Ipratropium-native (Ipratropium-NATIV)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceIpratropium bromideIpratropium bromide
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    • Dosage form: & nbspinhalation solution
    Composition:

    Per 1 ml:

    Active substance:

    Ipratropium bromide monohydrate

    0.261 mg

    in terms of ipratropium bromide

    0.250 mg

    Excipients:

    Sodium benzoate

    0.500 mg

    Disodium edetate dihydrate

    0.554 mg

    Citric acid monohydrate

    1.640 mg

    Sodium hydroxide

    to pH 3.4 ± 0.1

    Purified water

    up to 1 ml
    Description:Transparent, colorless or almost colorless liquid.
    Pharmacotherapeutic group:M-holinoblokator
    ATX: & nbsp

    R.03.B.B.01   Ipratropium bromide

    Pharmacodynamics:

    Ipratropium bromide is a bronchodilator that blocks m-holinoretseptory smooth muscles of the tracheobronchial tree and suppresses reflex narrowing of the bronchi (bronchoconstriction). Having a structural similarity with the molecule of acetylcholine, it is its competitive antagonist.

    Anticholinergics (m-holinoblokatory) prevent an increase in the intracellular concentration of calcium ions, which occurs due to the interaction of acetylcholine with muscarinic receptors located in the smooth muscles of the bronchi. The release of calcium ions occurs with the help of secondary mediators (mediators), which include ITF (inositol triphosphate) and DAG (diaciglycerol).

    Ipratropium bromide effectively prevents bronchoconstriction resulting from the inhalation of cigarette smoke, cold air, the effects of various bronchospasmic substances, and also inhibits bronchospasm associated with the influence of the vagus nerve.

    With inhalation, it practically does not have a resorptive effect.

    The bronchodilation occurring after inhalation of ipratropium bromide is mainly a consequence of the local and specific effects of the drug on the lungs, rather than the result of its systemic effect.

    After taking ipratropium bromide in patients with bronchospasm due to chronic obstructive pulmonary disease, there is a significant improvement in lung function within 15 minutes, reaching a maximum after 1-2 hours and lasting up to 4-6 hours.

    Pharmacokinetics:

    The therapeutic effect of ipratropium bromide is a consequence of its local action in the airways. The development of bronchodilation is not parallel to pharmacokinetic parameters.

    Suction

    After inhalation in the lungs, 10-30% of the administered dose of ipratropium bromide usually falls (depending on the dosage form and inhalation method). Most of the dose is swallowed and enters the gastrointestinal tract.

    Part of the dose of ipratropium bromide, which enters the lungs, quickly reaches the systemic blood flow (within a few minutes).

    The total systemic bioavailability of ipratropium bromide, administered orally and by inhalation, is 2% and 7-28%, respectively, on the basis that the total renal excretion (within 24 hours) of the parent compound is approximately 46% of the intravenously administered dose, less than 1% of the amount of dose administered orally and approximately 3-13% of the inhaled dose of ipratropium bromide.

    Distribution

    The kinetic parameters describing the distribution of ipratropium bromide were calculated on the basis of its plasma concentrations after intravenous administration.There is a rapid two-phase decrease in the concentration of ipratropium bromide in blood plasma. Apparent volume of distribution during the state of equilibrium concentration (Css) is approximately 176 liters (≈2.4 liters / kg).

    Ipratropium bromide binds to blood plasma proteins (albumins and α-1 acid glycoprotein) to a minimum extent (less than 20%).

    Ipratropium bromide, which is a quaternary amine, does not penetrate the blood-brain barrier.

    Metabolism

    After intravenous ipratropium bromide, approximately 60% of the dose is metabolized by oxidation, mainly in the liver and partially excreted in the urine. The major metabolites that are excreted in the urine bind to muscarinic receptors weakly and are considered inactive. After inhalation, ipratropium bromide of about 77% of the systemic available dose is metabolized by hydrolysis of the ester bond (41%) and conjugation (36%).

    Excretion

    The half-life (T1/2) during the terminal phase is approximately 1.6 hours. The total clearance of ipratropium bromide is 2.3 l / min, and the renal clearance is 0.9 l / min.

    The total renal excretion within 6 days of an isotope-labeled dose, including the parent compound and all metabolites, is 72.1% after intravenous administration, 9.3% after oral administration, and 3.2% after inhalation.Excretion through the intestine of an isotope-labeled dose is 6.3% after intravenous administration, 88.5% after oral administration, and 69.4% after inhalation,

    Half-life (T1/2) of the starting compound and metabolites with intravenous administration is about 2-3 hours.

    Indications:

    - Chronic obstructive pulmonary disease (including chronic obstructive bronchitis, pulmonary emphysema);

    - brohnhialnaya asthma (light and moderate severity).

    Contraindications:

    - Hypersensitivity to atropine and its derivatives;

    - Pincreased sensitivity to ipratropium bromide or to other components of the drug;

    - atozrast to 18 years.

    Carefully:

    Patients with diseases such as angle-closure glaucoma, obstruction of the urinary tract, prostatic hyperplasia and cystic fibrosis.

    Pregnancy and lactation:

    Pregnancy: the safety of ipratropium bromide during pregnancy in humans is not established. When prescribing ipratropium bromide during a possible or confirmed pregnancy, it is necessary to take into account the ratio of the prospective benefit from the appointment of the drug to the mother and the possible risk to the fetus.

    Breastfeeding period: data on the penetration of ipratropium bromide into breast milk are absent. However, since many drugs are excreted in breast milk, caution should be used to prescribe ipratropium bromide women in the period of breastfeeding.

    Dosing and Administration:

    The preparation Ipratropium-native is intended only for inhalation by inhalation through the mouth with the aid of a nebulizer.

    The preparation Ipratropium-native is not intended for injection or for oral administration!

    In 20 drops of the preparation Ipratropium-native (about 1 ml) contains 0.250 mg of ipratropium bromide, respectively 1 drop of the drug contains 0.0125 mg of ipratropium bromide.

    Dosing regimen is selected individually.

    The preparation Ipratropium-native must be used under the supervision of a doctor only with the help of a nebulizer of any design that turns the drug solution into an aerosol for inhalation.

    Since many nebulizers operate only in the presence of a constant flow of air, it is possible that the sprayed product will enter the environment. Given this, Ipratropium-native preparation should be used in well-ventilated rooms.

    Do not exceed the recommended daily dose during both emergency and maintenance therapy.

    If the treatment does not lead to a significant improvement or if the patient's condition worsens (sudden or rapid shortness of breath (difficulty breathing)), you should immediately consult a doctor.

    If the doctor is not assigned otherwise, the following dosing regimen is recommended:

    Supportive treatment:

    Adults (including the elderly): 2 ml of Ipratropium-native preparation (40 drops = 0.5 mg ipratropium bromide) 3-4 times a day.

    The maximum daily dose is 8.0 ml of the preparation Ipratropium-native (2 mg ipratropium bromide).

    Acute bronchospasm:

    Adults (including the elderly): 2.0 ml of the preparation Ipratropium-native (40 drops = 0.5 mg ipratropium bromide); repeated inhalations are possible until the patient's condition is stabilized, the interval between, inhalations is determined by the doctor. Ipratropium-native can be used in conjunction with inhalation and β2-adrenomimetics.

    To ensure proper use of the product, please read these instructions for use carefully.

    The recommended dose of Ipratropium-native immediately before use should be diluted with 0.9% sodium chloride solution until the volume reaches 3-4 ml,pour into a nebulizer and inhalation. The solution remaining after inhalation should not be used again, poured out.

    The speed and duration of inhalation may depend on the inhalation method and the type of nebulizer. The duration of inhalation should be monitored by the expenditure of diluted Ipratropium-native preparation. When using a centralized oxygen system, the solution is best used at a flow rate of 6-8 liters per minute. For inhalations it is recommended to use nebulizers with a mouthpiece (mouthpiece). When using a nebulizer with a mask, use a mask of the appropriate size.

    Keep the nebulizer clean.

    Side effects:

    Many of these unwanted reactions may be due to the anticholinergic properties of ipratropium bromide.

    A drug Ipratropium-native, Like any inhalation therapy, it can cause local irritation.

    The most frequent adverse reactions reported in clinical trials were headache, pharyngeal irritation, coughing, dry mouth, gastrointestinal motility disorders (including constipation, diarrhea and vomiting), nausea and dizziness.

    Undesired reactions are distributed according to the frequency of occurrence. The following criteria were used to estimate the frequency: very often (> 1/10); often (from 1/100 to 1/10); infrequently (from 1/1000 to 1/100); rarely (from 1/10000 to 1/1000); very rarely (<1/10000), (including individual messages); frequency is unknown.

    Infectious and parasitic diseases: often - flu-like symptoms, upper respiratory tract infections; infrequently - urinary tract infections.

    Immune system disorders: infrequently - hypersensitivity, anaphylactic reactions, angioedema (Quincke's edema);

    Disturbances from the nervous system: often - headache, dizziness.

    Disturbances on the part of the organ of sight: infrequently - blurred vision, mydriasis, increased intraocular pressure, glaucoma, acute pain in the eyes, the appearance of an aura around the subjects, conjunctival hyperemia, corneal edema; rarely - violation of accommodation.

    Heart Disease: infrequent - palpitation, supraventricular (supraventricular) tachycardia; rarely - atrial fibrillation, increased heart rate.

    Vascular disorders: frequency unknown - lowering of blood pressure (hypotension).

    Disturbances from the respiratory system, organs of the chest and mediastinum: often - pharynx irritation, cough, shortness of breath; infrequently - bronchospasm, paradoxical bronchospasm, laryngospasm, pharyngeal edema, dry pharynx, sinusitis.

    Disorders from the gastrointestinal tract: often - dry mouth, nausea, a violation of the motility of the gastrointestinal tract; infrequently - diarrhea, constipation, vomiting, dyspepsia, changes in taste, stomatitis.

    Disturbances from the skin and subcutaneous tissues: infrequently - rash, itching; rarely - hives.

    Disorders from the kidneys and urinary tract: infrequently - retention of urine.

    If any of the above at instructions for adverse reactions are aggravated or you notice any other adverse reactions not indicated at instructions, report this doctor.

    Overdose:

    Symptoms: specific symptoms of overdose are not revealed. Given the breadth of the therapeutic effect and the local way of using the drug Ipratropium-native, the occurrence of any major anticholinergic symptoms is unlikely.There may be minor manifestations of systemic anticholinergic action, such as dry mouth, accommodation disorders, increased heart rate.

    Treatment: symptomatic therapy.

    Interaction:

    With simultaneous application of β2-adrenomimetiki and xanthine derivatives potentiate the bronchodilating effect of the drug.

    The anticholinergic effect is enhanced by antiparkinsonian agents, quinidine, tricyclic antidepressants.

    When combined with other anticholinergics, an additive effect is noted.

    Patients with closed-angle glaucoma should use the preparation with extreme caution Ipratropium-native together with inhaled β2-adrenomimetics, as the risk of developing an acute attack of glaucoma increases.

    Ipratropium-native, solution for inhalation, should not be administered concomitantly with the inhalation solution of cromoglycic acid, taking into account the possibility of precipitation (precipitation).

    Special instructions:

    It is not recommended to use the preparation Ipratropium-native for emergency relief of an attack of bronchial asthma (as the bronchodilator effect develops later than in β2adrenomimetics).

    In patients with cystic fibrosis, the risk of developing motor disorders of the gastrointestinal tract is increased.

    Ipratropium-native can be used for combined inhalations simultaneously with such inhalation solutions as: ambroxol, bromohexine and fenoterol.

    The preparation Ipratropium-native contains an auxiliary substance (stabilizer), disodium edetate, which during inhalation can cause a narrowing of the lumen of the bronchi; the occurrence of bronchospasm in patients with hyperreactivity of the respiratory tract.

    After applying Ipratropium-native, hypersensitivity reactions of immediate type may occur, as indicated by cases of rash, hives, angioedema, pharyngeal edema, bronchospasm and anaphylactic reactions. Patients should be able to correctly apply Ipratropium-native, a solution for inhalation.

    Do not let the solution enter the eyes!

    It is necessary to pay special attention to the need to protect the eyes of patients who are predisposed to developing glaucoma from getting Ipratropium-native. In the event of any symptom of an attack of angle-closure glaucoma (pain in the eye, discomfort, blurred vision,appearance of a halo and color spots in front of the eyes in combination with conjunctival and corneal hyperemia), it is necessary to start using drops that cause a narrowing of the pupil, and immediately go to the ophthalmologist.
    The use of Ipratropium-native does not lead to positive results of doping tests in athletes.
    Effect on the ability to drive transp. cf. and fur:

    Data on the effect of the drug Ipratropium-native there is no ability to drive vehicles and manage mechanisms. In case of development of such adverse reactions as dizziness, accommodation disorders, mydriasis and blurred vision, it is necessary to refrain from driving vehicles and controlling mechanisms, as well as from engaging in other potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:Solution for inhalation, 0.25 mg / ml.
    Packaging:

    For 20 ml of the drug in bottles of dark glass with a polyethylene dropper and a screwed polypropylene lid.

    One bottle with instructions for use is placed in a cardboard box.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Do not freeze.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003139
    Date of registration:11.08.2015 / 30.03.2016
    Expiration Date:11.08.2020
    The owner of the registration certificate:NATIVA, LLC NATIVA, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp27.11.2017
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