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Pulmicort suspension for inhalation 0.5 mg/ml 2 ml container 20 pcs. in Voronezh
An easily resuspended, white or off-white, sterile suspension in LDPE containers containing a single dose.
Absorption.
Inhaled budesonide is rapidly absorbed. In adults, the systemic bioavailability of budesonide after inhalation of Pulmicort® suspension through a nebulizer is approximately 15% of the total prescribed dose and about 40–70% of the delivered dose. Cmax in blood plasma is achieved 30 minutes after the start of inhalation.
Metabolism and distribution.
Plasma protein binding averages 90%. Vd of budesonide is approximately 3 l/kg. After absorption, budesonide undergoes intense biotransformation (more than 90%) in the liver with the formation of metabolites with low glucocorticosteroid activity. The glucocorticosteroid activity of the main metabolites 6β-hydroxy-budesonide and 16α-hydroxyprednisolone is less than 1% of the glucocorticosteroid activity of budesonide.
Excretion.
Budesonide is metabolized mainly by the enzyme CYP3A4. Metabolites are excreted unchanged in the urine or in conjugated form. Budesonide has a high systemic clearance (about 1.2 l/min). The pharmacokinetics of budesonide is proportional to the administered dose of the drug.
The pharmacokinetics of budesonide in children and patients with impaired renal function have not been studied. In patients with liver disease, the residence time of budesonide in the body may increase.
Budesonide, an inhaled corticosteroid, in 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 when using systemic corticosteroids. Reduces the severity of edema of the bronchial mucosa, mucus production, sputum formation and airway hyperreactivity. It is well tolerated during long-term treatment and does not have mineralocorticosteroid activity.
The time for the onset of the therapeutic effect after inhalation of one 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 content of cortisol in plasma and urine while taking Pulmicort® was shown. At recommended doses, the drug has significantly less effect on adrenal function than prednisone at a dose of 10 mg, as shown in ACTH tests.
To minimize the risk of fungal infection of the oropharynx, the patient should be instructed to thoroughly rinse the mouth with water after each inhalation of the drug.
Co-administration of budesonide with ketoconazole, itraconazole or other potential CYP3A4 inhibitors should be avoided. If budesonide and ketoconazole or other potential CYP3A4 inhibitors have been prescribed, the time between doses should be increased to the maximum possible.
Due to the possible risk of weakening adrenal function, special attention should be paid to patients who are switching from oral corticosteroids to taking Pulmicort®. Also, special attention should be paid to patients who have taken high doses of corticosteroids or who have been receiving the highest recommended doses of inhaled corticosteroids for a long time. In stressful situations, these patients may exhibit signs and symptoms of adrenal insufficiency. In case of stress or in cases of surgical intervention, it is recommended to carry out additional therapy with systemic corticosteroids.
Particular attention should be paid to patients who are transferred from systemic to inhaled GCS (Pulmicort®), or in cases where a violation of the pituitary-adrenal function can be expected. In such patients, the dose of systemic corticosteroids should be reduced with extreme caution and the hypothalamic-pituitary-adrenal function should be monitored. Patients may also require the addition of oral corticosteroids during stressful situations, such as trauma or surgery.
When switching from oral corticosteroids 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 corticosteroids may be necessary. In rare cases, symptoms such as fatigue, headache, nausea and vomiting may occur, indicating systemic insufficiency of GCS.
Replacing oral corticosteroids with inhaled ones sometimes leads to the manifestation of concomitant allergies (for example, rhinitis and eczema), which were previously treated with systemic drugs.
In children and adolescents receiving treatment with corticosteroids (regardless of the method of delivery) for an extended period, it is recommended to regularly monitor growth parameters. When prescribing GCS, the balance between the benefits of using the drug and the possible risk of growth retardation should be taken into account.
The use of budesonide at a dose of up to 400 mcg/day in children over 3 years of age did not lead to systemic effects. Biochemical signs of a systemic effect of the drug may occur when taking the drug at a dose of 400 to 800 mcg/day. When the dose exceeds 800 mcg/day, systemic effects of the drug are common.
The use of corticosteroids for the treatment of bronchial asthma may cause growth impairment. The results of observations of children and adolescents receiving budesonide for a long period (up to 11 years) showed that the growth of patients reaches the expected normative indicators for adults.
Therapy with inhaled budesonide 1 or 2 times a day has shown effectiveness for the prevention of bronchial asthma due to physical exertion.
Impact on the ability to drive a car or use other machinery.
Pulmicort® does not affect the ability to drive a car or use other machinery.
Using Pulmicort® using a nebulizer
Pulmicort® is used for inhalation using an appropriate nebulizer equipped with a mouthpiece and a special mask. The nebulizer is connected to a compressor to create the required air flow (5–8 l/min); the filling volume of the nebulizer should be 2–4 ml.
It is important to inform the patient about the following:
— you must carefully read the instructions for using the drug;
— ultrasonic nebulizers are not suitable for the use of Pulmicort® suspension;
— Pulmicort® suspension is mixed with 0.9% sodium chloride solution or with solutions of terbutaline, salbutamol, fenoterol, acetylcysteine, sodium cromoglycate and ipratropium bromide; the diluted suspension is used within 30 minutes;
- after inhalation, you should rinse your mouth with water to reduce the development of oropharyngeal candidiasis;
— to prevent skin irritation, after using the mask, rinse your face with water;
- It is recommended to regularly clean the nebulizer in accordance with the manufacturer's instructions.
In cases where a child cannot independently inhale through a nebulizer, a special mask is used.
How to use Pulmicort® using a nebulizer
1. Before use, carefully shake the container with a gentle rotational motion.
2. Hold the container straight upright and open it by turning and tearing off the “wing”.
3. Carefully place the open end of the container into the nebulizer and slowly squeeze out the contents of the container.
The container containing a single dose is marked with a line. If the container is turned upside down, this line will show a volume of 1 ml.
If only 1 ml of suspension is to be used, squeeze out the contents of the container until the surface of the liquid reaches the level indicated by the line.
Store the opened container in a place protected from light. An opened container must be used within 12 hours.
Before using the remaining liquid, carefully shake the contents of the container with a rotational motion.
Note
1. After each inhalation, rinse your mouth with water.
2. If the patient uses a mask, make sure that the mask fits tightly to the face when inhaling. Wash your face after inhalation.
Cleaning
The nebulizer chamber, mouthpiece or mask should be cleaned after each use.
Wash the nebulizer chamber, mouthpiece or mask with warm water using a mild detergent or in accordance with the manufacturer's instructions. Rinse and dry the nebulizer well by connecting the chamber to the compressor or air inlet valve.
PULMICORT Susp. d/inhal. 0.25 mg/ml 2 ml No. 20
Directions for use and doses
The dose of the drug is selected individually.
If the recommended dose does not exceed 1 mg/day, the entire dose of the drug can be taken at one time (at one time). If you take a higher dose, it is recommended to divide it into two doses. Recommended starting dose: Children 6 months and older: 0.25-0.5 mg per day. If necessary, the dose can be increased to 1 mg/day. Adults/elderly patients: 1-2 mg per day. Maintenance dose: 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. Dose determination table.
Dose, mg | Volume of the drug 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 |
It is advisable to determine the minimum effective maintenance dose for all patients. If it is necessary to achieve an additional therapeutic effect, it is possible to recommend increasing the daily dose (up to 1 mg/day) of Pulmicort instead of combining the drug with oral glucocorticosteroids; due to a lower risk of systemic effects. Patients receiving oral glucocorticosteroids Cancellation of oral glucocorticosteroids should begin when the patient's health is stable. For 10 days, it is necessary to take a high dose of Pulmicort while taking oral glucocorticosteroids at the usual dose. Subsequently, over the course of a month, the dose of oral glucocorticosteroids (for example, 2.5 mg of prednisolone or its analogue) should be gradually reduced to the minimum effective dose.
In many cases, it is possible to completely stop taking oral glucocorticosteroids. Since Pulmicort, administered as a suspension through a nebulizer, enters the lungs when inhaled, it is important to instruct the patient to inhale the drug through the nebulizer mouthpiece calmly and evenly. There are no data on the use of budesonide in patients with renal failure or impaired liver function. Taking into account the fact that budesonide is eliminated by biotransformation in the liver, an increase in the duration of action of the drug can be expected in patients with severe liver cirrhosis. Stenosing laryngotracheitis (false croup): Children 6 months and older: 2 mg per day. The dose of the drug can be taken at one time (at a time) or divided into two doses of 1 mg each with an interval of 30 minutes.
Using Pulmicort using a nebulizer.
Pulmicort is used for inhalation using an appropriate nebulizer equipped with a mouthpiece and a special mask. The nebulizer is connected to a compressor to create the required air flow (5-8 l/min), the filling volume of the nebulizer should be 2-4 ml.
It is important to inform the patient: carefully read the instructions for use of the drug; Ultrasonic nebulizers are not suitable for the use of Pulmicort suspension; Pulmicort suspension is mixed with 0.9% sodium chloride solution or with solutions of terbutaline, salbutamol, fenoterol, acetylcysteine, sodium cromoglycate and ipratropium bromide; the diluted suspension should be used within 30 minutes. after inhalation, you should rinse your mouth with water to reduce the development of oropharyngeal candidiasis; to prevent skin irritation, after using the mask, rinse your face with water; It is recommended to regularly clean the nebulizer in accordance with the manufacturer's instructions; In cases where a child cannot independently inhale through a nebulizer, a special mask is used.
How to use Pulmicort using a nebulizer. Before use, gently shake the container with a gentle swirling motion. Hold the container straight upright (as shown in the picture) and open it by twisting and tearing off the “wing”. Carefully place the open end of the container into the nebulizer and slowly dispense the contents of the container. The container containing a single dose is marked with a line. If the container is turned upside down, this line will show a volume of 1 ml. If only 1 ml of suspension is to be used, 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. An opened container must be used within 12 hours. Before using the remaining liquid, carefully shake the contents of the container with a rotational motion.
Note. After each inhalation, rinse your mouth with water. If you use a mask, make sure that the mask fits snugly against your face when inhaling. Wash your face after inhalation.
Cleaning. The nebulizer chamber, mouthpiece or mask should be cleaned after each use. Wash the nebulizer chamber, mouthpiece or mask with warm water, using a mild detergent, or according to the manufacturer's instructions. Rinse and dry the nebulizer well by connecting the chamber to the compressor or air inlet valve.