PULMYKORT

Active material: Budesonide
When ATH: R03BA02
CCF: GCS for inhalation
ICD-10 codes (testimony): J44, J45
When CSF: 04.03
Manufacturer: ASTRAZENECA AB (Sweden)

Pharmaceutical form, composition and packaging

Suspension for inhalations dosed white or nearly white, easy resuspendiruemaâ.

Excipients: sodium chloride, sodium citrate, disodium эdetat (the sodium salt of ethylenediaminetetraacetic acid (dvuzameŝennaâ)), polysorbate 80, lemon acid (Anhydrous), Purified water.

2 ml (1 dose) – adjust the plastic containers (5) – envelopes made of laminated foil (4) – packs cardboard.

* international non-proprietary name, recommended by the WHO – ʙudezonid.

Pharmacological action

SCS for inhalations with a pronounced local anti-inflammatory effect.

Budesonide, in recommended doses, anti-inflammatory in the bronchi, reducing the severity of symptoms and the frequency of exacerbations of asthma with fewer side effects, than using systemic CORTICOSTEROIDS. Reduces the severity of bronchial mucosa oedema, mucus production, Education sputum and airway hyperresponsiveness. Well tolerated in long-term care, It has no mineralocorticoid activity.

Time of beginning of therapeutic effect after inhalation of a single dose of the drug is several hours. The maximum therapeutic effect is achieved through the 1-2 weeks after treatment.

Budesonide has a preventive effect for bronchial asthma and does not affect the acute manifestations of disease.

Shown a dose-dependent effect on cortisol in the plasma and urine in the face of the reception Pul′mikorta^®. In recommended doses, the drug has a much smaller effect on adrenal function, than prednisone dose 10 mg, as was shown in the ACTH tests.

Pharmacokinetics

Absorption

After inhalation of budesonide is rapidly absorbed. In the adult system bioavailability budesonide, after inhalation Pul′mikorta^® via nebulizer, approximately 15% of the total assigned dose and about 40-70% from the delivered. C_max plasma levels achieved after 30 minutes after the start of inhalation.

Distribution and metabolism

Linking plasma proteins averages 90%. V_d budesonide – about 3 l / kg.

Budesonide undergoes intensive biotransformation (more 90%) in the liver with the formation of metabolites with low glûkokortikosteroidnoj activity. Glûkokortikosteroidnaâ activity of major metabolites (6β-hydroxy-budesonide and 16α-gidroksiprednizolona) is less than 1% glûkokortikosteroidnoj activity of budesonide. Budesonide is metabolized involving mainly the enzyme CYP3A4.

Deduction

Budesonide return with urine in the form of unmodified or conjugated metabolites. Budesonide has a high ground clearance system (about 1.2 l / min). Pharmacokinetics of budesonide is proportional to the magnitude of the input dosage.

Pharmacokinetics in special clinical situations

Pharmacokinetics of budesonide in children and patients with impaired kidney function was not studied.

In patients with liver disease may increase the time of budesonide in your body.

Testimony

- Bronchial asthma, requiring maintenance therapy GKS;

- Chronic obstructive pulmonary disease (COPD).

Dosage regimen

Dose Pulmicort^® set individually. In that case, If the recommended dose is not exceeded 1 mg / day, the entire drug dose injected a lump sum (at one time). When used in a higher dose of the drug is recommended to split it into 2 admission.

The initial dose for Adult (incl. elderly patients) is 1-2 mg / day. The maintenance dose is 0.5-4 mg / day. In the case of severe exacerbations dose can be increased.

For children 6 months and older The recommended starting 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.

Determination of dosage

* dilute the 0.9% solution of sodium chloride up to volume 2 ml.

For all patients it is desirable to determine minimum effective dose.

If necessary make additional therapeutic effect can be to recommend an increase in the daily dose (to 1 mg / day) Pul′mikorta^® instead of drug combinations with SCS for the reception inside due to a lower risk of developing systemic effects.

Patients, receive GSK for intake

The abolition of the SCS for the reception inside should start against the background of a stable state of health of a patient. During 10 days prescribe high doses of the drug Pulmicort^® against the backdrop of the admission of GKS inside in the usual dose. Later during the month, you should gradually reduce the dosage of SCS, taken inside (eg, by 2.5 mg of prednisone or its analogue), to the minimum effective dose. In many cases, unable to completely opt-out from receiving GKS inside.

No data on the use of budesonide do patients with renal insufficiency or impaired liver. Taking into account the fact, What is budesonide biotransformiroetsa in the liver, You can expect an increase in the duration of action of the drug in patients with cirrhosis of the liver.

Use Pul′mikorta^® via nebulizer

PULMICORT^® applied for inhalations using the appropriate nebulizer, equipped with a mouthpiece and a special mask. Nebulizer is connected with a compressor to create airflow (5-8 l / min), filling volume nebulizer should be 2-4 ml.

Because Pulmicort^®, applied in the form of suspensions using nebulizer, is drawn into the lungs during inhalation, It is important to instruct the patient to inhale the medication through the nebulizer mouthpiece calmly and evenly.

In cases, When a child cannot do breath through the nebulizer, a special mask.

The patient must be informed of the need to carefully read the instructions for use of the drug, as well as, Pul′mikorta to apply^® in the form of suspensions are not suitable for ultrasonic nebulizers. The suspension is mixed with 0.9 % solution of sodium chloride or solutions with terbutaline, salbutamol, fenoterola, acetylcysteine, sodium cromoglycate and ipratropiuma bromide. The patient should remember that, that after inhalation rinse mouth with water to reduce the risk of oropharyngeal candidiasis and that to prevent skin irritation after using the mask should wash the skin with water. You should also know, that diluted slurry Pulmicort^® should be used within 30 m.

It is recommended to regularly clean the nebulizer according with the instructions of the manufacturer.

Nebulizer Chamber should be cleaned after each use.

Camera nebulizer and mouthpiece or mask wash with warm water, using a mild detergent (in accordance with the instructions of the manufacturer). Nebulizer should be well rinsed and dried, connecting the camera with the compressor or air valve input.

Rules for the use of Pul′mikorta ® using a nebulizer

1. Before use, gently shake the container light rotational movement.

2. Keep the container straight vertically and open it, turning and lifting “Wing”.

3. Carefully place the open end of the container in the nebulizer and slowly give out the contents of a container.

Container, containing a single dose, marked line. If the container turn, This line will show the amount, equal 1 ml.

If you want to use only 1 ml suspension, the contents of a container are squeezed so far, until the surface of the liquid will not reach the level of, marked line.

Open container store in dark place. Open container must be used within 12 no.

Before, How to use fluid balance, the contents of a container care ustraherve rotary motion.

Side effect

To 10% patients, taking the drug, may experience the following side effects:

CNS: possible nervousness, excitability, depression, behavioral disturbances.

In some cases, symptoms may occur, caused by the systemic consequences of the SCS (including hypoadrenalism).

Other: rarely – the appearance of bruises on the skin, skin irritation when using a nebulizer with mask.

Contraindications

- Children up to age 6 Months;

- Hypersensitivity to the drug.

FROM caution (requires more careful monitoring of patients) should appoint drug patients with active form of pulmonary tuberculosis, fungal, viral, bacterial infections of the respiratory system, cirrhosis of the liver.

Pregnancy and lactation

Prenatal care, taking budesonide, did not reveal fetal abnormalities, Nevertheless, the risk cannot be completely eliminated their development, Therefore, when the pregnancy with regard to the possibility of worsening asthma, you should use the minimum effective dose of the drug.

Budesonide is excreted in breast milk, However, when applying Pul′mikorta^® in therapeutic doses, the effects on a child is not marked. PULMICORT^® can be used in breast vksarmlivanii.

Cautions

In appointing the drug Pulmicort^® should take into account a possible manifestation of systemic CORTICOSTEROIDS.

To minimize the risk of fungal lesions of oropharynx, should instruct the patient on the need to carefully rinse your mouth with water after each inhalation medication.

To prevent skin irritation after using a nebulizer with mask face wash.

You should avoid joint appointment with budesonide ketoconazole, itrakonazolom or other potential inhibitors of CYP3A4. When, If such a combination is needed, You should increase the time between doses of drugs to the greatest possible.

Because of the possible risk of weakening the napochechnikov, particular attention should be paid to patients, who transferred from systemic CORTICOSTEROIDS at the reception Pul′mikorta^®. Also, special attention should be given to patients, took high doses of CORTICOSTEROIDS or long receiving the highest recommended dose of inhaled CORTICOSTEROIDS. In stressful situations, such patients may experience signs and symptoms of adrenal insufficiency. When stress or surgery recommended supplemental systemic CORTICOSTEROIDS.

Particular attention should be paid to patients, who transferred from system to inhaled CORTICOSTEROIDS (PULMICORT^®) in cases, When can we expect the development of the pituitary-adrenal insufficiency. In these patients, you should be very careful in lowering the dose of CORTICOSTEROIDS for systemic use, and monitor the performance of the function of the hypothalamic-pituitary-adrenal system. This category of patients may require supplemental GCS for intake during stressful situations, trauma, surgery.

When switching from oral CORTICOSTEROIDS for use Pul′mikorta^® may develop pain in the muscles and joints, that sometimes leads to a temporary increase in dose CORTICOSTEROIDS for intake. In rare cases, marked fatigue, headache, nausea and vomiting, indicating system failure GKS.

When switching from oral CORTICOSTEROIDS to inhaled sometimes may exacerbate existing allergic reactions, rhinitis and eczema, formerly stoped systemic drugs.

Pul′mikortom Therapy^® when used 1 or 2 times/day showed efficacy for prevention of asthma physical effort.

Use in Pediatrics

In children and adolescents, receiving corticosteroids (any form) for a long period, It is recommended that you regularly monitor the growth. In appointing SCS should weigh the anticipated benefits from the use of the drug and the potential risk of growth retardation.

Use budesonide dose to 400 g/day at older children 3 years not resulted in systemic effects. Biochemical signs of systemic effects of the drug can occur when use of the drug in the dose of 400 to 800 mg / day. If you exceed the dose 800 µg/day systemic effects of the drug are common.

The use of CORTICOSTEROIDS for treatment of bronchial asthma can cause growth disorder. The results of observation of children and adolescents, receiving budesonide for a long period (to 11 years), shown, that growth reaches expected patients adhere to the standard ratios for adults.

Effects on ability to drive vehicles and management mechanisms

Drug Pulmicort^® does not affect the ability to study potentially hazardous activities, require attention and speed of psychomotor reactions.

Overdose

In acute overdose drug Pulmicort^® clinical manifestations does not occur.

After prolonged use of the drug in doses, greatly exceeding recommended, the development of systemic effects GKS as Cushing's and suppress adrenal function.

Drug Interactions

Unknown clinically meaningful interaction with other drugs budesonide, used in the treatment of bronchial asthma.

When ketoconazole (dose 200 mg 1 time / day) increases plasma concentration of budesonide (received inside the dose 3 mg 1 time / day) on average 6 time. In accept ketoconazole cherez 12 h after administration of budesonide concentrations of plasma of blood increased an average of 3 times. Information about such interaction npi as budesonide inhalation intake is missing, However, it is anticipated, as in this case, you should expect an increase in the concentration of plasma budesonide. In case of necessity of reception of ketoconazole and budesonide should increase the time between doses of drugs to the greatest possible. You should also consider reducing the dose of budesonide.

Another potential CYP3A4 inhibitor, such as itraconazole, also significantly increases plasma concentrations of budesonide

Provisional inhalation beta-adrenostimulâtorov expands bronchi, improves the flow of inhaled budesonide and enhances its therapeutic effect.

Phenobarbital, phenytoin, rifampicin reduces effectiveness while applying Pul′mikorta^® (through induction mikrosomalnogo oxidation enzymes).

Methandrostenolone, estrogens increase the effect of budesonide.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or below 30 ° C. Shelf life – 2 year.

After opening the envelope contained therein containers should be used within 3 months. Containers should be stored in an envelope to protect them from the light.

Open container should be stored in a dark place and use within 12 no.