Ipraterol aeronautical
Ipraterol-aeronativ: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. Drug interactions
- 12. Analogs
- 13. Terms and conditions of storage
- 14. Terms of dispensing from pharmacies
- 15. Reviews
- 16. Price in pharmacies
Latin name: Ipratropium-aeronativ
ATX code: R03AL01
Active ingredient: fenoterol (Fenoterol), ipratropium bromide (Ipratropium Bromide)
Manufacturer: JSC Pharmstandard-Leksredstva (Russia); Nativa, OOO (Russia)
Description and photo update: 2019-08-07
Prices in pharmacies: from 296 rubles.
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Ipraterol-aeronautical is a combined bronchodilator, m-cholinergic receptor blocker.
Release form and composition
The drug is produced in the form of an aerosol for inhalation metered: a clear solution, colorless or with a slight yellow tint, when leaving the container, it is sprayed in the form of an aerosol stream (200 doses of a solution under pressure, in stainless steel cylinders with a dosing valve and a spray nozzle, in a cardboard box 1 cylinder and instructions for use of Ipraterol-aeronaut).
1 dose contains:
- active ingredients: ipratropium bromide monohydrate - 0.021 mg (equivalent to the content of 0.02 mg ipratropium bromide); fenoterol hydrobromide - 0.05 mg;
- auxiliary components: absolute ethanol, triethyl citrate, citric acid monohydrate, propellant R134a (1,1,1,2-tetrafluoroethane).
Pharmacological properties
Pharmacodynamics
Ipraterol-aeronautic is a combined bronchodilator containing two components with bronchodilator activity: ipratropium bromide and fenoterol.
The active components of the Ipraterol aerosol aerosol complement each other's action, enhancing the spasmolytic effect on the muscles of the bronchi, which provides a wide range of therapeutic action for bronchopulmonary pathologies accompanied by airway obstruction. The complementary action contributes to the achievement of the desired clinical effect when using a lower dose of the beta-adrenergic component. That allows for an individual selection of an effective dose that almost does not cause side effects.
Ipratropium bromide
M-anticholinergic, a quaternary ammonium derivative, inhibits reflexes that are triggered by the vagus nerve. Possessing anticholinergic (parasympatholytic) properties, ipratropium bromide, as a result of the interaction of acetylcholine with muscarinic receptors of bronchial smooth muscles, helps prevent an increase in the intracellular content of calcium ions. Calcium ions are indirectly released by the system of secondary mediators, including inositol triphosphate (ITP) together with diacylglycerol (DAG).
When administered by inhalation, the bronchodilating effect of ipratropium bromide is mainly due not to systemic, but to local anticholinergic action. With bronchospasm associated with such chronic obstructive pulmonary diseases as chronic bronchitis or pulmonary emphysema, an increase in peak expiratory flow rate by 15% (or more) and forced expiratory volume in 1 second is noted within 1/4 hour. The maximum effect is achieved within 1–2 hours after administration and in most cases lasts 6 hours.
The negative effect of ipratropium bromide on gas exchange, mucus secretion in the airways or mucociliary clearance has not been established.
Fenoterol
Beta 2 -adrenergic agonist; in a therapeutic dose, selectively excites beta 2 -adrenergic receptors, when high doses are used, its effect on beta 1 -adrenergic receptors is activated. This explains such a beta-adrenostimulating effect of the drug on cardiac activity, such as an increase in heart rate (HR) and their strength, as well as an increase in the QTc interval.
After administration, fenoterol immediately blocks the release of mediators of inflammation and bronchial obstruction from mast cells, has a relaxing effect on the smooth muscles of the bronchi and blood vessels. Prevents the development of immediate hypersensitivity reactions (bronchospastic reactions caused by the influence of cold air, histamine, methacholine or allergens). In addition, with the use of higher doses of fenoterol, there is an increase in mucociliary clearance.
The systemic effects of fenoterol when used with metered-dose aerosol inhalers are noted if the recommended doses are exceeded. They may also be higher after using the drug with nebulizers (vials with a standard dose of solution for inhalation), compared with using at recommended doses using metered-dose aerosol inhalers. Most often, beta-adrenergic receptor agonists (beta 2 -adrenomimetics) are the cause of tremors.
The bronchodilatory (bronchodilatory) effect of ipratropium aeronautical is achieved as a result of the action of ipratropium bromide and fenoterol on various pharmacological targets.
Pharmacokinetics
Pharmacokinetic characteristics of ipratropium bromide:
- absorption: after inhalation, from 10 to 30% (depending on the inhalation system used) of the administered dose gets into the lungs and within a few minutes ipratropium bromide reaches the systemic circulation. The remainder of the dose, after swallowing, enters the gastrointestinal tract (GIT). When inhaled, the total systemic bioavailability of the substance is 7–28%;
- distribution: a biphasic decrease in the concentration of ipratropium bromide in plasma occurs rapidly. During the period of equilibrium concentration (Css), the apparent volume of distribution (Vd) is approximately 176 L or 2.4 L / kg. Through the blood-brain barrier, the placental barrier and into breast milk, the m-anticholinergic blocker does not penetrate, does not accumulate. Binds to plasma proteins at a level of less than 20%;
- metabolism: ipratropium bromide is metabolized mainly in the liver by oxidation with the formation of up to 8 metabolites that weakly bind to muscarinic receptors and are considered inactive;
- excretion: ipratropium bromide is excreted in the form of metabolites - 75%, the rest - unchanged, mainly through the intestines, partly by the kidneys.
Pharmacokinetic characteristics of fenoterol:
- absorption: the lower respiratory tract after inhalation of aerosol Ipraterol-aeronautical reaches about 10-30% fenoterol (depends on the inhalation system used); up to 70% of the dose is deposited in the upper respiratory tract and is swallowed, entering the gastrointestinal tract. Its absorption is biphasic, up to 30% is absorbed quickly, with a half-life (T 1/2) of 11 minutes; 70% - slowly with T 1/2 = 120 minutes. There is no correlation between the level of fenoterol in blood plasma after inhalation and the total plasma concentration of the substance in the blood (AUC). After inhalation, the bronchodilating effect of Ipraterol-aeronautic lasts from 3 to 5 hours, comparable to that after intravenous administration, high concentrations of the active substance in the systemic circulation are not maintained;
- distribution: during the period of equilibrium concentration (Css), the apparent volume of distribution (Vd) of fenoterol is approximately 189 l or 2.7 l / kg. Plasma protein binding occurs at a level of 40–55%. Fenoterol is intensively distributed throughout organs and tissues, overcomes the placental barrier unchanged, is excreted in breast milk;
- metabolism: the substance is metabolized in the liver by conjugation with sulfates and glucuronides. The swallowed dose is biotransformed due to the effect of the first passage through the liver, it does not affect the level of the active substance in the blood plasma achieved after inhalation;
- excretion: approximately 85% of fenoterol is biotransformed, including excretion in the bile; after inhalation within 24 hours through the kidneys 2% of the dose is excreted unchanged.
In patients with diabetes mellitus, the pharmacokinetics of the combination of ipratropium bromide and fenoterol have not yet been studied.
Indications for use
The use of aerosol Ipraterol-aeronautical is indicated for the prevention and symptomatic therapy of the following respiratory diseases with reversible obstruction:
- bronchial asthma;
- chronic obstructive pulmonary disease;
- chronic bronchitis, uncomplicated or complicated by pulmonary emphysema.
Contraindications
Absolute:
- tachyarrhythmia;
- hypertrophic obstructive cardiomyopathy;
- I trimester of pregnancy;
- age up to 6 years;
- hypersensitivity to ipratropium bromide and other atropine-like drugs, fenoterol and / or auxiliary components of the drug.
Precautions should be taken to prescribe the aerosol Ipraterol-aeronative for cystic fibrosis, severe organic diseases of the heart and blood vessels, arterial hypertension, chronic heart failure, arrhythmia, coronary heart disease, aortic stenosis, within 3 months after myocardial infarction, with angle-closure glaucoma, insufficiently controlled sugar diabetes, bladder neck obstruction, prostatic hyperplasia, hyperthyroidism, pheochromocytoma, children and adolescents aged 6–18 years, in the II – III trimester of pregnancy, during lactation.
Ipraterol-aeronativ, instructions for use: method and dosage
Aerosol Ipraterol-aeronautical is used by inhalation, by spraying into the oral cavity.
Patients should be instructed on the rules for inhalation with a metered aerosol.
Before using the inhaler for the first time, check its operation. After removing the protective cap from the mouthpiece and shaking the inhaler well, press the bottle, directing the jet into the air. It is recommended that similar testing be performed after a week or longer break in the use of the balloon.
During the procedure, patients comply with the rules and the following sequence of actions:
- Remove the protective cap from the inhaler mouthpiece and vigorously shake its contents.
- They make a slow and full exhalation, holding the balloon upside down, tightly clasp the mouthpiece with your lips.
- Take the deepest possible inhalation while simultaneously quickly pressing on the bottom of the balloon to simultaneously release one dose.
- They hold their breath for a few seconds, after which they remove the mouthpiece from the mouth and exhale slowly through the nose.
- The procedure is repeated if necessary to take a second inhalation dose.
- Close the mouthpiece after inhalation with a protective cap.
The dose is selected individually, taking into account clinical indications.
Recommended dosage for patients over 6 years of age:
- seizure therapy: usually 2 doses; if within 5 minutes the symptoms are not stopped and breathing is not relieved, an additional inhalation of 2 doses is indicated. If there is no effect after 4 doses, the patient needs immediate medical attention;
- intermittent and long-term treatment: on average, 1-2 inhalation doses 3 times a day; the maximum amount per day should not exceed 8 inhalations. In bronchial asthma, the procedure should be carried out only to relieve seizures.
The use of Ipraterol Aeronautic in children should be carried out only under the supervision of adults.
The rules for caring for the inhaler should be followed. Once every 7 days, it is required to rinse the inhaler mouthpiece with warm water. To do this, you need to remove the can from the plastic case, rinse the case and cap under running water and dry them. Then put the can in the case and put on the cap. Do not immerse a metal can in water.
After 200 inhalations, the balloon should be replaced.
It should be borne in mind that a special plastic mouthpiece is provided only for accurate dosing of Ipraterol Aeronautic and should not be used with other metered aerosols.
The solution of the drug is in the container under pressure, therefore, it must not be opened or allowed to heat above 50 ° C!
Side effects
- from the respiratory system, chest and mediastinal organs: often - cough; infrequently - dysphonia, pharyngitis; rarely - dryness of the pharynx, irritation of the pharynx, bronchospasm, laryngospasm, pharyngeal edema, paradoxical bronchospasm;
- from the nervous system: infrequently - headache, tremor, dizziness;
- mental disorders: infrequently - nervousness; rarely - anxiety, mental disorders (mental disorders);
- on the part of the organ of vision: rarely - eye pain, increased intraocular pressure, blurred vision, conjunctival hyperemia, accommodation disturbances, corneal edema, mydriasis, the appearance of colored spots before the eyes and a halo around the observed objects, glaucoma;
- from the heart: infrequently - palpitations, tachycardia; rarely - myocardial ischemia, arrhythmia, atrial fibrillation, supraventricular tachycardia, atrial fibrillation;
- from the side of metabolism and nutrition: rarely - hypokalemia;
- from the gastrointestinal tract: infrequently - dry mouth, nausea, vomiting; rarely - oral edema, glossitis, stomatitis, gastrointestinal motility disorders, diarrhea, constipation;
- dermatological reactions: rarely - skin rash, itching, urticaria, sweating;
- from the musculoskeletal system: rarely - muscle weakness, myalgia, muscle spasms;
- from the urinary system: rarely - urinary retention;
- from the immune system: rarely - hypersensitivity reactions, Quincke's edema, anaphylactic reactions;
- laboratory and instrumental indicators: infrequently - increased systolic blood pressure; rarely - a decrease or increase in diastolic blood pressure.
Overdose
- symptoms: the appearance of tremor, arterial hypertension or arterial hypotension, palpitations, tachycardia, angina pectoris, arrhythmias, flushing of the face, metabolic acidosis, hyperglycemia, hypokalemia, an increase in pulse pressure, i.e. an increase in the interval between systolic and diastolic blood pressure. Perhaps - a violation of accommodation, a feeling of dry mouth;
- treatment: the use of aerosol Ipraterol-aeronautical should be discontinued, sedatives and tranquilizers should be taken, in case of a serious condition of the patient, intensive therapy is recommended taking into account the indicators of the acid-base balance of the blood. It is possible to use selective beta-blockers as a specific antidote. When selecting a dose of a beta-blocker for patients with bronchial asthma or chronic obstructive pulmonary disease, the likelihood of increased bronchial obstruction, the risk of severe bronchospasm, including fatal ones, should be taken into account.
special instructions
In cases of a rapid unexpected increase in shortness of breath (difficulty breathing), an urgent need to consult a doctor.
There is a risk of an immediate hypersensitivity reaction, the manifestations of which may be urticaria, rash, bronchospasm, oropharyngeal edema, Quincke's edema, anaphylactic shock.
Paradoxical bronchospasm can pose a threat to life, therefore, if it occurs, an immediate cessation of the use of the ipraterol aerosol aerosol is required and the appointment of alternative therapy.
With prolonged use of the drug in patients with bronchial asthma, it should be used only as needed. It is important to consider the need to conduct or enhance concomitant anti-inflammatory therapy, which will control the inflammatory processes of the respiratory tract and the course of bronchial asthma.
For mild chronic obstructive pulmonary disease, symptomatic therapy may be preferable to regular use.
The systematic use of increasing doses of Ipraterol-aeronautical in order to relieve bronchial obstruction contributes to an uncontrolled worsening of the course of the disease. With increased bronchial obstruction, the use of a dose of beta 2 -adrenomimetics higher than the recommended dose for a long time poses a danger to the patient's life. Therefore, in order to prevent the worsening of the course of the disease with an insufficient effect of the drug, a new treatment regimen for the patient should be prescribed, involving the simultaneous use of adequate doses of inhaled glucocorticosteroids. The use of other sympathomimetic bronchodilators in combination with the ipraterol aerosol aerosol should be carried out only under medical supervision.
Patients should be instructed on the need to protect their eyes from accidental ingestion of the solution, especially if they have a predisposition to angle-closure glaucoma. Symptoms of acute angle-closure glaucoma include conjunctival hyperemia, corneal edema and redness of the eyes, blurred vision, eye pain or discomfort, color spots or halos around objects. If any combination of the listed symptoms appears, you should consult a specialist.
When prescribing the drug to patients after a recent myocardial infarction with severe organic diseases of the heart and blood vessels, insufficiently controlled diabetes mellitus, pheochromocytoma, hyperthyroidism or obstruction of the urinary tract, it is necessary to take into account the systemic effects that Ipraterol aeronautical can cause, and carefully weigh the potential risk and benefits of the proposed therapy.
Ipraterol aeronautical has a negative effect on the cardiovascular system, therefore, patients with concomitant serious cardiac pathologies should consult a doctor if they develop pain in the heart and other symptoms that indicate worsening heart disease. It should be borne in mind that shortness of breath and chest pain can be symptoms of both pulmonary and cardiac etiology.
With the use of beta 2 -adrenomimetics, the risk of hypokalemia increases. With hypoxia, the negative effect of hypokalemia on the heart rate may increase.
In athletes, the use of Ipraterol-aeronautical can cause positive results of doping tests, this is due to the presence of fenoterol in the aerosol.
Influence on the ability to drive vehicles and complex mechanisms
During the period of treatment, patients are advised to be careful when performing potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions, due to the risk of adverse reactions. In case of blurred vision, mydriasis, dizziness, tremor, violation of accommodation, one should refrain from driving and working with complex mechanisms.
Application during pregnancy and lactation
The use of Ipraterol aeronautical in the first trimester of pregnancy is contraindicated.
It is recommended to be careful when prescribing the drug in the II and III trimesters of pregnancy or during lactation. Consideration should be given to the inhibitory effect of ipraterol aeronautical on uterine contractility.
The safety of using this combined bronchodilator during breastfeeding has not been established, therefore, during lactation, the use of an aerosol is allowed only in cases where the therapeutic effect for the mother exceeds the potential threat to the child.
Pediatric use
The use of the Ipraterol aerosol aerosol is contraindicated for the treatment of children under 6 years of age.
The drug should be prescribed with caution to children and adolescents aged 6-18 years.
Dosed aerosol for inhalation in children should be used under the supervision of adults.
Drug interactions
- beta-adrenomimetics, anticholinergics (including systemic action), theophylline and other xanthine derivatives: these drugs can enhance the bronchodilatory effect of the aerosol and aggravate side effects;
- beta-blockers: a combination with beta-blockers can significantly weaken the bronchodilatory effect of ipraterol aeronautical;
- diuretics, xanthine derivatives, glucocorticosteroids: as part of concomitant therapy, they can cause an increase in hypokalemia associated with taking beta-adrenergic agonists. Therefore, during the period of treatment, the level of potassium in the blood serum should be monitored, especially in patients with severe obstructive respiratory diseases;
- Digoxin: Patients with hypokalemia receiving digoxin may have an increased risk of arrhythmias;
- monoamine oxidase inhibitors, tricyclic antidepressants, oxytocin, levodopa, levothyroxine: these agents can cause an increase in the beta-adrenergic action of the drug;
- inhalation agents for general anesthesia (including enflurane, halothane, trichlorethylene): inhalation of these agents may increase the adverse effect of ipraterol aeronautical on the cardiovascular system.
Analogs
The analogues of Ipraterol-aeronativ are Ipraterol-native, Berodual, Berodual N, Fenipra, Inspirax, Astmasol-SOLOfarm and others.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C away from heating devices in a dark place, do not freeze.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Ipraterol-aeronaut
In most cases, patients leave positive reviews about the ipraterol aerosol aerosol. In chronic obstructive pulmonary disease, it is noted that with the use of the drug, shortness of breath and cough are significantly reduced. Used to relieve attacks of bronchial asthma, Ipraterol aeronautical acts instantly.
The disadvantages of the drug most often include an unpleasant aftertaste after the procedure.
The price of Ipraterol-aeronaut in pharmacies
The price of Ipraterol-aeronautical for a package containing 1 aerosol can is about 370 rubles.
Ipraterol-aeronativ: prices in online pharmacies
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Drug name Price Pharmacy |
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Ipraterol aeronautic 20 mcg / dose + 50 mcg / dose 200 doses aerosol for inhalation metered dose 10 ml 1 pc. 296 r Buy |
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Ipraterol-Aeronativ aerosol for in. dosage. 20mcg + 50mcg / dose 200 doses 357 r Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
