Berotek N, aerosol 100 mcg/dose 200 doses

Berotec N is a bronchodilator.

Preferentially stimulates beta₂-adrenoreceptors. It relaxes the smooth muscles of the bronchi and blood vessels and counteracts the development of bronchospastic reactions caused by histamine, methacholine, cold air and allergens (immediate-type hypersensitivity reactions). Immediately after prescription, fenoterol blocks the release of mediators of inflammation and bronchoobstruction from mast cells. In addition, when using fenoterol in higher doses, increased mucociliary clearance has been noted.

The beta-adrenergic effects of the drug on cardiac activity (increased strength and HR) are due to the vascular action of fenoterol, the stimulation of beta₂ adrenoreceptors of the heart, and when using doses higher than the therapeutic doses, stimulation of beta₁ adrenoreceptors. Tremor is the most common undesirable effect when using beta-agonists.

The drug reduces myometrial contractile activity and tone.

Pharmacodynamics

Phenoterol prevents and quickly stops bronchospasm of various genesis. Onset of action after inhalation – 5 minutes, maximum – 30-90 minutes, duration – 3-6 hours.

Pharmacokinetics

. Depending on the inhalation method and the inhalation system used, about 10-30% of the active ingredient released from the aerosol product after inhalation reaches the lower airways, and the rest is deposited in the upper airways and swallowed. As a result, some amount of inhaled fenoterol enters the GI tract. After inhalation of 1 dose of the drug, the degree of absorption is 17% of the administered dose. Absorption is biphasic – 30% of phenoterol hydrobromide is quickly absorbed with T_1/2 11 min, and 70% is slowly absorbed with T_1/2 120 min.

After oral administration, approximately 60% of phenoterol hydrobromide is absorbed. Time to reach plasma C_max is 2 hours. Binding to plasma proteins is 40-55%. Metabolized in the liver. It is excreted by kidneys and with bile as inactive sulphate conjugates.

In parenteral administration, fenoterol hydrobromide is excreted according to a three-phase model with T_1/2 of 0.42 min, 14.3 min and 3.2 h. Biotransformation of fenoterol hydrobromide in humans proceeds exclusively by conjugation with sulfates primarily in the intestinal wall.

Phenoterol hydrobromide may pass unchanged through the placental barrier and into the breast milk.

Indications

Prevention and management of bronchospasm in bronchial asthma, chronic obstructive bronchitis, pulmonary emphysema.

Prevention of asthma of physical effort.

The symptomatic treatment of bronchial asthma and chronic obstructive pulmonary disease.

Active ingredient

Composition

Active ingredient:

Phenoterol hydrobromide – 100 mcg.

Auxiliary substances:

citric acid anhydrous – 0.001 mg,

ethanol absolute – 15.597 mg,

purified water – 1.04 mg,

1,1,1,1,2-tetrafluoroethane (HFA 134a, propellant) – 35.252 mg.

How to take, the dosage

Adults and adolescents over 12 years of age

Bronchial asthma attacks and other conditions with reversible airway obstruction

In most cases 1 inhaled dose is sufficient to stop bronchospasm; if no relief of breathing occurs within 5 minutes, inhalation may be repeated.

If there is no relief after 2 doses, and additional inhalations are needed, you should talk to your doctor right away.

Preventing physical effort asthma

1 to 2 inhaled doses before exercise, up to 8 inhalations/day.

Children 6 to 12 years of age

Bronchial asthma attacks and other conditions with reversible airway obstruction

In most cases, 1 inhaled dose is sufficient to relieve bronchospasm; if no relief of breathing occurs within 5 minutes, inhalation may be repeated.

If there is no effect after 2 inhalations, and additional inhalations are needed, you should seek medical advice right away.

Preventing physical effort asthma

1 to 2 inhaled doses before exercise, up to 8 inhalations/day.

Children 4 to 6 years of age

Because of limited experience with use in children younger than 6 years of age, the drug should only be used as prescribed by a physician and under adult supervision.

Bronchial asthma attacks and other conditions accompanied by reversible airway obstruction

One inhaled dose is sufficient to relieve bronchospasm. If there is no effect, medical attention should be sought without delay.

Prevention of physical effort asthma

1 inhaled dose before exercise, up to 4 inhalations/day.

The rules for use of the medication

The dosed aerosol must be used correctly for maximum effect.

The first time you use a metered dose aerosol, press the bottom of the spray twice.

The following rules should be followed each time you use the aerosol dispenser.

The can is designed for 200 inhalations. The can should be changed after that. The can may still have some content, but the amount of medicine released will decrease.

The inhaler should be flushed at least once a week.

It is important to keep the tip of the inhaler clean so that the medicine does not accumulate and block the spray.

To clean, first remove the dust cap and remove the container from the inhaler. Rinse the inhaler with warm water to remove any accumulated medication and/or visible dust.

After cleaning, shake the inhaler and allow it to air dry without the use of heating devices. When the mouthpiece is dry, put the container and dust cap back in place.

The plastic mouthpiece is designed specifically for Berotec® H metered-dose aerosol and is used for precise dispensing of the product. The mouthpiece should not be used with other dispensed aerosols. Berotec® H Dispensed Aerosol must also not be used with other adapters.

Interaction

Beta-adrenomimetics and anticholinergic agents, xanthine derivatives (including theophylline), cromoglycic acid, GCS and diuretics may increase the effect and side effects of fenoterol. The bronchodilator effect of fenoterol may be significantly impaired with concomitant use of beta-adrenoblockers.

Berotec® H should be used with caution in patients receiving MAO inhibitors and tricyclic antidepressants because these drugs can potentiate the effects of fenoterol.

The agents for inhalation anesthesia containing halogenated hydrocarbons (including halothane, trichloroethylene, enflurane) may increase the effect of fenoterol on the cardiovascular system (possible arrhythmias). Simultaneous administration of bronchodilators with a similar mechanism of action leads to additive effects and overdose phenomena.

Special Instructions

When using Berotec® H aerosol for the first time, patients may notice that the new aerosol tastes slightly different from the previous Freon-containing aerosol. Patients should be warned about this when switching from Berotec® H containing Freon to Berotec® H that does not contain Freon. Patients should be aware that Berotec® H containing Freon and Berotec® H not containing Freon are fully interchangeable and that changes in taste do not affect the efficacy or safety of the product.

Other sympathomimetic bronchodilators may be used with Berotec®H only under medical supervision. In acute, rapidly increasing dyspnea (difficulty in breathing), consult a physician immediately.

Long-term use:

If bronchial obstruction worsens, it is unacceptable and may even be risky to increase the frequency of β2 adrenoreceptor agonists contained in products such as Berotec® N inhalation aerosol dosed beyond the recommended doses. In such a situation, the treatment plan and especially the adequacy of anti-inflammatory therapy should be reviewed.

The treatment with β2 adrenoreceptor agonists may result in severe hypokalemia. Particular caution should be exercised in severe bronchial asthma since this effect may be enhanced by concomitant use of xanthine derivatives, GCS and diuretics. In hypoxia, the effect of hypokalemia on the heart rate may increase. In such situations, regular monitoring of serum potassium concentration is recommended.

In rare cases, myocardial ischemia associated with β2 adrenoreceptor agonists has been observed.

Hypokalemia in patients who receive digoxin increases sensitivity to cardiac glycosides and may cause arrhythmias.

Impact on driving and operating ability

There is no established effect of the drug on the patient’s ability to perform work requiring increased attention and quick psychomotor reactions.

Contraindications

Hypersensitivity, hypertrophic obstructive cardiomyopathy, tachyarrhythmias, cardiac defects, aortic stenosis, decompensated diabetes, thyrotoxicosis, glaucoma, threatened abortion, pregnancy (I trimester).

Side effects

Immune system disorders: hypersensitivity.

Metabolism disorders: hypokalemia.

Nervous system disorders: agitation, nervousness, tremor, headache, dizziness.

Cardiovascular system disorders: myocardial ischemia, arrhythmia, tachycardia, palpitations, increased systolic BP, decreased diastolic BP.

Respiratory system: paradoxical bronchospasm, irritation of the larynx and pharynx.

Digestive system disorders: nausea, vomiting.

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

Muscular system disorders: muscle spasm, myalgia, muscle weakness.

Overdose

Symptoms: tachycardia, palpitations, tremors, decreased/increased BP, increased pulse pressure, anginal pain, arrhythmias and facial hyperemia.

Treatment: prescription of sedatives, tranquilizers, in severe cases intensive symptomatic therapy is indicated. As specific antidotes the prescription of beta-adrenoblockers (preferably selective beta1-adrenoblockers) is recommended. However, it is necessary to consider the possibility of increasing bronchial obstruction and choose the dose of these drugs carefully in patients with bronchial asthma.