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

A clear, colorless liquid, free from suspended particles, placed under pressure into a single stainless steel canister, equipped with a metering valve with a plastic rod.

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 bronchoconstriction resulting from the inhalation of cigarette smoke, cold air, the effects of various bronchospasmodiruyuschih substances, as well as 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® H (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 performed in patients with bronchospasm due to chronic obstructive pulmonary disease,chronic bronchitis and pulmonary emphysema, a significant improvement in lung function was observed for 15 minutes, peaked in 1-2 hours and lasted up to 4-6 hours.

In patients with bronchial asthma, a significant improvement in the function of external respiration is noted in 51% of patients.

Pharmacokinetics:

The therapeutic effect of ATROventa ® H is a consequence of its local action in respiratory tract.

The development of bronchodilation is not parallel to pharmacokinetic parameters.

After inhalation in the lungs, usually (depending on the dosage form and inhalation method) 10-30% of the administered dose preparation. 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. 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.

Kinetic parameters describing 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. The apparent volume of distribution during the state 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 (chronic obstructive bronchitis, emphysema);

- bronchial asthma (mild and moderate), especially with concomitant diseases of the cardiovascular system.

Contraindications:

- Hypersensitivity to atropine and its derivatives;

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

- pregnancy (I trimester);

- the drug is contraindicated in patients who have previously been allergic to soy or peanuts. In such patients, other ATROventa® H dosage forms (inhalation solutions) that do not contain soy lecithin can be used.

Carefully:

- Closed-angle glaucoma;

- Obstruction of the urinary tract (prostatic hyperplasia);

- lactation period;

- Children's age (up to 6 years).

Pregnancy and lactation:

Safety of Atrovent® H during pregnancy is not established in humans.When prescribing the drug during a possible or confirmed pregnancy, it is necessary to take into account the ratio of the intended use of the drug and the possible risk to the fetus. In pre-clinical studies, there was no embryotoxic and teratogenic effect of the drug in inhalation and intranasal administration of doses significantly exceeding the recommended therapeutic dose for humans.

Data on the penetration of Atrovent® H into breast milk are absent. Although insoluble quaternary cations penetrate breast milk, it is unlikely that Atrovent® H will have a significant effect on inhalation use. However, since many drugs are excreted in breast milk, care should be taken to place Atrovent® H in women during lactation.

Dosing and Administration:

Dosing should be carried out 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 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. The following doses are recommended (unless another dosing regimen is prescribed):

Adults and children over 6 years of age:

2 inhalation doses (injection) 4 times a day. Since the need for increasing doses indicates the possible need for additional methods of treatment, as a rule, over 12 inhalation doses should not be used during the day.

To treat sudden exacerbations of chronic obstructive pulmonary disease, ATROVENT® solution for inhalation can be indicated.

In children, the metered aerosol ATROVENTA® H should only be used

after consulting a doctor and under the supervision of adults (due to insufficient information).

Use of a dosed aerosol

Proper use is essential for successful therapy.

Before first use

Before using the inhaler for the first time, press the bottom of the cylinder 2 times.

Before each use the following rules must be observed:

1. Remove the protective cap.

2. Take a deep breath out.

3. Hold the inhaler as shown in Fig. 1 and tightly grasp the mouthpiece.Arrow and bottom of the cylinder should be pointed upwards.

4. Take as deep as possible a breath and simultaneously sharply press on the bottom of a cylinder. This will release one inhalation dose. Hold your breath for a few seconds, then take the mouthpiece out of your mouth and exhale. Repeat for the second inhalation dose.

5. After using the inhaler, put on the protective cap.

6. If the metered aerosol inhaler is not used for three days, then before its application should be pressed on the valve once.

The balloon is not transparent, therefore it is impossible to determine by eye when it becomes empty. The inhaler contains 200 inhalation doses. After using all the doses, it may seem that the bottle still contains a small amount of liquid. However, the inhaler should be replaced in such cases, since it may contain an insufficient amount of the drug.

The amount of the drug in your inhaler can be checked in the following way:

- Shake the can, it will show if there is any liquid left in it.

- Another way. Remove the plastic mouthpiece from the bottle and place the can in a container of water.The content of the balloon can be estimated depending on its position in the water (Fig. 2).

Clean the inhaler at least once a week. It is important to keep the mouthpiece of the inhaler clean in order to prevent the ingestion of a drug that can block the release of the aerosol.

During cleaning, first remove the protective cap and remove the cylinder from the inhaler. Pass a stream of warm water through the inhaler, make sure the product is removed and / or visible mud (Figure 3).

After cleaning, shake the inhaler and allow it to air dry without using heaters. Once the mouthpiece has dried, insert the can into the inhaler and put on the protective cap (Figure 4).

PRECAUTIONS:

The plastic mouthpiece was developed specifically for the use of the aerosol ATROVENT® H, and serves to accurately dispense this drug. This mouthpiece should not be used with other metered aerosols. Do not use ATROVENT® H metered aerosol with other mouthpieces. The aerosol in the cylinder is under pressure. The container must not be opened or stored above 50 ° C.

Side effects:

Many of these undesirable effects may be a consequence of the anticholinergic properties of ATROVENTA® N.

ATROVENT® H, 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 studies were headache, pharyngeal irritation, coughing, dry mouth, gastrointestinal motility disorders (including constipation, diarrhea and vomiting), nausea and dizziness

Violations from the immune side systems

- hypersensitivity;

- anaphylactic reaction.

Disturbances from the nervous system

- headache;

- dizziness;

Disturbances on the part of the organ of sight

- blurring of vision;

- mydriasis;

- increased intraocular pressure;

- glaucoma;

- Pain in the eyes;

- the appearance of a halo around objects;

- hyperemia of the conjunctiva;

- corneal edema;

- violations 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 way of using ATROVENTA® H, the appearance of any serious 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:

Beta₂-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.

Special instructions:

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

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

ATROVENT® H 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).

Care should be taken to prevent the aerosol from entering the eyes. Since the metered aerosol is applied through the mouthpiece and the use of aerosol is controlled by hands, the risk of its entry into the eye is small.

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® H they may experience such undesirable sensations as dizziness, accommodation disorders, 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:

Aerosol for inhalation dosed, 20 mcg / dose.

Packaging:

For 10 ml (200 doses) in a stainless steel can with a metering valve and a mouthpiece with a protective cap with the company logo.

Balloon with instructions for use in a cardboard box.

Storage conditions:

Store at a temperature of no higher than 25 ° C, in a place protected from light.

Keep out of the reach of children.

Shelf life:

36 months.

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

Terms of leave from pharmacies:On prescription

Registration number:П N014363 / 01

Date of registration:14.03.2008

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

Manufacturer: & nbsp

BOEHRINGER INGELHEIM INTERNATIONAL, GmbH Germany

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

Information update date: & nbsp02.11.2015

Illustrated instructions

Instructions

Atrovent® H (Atrovent® N)