Inspirax 20mcg + 50mcg/dose 200doses

Inspirax instruction

You can buy Inspirax here

The metered-dose aerosol for inhalation is colorless or light yellow, or light brown. or with a brownish-yellowish tint, a clear solution with the smell of ethanol, which is under pressure in a metal monoblock container with a metering valve, equipped with an inhaler nozzle with a protective cap; the drug is sprayed in the form of an aerosol cloud when exiting the container.
1 dose
ipratropium bromide monohydrate 0.021 mg
which corresponds to the content of ipratropium bromide 0.02 mg
fenoterol hydrobromide 0.05 mg
Excipients: ethanol (absolute ethyl alcohol) - 13.313 mg, purified water - 0.799 mg, anhydrous citric acid - 0.001 mg, hydrofluoroalkane (HFA-134a) - 39.07 mg.
200 doses - metal cylinders (1) with a metering valve and a spray nozzle - cardboard packs.

pharmachologic effect

Combined bronchodilator drug. It contains two components with bronchodilator activity: ipratropium bromide - m-anticholinergic, and fenoterol hydrobromide - beta2-adrenergic agonist.
Ipratropium bromide is a quaternary ammonium derivative with anticholinergic (parasympatolytic) properties. Bronchodilation with the inhalation of ipratropium bromide is mainly due to local and not 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. Anticholinergics 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 diacylglycerol. Ipratropium bromide does not adversely affect mucus secretion in the airways, mucociliary clearance and gas exchange.
Fenoterol selectively stimulates β2-adrenergic receptors in a therapeutic dose. Stimulation of β1-adrenergic receptors occurs with the use of phenoterol in high doses. 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 inflammatory mediators and bronchial obstruction from mast cells. In addition, with the use of phenoterol in higher doses, an increase in mucociliary clearance was noted.
The effect of Inspirax on cardiac activity, such as an increase in the frequency and strength of heart contractions, is due to the vascular effect of phenoterol, stimulation of β2-adrenergic receptors of the heart, and when used in doses exceeding therapeutic, stimulation of β1-adrenergic receptors. As with other beta-adrenergic drugs, the QTc interval was prolonged when used in high doses.
The most common adverse effect when using β-adrenoreceptor agonists is tremor. In contrast to the effect on the smooth muscles of the bronchi, tolerance may develop to the systemic influence of β-adrenoreceptor agonists, however, the clinical significance of this manifestation has not been elucidated.
With the combined use of ipratropium bromide and fenoterol, the bronchodilating effect is achieved by exposure to various pharmacological targets. These substances complement each other, as a result, the antispasmodic effect on the muscles of the bronchi is enhanced and a wide range of therapeutic effects is provided for bronchopulmonary diseases accompanied by airway obstruction. The complementary effect is such that to achieve the desired effect, a lower dose of the beta-adrenergic component is required, which allows you to individually select an effective dose with almost no side effects.
In patients with bronchospasm associated with COPD (chronic bronchitis and pulmonary emphysema), a significant improvement in lung function (increase in FEV1 and peak expiratory flow rate by 15% or more) was noted for 15 minutes, the maximum effect was achieved after 1-2 hours and continued in most patients up to 6 hours after administration.

Pharmacokinetics

The therapeutic effect of the combination of ipratropium bromide and phenoterol hydrobromide is a consequence of local action in the respiratory tract. There is no evidence that the pharmacokinetics of the combination drug is different from that of each of the individual components.

Ipratropium bromide

With the inhalation route of 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 boundary of the determination, and it can only be measured using high doses of the active substance. After inhalation, 10-30% of the administered dose of Inspirax usually gets into the lungs (depending on the dosage form and method of inhalation). Most of the dose is swallowed and enters the digestive tract. The part of the dose that reaches the lungs quickly reaches the systemic circulation (within a few minutes). The total systemic bioavailability of ipratropium bromide, used by inhalation, is 7-28%.
Being a derivative of quaternary nitrogen, it is poorly soluble in fats and weakly penetrates biological membranes. Does not cumulate. Ipratropium bromide binds to plasma proteins to a minimum extent (less than 20%).
Metabolized in the liver. Up to 8 ipratropium metabolites are known, which weakly bind to muscarinic receptors. It is excreted mainly through the intestines, as well as by the kidneys. About 25% is excreted unchanged, the rest - in the form of numerous metabolites.

Fenoterol

Depending on the method of inhalation 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 phenoterol enters the gastrointestinal tract. Absorption is biphasic - 30% of phenoterol is rapidly absorbed with T1 / 2 for 11 minutes, 70% is absorbed slowly with T1 / 2 for 120 minutes. There is no correlation between plasma concentrations of phenoterol achieved after inhalation and AUC. The long bronchodilating effect of Inspirax after inhalation, comparable with the corresponding effect achieved after iv administration, is not supported by high concentrations of the active substance in the systemic circulation. After oral administration, about 60% of phenoterol is absorbed. The time to reach Cmax in plasma is 2 hours.
Binding to plasma proteins 40-55%. Fenoterol in unchanged form crosses the placental barrier and is excreted in breast milk.
Metabolized in the liver. After 24 hours, 60% of the intravenous dose and 35% of the oral dose are excreted in the urine. This fraction of the active substance undergoes biotransformation due to the effect of the "first passage" through the liver, as a result of which the bioavailability of Inspirax after oral administration drops to approximately 1.5%. This explains the fact that the swallowed amount of Inspirax has almost no effect on the level of the active substance in the blood plasma achieved after inhalation. Biotransformation of phenoterol in humans proceeds predominantly by conjugation with sulfates in the intestinal wall.
It is excreted by the kidneys and with bile in the form of inactive sulfate conjugates. With parenteral administration, fenoterol is derived, respectively, in a three-phase model with T1 / 2 - 0.42 min, 14.3 min and 3.2 h.

Indications

Prevention and symptomatic treatment of obstructive airways diseases with reversible airway obstruction, such as bronchial asthma and especially COPD, chronic bronchitis with or without pulmonary emphysema.

Dosage regimen

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 stopped after a sufficient reduction in symptoms has been 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 those cases when a fast-acting β-adrenergic receptor agonist in a low dose is not effective enough. The inhalation solution can be recommended for patients in the case when the aerosol for inhalation cannot be used or, if necessary, use in higher doses.
In adults (including the elderly) and adolescents over 12 years old with acute attacks of bronchospasm, depending on the severity of the attack, the doses can vary from 1 ml (1 ml = 20 drops) to 2.5 ml (2.5 ml = 50 drops). In especially severe cases, it is possible to use Inspirax in doses reaching 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 the age of 6 years (body weight <22 kg) due to the fact that information on the use of Inspirax in this age group is limited, it is recommended to use the following dose (only under medical supervision): 0.1 ml (2 drops) per kg body weight, but not more than 0.5 ml (10 drops).

Rules for using Inspirax

The solution for inhalation should be used only for inhalation (with a suitable nebulizer) and should not be used orally.
The recommended dose should be diluted with 0.9% sodium chloride solution to a final volume of 3-4 ml, and apply (completely) using a nebulizer.
The solution for inhalation should not be diluted with distilled water.
Dilution of the solution should be carried out each time before use; residues of 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 the diluted solution.
The inhalation solution can be used using various commercial nebulizer models. The dose reaching the lungs and the systemic dose depend on the type of nebulizer used and may be higher than the corresponding doses when using a metered-dose aerosol (which depends on the type of inhaler). In cases where there is wall oxygen, the solution is best used at a flow rate of 6-8 l / min.
Follow the instructions for use, maintenance and cleaning of the nebulizer.

Dosage inhalation aerosol

The dose is set individually.
To stop the 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 of immediate medical attention if there is no effect after 4 inhalation doses and the need for additional inhalations.
Dosage aerosol in children should be used only as directed by a doctor and under the supervision of adults.
For long-term and intermittent therapy, 1-2 inhalations per 1 dose are prescribed, up to 8 inhalations / day (on average, 1-2 inhalations 3 times / day).
In bronchial asthma, Inspirax should be used only as needed.

Rules for using 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.
Each time you use a metered-dose aerosol, the following rules must be observed.
1. Remove the protective cap.
2. Take a slow, deep exhale.
3. Holding the balloon, grasp the mouthpiece with your lips. The cylinder should be directed upside down.
4. Taking the deepest possible breath, simultaneously quickly press the bottom of the balloon 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.
5. Put on the protective cap.
6. If the aerosol container has not been used for more than 3 days, before use, press the bottom of the container once until an aerosol cloud appears.
The balloon 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.
Since the balloon is opaque, the amount of preparation in the balloon can be determined as follows: having removed the plastic mouthpiece from the balloon, the balloon is immersed in a container filled with water. The amount of drug is determined depending on the position of the container 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 the particles of Inspirax do not block the release of the aerosol.
During cleaning, first remove the protective cap and remove the balloon from the inhaler. A stream of warm water is passed through the inhaler; make sure to remove Inspirax and / or visible dirt. After cleaning, shake the inhaler and allow it to dry in air without using heaters. As soon as the mouthpiece dries, insert the bottle into the inhaler and put on the protective cap.
The contents of the container are under pressure. The cylinder must not be opened and exposed to heat above 50 ° C.

Side effect

The frequency 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 single messages; frequency is unknown (frequency cannot 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.
Mental disorders: infrequently - nervousness; rarely - a sense of anxiety, mental disturbances.
From the nervous system: infrequently - headache, dizziness, tremor.
From the side of the organ of vision: rarely - glaucoma, increased intraocular pressure, impaired accommodation, mydriasis, blurred vision, eye pain, corneal edema, conjunctival hyperemia, the appearance of a halo around objects and colored spots in front of the eyes.
From the cardiovascular system: infrequently - tachycardia, palpitations, 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, pharyngeal irritation, pharyngeal edema, laryngospasm, paradoxical bronchospasm, dry throat.
From the digestive system: infrequently - vomiting, dry mouth, nausea; rarely - stomatitis, glossitis, gastrointestinal motility, constipation, diarrhea, and swelling of the oral cavity.
Dermatological reactions: rarely - urticaria, skin rash, pruritus, angioedema, hyperhidrosis.
From the musculoskeletal system: rarely - muscle weakness, myalgia, muscle spasm.
From the urinary system: rarely - urinary retention.

Contraindications

Hypertrophic obstructive cardiomyopathy; tachyarrhythmia; I and III trimesters of pregnancy; children under 6 years old (aerosol for inhalation); hypersensitivity to fenoterol and other components of Inspirax; hypersensitivity to atropine-like drugs.
Precautions: angle-closure glaucoma, arterial hypertension, diabetes mellitus, recent myocardial infarction (within the last 3 months), diseases of the heart and blood vessels (chronic heart failure, coronary heart disease, arrhythmia, aortic stenosis, severe lesions of the cerebral and peripheral arteries), hyperthyroidism, pheochromocytoma, prostatic hyperplasia, obstruction of the bladder neck, cystic fibrosis, II trimester of pregnancy, lactation, childhood and adolescence from 6 to 18 years (aerosol for inhalation).

Pregnancy and lactation

Preclinical studies and experience with the combination of ipratropium bromide and fenoterol show that the components of Inspirax do not have a negative effect during pregnancy. The possibility of the inhibitory effect of phenoterol on the contractile activity of the uterus should be taken into account. Inspirax is contraindicated in the first and third trimesters of pregnancy (the possibility of weakening labor by fenoterol). Use the drug with caution in the second trimester of pregnancy.
Fenoterol is excreted in breast milk. No evidence has been obtained that ipratropium bromide passes into breast milk. The use of Inspirax during breastfeeding is possible only if the potential benefit to the mother outweighs the potential risk to the baby.

Use in children

Aerosol for inhalation is contraindicated in children under 6 years of age.
Precautions should be prescribed a drug in the form of an aerosol for inhalation to patients aged 6 to 18 years.

special instructions

The patient should be informed that in the event of an unexpectedly rapid increase in shortness of breath (difficulty breathing), consult a doctor immediately.
Paradoxical bronchospasm
Inspirax can cause paradoxical bronchospasm, which can be life threatening. In the case of the development of paradoxical bronchospasm, the use of the drug should be stopped immediately and switch to alternative therapy.

Long-term use

In patients with bronchial asthma, Inspirax should be used only as needed. In patients with mild COPD, symptomatic treatment may be preferable to regular use.
In patients with bronchial asthma, one should remember about the need to conduct or strengthen anti-inflammatory therapy to control the inflammatory process of the respiratory tract and the course of the disease.
The regular use of increasing doses of drugs containing beta2-adrenergic agonists to relieve bronchial obstruction can cause an 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 not justified, but also dangerous. To prevent a life-threatening worsening 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.
Other sympathomimetic bronchodilators should be prescribed simultaneously with Inspirax only under medical supervision.

Violations of the organ of vision

Inspirax should be prescribed with caution to patients predisposed to the development of angle-closure glaucoma. There are separate reports of complications from the organ of vision (for example, increased intraocular pressure, mydriasis, angle-closure glaucoma, eye pain) that developed when inhaled ipratropium bromide (or ipratropium bromide in combination with β2-adrenoreceptor agonists) gets into the eyes. Symptoms of acute angle-closure glaucoma can be pain or discomfort in the eyes, blurred vision, the appearance of a halo in objects and colored spots in front of the eyes in combination with corneal edema and redness of the eyes due to conjunctival injection of blood vessels. If any combination of these symptoms is noted, the use of eye drops that reduce intraocular pressure is indicated, and immediate consultation with a specialist. Patients should be instructed on the proper use of the inhalation solution. To prevent the solution from getting into the eyes, it is recommended that the solution used with a nebulizer be inhaled through the mouthpiece. In the absence of a mouthpiece, a mask should be used that fits close to the face. Particular care should be taken to protect the eyes of patients predisposed to the development of glaucoma.

System effects

In diseases such as recent myocardial infarction, diabetes mellitus with inadequate glycemic control, severe organic heart and vascular diseases, hyperthyroidism, pheochromocytoma or obstruction of the urethra (for example, with prostatic hyperplasia or obstruction of the bladder neck), the drug should only be prescribed after a thorough assessment of the risk / benefit ratio, especially when used in doses exceeding the recommended ones.

Effects on the cardiovascular system

Post-marketing studies have reported rare cases of myocardial ischemia when taking β-adrenoreceptor agonists. Patients with concomitant serious heart diseases (e.g., coronary heart disease, arrhythmias, or severe heart failure) receiving Inspirax should be warned about the need to see a doctor in case of pain in the heart or other symptoms indicating worsening heart disease. Symptoms such as shortness of breath and chest pain should be noted. they can be both cardiac and pulmonary etiology.

Hypokalemia

When using β2-adrenoreceptor agonists, hypokalemia may occur.
In athletes, the use of Inspirax, due to the presence of phenoterol in its composition, can lead to positive results of doping tests.

Excipients

The preparation in the form of an aerosol for inhalation contains a preservative, benzalkonium chloride, and a stabilizer - disodium edetate dihydrate. During inhalation, these components can cause bronchospasm in sensitive patients with airway hyperresponsiveness.

Impact on the ability to drive vehicles and mechanisms

The effect of Inspirax on the ability to drive vehicles and use mechanisms has not been specifically studied. However, patients must be informed that during treatment with the drug, the development of such undesirable effects as dizziness, tremor, disturbance of accommodation, mydriasis, blurred vision is possible. Therefore, caution should be recommended when driving or using machinery. If patients experience the above unwanted sensations, you should refrain from such potentially dangerous actions as driving vehicles or operating machinery.

Drug interaction

The simultaneous use of other beta-adrenergic agonists, anticholinergics, and xanthine derivatives (e.g., theophylline) can enhance the bronchodilator effect of Inspirax.
Perhaps a significant weakening of the bronchodilatory effect of the drug while the appointment of beta-blockers.
Hypokalemia associated with the use of beta-adrenergic agonists 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 heart rate. In such cases, it is recommended to monitor the concentration of potassium in the blood serum.
Beta2-adrenergic agonists should be prescribed with caution to patients receiving MAO inhibitors and tricyclic antidepressants, as these drugs can enhance the effects of beta-adrenergic drugs.
The use of inhaled halogenated anesthetics, for example, halothane, trichlorethylene or enfluran, may enhance the effect of beta-adrenergic agents on the cardiovascular system.
The combined use of Inspirax with cromoglicic acid and / or GCS increases the effectiveness of therapy.

Terms of sell

You don't need a prescription to buy Inspirax.