Active substanceBudesonideBudesonide
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  • Dosage form: & nbspsuspension for inhalation dosed
    Composition:In 1 ml of the suspension contains:
    Active ingredient: budesonide (budesonide micronized) 0.25 mg or 0.5 mg.
    Auxiliary ingredients: sodium chloride 8.5 mg, sodium citrate 0.5 mg, edetate disodium (sodium salt of ethylenediaminetetraacetic acid (disodium) EDDS) 0.1 mg, polysorbate 80 0.2 mg, citric acid (anhydrous) 0.28 mg, purified water up to 1 ml.
    Description:Easily resuspended sterile white or almost white suspension in low density polyethylene containers containing a single dose.
    Pharmacotherapeutic group:Glucocorticosteroid for topical application.
    ATX: & nbsp

    R.03.B.A.02   Budesonide

    Pharmacodynamics:Budesonide, an inhaled glucocorticosteroid, at recommended doses has an anti-inflammatory effect in the bronchi, reducing the severity of symptoms and the frequency of exacerbations of bronchial asthma with a lower incidence of side effects than with systemic glucocorticosteroids. Reduces the severity of the bronchial mucosa edema, mucus production, sputum formation and airway hyperreactivity. Well tolerated with long-term treatment, does not have mineralocorticosteroid activity.
    The time to start the therapeutic effect after inhalation of a single dose of the drug is several hours. The maximum therapeutic effect is achieved 1-2 weeks after treatment. Budesonide has a preventive effect on the course of bronchial asthma and does not affect the acute manifestations of the disease.
    A dose-dependent effect on cortisol levels in plasma and urine was demonstrated on the background of Pulmicort's acceptance. In recommended doses, the drug has a significantly lower effect on adrenal function than prednisone in a dose of 10 mg, as was shown in ACTH tests.
    Pharmacokinetics:Absorption Inhalable budesonide quickly absorbed. In adults, the systemic bioavailability of budesonide after inhalation of the Pulmicort suspension through the nebulizer is approximately 15% of the total prescribed dose and about 40-70% of the delivered. The maximum concentration in blood plasma is reached in 30 minutes after the beginning of inhalation.
    Metabolism and distribution The connection with plasma proteins is on average 90%. The volume of budesonide distribution is approximately 3 l / kg. After suction budesonide is subjected to intensive biotransformation (more than 90%) in the liver with the formation of metabolites with low glucocorticosteroid activity. The glucocorticosteroid activity of the major metabolites of beta-hydroxy-budesonide and 16α-hydroxy-prednisolone is less than 1% of the glucocorticosteroid activity of budesonide.
    Excretion Budesonide is metabolized mainly with the participation of the enzyme CYP3A4. Metabolites are excreted unchanged in urine or in conjugated form. Budesonide has a high system clearance (about 1.2 l / min). The pharmacokinetics of budesonide is proportional to the magnitude of the administered dose of the drug.
    The pharmacokinetics of budesonide in children and patients with impaired renal function has not been studied. In patients with liver disease, budesonide can be longer in the body.
    Indications:-Bronchial asthma requiring maintenance therapy with glucocorticosteroids.
    Chronic obstructive pulmonary disease (COPD).
    Stenosing laryngotracheitis (false croup).
    Contraindications:-Increased sensitivity to budesonide.
    -Children under 6 months.
    Carefully:More careful monitoring of patients is required: in patients with fungal, viral, bacterial infections of the respiratory system, liver cirrhosis; when prescribing should take into account the possible manifestation of the systemic action of glucocorticosteroids.
    Pregnancy and lactation:Pregnancy: monitoring of pregnant women taking budesonide, did not reveal anomalies in the fetus, nevertheless, the risk of their development can not be completely ruled out, therefore, during pregnancy, the minimal effective dose of budesonide should be used in connection with the possibility of worsening of the course of bronchial asthma.
    Lactation: Budesonide penetrates into breast milk, however, when applying Pulmicort in therapeutic doses, no effect was observed on the baby. Pulmicort can be used during breastfeeding.
    Dosing and Administration:The dose of the drug is selected individually. In the event that the recommended dose does not exceed 1 mg / day, the entire dose of the drug can be taken at a time (one time). In case of taking a higher dose, it is recommended to divide it into two doses.
    Recommended initial dose:
    Children 6 months and older: 0.25-0.5 mg per day. If necessary, the dose may be increased to 1 mg / day.
    Adults / elderly patients: 1-2 mg per day.
    Dose with maintenance treatment:
    Children 6 months and older: 0.25-2 mg per day.
    Adults: 0.5-4 mg per day. In case of severe exacerbations, the dose may be increased.
    Table for determining the dose

    Dose, mg

    Amount of preparation

    Pulmicort suspension for inhalation

    0.25 mg / ml

    0.5 mg / ml

    0,25

    1 ml *


    0,5

    2 ml


    0,75

    3 ml


    1

    4 ml

    2 ml

    1,5

    -

    3 ml

    2

    -

    4 ml


    *) should be diluted with 0.9% solution of sodium chloride to a volume of 2 ml
    For all patients, it is desirable to determine the minimum effective maintenance dose.
    If it is necessary to achieve an additional therapeutic effect, an increase in the daily dose (up to 1 mg / day) of Pulmicort can be recommended instead of the combination of the drug with oral glucocorticosteroids; due to a lower risk of systemic effects.
    Patients receiving oral glucocorticosteroids
    Cancellation of oral glucocorticosteroids should be started against a background of stable patient health. Within 10 days, it is necessary to take a high dose of Pulmicort against oral glucocorticosteroids in the usual dose. In the future, during a month, gradually reduce the dose of oral glucocorticosteroids (for example, 2.5 mg of prednisolone or its analog) to the minimum effective dose. In many cases it is possible to completely stop taking oral glucocorticosteroids.Since Pulmicort, used as a suspension with a nebulizer, enters the lungs during inspiration, it is important to instruct the patient to inhale the drug through the nebulizer mouthpiece calmly and smoothly.
    There is no data on the use of budesonide in patients with renal insufficiency or liver dysfunction. Taking into account the fact that budesonide is deduced by biotransformation in the liver, we can expect an increase in the duration of the drug in patients with severe hepatic cirrhosis.
    Stenosing laryngotracheitis (false croup):
    Children 6 months and older: 2 mg per day. The dose of the drug can be taken at a time (once) or divided into two divided doses of 1 mg at intervals of 30 minutes.

    The use of pulmicort with a nebulizer

    The pulmicort is used for inhalations using an appropriate nebulizer equipped with a mouthpiece and a special mask. The nebulizer is connected to the compressor to create the required air flow (5-8 l / min), the nebulizer filling volume should be 2-4 ml.

    It is important to inform the patient:

    carefully read the instructions for use;

    • for the use of a pulmicorta suspension is not suitable ultrasonic nebulizers;

    • The poolmixture slurry is mixed with 0.9 % solution of sodium chloride or with solutions of terbutaline, salbutamol, fenoterol, acetylcysteine, sodium cromoglicate and ipratropium bromide; the diluted suspension should be used within 30 minutes.

    • After inhalation, rinse the mouth with water to reduce the development of candidiasis of the oropharynx;

    • to prevent skin irritation after using the mask, you should wash your face with water;

    • It is recommended that the nebulizer be cleaned regularly according to the manufacturer's instructions;

    In cases where a child can not independently inhale through a nebulizer, a special mask is used.

    How to use Pulmicort® with a nebulizer

    1. Before use, shake the container gently with a slight rotational motion.

    2. Hold the container straight upright (as shown in the picture) and open it, turning and tearing off the "wing".

    3. Gently place the container open end into the nebulizer and slowly squeeze out the contents of the container.

    A container containing a single dose is marked with a line.If the container is turned over, this line will show a volume equal to 1 ml.

    If it is necessary to use only 1 ml of the suspension, the contents of the container are squeezed out until the surface of the liquid reaches the level indicated by the line.

    The open container is stored in a place protected from light. The open container should be used within 12 hours.

    Before using the remainder of the liquid, the contents of the container are gently shaken by rotational movement.

    Note

    After each inhalation, rinse your mouth with water.

    If you are using a mask, make sure that the mask is snug against the face during inhalation. Wash your face after inhalation.

    Cleaning

    The nebulizer chamber, mouthpiece or mask should be cleaned after each use. The nebulizer chamber, mouthpiece or mask is washed with warm water, using a mild detergent or in accordance with the manufacturer's instructions. Rinse well and dry the nebulizer by connecting the chamber to the compressor or the air inlet valve.

    Side effects:The frequency of undesirable effects is as follows:
    Often (> 1/100, <1/10); Infrequently (> 1/1000, <1/100); Rarely (> 1/10000, <1/1000); Very rarely (<1/10000), including individual messages.
    Up to 10% of patients taking the drug may experience the following side effects:

    Often

    Airways:

    Candidiasis of the oropharynx, irritation of the mucous pharynx, cough, hoarseness of voice, dry mouth

    Rarely

    Are common:



    Leather:



    Airways:

    Central nervous system:



    The immune system:









    Gastrointestinal tract:

    Angioedema



    Appearance of bruises on the skin.



    Bronchospasm

    Nervousness, excitability, depression, behavioral disorders

    Hypersensitivity reactions of immediate and delayed type, including rash, contact dermatitis, hives, angioedema, bronchospasm and anaphylactic reaction.

    Nausea.

    Rarely

    Laboratory indicators:



    Sense organs:

    Reduction of bone mineral density (systemic action).

    Cataract, glaucoma (systemic action).


    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:There was no interaction of budesonide with other drugs used in the treatment of bronchial asthma.
    Ketoconazole (200 mg once a day) increases the plasma concentration of oral budesonide (3 mg once a day) by an average of 6 times when taken together. When taking ketoconazole 12 hours after taking budesonide, the concentration of the latter in the blood plasma increased by an average of 3 times. Information on this interaction with budesonide in the form of inhalation is not available, but it is expected that in this case, an increase in the concentration of budesonide in blood plasma should be expected. If you need to take ketoconazole and budesonide, you should increase the time between taking the drugs to the maximum possible. You should also consider the possibility of reducing the dose of budesonide. Another potential inhibitor of CYP3A4, for example, itraconazole, also significantly increases the plasma concentration of budesonide. Preliminary inhalation of beta-adrenostimulants expands bronchi, improves the flow of budesonide into the respiratory tract and enhances its therapeutic effect. Phenobarbital, phenytoin, rifampicin reduce the effectiveness (induction of enzymes of microsomal oxidation) budesonide.
    Methandrostenolone, estrogens strengthen the action of budesonide.
    Special instructions:To minimize the risk of fungal oropharyngeal injury, the patient should be instructed to thoroughly rinse the mouth with water after each inhalation of the drug.
    Joint administration of budesonide with ketoconazole, itraconazole or other potential inhibitors of CYP3A4 should be avoided. If budesonide and ketoconazole or other potential inhibitors of CYP3A4 have been prescribed, the time between taking the drugs to the maximum possible should be increased.
    Because of the possible risk of weakening adrenal function, special attention should be given to patients who are transferred from oral glucocorticosteroids to Pulicicort. Also, special attention should be given to patients taking high doses of glucocorticosteroids, or who received long-term maximum recommended doses of inhaled glucocorticosteroids. In stressful situations, such patients may show signs and symptoms of adrenal insufficiency.When stress or in cases of surgical intervention, additional therapy with systemic glucocorticosteroids is recommended. Particular attention should be given to patients who are transferred from systemic to inhaled glucocorticosteroids (Pulmicort) or in the case where a disorder of the pituitary-adrenal function can be expected. In such patients, it is necessary with special care to reduce the dose of systemic glucocorticosteroids and control the hypothalamic-pituitary-adrenal function. Patients may also require the addition of oral glucocorticosteroids during periods of stressful situations such as trauma, surgery, etc.
    When switching from oral glucocorticosteroids to Pulmicort, patients may experience previously observed symptoms, such as muscle pain or joint pain. In such cases, a temporary increase in the dose of oral glucocorticosteroids may be necessary. In rare cases, such symptoms as fatigue, headache, nausea and vomiting, indicating a systemic insufficiency of glucocorticosteroids, can be observed.
    Replacement of oral glucocorticosteroids by inhalation sometimes leads to the manifestation of concomitant allergies, for example, rhinitis and eczema, which were previously stopped by systemic drugs.
    For children and adolescents receiving treatment with glucocorticosteroids (regardless of the method of delivery) for an extended period, it is recommended that growth rates be regularly monitored. When prescribing glucocorticosteroids, one should take into account the relationship between the benefits of using the drug and the possible risk of slowing growth.
    The use of budesonide in a dose of up to 400 micrograms per day in children older than 3 years did not lead to systemic effects. Biochemical signs of the systemic effect of the drug may occur when taking the drug at a dose of 400 to 800 micrograms per day. When the dose exceeds 800 mcg per day, the systemic effects of the drug are often encountered. The use of glucocorticosteroids for the treatment of bronchial asthma can cause dysplasia. The results of observations of children and adolescents who received budesonide for a long period (up to 11 years), showed that the growth of patients reaches the expected normative indicators for adults.
    Inhalation therapy budesonide om 1 or 2 times a day showed efficacy for the prevention of bronchial asthma physical effort.
    Effect on the ability to drive transp. cf. and fur:The pulmicort does not affect the ability to drive a car or other machinery.
    Form release / dosage:Suspension for inhalations dosed with 0.25 mg / ml and 0.5 mg / ml.
    Packaging:2 ml of the drug in a container of low-density polyethylene. 5 containers are connected in one sheet. A sheet of 5 containers is packed in an envelope made of laminated foil. 4 envelopes in a cardboard box with instructions for use.
    Storage conditions:At temperatures below 30 ° C. Keep out of the reach of children.
    The drug in containers should be used within 3 months after opening the envelope. The open container should be used within 12 hours. Containers should be stored in an envelope to protect them from light.
    Shelf life:2 years. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N013826 / 01
    Date of registration:14.09.2007 / 27.10.2015
    Expiration Date:Unlimited
    The owner of the registration certificate:AstraZeneca ABAstraZeneca AB Sweden
    Manufacturer: & nbsp
    Representation: & nbspAstraZeneca Pharmaceuticals Ltd.AstraZeneca Pharmaceuticals Ltd.
    Information update date: & nbsp10.10.2016
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