2010/12/17

Berotec

Release form, composition and packing Berotec 
Solution for inhalation transparent, colorless or nearly colorless, free from particles, with an almost imperceptible odor. 1 ml (20 drops), fenoterol hydrobromide, 1 mg. Excipients: benzalkonium chloride, disodium edetate dihydrate, sodium chloride, hydrochloric acid, distilled water.

Clinico-pharmacological group: bronchodilator medication - beta 2-adrenoceptor agonists.

Pharmacological action

Bronchodilator medication, beta2-adrenoceptor agonists. Binding to β2-adrenoceptors, activates adenylyl cyclase via Gs-protein stimulyatorny with subsequent increase of cAMP formation, which in turn activates protein kinase A. The latter phosphorylates the target protein in the cells of smooth muscles, which in turn leads to phosphorylation of myosin light chain kinase, inhibition fosfoinozina hydrolysis and opening of calcium-activated potassium channels fast.

Thus, fenoterol, relaxes smooth muscles of the bronchi and vessels, and also prevents the development of bronchospasm due to the influence of such factors bronhokonstriktornyh as histamine, methacholine, cold air and allergies (immediate type reaction). After taking the drug inhibited the release of mast cell inflammatory mediators.

In addition, after receiving fenoterol at high doses there is increasing mucociliary transport. Fenoterol also shows properties of a stimulator of respiration. Beta-adrenergic effect of the drug on heart function, such as increasing the frequency and strength of heart contractions, due to the vascular action of fenoterol, stimulation of β2-adrenergic receptors of heart, and with the use of doses higher than therapeutic, the stimulation of β1-adrenergic receptors. While taking the drug at high doses the effect is observed at the level of metabolism: lipolysis, glycogenolysis, hyperglycemia, and hypokalemia (the latter is due to increased absorption of potassium of skeletal muscle).

Fenoterol (at high concentrations) inhibits the contractile activity of the uterus. There is insufficient data on the impact of fenoterol hydrobromide on metabolism in diabetes mellitus. Fenoterol alerts and quickly relieves bronchospasm various origins (physical exercise, cold air, the early response to exposure to the allergen). Onset of action of the drug after inhalation - 5 minutes, maximum action - through 30-90 minutes duration - 3-6 hours

Pharmacokinetics

Suction

Depending on the method of inhalation and the inhalation system used by about 10-30% of fenoterol hydrobromide reaches the lower respiratory tract, and the rest is deposited in the upper respiratory tract and swallowed. As a result, a number of inhaled fenoterol hydrobromide enters the gastrointestinal tract. After inhalation of one dose level of absorption is 17% of the dose. Absorption is biphasic: 30% of fenoterol hydrobromide sucked period poluabsorbtsii 11 min, 70% is absorbed slowly with a period poluabsorbtsii 120 min. There is no correlation between the values of the concentration of fenoterol in the blood plasma is reached after inhalation, and the pharmacodynamic curve "time effect".

Prolonged bronchodilatory effect of the drug (3-5 h) after inhalation, comparable with the corresponding effect is achieved after IV administration is not supported by high concentrations of the active substance in the systemic circulation. After oral administration, absorbed about 60% of an oral dose. This part of the active substance biotransformation due to the effect of "first passage" through the liver.

As a result, bioavailability after oral administration is reduced to 1.5%. This explains the fact that the amount of drug swallowed almost no effect on the concentration of the active substance in the blood plasma is reached after inhalation. Time to reach Cmax - 2 hours

Distribution

Plasma protein binding - 40-55%. Fenoterol hydrobromide crosses the placental barrier and is excreted in breast milk.

Metabolism

Biotransformed in the liver by conjugation with sulphates mainly in the intestinal wall.

Breeding

Excreted in the urine and bile as inactive sulphate conjugates.

Statement
relief of asthma attacks;
prevention of exercise-induced asthma;
symptomatic treatment of bronchial asthma or other conditions, accompanied by a reversible narrowing of the airways (including obstructive bronchitis). In patients with bronchial asthma and chronic obstructive pulmonary disease responding to therapy with corticosteroids should be considered the need for concomitant anti-inflammatory therapy;
As bronhorasshiryayuschego funds to inhalation of other drugs (antibiotics, mucolytics, corticosteroids);
for bronchodilation tests in the study of respiratory function.

Dosing regimen

Inhaled drug is prescribed. Keep in mind that 20 drops = 1 ml, 1 drop contains 50 micrograms of fenoterol hydrobromide.

Treatment is carried out under the supervision of a physician. For relief of asthma attacks for adults (including elderly patients) and children over 12 years, to appoint 0.5 ml (10 drops = 500 mg fenoterol hydrobromide). In severe cases, appoint 1-1.25 ml (20-25 drops = 1-1.25 mg fenoterol hydrobromide). In very severe cases, appoint 2 ml (40 drops = 2 mg fenoterol hydrobromide).

Children aged 6 to 12 years (body mass 22-36 kg) designate 0.25-0.5 ml (5-10 drops = 250-500 micrograms fenoterol hydrobromide). In severe cases, take 1 ml (20 drops = 1 mg fenoterol hydrobromide). In extreme cases prescribed 1.5 ml (30 drops = 1.5 mg fenoterol hydrobromide).

For the prevention of bronchial asthma of physical effort for adults (including elderly patients) and children aged 6 to 12 years (body mass 22-36 kg) to designate 0.5 ml (10 drops = 500 mg fenoterol hydrobromide), 4 times / day.

For the symptomatic treatment of bronchial asthma and other conditions involving a reversible narrowing of airways, adults (including elderly patients) and children aged 6 to 12 years (body mass 22-36 kg) to designate 0.5 ml (10 drops = 500 mg fenoterol hydrobromide), 4 times / day.

Children under 6 years of age (weighing less than 22 kg) due to the fact that information about the use of the drug in this age group is limited, we recommend the use of the next dose (only with medical supervision): 50 mg / kg (5-20 drops = 0.25-1 mg) 3 times a day.

Treatment is initiated with the lowest dose.

Terms of use of the drug

The recommended dose should be diluted with saline to a final volume of 3-4 mL, and apply (in full) with the help of an inhaler.

Solution for inhalation should not be diluted with distilled water. Dilution of the solution should be carried out each time before use; residues diluted solution should be destroyed. Dosing may depend on the method of inhalation and type of inhaler. The duration of inhalation can be controlled by spending diluted volume. Solution for inhalation can be applied using a commercially available inhalers. In the presence of oxygen breathing apparatus better solution inhaled at a flow rate of 8.6 l / min. If necessary, spend the next inhalation at intervals of not less than 4 hours

Side effect

The most common adverse effects are fine tremor of skeletal muscles, nervousness, headache, dizziness, tachycardia, increased heart rate.
With the cardiovascular system: rarely (when used in high doses) - decrease in diastolic pressure, increased systolic blood pressure, arrhythmia, angina.
From a metabolism: Hyperglycemia, hypokalemia expressed.
Co of the respiratory system: cough, local irritation, rarely - paradoxical bronchospasm.
From the digestive system: nausea, vomiting.

Other: possible increased sweating, fatigue, myalgia, muscle cramps, weakening of the motility of upper urinary tract is rare - the skin or allergic reactions (especially in patients with hypersensitivity).

Contraindications
tachyarrhythmia;
hypertrophic obstructive cardiomyopathy;
Hypersensitivity to fenoterol hydrobromide and other ingredients.

Precautions should be prescribed the drug in diabetes, recent myocardial infarction, severe diseases of the cardiovascular system, hypertension, hypotension, intestinal atony, hyperthyroidism, pheochromocytoma, hypokalemia.

Pregnancy, lactation

Revealed no adverse effects of the drug on pregnancy. Nevertheless, during pregnancy (especially in the I trimester) drug is given only in cases where the expected benefit to the mother justifies the potential risk to the fetus. Should be aware of the oppressive fenoterol on uterine contractile activity. It is known that fenoterol is excreted in breast milk. Safety of the drug during lactation is not established.

Cautions

In case of sudden appearance and rapid progression of dyspnea the patient should also consult a doctor immediately. Regular use berotek in increasing doses for relief of bronchial obstruction can cause uncontrolled deterioration of the disease.

In the event the bronchial obstruction simply increasing the dose

Berotek longer recommended for a long time not only justified, but also dangerous. To prevent life-threatening deterioration of the disease should consider revising the treatment plan the patient and an adequate anti-inflammatory therapy with inhaled corticosteroids. Other sympathomimetic bronchodilators should be administered simultaneously with berotek only under medical supervision. In the appointment of beta2-agonists may develop hypokalemia.

In this regard, special care is required in severe asthma, as In this case, hypokalemia may result from the simultaneous use of beta2-agonists, ksantinovyh derivatives, steroids and diuretics. In addition, hypoxia may increase the influence of hypokalemia on cardiac rhythm. It is recommended that monitoring of potassium levels in blood plasma.