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

Glucocorticosteroid synthetic (GCS) for topical application, has anti-inflammatory, anti-allergic and immunosuppressive effects. Increases the production of lipomodulin, which is an inhibitor of phospholipase A, inhibits the release of arachidonic acid, inhibits the synthesis of metabolic products of arachidonic acid-cyclic endoperoxides and prostaglandins (Pg). It prevents the accumulation of neutrophils, reduces inflammation and production of cytokines, inhibits the migration of macrophages, reduces the intensity of infiltration processes, the formation of a chemotaxis substance; inhibits the release of mast cells from inflammatory mediators.

Increases the number of active beta-adrenergic receptors, restores bronchial response to bronchodilators, reducing the frequency of their use, reduces edema of the bronchial mucosa, mucus production, sputum formation and reduces airway hyperreactivity. Improves mucociliary transport.Well tolerated in long-term treatment has no mineralokortikosteroidnoy activity at recommended doses has almost no systemic exposure.

The therapeutic effect begins, a few hours after inhalation. The maximum therapeutic effect develops only a few days after the administration of therapeutic doses of inhaled budesonide, an average of 5-7 days.

Inhalation of budesonide is able to prevent an attack of bronchial asthma, but does not arrest acute bronchospasm.

Pharmacokinetics:

Absorption is low. After inhalation reaches 20-25% of small bronchi, the dose received by the gastrointestinal tract (GIT) and almost completely absorbed (90%) of biotransformation in the liver to inactive metabolites. Systemic bioavailability of budesonide is 38% of the dose, and 1/6 of this value is formed by the ingestion of the drug. The time of the maximum concentration in the blood plasma is 15-45 min after inhalation. The connection with plasma proteins is 88%.

The volume of budesonide distribution is approximately 3 l / kg. Has a high system clearance - 84 l / h.The half-life is 2.8 hours, the maximum concentration in blood plasma is 0.01 mmol / l. Output through the intestine in the form of metabolites - 10%, kidneys - 70%.

Indications:Bronchial asthma (BA), requiring maintenance therapy for GCS, chronic obstructive pulmonary disease (COPD).

Contraindications:Hypersensitivity to the components of the drug, children under 16 years.

Carefully:Active and inactive forms of tuberculosis, fungal, bacterial and viral infections of the respiratory system, pregnancy, lactation.

Pregnancy and lactation:

Clinical data on the increase in the frequency of fetal abnormalities on the background of the use of budesonide in pregnancy at recommended doses, as well as the isolation of budesonide with breast milk, are absent. .

Care should be taken during pregnancy and lactation. The purpose of the drug is rational if the use of its use for the mother exceeds the potential risk to the fetus or child.

Dosing and Administration:

Benacort is used by inhalation, with the help of an individual portable inhaler Cyclochaler. A single dose of the drug contains 200 μg budesonide.The daily dose of Benacorta in the treatment of asthma and COPD is selected individually, taking into account the severity of the course of bronchial asthma and the maintenance dose of tableted GCS. As an initial daily dose, 2-8 single doses per day are recommended (400-1600 μg budesonide). For maintenance treatment, usually 1-4 single doses per day (200-800 μg budesonide). During the exacerbation of bronchial asthma, the daily dose of Benacort can be increased to 2000 μg (the maximum daily dose). The daily dose of Benacorta is inhaled in 2-4 doses.

Duration of treatment to 3-12 months, depending on the severity of asthma.

Preliminary inhalation of beta2-adrenomimetics (eg, salbutamol) expands the bronchi and improves the flow of budesonide into the respiratory tract, thereby enhancing its therapeutic effect.

In case the patient took the GCS orally, the translation for Benacort's treatment should be carried out with the patient's stable state of health, for 10-14 days they combine inhalation and ingestion of GCS inside. Within 10 days, it is recommended to take high doses of Benacort while taking oral glucocorticosteroids in a selected dose.In the future, the dose of oral glucocorticosteroids should be gradually reduced (for example, 2.5 mg prednisolone) to the lowest possible level or complete cancellation. In many cases it is possible to completely stop taking oral glucocorticosteroids. There are no data on the use of budesonide in patients with renal insufficiency or liver dysfunction. Since the excretion of budesonide occurs due to biotransformation in the liver, an increase in the duration of action of the drug in patients with severe hepatic cirrhosis can be expected.

Children, over 16 years of age: an initial dose of 200-800 mcg / day. If necessary, the dose may be increased to 1000 mcg / day.

The maintenance dose is 200-800 μg / day.

Side effects:

Often (> 1/100): cough, dry mouth, hoarseness, dysphonia, irritation of the oral and pharyngeal mucosa, candidal stomatitis, dryness of the pharyngeal mucosa, headache, nausea.

Rarely (<1/1000): bruising or thinning of the skin, unpleasant taste sensations, paradoxical bronchospasm (for prophylaxis - combination of inhalations with beta2-adrenomimetics), esophageal candidiasis.

High doses of the drug can lead to the development of systemic side effects depletion of the adrenal cortex, hyperglycemia, arterial hypertension.

Overdose:In acute overdose, clinical manifestations do not occur. With prolonged use of the drug in doses much higher than recommended, a systemic glucocorticosteroid effect may develop in the form of hypercorticoidism and suppression of adrenal function.

Interaction:

In the treatment of bronchial asthma, Benacorte is well combined with beta2-adrenomimetics, cromoglycic acid or nedocromil, methylxanthines and ipratropium bromide. Phenobarbital, phenytoin, rifampicin reduce the effectiveness (induction of microsomal liver enzymes). Methandienone, estrogens increase the concentration of budesonide in blood plasma.

The administration of 200 mg of ketoconazole once a day increases the concentration in the plasma of a tolerated budesonide in a dose of 3 mg on average 6-fold. With the appointment of ketoconazole 12 hours after the administration of budesonide, the concentration in the plasma of the latter increases 3 times. Information on such interactions with inhaled dosage forms of budesonide is absent, but a noticeable increase in plasma drug concentration should be expected.

Other potential inhibitors of the CYP3A4 isoferment, for example itraconazole, also significantly increases the plasma concentration of budesonide.

Special instructions:

Benacort is not intended for relief of acute symptoms of asthma and COPD.

Follow the instructions for the use of the inhaler - "Cyclochaler". After inhalation it is recommended to hold your breath for 10 seconds. The presence of sodium benzoate in the composition of the drug reduces the risk of developing candidiasis of the upper respiratory tract, since the sodium benzoate solution has antifungal properties.

After using the drug, rinse your mouth with water to reduce the risk of candidal stomatitis.

When switching from oral glucocorticosteroids to Benacourt, lowering the dosage of systemic GCS should be done very slowly and in small doses (for example, 2.5 mg of prednisolone). In patients who were on long-term therapy with systemic GCS, available syndrome

pseudo-rheism. In these cases, sometimes is necessary temporarily increase the dose of oral GCS. In rare cases, symptoms such as fatigue, headaches, nausea, vomiting are observed.After complete cancellation, prolonged observation of the patient (risk of developing adrenal insufficiency) is recommended, as well as an evaluation of the function of external respiration. Benacort does not affect the ability to engage in potentially hazardous activities requiring special attention and quick reactions (driving and other vehicles, working with moving mechanisms, dispatcher and operator work, etc.).

rules use of the inhaler "Cyclochaler"

The Cyclochaler is an individual portable device for dispensing and injecting powder dosage forms into the human respiratory tract.

The inhaler consists of a protective cover and casing.

Inhalation technique

1.Remove the protective cover and shake the inhaler.

2. To measure one dose of the drug, pull the dispenser from the body of the inhaler to the stop and holding the inhaler vertically, tap with your free hand on the bottom of the body (3-5 times). Return the dispenser to its original position.

3. Make a calm and full exhalation, tightly grasp the mouthpiece of the inhaler with your lips, forcibly and deeply inhale the drug and hold your breath for a full breath for 10 seconds.Take the mouthpiece out of your mouth and make a slow exhalation so that the exhaled air does not get into the inhaler. If you feel that a deep breath did not work and you did not inhale the whole dose, calm your breathing and, without measuring the dose, take another breath.

4.Put the protective cover on the body of the inhaler.

Note. The developed cough testifies to the deposition of the drug particles in the trachea and large bronchi. In this case, you should clear your throat, rinse your mouth and throat with water. After breathing becomes calm, you can repeat the inhalation.

The inhaler is a device for individual use.

Attention!

Incorrect use of the inhaler and poor inhalation technique can cause a low effectiveness of the drug. Training and development of the correct technique of inhalation should be carried out by the patient in the presence of the attending physician.

Maintenance. In case of contamination, wipe the inhaler dry with a soft cloth. Rinse the inhaler with water is not allowed.

Form release / dosage:Apparatus for inhalation dosed with 200 μg / dose, 100 and 200 doses.

Packaging:By 1.0 g (100 doses) or 2.0 g (200 doses) in a Cyclochaler inhaler in a sealed polyethylene bag is placed together with the instruction in a cardboard pack.

Storage conditions:Store at a temperature not exceeding 25 ° C in a dry place protected from light and out of the reach of children.

Shelf life:3 years. Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002275 / 01-2003

Date of registration:21.05.2008 / 28.03.2012

Expiration Date:Unlimited

The owner of the registration certificate:PULMOMED, CJSC PULMOMED, CJSC Russia

Manufacturer: & nbsp

PULMOMED, CJSC Russia

Information update date: & nbsp22.01.2017

Illustrated instructions

Instructions

Benacort® (Benacort)