (including elderly patients) and children over 12 years appointed 0.5 ml (10 drops = 500 μg fenoterola hydrobromide). IN severe cases appointed 1-1.25 ml (20-25 drops = 1-1.25 mg fenoterola hydrobromide). IN very severe cases appointed 2 ml (40 drops = 2 mg fenoterola hydrobromide).

To cupping attacks of bronchial asthma children aged 6 to 12 years (body weight 22-36 kg) appointed 0.25-0.5 ml (5-10 drops = 250-500 mcg fenoterola hydrobromide). IN severe cases appointed 1 ml (20 drops = 1 mg fenoterola hydrobromide). IN very severe cases appointed 1.5 ml (30 drops = 1.5 mg fenoterola hydrobromide).

To Prevention of bronchial asthma physical effort adult (including elderly patients) and children aged 6 to 12 years (body weight 22-36 kg) appointed 0.5 ml (10 drops = 500 μg fenoterola hydrobromide) 4 times / day.

To symptomatic treatment of bronchial asthma and other conditions, accompanied by reversible airway narrowing, adult (including elderly patients) and children aged 6 to 12 years (body weight 22-36 kg) appointed 0.5 ml (10 drops = 500 μg fenoterola hydrobromide) 4 times / day.

Children under 6 years (weighing less than 22 kg) because, Information about use of the drug in this age group is limited, recommended next dose (only under medical supervision): 50 mg / kg (5-20 drops = 0.25-1 mg) 3 times / day. Treatment starts with the lowest recommended dose.

Terms of use of the drug

The recommended dose should be diluted with saline to a final volume, constituent 3-4 ml, and apply (fully) using a nebulizer.

Inhalation Solution should not be diluted with distilled water.

Dilution should be carried out every time before use; the remains of the diluted solution should be destroyed.

Dosage can depend on the method of inhalation and kind of inhaler. The duration of inhalation can be controlled by spending diluted volume.

Mortar for inhalations can be applied using commercially available inhalers. In the presence of oxygen-breathing equipment solution ingalirovti better when flow velocity 6-8 l / min. If necessary, the subsequent inhalation out at intervals of not less than 4 no.

Side effect

The most common adverse effects They are fine tremor of skeletal muscles, nervousness, headache, dizziness, tachycardia, increased heart.

Cardio-vascular system: rarely (when used in high doses) – lowering diastolic pressure, increased systolic pressure, Arrhythmia, angina.

Metabolism: giperglikemiâ, severe hypokalemia.

Co respiratory system: cough, Local irritation; rarely - paradoxical bronchospasm.

From the digestive system: nausea, vomiting.

Other: There may be increased sweating, weakness, myalgia, muscle spasms, the weakening of the motility of the upper sections of the urinary tract, tolerance; rarely – skin or allergic reactions (especially in patients with a heightened sensitivity).

Contraindications

- Dryness;

- Gipertroficheskaya obstruktivnaya cardiomyopathy;

- Hypersensitivity to the drug.

FROM caution should be prescribed for patients with diabetes, recent myocardial infarction, heavy cardiovascular diseases, hypertension, hypotension, intestinal atony, gipertireoze, pheochromocytoma, hypokalemia.

Pregnancy and lactation

The results of the preclinical experimental research in conjunction with the experience of clinical application of drug Berotek^® indicates, that it does not cause any adverse events during pregnancy. Nonetheless, should exercise normal caution against use of drugs during pregnancy (especially in the first third of the).

Remember about depressing effects on uterine activity oxytocics fenoterola.

Preclinical studies have shown, that fenoterol enters breast milk. The safety of the drug in lactation has not been established.

Cautions

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^® increasing doses to relieve bronchial obstruction can cause uncontrolled deterioration of the disease. In the case of reinforcement of bronchial obstruction simply increasing doses of Beroteka^® more recommended for a long time not only is not 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^® 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).

The simultaneous application Beroteka^® with holinoliticakimi and mukoliticakimi drugs (Atrovent, Lazolvan in the form of solutions for inhalation and/or aerosol containers with a metering valve).

Overdose

Symptoms: may cause symptoms, associated with excessive stimulation of β-adrenergic receptors, – tachycardia, increased heart, tremor, arterial hypertension, hypotension, an increase in pulse pressure, angina, Arrhythmia, flushing of the face.

Treatment: use of sedatives, trankvilizatorov, in severe cases, shows intensive symptomatic therapy.

As specific antidotes recommended appointment cardioselective beta₁-adrenoblokatorov. It is necessary to take into account the possible reinforcement of bronchial obstruction and carefully pick up the dose of these drugs in patients with bronchial asthma.

Drug Interactions

Together with the use of beta-adrainomimetikov, anticholinergics, Xanthine derivatives (eg, teofillina), GCS, diuretics may increase side effects.

Possibly significant weakening of bronchodilator action fenoterola while applying beta-adrenoblokatorov.

Should be cautious appoint Berotek^® 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, halothane, trichlorethylene, enfluran) may increase the effect of fenoterola on cardiovascular system (may develop arrhythmias due to sensitization myocardial fenoterolu).

Joint appointment with other bronholitikami with similar mechanism of action leads to additive effect and development overdose.

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 30 ° C; Do not freeze. Shelf life – 5 years.