Description
Release form
Dosage inhalation aerosol.
Packing
Bottle of 10 ml.
Pharmacological action
Combined bronchodilator. It contains two components with bronchodilator activity: ipratropium bromide – m-anticholinergic, and fenoterol hydrobromide – beta2-adrenergic agonist.
When inhaled, ipratropium bromide bronchodilation is mainly due to local and not systemic anticholinergic action.
ipratropium bromide is a quaternary ammonium compound. It has anticholinergic (parasympatolytic) properties. Ipratropium inhibits reflexes mediated by the vagus nerve, counteracting the effect of acetylcholine, a neurotransmitter released from nerve endings. Anticholinergics prevent an increase in the intracellular concentration of cyclic guanosine monophosphate (cGMP) in the smooth muscles of the bronchi, arising from the interaction of acetylcholine with m-cholinergic receptors.
Significant improvement in lung function (increase in FEV1 and the average volumetric rate of forced expiration by 15% or more) in patients with COPD with bouts of bronchospasm occurs within 15 minutes, the maximum effect is achieved after 1-2 hours and continues in most patients up to 6 hours after administration .
In 40% of patients with bronchospasm associated with bronchial asthma, there is a significant improvement in lung function (increase in FEV1 by 15% or more).
Ipratropium bromide does not adversely affect mucus secretion in the airways, mucociliary clearance, and gas exchange.
Fenoterol hydrobromide has a direct sympathomimetic effect. At therapeutic doses, it selectively stimulates bronchial β 2 -adrenoreceptors. At higher doses, it has the ability to stimulate 1-adrenergic receptors. Binding to β 2 -adrenoreceptors activates adenylate cyclase with the participation of a stimulating Gs protein. An increased level of cyclic AMP activates protein kinase A, which then phosphorylates the target proteins in smooth muscle cells. This, in turn, leads to phosphorylation of the myosine kinase light chain, inhibition of the hydrolysis of phosphoinositide and the opening of potassium channels activated by calcium.
Fenoterol relaxes the smooth muscles of the bronchi and blood vessels and counteracts the development of bronchospastic reactions due to the effects of histamine, methacholine, cold air and allergens (immediate hypersensitivity reactions). Immediately after administration, fenoterol blocks the release of bronchoconstrictor inflammatory mediators from mast cells. The use of phenoterol in higher doses increases mucociliary clearance.
At higher plasma concentrations of fenoterol, uterine contractility is inhibited. In addition, when used in high doses, metabolic effects are observed: lipolysis, glycogenolysis, hyperglycemia and hypokalemia. Hypokalemia is mainly due to increased incorporation of potassium ions into skeletal muscle.
Beta-adrenergic effect of the drug on cardiac activity, such as an increase in heart rate and heart rate, is due to the vascular effect of fenoterol, stimulation of 2-adrenoreceptors of the heart, and when used in doses exceeding therapeutic, stimulation of 1-adrenergic receptors. As with other beta-adrenergic drugs, a prolongation of the QTc interval was observed when used in high doses.
The most commonly observed undesirable effect of 2-adrenoreceptor stimulants is tremor. In contrast to exposure to smooth muscles of the bronchi, systemic effects of stimulants of β 2 -adrenoreceptors may develop tolerance.
Fenoterol prevents the development of bronchoconstriction caused by various stimuli, such as physical activity, cold air and allergens (immediate hypersensitivity reactions).
With the combined use of ipratropium bromide and phenoterol, the bronchodilating effect is achieved by exposure to various pharmacological targets. These substances complement each other, as a result, the bronchodilator effect is enhanced and a wide range of therapeutic effects is provided for bronchopulmonary diseases accompanied by constriction of the respiratory tract. The complementary effect is such that to achieve the desired effect, a lower dose of the beta-adrenergic component is required, which facilitates the individual dosage of the drug and helps to minimize side effects.
Indications
Prevention and symptomatic treatment of obstructive airways diseases with reversible bronchospasm:
COPD.
Bronchial asthma.
Chronic bronchitis, complicated or not complicated by emphysema.
Contraindications
Hypertrophic obstructive cardiomyopathy.
Tachyarrhythmia.
I trimester of pregnancy.
Children under 6 years old.
Hypersensitivity to the drug.
Hypersensitivity to atropine-like substances.
Precautions: use the drug for angle-closure glaucoma, coronary insufficiency, arterial hypertension, inadequately controlled diabetes mellitus, recent myocardial infarction, severe organic diseases of the cardiovascular system, hyperthyroidism, pheochromocytoma, prostatic hypertrophy, obstruction of the bladder neck, with cystic fibrosis, in children over 6 years old.
Use during pregnancy and lactation
The drug is contraindicated for use in the first trimester of pregnancy and during lactation (breastfeeding). given the ability of many drugs to pass into breast milk. Berodual ®N should be used with caution during lactation (breastfeeding).
Special instructions
For prolonged use in patients with bronchial asthma or mild to moderate forms of COPD, symptomatic treatment may be preferable to regular use.
With prolonged use in patients with bronchial asthma or steroid-dependent forms of COPD, remember that it is necessary to conduct or strengthen anti-inflammatory therapy to control the inflammatory process of the respiratory tract and the course of the disease.
Regular use of Berodual N in increasing doses for relief of bronchial obstruction can cause uncontrolled worsening of the disease. In the case of increased bronchial obstruction, a simple increase in the dose of Berodual H more than recommended for a long time is not only not justified, but also dangerous. To prevent life-threatening deterioration of the course of the disease, consideration should be given to revising the patient’s treatment plan and adequate anti-inflammatory therapy with inhaled corticosteroids.
The patient should be informed that in case of sudden development and rapid progression of shortness of breath, it is necessary to consult a doctor.
Other sympathomimetic bronchodilators should be administered concurrently with Berodual H only under medical supervision.
The patient should be informed about the rules for using the inhaler.
Pain in the eye, blurred vision, sensation of a halo or colored spots in front of the eyes combined with reddening of the eye as a conjunctival or corneal injection can be signs of an acute attack of angle-closure glaucoma. If these symptoms appear in any combination, the patient should begin treatment with eye drops, which cause narrowing of the pupil, and immediately seek specialized medical help.
Patients with a history of cystic fibrosis may have gastrointestinal motility disorders when using Berodual N.
Consideration should be given to the need for concomitant anti-inflammatory therapy for COPD in patients with corticosteroids and bronchial asthma.
Composition
1 dose contains:
active ingredients: fenoterol hydrobromide 50 mg ipratropium bromide monohydrate, 21 mg, which corresponds to the content of ipratropium bromide 20 mcg.
excipients: absolute ethanol, purified water, citric acid, tetrafluoroethane (HFA 134a, propellant).
Dosage and administration
Dose set individually.
To stop asthma attacks, adults and children over 6 years of age are prescribed 2 inhalation doses. If breathing relief does not occur within 5 minutes, another 2 inhalation doses may be prescribed.
The patient should be informed that if there is no effect after 4 inhalation doses and the need for additional inhalations, consult a doctor immediately.
Dosage aerosol Berodual ®N in children should be used only as directed by a doctor and under the supervision of adults.
For prolonged and intermittent therapy, 1-2 inhalations per 1 dose are prescribed, up to 8 inhalations / day (on average, 1-2 inhalations 3 times / day).
Terms of use of the drug
The patient should be instructed on the proper use of metered-dose aerosol. Before using metered-dose aerosol for the first time, double-click on the bottom of the spray can.
The following rules must be observed every time you use a metered-dose aerosol:
Remove the protective cap.
Take a slow, deep exhale.
Holding the bottle, grasp the mouthpiece with your lips. The cylinder should be directed upside down.
Taking the deepest breath possible, simultaneously quickly press the bottom of the container until 1 inhaled dose is released. Hold your breath for a few seconds, then remove the mouthpiece from your mouth and slowly exhale. Repeat for the 2nd inhalation dose.
Put on the protective cap.
If the aerosol can has not been used for more than 3 days, before use it is necessary to press the bottom of the cylinder once until an aerosol cloud appears.
The cylinder is designed for 200 inhalations. Then the cylinder should be replaced. Although some contents may remain in the balloon, the amount of drug released during inhalation is reduced.
Side effects
From the side of the central nervous system: often – small tremor of skeletal muscle, nervousness sometimes – headache, dizziness, (especially in patients with aggravating factors) in isolated cases – mental changes.
From the cardiovascular system: sometimes – tachycardia, palpitations (especially in patients with risk factors) rarely (when used in high doses) – decreased diastolic blood pressure, increased systolic blood pressure, arrhythmia, fibrillation, supraventricular tachycardia.
From the side of the water-electrolyte balance: sometimes – severe hypokalemia.
From the side of the respiratory system: sometimes – cough, local irritation (pharyngitis) rarely – paradoxical bronchospasm.
From the digestive system: often – dry mouth sometimes – nausea, vomiting rarely – reversible gastrointestinal motility (constipation, diarrhea).
From the side of the organ of vision: rarely – reversible disturbance of accommodation, mydriasis, increased intraocular pressure, angle-closure glaucoma, pain in the eyeball.
Allergic reactions: rarely – skin rash, angioedema of the tongue, lips, face, urticaria, laryngospasm, laryngeal edema, anaphylactic shock.
Other: increased sweating, weakness, myalgia, cramps are rare – reversible urinary retention.
Drug Interactions
Beta-adrenergic agonists and anticholinergics, xanthine derivatives (including theophylline) can enhance the bronchodilator effect of Berodual H.
When other beta-adrenergic agonists enter the systemic anticholinergic blood stream .h. theophylline) may increase side effects.
Perhaps a significant weakening of the bronchodilator action of Berodual N with the simultaneous appointment of beta-blockers.
With simultaneous use with MAO inhibitors and tricyclic antidepressants, the effect of Berodual N. is enhanced.
With the use of Berodual H, hypokalemia may develop, which can be enhanced when given simultaneously with xanthine derivatives, corticosteroids and diuretics. This fact should be considered when treating patients with severe obstructive airway diseases.
Hypokalemia increases the risk of arrhythmias in patients receiving digoxin. In addition, with hypoxia, the negative effect of hypokalemia on the heart rate is enhanced. In such cases, it is recommended that serum potassium levels be monitored.
Inhalation anesthetics containing halogenated hydrocarbons (including halothane, trichlorethylene, enflurane) can enhance the effect of Berodual H on the cardiovascular system.
overdose
Symptoms are mainly due to the action of phenoterol hydrobromide and are caused by excessive stimulation of -adrenoreceptors: tachycardia, palpitations, tremor, arterial hypo- or hypertension, increased a pulsaritis.
Symptoms of overdose and ipratropium bromide: dry mouth, disturbance of accommodation – in connection with the wide breadth of therapeutic action and inhalation use, as a rule, are little expressed and have a transient character.
Treatment: prescription of sedatives, tranquilizers. If necessary – intensive care. As a specific antidote, the use of beta-blockers, preferably selective beta-blockers, is possible. However, it should be remembered that there may be an increase in bronchial obstruction under the influence of beta blockers and a careful dose selection for patients with bronchial asthma or COPD, due to the risk of severe bronchospasm, which can be fatal.
Storage conditions
Keep out of the reach and sight of children at temperatures not exceeding 25 ° C.
The contents of the cylinder are under pressure. The cylinder cannot be opened and heated above 50 ° C.
Shelf life
3 years.
Prescription conditions
pharmacy Prescription
Dosage form
aerosol for inhalation
Prescribing
Prescribing
Nursing mothers, As prescribed by a doctor, Doctor as prescribed by a doctor, Pregnant women as prescribed by a doctor 6 years old
Beringer Ingelyhaym, Austria
