Composition, form of production and packaging
Powder for inhalation dosed in the form of round granules from white to almost white color, easily destroyed at the slightest mechanical effect; a small part can be present in the form of a powder.
1 dose
budesonide 100 Ојg
200 doses - turbuhaler (1) consisting of a dispenser, a powder storage tank, a desiccant tank, a mouthpiece and a lid - packs of cardboard.
Powder for inhalation dosed in the form of round granules from white to almost white color, easily destroyed at the slightest mechanical effect; a small part can be present in the form of a powder.
1 dose
budesonide 200 Ојg
100 doses - plastic inhalers (1) consisting of a dosing device, a powder storage tank, a desiccant tank, a mouthpiece and a lid - packs of cardboard.
200 doses - plastic inhalers (1) consisting of a dispenser, a powder storage tank, a desiccant tank, a mouthpiece and a lid - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2008.
PHARMACHOLOGIC EFFECT
Glucocorticosteroid for topical application.
Budesonide is a glucocorticosteroid with a strong local anti-inflammatory effect.
The exact mechanism of action of glucocorticosteroids in the treatment of bronchial asthma is not fully understood. An anti-inflammatory effect, such as inhibiting the release of inflammatory mediators and a cytokine-mediated immune response, is perhaps the most important. The affinity of budesonide to the receptors of glucocorticosteroids is 15 times higher than that of prednisolone.
The anti-inflammatory effect of budesonide is mediated by a decrease in the degree of airway obstruction during an early and late allergic response. Budesonide reduces airway reactivity in response to inhalation of histamine and methacholine.
The sooner the bronchial asthma of the persistent current is started with treatment with budesonide, the greater the improvement in lung function should be expected.
A dose-dependent effect on the cortisone content in plasma and urine is shown on the background of Pulmicort Turbuhaler intake. 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.
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 can occur when taking the drug 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 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 indices for adults. Therapy with inhaled budesonide 1 or 2 times / day has shown effectiveness for the prevention of asthma physical effort.
PHARMACOKINETICS
Absorption
Inhaled budesonide is rapidly absorbed. After inhalation using Turbuhaler about 25-35% of the measured dose gets into the lungs. The maximum concentration in the blood plasma is reached 30 minutes after inhalation. Systemic bioavailability of the drug is about 38% of the dose.
Metabolism and distribution
The binding to plasma proteins is on average 90%. The volume of budesonide distribution is approximately 3 l / kg. After absorption, budesonide undergoes intensive (more than 90%) biotransformation in the liver to form metabolites with low glucocorticosteroid activity. Glucocorticosteroid activity of the main metabolites of 6? -hydroxybudesonide and 16? -hydroxprednisolone is less than 1% of the glucocorticosteroid activity of budesonide.
Excretion
Budesonide is metabolized mainly with the participation of the enzyme CYP 3A4. Metabolites are excreted unchanged in urine or in conjugated form. A small amount of unmodified budesonide is excreted in the urine. Budesonide has a high system clearance (about 1.2 l / min). Pharmacokipetik budesonide is proportional to the amount of the administered dose of the drug.
The pharmacokinetics of budesonide in children and patients with impaired renal function is unknown. In patients with liver disease, budesonide can be longer in the body.
INDICATIONS
- bronchial asthma, requiring maintenance therapy with glucocorticosteroids to control the inflammatory process.
- chronic obstructive pulmonary disease (COPD).
DOSING MODE
The dose of Pulmicorta Turbuhaler is selected individually. Recommended doses of the drug in the case of the onset of inhaled glucocorticosteroid therapy in the period of severe exacerbations of bronchial asthma, as well as against a dose reduction or withdrawal of oral GCS, are as follows:
Children older than 6 years : 100-800 mcg / day (the total daily intake of the drug can be divided into 2-4 inhalations). In the event that the recommended dose does not exceed 400 mcg / day, the entire dose of the drug can be taken at a time (one time).
In children, the transition to a single dose should be performed under the supervision of a pediatrician.
Adults : the usual dose is 200-800 mcg / day (the total daily dose of the drug can be divided into 2-4 inhalations). For the treatment of severe exacerbation of bronchial asthma, the daily dose can be increased to 1600 Ојg. If the recommended dose does not exceed 400 mcg / day, the entire dose of the drug can be administered at a time (one time).
When selecting a maintenance dose, it is necessary to strive to prescribe the minimum effective dose.
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. Pulmicort Turbuhaler has a preventive effect on the course of bronchial asthma and does not affect the acute manifestations of the disease.
The best efficacy of budesonide was demonstrated when using Turbuhaler compared with a similar dose of budesonide in the form of a dosed aerosol. In the case of a patient in a stable condition from Pulmicort in aerosol form to Pulmicort Turbuhaler, the possibility of reducing the daily dose of budesonide should be considered. To increase the therapeutic effect, an increase in the daily dose of Pulmicort turbuhaler may be recommended instead of the combination of the drug with oral glucocorticosteroids, due to a lower risk of developing systemic effects.
Patients receiving oral glucocorticosteroids:
The abolition of oral glucocorticosteroids should be carried out against a background of stable patient health. Within 10 days it is recommended to take a high dose of Pulmicort 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 or its analogues) to the lowest possible level. In many cases, it is possible to completely stop taking oral glucocorticosteroids.
There is no data on the use of budesonide in patients with renal insufficiency or liver dysfunction. Taking into account the excretion of budesonide due to biotransformation in the liver, an increase in the duration of action of the drug in patients with severe cirrhosis of the liver can be expected.
The drug contained in the Turbuhaler, enters the patient's airways along with the air streams while performing an active inspiration through the Turbuhaler mouthpiece.
It is important to convince the patient to carefully read the instructions for using Pulmicort Turbuhaler.
To be sure that the optimal dose of the drug has entered the lungs, take a deep and strong breath through Turbuhaler's mouthpiece.
Under no circumstances exhale through the mouthpiece.
After inhalation of the required dose of the drug, rinse the mouth with water in order to minimize the risk of fungal infection of the oropharynx.
How to use Pulmicort Turbuhaler
Turbuhaler - multi-dose inhaler, which allows you to dose and inhale the drug in very small doses. When you inhale, the powder from Turbuhaler is delivered and the lungs. Therefore, it is important that you take a deep and deep breath through the mouthpiece.
Turbuhaler is very simple to use. Just follow the instructions below:
1. Unscrew and remove the cap.
2. Hold the inhaler vertically with the dispenser down. Load the dose into the inhaler by turning the dispenser counter-clockwise until it stops, and then turn the dispenser to its original position until it clicks.
3. Exhale. Do not exhale through the mouthpiece. Before exhaling, remove the inhaler from the mouth.
4 Gently squeeze the mouthpiece with your teeth, squeeze your lips and inhale deeply and strongly through your mouth. The mouthpiece can not be chewed and strongly compressed with teeth.
If more than one dose is required, repeat steps 2-5.
5. Close the inhaler cap.
6. Rinse your mouth with water.
Important! Never exhale through the mouthpiece. Always close the inhaler cap tightly after use.
Since the amount of inhaled powder is very small, you may not feel the taste of the powder after inhalation. However, if you followed the instructions, you can be sure. that they inhaled the necessary dose of the drug.
Cleaning. Regularly (once a week), clean the mouthpiece from the outside with a dry cloth. Do not use water or other liquids to clean the mouthpiece.
How do you know that the inhaler is empty?
The appearance of a red mark in the dose window means that approximately 20 doses remain in the inhaler. The inhaler is empty when the red mark reaches the bottom edge of the indicator dose window.
The sound that you hear, shaking the inhaler, is produced by a dehumidifying agent, not a medicine.
SIDE EFFECT
Up to 10% of patients taking the drug may experience the following side effects:
Frequent (> 1/100) Respiratory: Candidiasis of the oropharynx, irritation of the mucous pharynx, cough, hoarseness of the voice
Rare (<1/1000) General: Angioedema
Skin: Urticaria, rash, contact dermatitis
Respiratory tract: Bronchospasm
There may also be neuropsychiatric symptoms, such as nervousness, excitability, depression, behavioral disorders. Taking into account the risk of developing candidiasis of the oropharynx, the patient should thoroughly rinse the mouth with water after each inhalation of the drug.
In rare cases, symptoms can occur due to systemic effects of glucocorticosteroids, including adrenal hypofunction. In rare cases, bruises appeared on the skin.
CONTRAINDICATIONS
- children's age till 6 years;
- hypersensitivity to budesonide.
Caution should be exercised when treating patients with active or inactive forms of pulmonary tuberculosis, fungal, viral or bacterial infections of the respiratory system with inhaled glucocorticosteroids.
PREGNANCY AND LACTATION
Pregnancy :
While receiving pregnant women, budesonide has not been shown to increase the risk of developmental abnormalities in the fetus, however, the risk of their development can not be completely ruled out, therefore, in the course of pregnancy, the minimum effective dose of budesonide should be used in connection with the possibility of worsening of the course of bronchial asthma.
Animal studies have shown that glucocorticosteroids can cause abnormalities in fetal development, but these data can not be extrapolated to people receiving glucocorticosteroids at the recommended doses.
Lactation:
There is no data on the occurrence of budesonide in breast milk.
When prescribing a drug, consider the ratio of expected benefits to the mother and the potential risk to the child.
SPECIAL INSTRUCTIONS
To minimize the risk of fungal oropharyngeal injury, the patient should be instructed to rinse the mouth thoroughly with water after each inhalation of the drug.
Joint assignment of budesonide with ketoconazole, itraconazole or other potential inhibitors of CYP 3A4 should be avoided. In the event that budesonide and ketocanazole or vtracoazole or other potential inhibitors of CYP 3A4 have been prescribed, the time between taking the drugs to the maximum possible should be increased.
Because of the possible risk of weakening the pituitary-adrenal function, special attention should be given to patients who are transferred from oral glucocorticosteroids to Pulmicort. 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 paid to patients who are transferred from systemic to inhaled glucocorticosteroids (Pulmicort Turbuhaler) or in the case where a disorder of the pituitary-adrenal function can be expected. Such patients should be very careful to reduce the dose of systemic SCS and monitor the hormonal function of the adrenal glands. Patients may also require the administration of oral glucocorticosteroids in times of stressful situations such as trauma, surgery, etc.
When switching from oral glucocorticosteroids to Pulmicort Turbuhaler, patients may experience previously observed symptoms, such as muscle aches or joint pain.In such cases, a temporary increase in the dose of oral glucocorticosteroids may be necessary. In rare cases, symptoms such as a feeling of fatigue, headache, nausea and vomiting, indicating a systemic failure of GCS, can be observed.
The replacement of oral glucocorticosteroids by inhalation sometimes results in the manifestation of concomitant allergies, for example rhinitis and eczema, which were previously treated with 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.
Patients should be instructed about the need to consult a doctor in case of a decrease in the effectiveness of therapy with short-acting bronchodilators, as an independent increase in the frequency of use of the drug may lead to a delay in the appointment of adequate treatment. In the event of a sudden deterioration in the condition, consideration should be given to the possibility of a course of treatment with oral glucocorticosteroids.
Impact on the ability to drive vehicles and manage mechanisms
Pulmicort Turbuhaler does not affect the ability to drive a car or other machinery.
OVERDOSE
When an overdose of Pulmicort turbuhalerom in doses significantly exceeding the recommended, clinical manifestations does not arise. 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.
DRUG INTERACTION
There was no interaction of budesonide with other drugs used in the treatment of bronchial asthma.
Ketoconazole (200 mg / day) increases the plasma concentration of oral budesonide (3 mg / day) and an average of 6 times with a joint admission. When taking ketoconazole 12 hours after the administration of budesonide, the concentration of the latter and plasma increased by an average of 3 times. There is no information on such interaction when taking inhaled budesonide, but it is expected that in this case an increase in budesond concentration in blood plasma should be expected. Do not prescribe these drugs at the same time due to the lack of data. In case of necessity of co-administration of ketoconazole and budesovnd, the time between taking the medications should be increased to the maximum possible. You should also consider reducing the dose of budesonide. Other potential inhibitors of the CYP 3A4 enzyme (eg, itraconazole) also cause a significant increase in plasma concentrations of budesonide.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
Store at temperatures below 30 В° C, out of the reach of children. Shelf life - 2 years.
