Ipraterol Native 0.25mg/ml + 0.5mg/ml 20ml

Ipraterol Native instruction

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Release form and composition

The drug is available in the form of a solution for inhalation: a clear liquid, colorless or having a faint yellow hue (20 ml each in dark-colored glass bottles with an integrated polyethylene dropper, 1 bottle in a cardboard box and instructions for use of Ipraterol-native).
1 ml of solution contains:
    active substances: ipratropium bromide monohydrate - 0.261 mg (equivalent to 0.25 mg ipratropium bromide); fenoterol hydrobromide - 0.5 mg;
    auxiliary components: citric acid monohydrate, sodium edetate, sodium benzoate, sodium hydroxide (acidity 3.2), water for injection.

Pharmacodynamics

Ipraterol native is a bronchodilating drug containing two components with bronchodilator activity: m-anticholinergic blocker - ipratropium bromide and selective beta2-adrenergic agonist - phenoterol.
The bronchodilating effect of the inhalation solution of Ipraterol-native is achieved as a result of exposure to m-anticholinergic and beta2-adrenergic agonists on various pharmacological targets. Complementing the effect of each other, the active substances contribute to the strengthening of the antispasmodic effect on the muscles of the bronchi. The combined composition provides a wide range of therapeutic effects of the drug in bronchopulmonary pathologies accompanied by constriction of the respiratory tract, allowing you to achieve the desired effect when using a lower dose of the beta-adrenergic component. The combination of ipratropium bromide and fenoterol allows you to choose an individual effective dose, significantly reducing the risk of side effects.
Due to the fact that the action of the drug in the treatment of acute bronchoconstriction develops rapidly, it is effectively used to treat acute attacks of bronchospasm.

ipratropium bromide

ipratropium bromide is a quaternary ammonium derivative with a pronounced anticholinergic (parasympatolytic) effect. The substance has a depressing effect on the reflexes caused by the vagus nerve, thereby counteracting the mediator of acetylcholine released from the ends of the vagus nerve. Anticholinergics prevent the growth of intracellular levels of calcium ions, resulting from the interaction of acetylcholine and muscarinic receptors of the smooth muscles of the bronchi. A system of secondary mediators is indirectly involved in the release of calcium ions, including ITF (inositol triphosphate) and DAG (diacylglycerol).
When inhaled, bronchodilation is largely due not to the systemic but to the local anticholinergic action of ipratropium bromide.
After inhalation, a significant improvement in lung function in patients with bronchospasm associated with chronic obstructive pulmonary pathologies (including chronic bronchitis, pulmonary emphysema) occurs within 1/4 hour. There is an increase of 15% or more of forced expiratory volume in 1 second and peak expiratory flow rate. The maximum effect is achieved after 1-2 hours and in most patients lasts for 6 hours.
ipratropium bromide does not adversely affect mucociliary clearance, gas exchange, and mucus secretion in the airways.

Fenoterol hydrobromide

Fenoterol - 1- (3,5-Dioxyphenyl) -2- (para-hydroxy-a-methyl-phenethylamino) ethanol, an adrenoagonist of beta2-adrenergic receptors In therapeutic doses, fenoterol stimulates beta2-adrenergic receptors selectively, and its stimulating effect on beta1-adrenergic receptors appears only when high doses are used.
The relaxing effect of phenoterol on the smooth muscles of the bronchi and blood vessels helps to prevent the development of bronchospastic reactions that occur under the influence of methacholine, histamine, allergens and cold air. Its blocking effect on the release of inflammatory mediators and bronchial obstruction from mast cells occurs immediately after use. Against the background of the use of higher doses of fenoterol, an increase in mucociliary clearance is noted.
The vascular effect of fenoterol, stimulating beta2-adrenergic receptors of the heart, determines the beta-adrenergic effect of the drug on cardiac activity, causing an increase in the frequency and strength of heart contractions. Like other beta-adrenergic agents, high doses of fenoterol can cause a prolongation of the QTc interval. The clinical significance of this manifestation has not been established.
The most common side effect of beta-adrenergic agonists is tremor.

Pharmacokinetics

ipratropium bromide with inhalation is absorbed from the mucosa of the respiratory tract extremely weakly. Its plasma concentration can only be determined using special enrichment methods or the use of high doses. The total systemic bioavailability of the substance after inhalation is from 7 to 28%. Due to the use of ipratropium bromide in therapeutic doses, its plasma concentration is 1000 times lower compared to this indicator after intravenous administration or oral administration.
When phenoterol is inhaled, the lower respiratory tract reaches 10–30% (depending on the method of inhalation and the inhalation system used), the rest is swallowed and enters the gastrointestinal tract. There is no correlation between the levels of phenoterol, which are achieved after inhalation in the blood plasma and the pharmacodynamic curve "time - effect". The duration of the bronchodilator action is not supported in the systemic circulation by high concentrations of the active substance. After phenoterol is administered orally, about 60% of the dose is absorbed; it takes 2 hours to reach its maximum concentration (Cmax) in blood plasma.
Being a derivative of quaternary nitrogen, ipratropium bromide is poorly soluble in fatty media and is not capable of significant penetration through biological membranes, does not cumulate.
The binding of fenoterol to plasma proteins is 40–55%. Fenoterol overcomes the placental barrier unchanged, excreted in breast milk.
Metabolized ipratropium bromide in the liver with the formation of eight known Ipraterol metabolites. Their connection with muscarinic receptors is negligible.
Fenoterol is metabolized in the liver. Its biotransformation proceeds in the intestinal wall exclusively by conjugation with sulfates. A swallowed amount of the drug after inhalation practically does not affect the level of the active substance in the blood plasma.
The excretion of ipratropium bromide occurs mainly through the intestine: in unchanged form - about 25%, in the form of metabolites - the rest.
Fenoterol is excreted through the kidneys and intestines in the form of inactive sulfate conjugates.
The pharmacokinetic parameters of a drug containing a combination of ipratropium bromide and phenoterol in elderly and pediatric patients, patients with impaired liver and / or kidney function, and patients with diabetes mellitus have not been studied.

Indications for use

The use of Ipraterol inhalation solution is indicated for the prevention and symptomatic treatment of chronic obstructive airway diseases with reversible obstruction, including chronic obstructive pulmonary disease, bronchial asthma, chronic obstructive bronchitis without or with emphysema.

Contraindications

Absolute:
    tachyarrhythmia;
    hypertrophic obstructive cardiomyopathy;
    I trimester of pregnancy;
    hypersensitivity to the active components of Ipraterol-native, other atropine-like substances and auxiliary ingredients.
With caution, Ipraterol-native inhalation solution should be prescribed to patients with diabetes mellitus, angle-closure glaucoma, arterial hypertension, chronic heart failure, aortic stenosis, coronary heart disease, severe lesions of the cerebral and peripheral arteries, after a recent (within the last three months) heart attack myocardium, with hyperthyroidism, pheochromocytoma, bladder neck obstruction, prostatic hyperplasia, cystic fibrosis, in the II – III trimesters we take lactation, and children under the age of 6 years.

Instructions for use: method and dosage

Ipraterol-native is intended for use by inhalation using appropriate nebulizers.
Treatment is required under medical supervision (for example, in a hospital). At home, therapy is possible only after consulting a doctor and only in cases where low doses of a fast-acting beta-agonist are not effective enough. In addition, the inhalation solution can be recommended for use by patients who, for several reasons, cannot use the aerosol for inhalation or, if necessary, the appointment of higher doses.
Immediately before inhalation, the prescribed dose of the drug is diluted in a 0.9% sodium chloride solution until a total volume of 3-4 ml is obtained. Ready solution should be used immediately. Ipraterol native should not be used orally or diluted with distilled water.
Various commercial nebulizer models are suitable for inhalation. In the presence of wall oxygen, it is recommended to use Ipraterol-native at a flow rate of 6–8 l / min. You can control the duration of inhalation by spending the finished solution.
The doctor selects the dose individually, taking into account the method of inhalation and the type of nebulizer. Treatment should begin with the lowest therapeutic dose.
Recommended dosage of Ipraterol Native for adolescents over the age of 12 years and adult patients, including older and older ages:
    acute attacks of bronchial asthma: mild to moderate degree of attack - 20 drops (1 ml) per 1 inhalation; severe seizure (including patients in intensive care units) - up to 50 drops (2.5 ml) per 1 inhalation, with dose inefficiency for a moderate degree of seizures. The maximum single dose is 80 drops (4 ml), daily - 160 drops (8 ml);
    course and long-term treatment: 20–40 drops (1-2 ml) per 1 inhalation, no more than 4 procedures per day;
    moderate degree of bronchospasm, ventilation of the lungs (as an adjuvant): the lower dose level should be 10 drops (0.5 ml) per 1 inhalation.
Recommended dosage of ipraterol-native for children aged 6-12 years:
    acute attacks of bronchial asthma: 10–20 drops (0.5–1 ml) per 1 inhalation, in severe cases when it is not possible to quickly stop the symptoms, a single dose can be increased to 40 drops (2 ml) per 1 inhalation. For especially severe cases (with an inefficiency of 40 drops), it is possible to use a maximum dose of 60 drops (3 ml) per 1 inhalation only under medical supervision. The maximum daily dose is 80 drops (4 ml);
    course and long-term treatment: 10-20 drops per 1 inhalation, no more than 4 procedures per day;
    moderate degree of bronchospasm, ventilation of the lungs (as an adjuvant): 10 drops per 1 inhalation.
The use of ipraterol-native in children under the age of 6 years (body weight less than 22 kg) should be carried out only under close medical supervision. The size of one dose is determined based on 2 drops (0.1 ml) per 1 kg of the child’s weight, but not more than 10 drops per 1 inhalation. The maximum daily dose is 30 drops (1.5 ml).
Observe the instructions for use of the nebulizer, including thorough regular care for it.

Side effects

    from the central and peripheral nervous system: often - nervousness, small tremor of skeletal muscles; rarely - headache, dizziness; very rarely - a change in the psyche;
    on the part of the heart and blood vessels: often - tachycardia (including supraventricular tachycardia), palpitations (more often with aggravating factors); rarely (against the background of high doses) - arrhythmia (including atrial fibrillation), decreased diastolic blood pressure (DBP), increased systolic blood pressure (SBP);
    from the respiratory system: rarely - pharyngitis, local irritation of the respiratory tract, cough; very rarely - laryngospasm, paradoxical bronchospasm;
    from the gastrointestinal tract: often - dry mouth; infrequently - vomiting, constipation, impaired motility of the gastrointestinal tract, diarrhea (more often with cystic fibrosis);
    on the part of the organ of vision: when the solution enters the eyes - pain in the eyeball, increased intraocular pressure, mydriasis, glaucoma; very rarely - reversible accommodation disorders, glaucoma, the symptoms of which are conjunctival hyperemia, corneal (stromal) edema, discomfort or pain in the eyeball, blurred vision, the appearance of colored spots or a halo in front of the eyes;
    from the immune system: rarely - skin rash, urticaria, angioedema of the tongue, lips and / or face;
    other reactions: general weakness, hyperhidrosis (increased sweating), urinary retention, hypokalemia, myalgia.

Overdose

    symptoms: the most probable symptoms, usually associated with the action of phenoterol and caused by excessive stimulation of β-adrenergic receptors, include the appearance of tremors, increased blood pressure BP, an increase in the gap between SBP and DBP, tachycardia, palpitations, angina pectoris, arrhythmias, flushing, a feeling of heaviness behind the sternum, increased metabolic acidosis, bronchial obstruction. Due to an overdose of ipratropium bromide, a slight disturbance in the accommodation of the eyes, dry mouth can occur, taking into account the breadth of the therapeutic effect and the local method of use of the substance, they are usually weakly expressed and are transient;
    treatment: the use of the inhalation solution Ipraterol-native should be stopped, after which, taking into account the monitoring of acid-base balance of blood, sedatives, tranquilizers (anxiolytics) are prescribed. Intensive care may be required to treat severe cases of overdose. As a specific antidote, the use of selective beta1-blockers is allowed. In this case, a dose of beta-blocker should be carefully selected, taking into account the possible increase in bronchial obstruction in patients with chronic obstructive pulmonary disease or bronchial asthma, which can lead to severe bronchospasm, even death.

special instructions

In cases where an unexpected difficulty in breathing (shortness of breath) progresses rapidly, you should immediately consult a doctor.
With prolonged therapy, Ipraterol Native in patients with bronchial asthma or mild to moderate chronic obstructive pulmonary disease, symptomatic use of the drug is preferable.
In severe forms of chronic obstructive pulmonary disease and bronchial asthma, simultaneous appropriate anti-inflammatory therapy is required to control the inflammatory processes in the airways and the course of the disease.
If the use of regularly increasing doses is required for the relief of bronchial obstruction, this can cause an uncontrolled worsening of the course of the disease due to the content of beta2-adrenergic agonist in ipraterol-native. It is important to consider that a frequent increase in the dose of beta2-agonists for stopping increasing bronchial obstruction is unjustified and dangerous. Therefore, the treatment plan should be changed, supplementing it with such inhaled glucocorticosteroids, which will prevent inflammatory processes and life-threatening worsening of the course of the disease.
With cystic fibrosis, a violation of the motility of the gastrointestinal tract is possible.
It must be remembered that with hypoxia, the negative effect of hypokalemia on the heart rhythm may increase.
Use of other sympathomimetic bronchodilators at the same time as Ipraterol Native inhalation solution is possible only under medical supervision.
When prescribing Ipraterol-native, the patient should be instructed in detail about the rules for its use. Do not allow the solution to get into the eyes, especially in the case of an existing predisposition to the development of glaucoma. It is recommended that you use a mouthpiece or a mask that fits snugly to your face while using the nebulizer.

Influence on the ability to drive vehicles and complex mechanisms

Due to the likelihood of dizziness and blurred vision when using Ipraterol-native, patients should be careful when driving vehicles and working with complex mechanisms.

Pregnancy and lactation

Pregnant women are contraindicated in the use of Ipraterol-native in the first trimester of gestation.
With caution, a combined bronchodilator should be prescribed in the II– III trimesters of pregnancy, due to a possible weakening of labor, and during lactation.
It should be borne in mind that fenoterol can have an inhibitory effect on the contractile activity of the uterus and passes into breast milk.

Use in childhood

With caution, Ipraterol-native should be used in children under 6 years of age.

Drug interaction

With simultaneous use with ipraterol-native:
    other anticholinergics: their prolonged simultaneous use with Ipraterol-native is not recommended due to lack of data;
    cromoglicic acid, glucocorticosteroids: their additional purpose helps to increase the effectiveness of therapy;
    beta-adrenergic agonists, systemic anticholinergics, theophylline and other xanthine derivatives: concomitant therapy with these drugs can enhance the bronchodilating effect of the solution and lead to an exacerbation of unwanted reactions;
    beta-blockers: can contribute to a significant weakening of the bronchodilator action of Ipraterol Native;
    diuretics, xanthine derivatives, glucocorticosteroids: it is necessary to take into account the possible increase in existing hypokalemia with this combination, especially in patients with severe forms of obstructive airways diseases; with this combination, monitoring of serum potassium concentration is recommended;
    digoxin: in patients with hypokalemia, digoxin may increase the risk of arrhythmias. If it is necessary to take digoxin, regular monitoring of the level of potassium in the blood serum is required;
    monoamine oxidase inhibitors (MAOs), tricyclic antidepressants: caution should be exercised when they are combined with ipraterol-native in connection with an increase in its beta-adrenergic effect;
    halotane, trichlorethylene, enflurane: general anesthesia with inhalation of halogenated hydrocarbon anesthetics can increase the effect of the drug on the cardiovascular system.

Terms and conditions of storage

Keep out of the reach of children.
Store at temperatures up to 25 ° C in a dark place, do not allow freezing.
Shelf life is 2 years.

Reviews

Reviews about ipraterol native are quite controversial. Most patients indicate the effectiveness of the drug in the treatment of bronchial asthma, chronic bronchitis, pneumonia, relief of symptoms of shortness of breath. They note that the drug quickly facilitates breathing with attacks of suffocation, without causing at the same time side effects.

Terms of sell

You don't need a prescription to buy Ipraterol Native.