Atrovent - instructions for use, dose, side effects, contraindications

Excipients: benzalkonium chloride 0.10 mg, disodium edetate dihydrate 0.50 mg, sodium chloride 8.80 mg, hydrochloric acid 1 N (to adjust pH 3.4) 0.659 mg, purified water to 1.00 ml.

Description:

A clear, colorless or almost colorless liquid, practically free of particles.

Pharmacotherapeutic group:m-holinoblokator

ATX: & nbsp

R.03.B.B.01 Ipratropium bromide

Pharmacodynamics:

Bronchodilator. It blocks m-holinoretseptory smooth muscle tracheobronchial tree and suppresses reflex bronchoconstriction. Having a structural similarity with the molecule of acetylcholine, it is its competitive antagonist.Anticholinergic drugs 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 (diacylglycerol).

Effectively prevents the narrowing of the bronchi, resulting from the inhalation of cigarette smoke, cold air, the effects of various bronchospasmic substances, and also eliminates spasm of the bronchi associated with the influence of the vagus nerve.

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

Bronchodilation occurring after inhalation of ATROventa® (ipratropium bromide) is mainly a consequence of the local and specific effects of the drug on the lungs, and not the result of its systemic effect. In controlled 85-90-day studies conducted in patients with bronchospasm due to chronic obstructive pulmonary disease, chronic bronchitis and emphysema,a significant improvement in lung function was observed for 15 minutes, peaked in 1-2 hours and lasted up to 4-6 hours.

Pharmacokinetics:

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

After inhalation into the lungs, 10-30% of the administered dose of the drug 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 the drug, which enters the lungs, quickly reaches the systemic blood flow (within a few minutes).

The total renal excretion (within 24 hours) of the starting compound is approximately 46% of the intravenously administered dose, less than 1% of the dose administered orally and approximately 3-13% of the inhalation dose of the drug. Based on these data, it is calculated that the total systemic bioavailability of ipratropium bromide, administered orally and by inhalation, is 2% and 7-28%, respectively.

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 plasma concentration.Apparent volume of distribution during the state of equilibrium concentration (Css) is approximately 176 liters (≈ 2.4 l / kg). The drug binds to plasma proteins to a minimum degree (less than 20%). Ipratropium bromide, which is a quaternary amine, does not penetrate the blood-brain barrier.

The half-life period 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. After intravenous administration, approximately 60% of the dose is metabolized by oxidation, mainly in the liver.

The total renal excretion (within 6 days) of an isotope-labeled dose (including the parent compound and all metabolites) was 72.1% after intravenous injection, 9.3% after oral administration, and 3.2% after inhalation. The total isotope-labeled dose, excreted through the intestine, was 6.3% after intravenous injection, 88.5% after oral administration, and 69.4% after inhalation. Thus, the excretion of an isotope-labeled dose after intravenous administration is mainly through the kidneys. The half-life of the starting compound and metabolites is 3.6 hours.The main metabolites that are excreted in the urine bind to muscarinic receptors weakly, and are considered inactive.

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

- bronchial asthma (moderate and mild severity).

Contraindications:

- Hypersensitivity to atropine and its derivatives;

- hypersensitivity to ipratropium bromide or to other components of the drug.

Carefully:

Closed-angle glaucoma, obstruction of the urinary tract, prostatic hyperplasia; breastfeeding, children's age (up to 6 years).

Pregnancy and lactation:

Atrovent® safety during pregnancy in humans is not established. When prescribing the drug 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.

Data on the penetration of Atrovent® into breast milk are not available. However, since many drugs are excreted in breast milk, care should be taken to place Atrovent® in women during lactation.

Dosing and Administration:

(20 drops = about 1 ml, 1 drop = 0.0125 mg ipratropium bromide anhydrous)

Dosing regimen is selected individually. During treatment, patients should be under medical supervision. Do not exceed the recommended daily dose during both emergency and maintenance therapy.

If treatment does not lead to significant improvement or if the patient's condition worsens, a doctor's consultation is needed to develop a new therapy plan.

In case of sudden or rapid increase of dyspnea (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) and children over 12 years of age:

2.0 ml (40 drops = 0.5 mg) 3-4 times a day. The maximum daily dose is 8.0 ml (2 mg).

Children from 6 to 12 years old:

Treatment should be conducted under medical supervision;

on 1,0 ml (20 drops = 0,25 mg) 3-4 times a day. The maximum daily dose is 4 ml (1 mg).

Children under 6 years old:

Treatment should be conducted under medical supervision;

on 0,4-1,0 ml (8-20 drops = 0,1-0,25 mg) 3-4 times a day.

The maximum daily dose is 4 ml (1 mg).

Acute bronchospasm:

Adults (including the elderly) and children over 12 years of age:

2.0 ml (40 drops = 0.5 mg); repeated appointments are possible until the patient's condition is stabilized. The interval between inhalations is determined by the doctor. ATROVENT can be used in conjunction with inhaled β₂-adrenomimetics.

Children from 6 to 12 years old:

Treatment should be conducted under medical supervision.

1.0 ml (20 drops = 0.25 mg); repeated appointments are possible until the patient's condition is stabilized. The interval between inhalations is determined by the doctor. ATROVENT® can be used in conjunction with inhalation β₂-adrenomimetics.

Children under 6 years:

Treatment should be conducted under medical supervision.

0.4-1.0 ml (8-20 drops = 0.1-0.25 mg); repeated appointments are possible until the patient's condition is stabilized. The interval between inhalations is determined by the doctor. ATROVENT® can be used in conjunction with inhalation β₂-adrenomimetics.

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

The recommended dose of the drug should be diluted with 0.9% sodium chloride solution until the volume of the drug reaches 3-4 ml, pour into a nebulizer and inhalation. The drug should be diluted with 0.9% solution of sodium chloride each time immediately before use, the solution remaining after inhalation is poured.

Dosage may depend on the inhalation method and the type of nebulizer. The duration of inhalation can be controlled by the expenditure of diluted volume.

ATROVENT® inhalation solution can be used with various nebulizers available on the market. When using a centralized oxygen system, the solution is best used at a flow rate of 6-8 liters per minute.

Side effects:

Many of these unwanted effects may be due to the anticholinergic properties of ATROVENT®. ATROVENT®, like any inhalation therapy, can cause local irritation.

Adverse reactions of the drug were determined on the basis of data obtained in clinical studies and during pharmacological supervision of the use of the drug after its registration.

The most common side effects reported in clinical trials were headache, pharyngeal irritation, coughing, dry mouth, gastrointestinal motility disorders (including constipation, diarrhea and vomiting), nausea and dizziness

Immune system disorders

- hypersensitivity;

- anaphylactic reaction.

Disturbances from the nervous system

- headache;

- dizziness.

Disturbances on the part of the organ of sight

- blurred vision;

- mydriasis;

- increased intraocular pressure;

- glaucoma;

- Pain in the eyes;

- the appearance of a halo around objects;

- hyperemia of the conjunctiva;

corneal edema;

- violation of accommodation.

Heart Disease

- a feeling of palpitations;

- supraventricular tachycardia;

- atrial fibrillation;

- increased heart rate.

Disturbances from the respiratory, thoracic and mediastinal organs

- irritation of pharynx;

- cough;

- bronchospasm;

- paradoxical bronchospasm;

- laryngospasm;

- swelling of the pharynx;

- dryness of pharynx.

Disorders from the gastrointestinal tract

- dry mouth;

- nausea;

- disorders of motility of the gastrointestinal tract;

- diarrhea;

- constipation;

- vomiting;

- stomatitis;

- edema of the oral cavity.

Changes in the skin and subcutaneous tissues

- rash, itching;

- angioedema;

- hives.

Disorders from the kidneys and urinary tract

- retention of urine.

Overdose:

Symptoms of a specific overdose have not been revealed.Given the breadth of the therapeutic effect and the local use of ATROVENT®, the occurrence of any major anticholinergic symptoms is unlikely. There may be minor manifestations of systemic anticholinergic action, such as dry mouth, visual impairment, increased heart rate.

Treatment: symptomatic.

Interaction:

β₂-adrenergic agents and xanthine derivatives may enhance the bronchodilator effect of the drug.

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

With simultaneous use with other anticholinergics - additive action.

When using the Atrovent® solution for inhalation concomitantly with inhaled β-adrenomimetics in patients with occlusive glaucoma, the risk of developing an acute attack of glaucoma increases.

Atrovent® solution for inhalation should not be administered concomitantly with an inhaled solution of cromoglycic acid, given the possibility of precipitation.

Special instructions:

Patients with cystic fibrosis have an increased likelihood of developing a slowdown in the motility of the gastrointestinal tract.

ATROVENT® inhalation solution can be used for combined inhalations simultaneously with ambroxol solution for inhalation, bromhexine solution for inhalation and Berotek inhalation solution.

The drug contains a preservative benzalkonium chloride and the disodium edetate dihydrate stabilizer, which during inhalation can cause narrowing of the bronchus lumen; there may be a bronchospasm in sensitive patients with airways hyperreactivity.

After applying ATROVENTA®, immediate hypersensitivity reactions may occur, as indicated by rare cases of rash, hives, angioedema, edema of the oropharynx, bronchospasm and anaphylaxis.

ATROVENT® should be used with caution in patients who are predisposed to acute angular glaucoma, or in patients with concomitant obstruction of the urinary tract (eg, prostatic hyperplasia or bladder neck obstruction).

Patients should be able to correctly apply ATROVENT® solution for inhalation.Do not allow solution to enter the eyes. Patients who are predisposed to the development of glaucoma should be especially warned about the need to protect the eyes from getting the drug.

For inhalations it is recommended to use nebulizers with a tip for the mouth. When using a nebulizer with a mask, you should use a mask of the appropriate size.

Effect on the ability to drive transp. cf. and fur:

The effects of the drug on the ability to drive vehicles and the use of mechanisms have not been specifically studied. However, patients need to be informed that during treatment with ATROVENT® they may experience such undesirable sensations as dizziness, discomfort, accommodation, mydriasis and 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 a car or controlling machinery.

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

Packaging:

To 20 ml in a glass bottle of amber color with a polyethylene dropper and a screwed polypropylene cover with the control of the first opening.

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

Storage conditions:At a temperature of no higher than 30 ° C, do not allow freezing.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N015913 / 01

Date of registration:30.06.2009

The owner of the registration certificate:Boehringer Ingelheim International GmbHBoehringer Ingelheim International GmbH Germany

Manufacturer: & nbsp

INSTITUTO de ANGELI, S.r.L. Italy

Representation: & nbspBERINGER INGELCHAIM INTERNATIONAL GmbH BERINGER INGELCHAIM INTERNATIONAL GmbH Germany

Information update date: & nbsp02.11.2015

Illustrated instructions

Instructions

Atrovent® (Atrovent®)