Composition, form of production and packaging
Suspension for inhalation is dosed white or almost white, easily resuspendable.
budesonide (micronized) 250 Ојg
- "500 Ојg
Auxiliary substances: sodium chloride, sodium citrate, disodium edetate (sodium salt of ethylenediaminetetraacetic acid (disubstituted)), polysorbate 80, citric acid (anhydrous), purified water.
2 ml (1 dose) - single-dose polyethylene containers (5) - envelopes from laminated foil (4) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
GCS for inhalation use. Budesonide in recommended doses has 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 when using systemic GCS. Reduces the severity of the bronchial mucosa edema, mucus production, sputum formation and airway hyperreactivity. Well tolerated with long-term treatment, does not have mineralocorticoid 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 the cortisol content in plasma and urine is shown on the background of Pulmicort. At recommended doses, the drug has a significantly lower effect on adrenal function than prednisone at a dose of 10 mg, as shown in ACTH tests.
After inhalation budesonide is quickly absorbed. In adults, the systemic bioavailability of budesonide, after inhalation of Pulmicort through the nebulizer, is approximately 15% of the total prescribed dose and about 40-70% of the delivered dose. C max in blood plasma is achieved 30 minutes after the start of inhalation.
Distribution and Metabolism
The binding to plasma proteins is on average 90%. V d budesonide - approximately 3 l / kg.
Budesonide undergoes intensive biotransformation (more than 90%) in the liver with the formation of metabolites with low glucocorticoid activity. Glucocorticoid activity of the main metabolites (6? -hydroxy-budesonide and 16? -hydroxprednisolone) is less than 1% glucocorticoid activity of budesonide. Budesonide is metabolized mainly with the participation of the enzyme CYP3A4.
Budesonide is excreted in the urine in the form of unchanged or conjugated metabolites. 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.
Pharmacokinetics in special clinical cases
The pharmacokinetics of budesonide in children and patients with impaired renal function has not been studied.
In patients with liver disease, there may be an increase in the time of finding budesonide in the body.
- bronchial asthma requiring maintenance therapy for SCS;
- chronic obstructive pulmonary disease (COPD).
The dose of Pulmicort В® is set individually. In the event that the recommended dose does not exceed 1 mg / day, the entire dose of the drug is injected at a time (at a time). In case of taking a higher dose, it is recommended to divide it into 2 doses.
The initial dose for adults (including elderly patients) is 1-2 mg / day. The maintenance dose is 0.5-4 mg / day. In case of severe exacerbations, the dose may be increased.
Children at the age of 6 months and older, the recommended initial dose is 0.25-0.5 mg / day. If necessary, the dose may be increased to 1 mg / day. The maintenance dose is 0.25-2 mg / day.
Dose (mg) Amount of preparation
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 Pulicicort can be recommended instead of the combination of the drug with GCS for oral administration, due to a lower risk of systemic effects.
Patients receiving HSC for oral administration
Cancellation of GCS for oral administration should be started against a background of stable patient health. Within 10 days, high doses of PulmicortВ® are prescribed on the background of taking GCS inside at the usual dose. In the future, during the month should gradually reduce the dose of GCS taken internally (for example, 2.5 mg prednisolone or its analog), to the minimum effective dose. In many cases it is possible to completely refuse from receiving the GCS inside.
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 biotransformed in the liver, an increase in the duration of action of the drug in patients with severe hepatic cirrhosis can be expected.
Using a Pulcicort with a Nebulizer
Pulmicort В® 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.
Because Pulmicort В® , used in the form of 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 in a calm and steady manner.
In cases where a child can not independently inhale through a nebulizer, a special mask is used.
The patient should be informed of the need to carefully read the instructions for using the drug, and that ultrasonic nebulizers are not suitable for the use of Pulmicort in the form of a suspension. The suspension is mixed with 0.9% sodium chloride solution or with solutions of terbutaline, salbutamol, fenoterol, acetylcysteine, sodium cromoglicate and ipratropium bromide. The patient should remember that after inhalation, rinse the mouth with water to reduce the risk of developing candidiasis of the oropharynx and that, to prevent skin irritation after using the mask, you should wash your face with water. Also be aware that a dilute PulmicortВ® suspension should be used within 30 minutes.
It is recommended that the nebulizer be cleaned regularly according to the manufacturer's instructions.
The nebulizer chamber should be cleaned after each use.
The nebulizer chamber and the mouthpiece or mask are washed with warm water, using a mild detergent (according to the manufacturer's instructions). The nebulizer should be thoroughly rinsed and dried by connecting the chamber to the compressor or the inlet air valve.
Rules for using Pulmicort with a nebulizer
1. Before use, shake the container gently with a slight rotational movement.
2. Hold the container straight upright and open it, turning and tearing off the "wing".
3. Carefully 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.
Up to 10% of patients taking the drug may experience the following side effects:
Frequency of detection Body system / reaction Side effect type
Often (> 1/100) Respiratory tract Candidiasis of the oropharynx, irritation of the mucous membrane of the pharynx, cough, hoarseness of voice, dry mouth
Rarely (<1/1000) Allergic reactions Angioedema
Dermatologic reactions Hives, rash, contact dermatitis
Respiratory tract Bronchospasm
From the side of the central nervous system: nervousness, excitability, depression, behavior disorders are possible.
In some cases , symptoms can occur due to systemic effects of SCS (including adrenal hypofunction).
Other: rarely - the appearance of bruising on the skin, irritation of the skin of the face when using a nebulizer with a mask.
- Children's age up to 6 months;
- hypersensitivity to budesonide.
With caution (you need more careful monitoring of patients), you should prescribe the drug to patients with active pulmonary tuberculosis, fungal, viral, bacterial infections of the respiratory system, liver cirrhosis.
At appointment it is necessary to take into account possible or probable display of systemic action SGC.
PREGNANCY AND LACTATION
Observation of pregnant women taking budesonide did not reveal fetal development abnormalities, nevertheless, the risk of their development can not be completely excluded, therefore, in pregnancy, the minimum effective dose of the drug should be used in connection with the possibility of worsening of the course of bronchial asthma.
Budesonide excreted in breast milk, however, when applying Pulmicort in therapeutic doses, no effect was observed on the baby. Pulmicort В® can be used for breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
There is no data on the use of budesonide in patients with renal insufficiency .
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
There is no data on the use of budesonide in patients with impaired liver function . Taking into account the fact that budesonide is biotransformed in the liver, an increase in the duration of action of the drug in patients with severe hepatic cirrhosis can be expected.
APPLICATION FOR CHILDREN
Contraindicated in childhood up to 6 months.
To minimize the risk of fungal oropharyngeal disease, the patient should be instructed to rinse the mouth thoroughly with water after each inhalation of the drug.
To prevent skin irritation after using a nebulizer with a mask, the face should be washed.
Joint administration of budesonide with ketoconazole, itraconazole or other potential inhibitors of CYP3A4 should be avoided. If such a combination is necessary, you should increase the time between doses of the drugs to the maximum possible.
Because of the possible risk of weakening adrenal function, special attention should be paid to patients who are transferred from systemic SCS to Pulmicort. Also, special attention should be paid to patients taking high doses of GCS or who received long-term recommended maximum 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 GCS is recommended.
Particular attention should be given to patients who are transferred from systemic to inhaled glucocorticosteroids (PulmicortВ®) 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 GCS for systemic use and monitor the performance of the hypothalamic-pituitary-adrenal system. This category of patients may require additional prescription of GCS for oral administration during periods of stressful situations, such as trauma, surgery.
When switching from oral glucocorticosteroids to PulmicortВ®, patients may experience previously observed symptoms, such as muscle pain or joint pain. In such cases, a temporary increase in the dose of GCS for oral administration may be required. In rare cases, symptoms such as a feeling of fatigue, headache, nausea and vomiting, indicating a systemic failure of GCS, can be observed.
When switching from GCS for oral ingestion to inhalation, it is sometimes possible to exacerbate existing allergic reactions, rhinitis and eczema, which were previously treated with systemic drugs.
Pulmicort therapy when applied 1 or 2 times / day showed efficacy for the prevention of asthma physical effort.
Use in Pediatrics
In children and adolescents receiving treatment with GCS (any form) for an extended period, it is recommended to regularly monitor growth rates. When appointing GCS, it is necessary to evaluate the ratio of the prospective benefit from the use of the drug and the potential risk of slowing growth.
The use of budesonide in a dose of up to 400 Ојg / 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 the drug is used at a dose of 400 to 800 mcg / day. When the dose exceeds 800 mcg / day, the systemic effects of the drug are often encountered.
The use of GCS to treat 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 indices for adults.
Impact on the ability to drive vehicles and manage mechanisms
Pulmicort В® does not affect the ability to drive a car or other machinery.
In acute overdose of the drug Pulmicort В® clinical manifestations do not arise.
With prolonged use of the drug in doses much higher than recommended, it is possible to develop systemic effects of GCS in the form of hypercorticism and suppression of adrenal function.
There was no interaction of budesonide with other drugs used in the treatment of bronchial asthma.
When combined, ketoconazole (at a dose of 200 mg 1 time / day) increases the plasma concentration of budesonide (ingested at a dose of 3 mg 1 time / day) by an average of 6 times. When taking ketoconazole 12 hours after the administration of budesonide, the concentration of the latter in the blood plasma increased by an average of 3 times. There is no information on such interaction between taking budesonide in the form of inhalation, but it is expected that in this case an increase in budesonide concentration in blood plasma should be expected. If it is necessary to take ketoconazole and budesonide, you should increase the time between doses of the drugs to the maximum possible. You should also consider the possibility of reducing the dose of budesonide.
Another potential inhibitor of CYP3A4, 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 when used simultaneously reduces the effectiveness of Pulmicort (due to the induction of microsomal oxidation enzymes).
Methandrostenolone, estrogens strengthen the action of budesonide.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children at a temperature below 30 В° C. Shelf life - 2 years. Do not use after the expiry date printed on the package.
After opening the envelope, the containers contained in it should be used within 3 months. Containers should be stored in an envelope to protect them from light.
The open container should be used within 12 hours.