Ipraterol-Aeronative aerosol 20mcg + 50mcg/dose 200doses
- 3 or more $21.80
- Availability:In Stock
Ipraterol-Aeronative instructionYou can buy Ipraterol-Aeronative on this pagepharmachologic effectCombined bronchodilator. Contains two components that have broncholytic activity: ipratropium bromide-m-cholinoblocker, and fenotero..
You can buy Ipraterol-Aeronative on this page
Combined bronchodilator. Contains two components that have broncholytic activity: ipratropium bromide-m-cholinoblocker, and fenoterol hydrobromide-beta2-adrenomimetic.
Ipratropium bromide is a quaternary ammonium derivative possessing anticholinergic (parasympatolytic) properties. Bronchodilation in the inhalation of ipratropium bromide is mainly due to local, rather than systemic, anticholinergic action. Ipratropium bromide inhibits the reflexes caused by the vagus nerve, counteracting the effects of acetylcholine - a mediator released from the ends of the vagus nerve. Anticholinergic drugs prevent an increase in the intracellular concentration of calcium ions, which occurs due to the interaction of acetylcholine with muscarinic receptors located on the smooth muscles of the bronchi. The release of calcium ions is mediated by a system of secondary mediators, including inositol triphosphate and diacylglycerin. Ipratropium bromide does not adversely affect the secretion of mucus in the respiratory tract, mucociliary clearance and gas exchange.
Fenoterol selectively stimulates β2-adrenergic receptors in a therapeutic dose. Stimulation of β1-adrenergic receptors occurs when fenoterol is used in high doses. Fenoterol relaxes the smooth musculature of the bronchi and vessels and counteracts the development of bronchospastic reactions due to the influence of histamine, methacholine, cold air and allergens (immediate-type hypersensitivity reactions). Immediately after administration, fenoterol blocks the release of inflammatory mediators and bronchial obstruction from mast cells. In addition, with the use of fenoterol at higher doses, there was an increase in mucociliary clearance.
The effect of Ipraterol-aeronative on cardiac activity, such as an increase in heart rate and strength, is due to vascular effects of fenoterol, stimulation of β2-adrenergic receptors of the heart, and when used in doses exceeding therapeutic, the stimulation of β1-adrenergic receptors. As with the use of other beta-adrenergic drugs, the QTc interval was prolonged when applied in high doses.
The most common undesirable effect with the use of β-adrenoreceptor agonists is tremor. In contrast to the effect on the smooth muscles of the bronchi, tolerance can develop in the systemic effect of β-adrenergic agonists, but the clinical significance of this manifestation is not clear.
In the joint application of ipratropium bromide and fenoterol bronchodilator effect is achieved by affecting various pharmacological targets. These substances complement each other, as a result of increased spasmolytic effect on the muscles of the bronchi and provides a great breadth of therapeutic effect for bronchopulmonary diseases, accompanied by airway obstruction. Complementary action is such that to achieve the desired effect, a lower dose of beta-adrenergic component is required, which allows individual selection of an effective dose with almost no side effects.
In patients with bronchospasm associated with COPD (chronic bronchitis and emphysema), a significant improvement in lung function (increase in FEV1 and peak exhalation rate by 15% or more) was noted within 15 minutes, the maximum effect was achieved after 1-2 hours and continued at most patients up to 6 h after administration.
The therapeutic effect of the combination of ipratropium bromide and fenoterol hydrobromide is a consequence of local action in the airways. There is no evidence that the pharmacokinetics of the combined preparation is different from that of each of the individual components.
In inhalation administration, ipratropium bromide is characterized by extremely low absorption from the mucous membrane of the respiratory tract. The concentration of the active substance in the plasma is at the lower limit of the determination, and it can be measured only by applying high doses of the active substance. After inhalation in the lungs, 10-30% of the administered dose of Ipraterol usually falls (depending on the dosage form and inhalation method). Most of the dose is swallowed and enters the digestive tract. Part of the dose of Ipraterol-aeronative, which enters the lungs, quickly reaches the systemic blood flow (within a few minutes). The total systemic bioavailability of ipratropium bromide, used by inhalation, is 7-28%.
Being a derivative of quaternary nitrogen, it dissolves poorly in fats and weakly penetrates biological membranes. Do not cumulate. Ipratropium bromide binds to plasma proteins to a minimum degree (less than 20%).
Metabolised in the liver. It is known up to 8 metabolites of ipratropium, which bind weakly to muscarinic receptors. It is excreted primarily through the intestine, as well as by the kidneys. About 25% is excreted unchanged, the rest - in the form of numerous metabolites.
Depending on the inhalation method and the inhalation system used, about 10-30% of the active substance reaches the lower respiratory tract, the rest is deposited in the upper respiratory tract and swallowed. As a result, a certain amount of inhaled fenoterol enters the digestive tract. Absorption is biphasic in nature - 30% of fenoterol is rapidly absorbed from T1 / 2 11 min, 70% is absorbed slowly from T1 / 2 120 min. There is no correlation between plasma concentrations of fenoterol achieved after inhalation and AUC. The prolonged bronchodilator effect of the drug after inhalation, comparable to the corresponding effect achieved after intravenous administration, is not supported by high concentrations of active substance in the systemic circulation. After oral administration, about 60% of fenoterol is absorbed. Time to reach Cmax in blood plasma - 2 h.
Binding to plasma proteins is 40-55%. Fenoterol in unchanged form penetrates the placental barrier and is excreted in breast milk.
Metabolised in the liver. After 24 hours, 60% of the administered intravenous dose and 35% of the ingested dose is excreted in the urine. This fraction of the active substance undergoes biotransformation due to the effect of "first passage" through the liver, as a result of which the bioavailability of Ipraterol-aeronative after oral administration drops to approximately 1.5%. This explains why the swallowed amount of Ipraterol-Aeronativ has practically no effect on the level of the active substance in the blood plasma, reached after inhalation. Biotransformation of fenoterol in humans occurs mainly by conjugation with sulfates in the intestinal wall.
It is excreted by the kidneys and with bile in the form of inactive sulfate conjugates. When parenteral administration of fenoterol is derived, respectively, the three-phase model with T1 / 2 - 0.42 min, 14.3 min and 3.2 h.
Prevention and symptomatic treatment of obstructive airway diseases with reversible airway obstruction, such as bronchial asthma and especially COPD, chronic bronchitis with or without emphysema.
Contraindications for Ipraterol-aeronative
Hypertrophic obstructive cardiomyopathy; tachyarrhythmia; I and III trimesters of pregnancy; children under 6 years of age (aerosol for inhalation); hypersensitivity to fenoterol and other components of the drug; increased sensitivity to atropine-like drugs.
Precautions: closed-angle glaucoma, arterial hypertension, diabetes mellitus, recent myocardial infarction (within the last 3 months), heart and vascular disease (chronic heart failure, IHD, arrhythmia, aortic stenosis, severe cerebral and peripheral arterial lesions), hyperthyroidism, pheochromocytoma, prostatic hyperplasia, bladder neck obstruction, cystic fibrosis, second trimester of pregnancy, lactation period, children and adolescence from 6 to 18 years (aerosol for inhalation).
Solution for inhalation
The dose should be selected individually, depending on the severity of the attack. Treatment usually begins with the lowest recommended dose and is discontinued after a sufficient reduction in symptoms is achieved.
Treatment should be carried out under medical supervision (for example, in a hospital). Treatment at home is possible only after consulting a doctor in cases where a fast-acting β-adrenoceptor agonist at a low dose is not effective enough. A solution for inhalation can be recommended to patients in the case where the aerosol for inhalation can not be used or if it is necessary to use in higher doses.
In adults (including the elderly) and adolescents older than 12 years with acute attacks of bronchospasm, depending on the severity of the attack, the doses may vary from 1 ml (1 ml = 20 drops) to 2.5 ml (2.5 ml = 50 drops). In particularly severe cases, Ipraterol-aeronative can be used in doses as high as 4 ml (4 ml = 80 drops).
In children aged 6-12 years with acute attacks of bronchial asthma, depending on the severity of the attack, the doses can vary from 0.5 ml (0.5 ml = 10 drops) to 2 ml (2 ml = 40 drops).
In children under 6 years of age (body weight <22 kg), because the information on the use of Ipraterol in this age group is limited, the following dose is recommended (only under medical supervision): 0.1 ml (2 drops) per kg body weight, but not more than 0.5 ml (10 drops).
The solution for inhalation should be used only for inhalations (with a suitable nebulizer) and not to be used orally.
The recommended dose should be diluted with 0.9% solution of sodium chloride to a final volume of 3-4 ml, and used (completely) with a nebulizer.
Solution for inhalation should not be diluted with distilled water.
Dilution of the solution should be carried out every time before use; the remnants of the diluted solution should be destroyed.
The diluted solution should be used immediately after preparation.
The duration of inhalation can be controlled by the expenditure of diluted solution.
A solution for inhalation can be used using various commercial models of nebulizers. The dose reaching the lungs and the system dose depend on the type of nebulizer used and may be higher than the corresponding dose when using a metered aerosol (depending on the type of inhaler). In those cases where there is wall oxygen, the solution is best used at a flow rate of 6-8 l / min.
Follow instructions for the use, maintenance and cleaning of the nebulizer.
Aerosol for inhalation dosed
The dose is set individually.
For relief of seizures, adults and children older than 6 years are prescribed 2 inhalation doses. If no breathing is achieved within 5 minutes, another 2 inhalation doses may be prescribed.
The patient should be informed of immediate medical attention if there is no effect after 4 inhalation doses and the need for additional inhalations.
Dosage aerosol in children should only be used as directed by a doctor and under the supervision of adults.
For long-term and intermittent therapy, 1-2 inhalations are prescribed for 1 intake, up to 8 inhalations / day (on average, 1-2 inhalations 3 times / day).
In bronchial asthma, Ipraterol should be used only as needed.
The patient should be instructed on the correct use of the metered aerosol.
Before using the metered aerosol for the first time, press the bottom of the canister twice.
Each time using a metered aerosol, the following rules must be observed.
1. Remove the protective cap.
2. Make a slow, deep exhalation.
3. Holding the balloon, grasp the mouthpiece with your lips. The cylinder should be pointed upside down.
4. While making the deepest inhalation, simultaneously quickly press the bottom of the cylinder until the release of 1 inhalation dose. Hold the breath for a few seconds, then take the mouthpiece out of the mouth and exhale slowly. Repeat the procedure to obtain the 2nd inhalation dose.
5. Put the protective cap on.
6. If the aerosol canister has not been used for more than 3 days, it is advisable to press the bottom of the cylinder once before applying the aerosol cloud.
The cylinder is designed for 200 inhalations. Then the cylinder should be replaced. Despite the fact that some contents may remain in the container, the amount of drug released by inhalation decreases.
Since the balloon is opaque, the amount of the drug in the bottle can be determined as follows: removing the plastic mouthpiece from the balloon, the balloon is immersed in a container filled with water. The amount of the preparation is determined depending on the position of the cylinder in the water.
The inhaler should be cleaned at least once a week. It is important to keep the mouthpiece of the inhaler clean so that Ipraterol particles do not block the release of the aerosol.
During cleaning, first remove the protective cap and remove the balloon from the inhaler. A jet of warm water is passed through the inhaler; It is necessary to be convinced of removal of a preparation and-or visible mud. After cleaning, shake the inhaler and allow it to air dry without using heaters. As soon as the mouthpiece has dried, insert the balloon into the inhaler and put on the protective cap.
The contents of the cylinder are under pressure. The cylinder should not be opened and subjected to heating above 50 ° C.
Side effects of Ipraterol-aeronative
The incidence of adverse reactions was determined in accordance with WHO recommendations: very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10 000, <1/1000); very rarely (<1/10 000), including individual messages; the frequency is unknown (the frequency can not be calculated from the available data).
On the part of the immune system: rarely - hypersensitivity reactions, anaphylactic reactions.
From the side of metabolism and nutrition: rarely - hypokalemia, metabolic acidosis.
Disorders of the psyche: infrequently - nervousness; rarely - a sense of anxiety, mental disorders.
From the nervous system: infrequently - headache, dizziness, tremor.
From the side of the organ of vision: rarely - glaucoma, increased intraocular pressure, accommodation disorders, mydriasis, blurred vision, eye pain, corneal edema, conjunctiva hyperemia, the appearance of an aura around objects and colored spots before the eyes.
From the side of the cardiovascular system: infrequently - tachycardia, palpitation, increased systolic blood pressure; rarely - arrhythmia, atrial fibrillation, supraventricular tachycardia, myocardial ischemia, increased diastolic blood pressure.
From the respiratory system: often - cough; infrequently - pharyngitis, dysphonia; rarely - bronchospasm, irritation of the pharynx, edema of the pharynx, laryngospasm, paradoxical bronchospasm, dryness of the pharynx.
On the part of the digestive system: infrequently - vomiting, dry mouth, nausea; rarely - stomatitis, glossitis, gastrointestinal motility disorders, constipation, diarrhea, edema of the oral cavity.
Dermatological reactions: rarely - urticaria, skin rash, itching, angioedema, hyperhidrosis.
From the musculoskeletal system: rarely - muscle weakness, myalgia, muscle spasm.
From the urinary system: rarely - urine retention.
Simultaneous use of other beta-adrenomimetics, anticholinergics and xanthine derivatives (for example, theophylline) can enhance the bronchodilator effect of Ipraterol.
Perhaps a significant weakening of the bronchodilator action of Ipraterol with the simultaneous administration of beta-blockers.
Hypokalemia associated with the use of beta-adrenomimetics can be enhanced by the simultaneous use of xanthine derivatives, corticosteroids and diuretics. This fact should be given special attention in the treatment of patients with severe forms of obstructive airway disease.
Hypokalemia can lead to an increased risk of arrhythmias in patients receiving digoxin. In addition, hypoxia can increase the negative effect of hypokalemia on the heart rhythm. In such cases, it is recommended to monitor the concentration of potassium in the blood serum.
Caution should be used to prescribe beta2-adrenomimetics to patients receiving MAO inhibitors and tricyclic antidepressants; these drugs can enhance the action of beta-adrenergic drugs.
The use of inhaled halogenated anesthetics, for example, halothane, trichlorethylene or enflurane, can enhance the effect of beta-adrenergic agents on the cardiovascular system.
Joint use of the drug with cromoglycic acid and / or GCS increases the effectiveness of therapy.
special instructions for Ipraterol-aeronative
The patient should be informed that in case of sudden rapid increase of dyspnea (difficulty breathing), you should immediately consult a doctor.
Ipraterol can cause a paradoxical bronchospasm, which can endanger life. If paradoxical bronchospasm develops, the drug should be stopped immediately and switched to alternative therapy.
In patients with bronchial asthma, Ipraterol should be used only as needed. In patients with mild COPD, symptomatic treatment may be preferable to regular use.
Patients with bronchial asthma should be aware of the need to conduct or enhance anti-inflammatory therapy to control the inflammatory process of the airways and the course of the disease.
Regular use of increasing doses of preparations containing beta2-adrenomimetics for the relief of bronchial obstruction can cause uncontrolled worsening of the course of the disease. In the case of increased bronchial obstruction, an increase in the dose of beta2-agonists is more than recommended for a long time, not only is not justified, but also dangerous. To prevent a life-threatening deterioration in the course of the disease, consideration should be given to reviewing the patient's treatment plan and adequate anti-inflammatory therapy with inhaled corticosteroids.
Other sympathomimetic bronchodilators should be administered simultaneously with the drug only under medical supervision.
Disturbances on the part of the organ of sight
Ipraterol should be administered with caution to patients who are predisposed to developing a closed-angle glaucoma. There are some reports of complications from the visual organ (eg, increased intraocular pressure, mydriasis, angle-closure glaucoma, eye pain) that develop when inhaled ipratropium bromide (or ipratropium bromide in combination with β2-adrenergic receptor agonists) enters the eye. Symptoms of acute closed-angle glaucoma may be pain or discomfort in the eyes, blurred vision, the appearance of a halo in subjects and color spots in front of the eyes in combination with corneal edema and red eyes, due to conjunctival vascular injection. If any combination of these symptoms is noted, the use of eye drops that reduce intraocular pressure and immediate specialist advice is indicated. Patients should be instructed about the proper use of the inhalation solution. To prevent the solution from entering the eyes, it is recommended that the solution used by the nebulizer be inhaled through the mouthpiece. If there is no mouthpiece, use a face mask that fits snugly. Particular care should be taken to protect the eyes of patients predisposed to developing glaucoma.
With such diseases as recent myocardial infarction, diabetes mellitus with inadequate glycemic control, severe organic diseases of the heart and vessels, hyperthyroidism, pheochromocytoma or obstruction of the urethra (for example, with prostatic hyperplasia or bladder neck obstruction), Ipraterol should only be prescribed after a thorough assessment of the risk / benefit ratio, especially when used at doses exceeding the recommended levels.
Influence on the cardiovascular system
In postmarketing studies, there were rare cases of myocardial ischemia with adrenoceptor agonists. Patients with concomitant serious cardiac diseases (eg, ischemic heart disease, arrhythmias or severe heart failure) receiving the drug should be warned of the need to see a doctor if there is heart pain or other symptoms indicating a worsening of heart disease. It is necessary to pay attention to such symptoms as shortness of breath and chest pain. they can be both cardiac and pulmonary etiology.
When using β2-adrenoreceptor agonists, hypokalemia may occur.
In athletes, the use of Ipraterol, in connection with the presence of phenoterol in its composition, can lead to positive results of doping tests.
The preparation in the form of an aerosol for inhalations contains a preservative, benzalkonium chloride, and a stabilizer-disodium edetate dihydrate. During inhalation, these components can cause bronchospasm in sensitive patients with airways hyperreactivity.
Impact on the ability to manage motor vehicles and mechanisms
The effect of the drug on the ability to manage motor vehicles and the use of mechanisms has not been specifically studied. However, patients need to be informed that during treatment with Ipraterol it is possible to develop such undesirable phenomena as dizziness, tremor, accommodation disorder, mydriasis, blurred vision. Therefore, care should be taken when driving vehicles or using mechanisms. If patients experience the above-mentioned undesirable feelings, one should refrain from such potentially dangerous actions as driving vehicles or controlling mechanisms.
Pregnancy and lactemia
Pre-clinical data and experience with the combination of ipratropium bromide and fenoterol indicate that the components of the drug do not adversely affect pregnancy. Consider the possibility of the inhibitory effect of fenoterol on contractile activity of the uterus. Ipraterol is contraindicated in the I and III trimesters of pregnancy (the possibility of weakening the labor of fenoterol). It should be used with caution in the II trimester of pregnancy.
Fenoterol is excreted in breast milk. Data confirming that ipratropium bromide penetrates into breast milk is not obtained. The use of the drug in the period of breastfeeding is possible only if the potential benefit to the mother exceeds the potential risk for the child.
Application in childhood
Aerosol for inhalation is contraindicated for use in children under 6 years of age.
Caution should be given to the preparation in the form of an aerosol for inhalation to patients aged 6 to 18 years.
Terms of sell
You can buy Ipraterol-aeronative without a prescription.