Description overdue on 08/20/2014

• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications
• Contraindications
• Side effects
• Budesonide: instructions for use and dosing regimen
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Cautions
• Analogs
• Synonyms
• During pregnancy (and lactation)
• Reviews
• Price, where to buy

Composition

The composition of each dose budesonide Iziheyler includes:

• 200 g of budesonide as active ingredient;
• 7, 8 mg of lactose monohydrate as an excipient.

Product form

The drug is available in the form of a homogeneous powder for inhalation, the color of which can vary from white to almost white. Each dose of powder containing 200 g of budesonide. One package is designed to budesonide 200 doses.

Each package is equipped with the drug inhaler made from a polymeric material. On the dosing part has a cap with a lock on the front of the affixed "Easyhaler", is provided on the side of the counter of the remaining doses.

Pharmacological action

The drug belongs to the pharmacotherapeutic group " Corticosteroids   Topical "and represents hormonal drug Which is used for the treatment and prevention asthma .

The therapeutic effect of the drug due to the activity included in its structure as the active substance budesonide, which is a synthetic analogue produced adrenal cortex   Hormone Cortisol   ( hydrocortisone ), Responsible for the regulation of the metabolism of carbohydrates and minerals in the body.

Once in the body, budesonide:

• has glucocorticoid   action;
• relieves the symptoms of inflammation;
• eliminates symptoms   allergic reactions .

Inhalation use are pronounced clinical effect is the fifth-seventh day course of therapy.

Pharmacodynamics and pharmacokinetics

Budesonide belongs to the category of non-halogenated glucocorticosteroids . When applied topically, it relieves the symptoms of inflammation mucous membrane of the respiratory tract .

Improvement of patients suffering from asthma , Can be observed as early as 24 hours after the first inhalation of the drug. However, the fact, to achieve maximum effect, it takes several weeks of continuous therapy.

The mechanism of action glucocorticosteroids   inflammatory process in asthma not exactly understood. Studies have shown that a number of budesonide provokes inhibitory effects on cells (including eosinophilic granulocytes . lymphocytes . makrofagotsity . mast cells   and neutrophilic granulocytes ), As well as mediators that are involved in the development of airway inflammation   allergic and nonallergic nature (including Cytokines . leukotrienes . eicosanoids   and histamine ).

Budesonide has expressed glucocorticoid   and mild mineralocorticoid activity. Standard studies in vitro, as well as studies conducted in experimental animals, led to the conclusion that the affinity (affinity) of the substance to specific receptors glucocorticoids   200 times higher than that of the Cortisol .

As for local antiinflammatory effect of budesonide, it is a thousand times the anti-inflammatory effect Cortisol . Animal studies have also demonstrated that the systemic activity when administered subcutaneously budesonide formulation exceeds systemic activity Cortisol   40 times, while for oral administration - 25 times.

Once in the body, budesonide:

• increases the production of protein lipokortina Which is an inhibitor of the enzymatic activity of phospholipase A2;
• hinders the process of release arachidonic acid   and it inhibits the synthesis of metabolic products ( prostaglandins   and cyclic endoperekisey );
• warns marginal congestion neutrophilic granulocytes ;
• inhibits the exudation of fluid and protein in the inflammation;
• reduces production Cytokine ;
• inhibits migration makrofagotsitov ;
• reduces the intensity of infiltration and granulation;
• reduces the intensity of the formation Substance chemotaxis, ie migration leukocytes   in inflammation (This property explains the efficacy of budesonide in the so-called "late" reactions allergies );
• It prevents the release of the highly immune cells   connective tissue involved in the adaptive Immunity   (also called mast cells ), Mediators of the inflammatory process;
• reduces the sensitivity of peripheral tissues to histamine   and serotonin While increasing the sensitivity to adrenaline ;
• increases the amount of active beta-adrenergic receptors;
• promotes recovery reactions to beta-adrenergic bronchodilators drugs after prolonged treatment thereof;
• It reduces the performance of tissue permeability barriers and the vascular walls;
• inhibits the proliferation of connective tissue in the inflammation;
• contributes to the stabilization of cell membranes;
• prevents the formation of the inflammation free radicals   and hinders the process of oxidative degradation lipids   under their influence.

When this material is well tolerated (even after prolonged use it) has no ISS activity and does not cause resorptive effects.

Budesonide is characterized by the ability to rapidly absorbed from the light . stomach   and gastrointestinal tract That is defined by its pronounced lipophilic properties and good tissue permeability.

After administration to the nasal cavity in a very small amount of the absorbent mucosally membranes of the nasal cavity   (only a fifth of the substance gets into systemic circulation ).

After use in the inhalation of budesonide alveoli   It gets about one fourth of a single dose of a substance.

About 90% has fallen into stomach   and intestinal tract   dose budesonide completely destroyed enzyme system P450   already in the "first pass" through the liver That is accompanied by the formation of two major active metabolites (their activity is less than 0, 01 from the activity of the starting material).

The small amounts of budesonide is metabolised in serum   and in light . The index of bioavailability entered in stomach   and intestines   substance is 10%. Regarding budesonide alveoli Then from about 25 to 30% of the amount absorbed.

The maximum concentration of drug in the plasma   It celebrated in about 15-45 minutes after the procedure, inhalation or injection into the the nasal cavity .

Indicator binding budesonide plasma protein albumin   85-95%. Systemic clearance of the drug, ie the volume plasma , Cleaned by him for a period of time when passing through kidneys It is estimated to be very high (84 liters per hour).

The half-life (half-life) is a little less than three hours (approximately 2, 8 hours). The substance is excreted primarily in the urine and faeces in the form of conjugated and unconjugated metabolites (partly - with bile   in the form of metabolites).

The half-life of plasma   in children, usually on the order of magnitude lower than in adult patients. In adult patients with liver disease   measure the bioavailability of budesonide may increase.

After oral indicators higher plasma concentrations Cmax and the time to reach maximum concentration after administration of the dose Tmax may vary. Thus, the rate of Tmax for different categories of patient can be in the range of from 30 to 600 minutes.

Systemic availability indicator substance after a single dose is characterized also variability: for example, patients who have been diagnosed granulomatous enteritis   ( Crohn's disease ), It is more than double that in the group of healthy volunteers.

Thus, in patients with   granulomatous enteritis   it is 21% and in healthy volunteers - only 9%. However, after administration of repeated doses of budesonide have investigated from the second group it approaches the value of the index in the first group.

Indications

Budesonide is indicated for patients who are diagnosed:

• bronchial asthma   (as in the light, and the moderate and severe forms);
• chronic obstructive pulmonary disease (COPD).

Contraindications

Contraindications to the appointment of the drug are:

• individual hypersensitivity   to budesonide;
• age of the child up to six years ;
• lactose intolerance , Glucose-galactose malabsorption or lactase deficiency (this is due to the fact that the drug is included as a subsidiary ingredient lactose ).

Be wary appoint patients with budesonide:

• pulmonary tuberculosis;
• cirrhosis of the liver;
• infections of the respiratory fungal, bacterial and viral nature of origin;
• glaucoma;
• hypothyroidism;
• osteoporosis.

Side effects

Treatment with inhaled budesonide in some cases can cause the development of Candida infections of the oropharynx . Experience with the drug indicates that the symptoms candidiasis   occur much less frequently, if you carry out the procedure inhalation before eating, and after it thoroughly rinse your mouth.

If, however, to avoid Candida infection   failed to stop treatment with inhaled is not required, but the patient appoint more effective against strains of Candida spp. local antifungal drugs .

Like most other glucocorticosteroids   for administration by inhalation, budesonide may provoke systemic adverse reactions, including:

• disruption of normal activities adrenal ;
• slowdown in patients childhood and adolescence;
• decline in bone mineral density;
• development Cataract   and Glaucoma ;
• increased susceptibility to various infectious diseases;
• impaired ability to adapt to stressful situations.

However, it should be noted that the probability of occurrence of such adverse reactions to the drug in the form of inhalation is significantly lower than for preparations intended for oral administration.

The filler used drug Budesonide Easyhaler lactose , Which contains a small amount milk proteins and which can cause allergic reactions   patients intolerant to it.

The possible negative consequences of receiving budesonide distributed frequency of their development. The most common reactions include hoarseness, cough, symptoms of irritation in the oropharynx, difficulty swallowing.

Rarely may experience hypersensitivity reactions, including the appearance of rashes on the skin, contact dermatitis, urticaria, angioneurotic edema and anaphylactic shock.

Endocrine system   rarely reacts to the reception of budesonide Hypo - Or hypercortisolism That is, respectively, a decrease or an increase in production adrenal hormones . In extremely rare cases, can be suppressed function adrenal .

Also not ruled out the likelihood of developing mental reactions, which may be expressed in the form of depressions, enhance aggression, irritability, anxiety, appearance of various types of psychoses, behavioral change in children, anxiety and increased physical activity.

In extremely rare cases, violations of the Nervous System   can manifest as excessive nervousness, irritability, and various kinds of sleep disorders.

In addition, in rare cases:

• symptoms bronchospasm ;
• the appearance of symptoms of the skin and subcutaneous tissue, which are expressed in the form hives . dermatitis . erythema . hematomas . angioedema   etc.;
• slowdown.

In extremely rare - eye diseases, and decreased bone density.

Budesonide: instructions for use and dosing regimen

Budesonide is for inhalation use. To ensure the best response to drug therapy is recommended to take it regularly.

When switching to Easyhaler Budesonide from other inhalation means a treatment regimen selected individually, based on the characteristics of the disease. At the same time also pay attention to the features previously prescribers regimen and route of administration of the drug.

The starting dose is also selected in accordance with the severity or level of control of the disease. The apparent therapeutic effect is noted, usually within a few days after the start of treatment, and it reaches its peak a few weeks after the first dose.

Budesonide dose is adjusted to achieve a complete control of the disease, and then gradually reduced to a minimum, which will remain in effective control over asthma .

The initial dose of budesonide is calculated as follows:

• 200-400 micrograms a day - for adult patients diagnosed bronchial asthma   mild (not higher than stage 2), including the elderly and adolescents older than twelve years (by the physician is allowed to increase the dose to 800 mg a day);
• 200-400 micrograms a day - for children aged six to twelve years of age (by the physician is allowed to increase the dose to 800 mg a day);
• to 1600 mg per day - adult patients diagnosed bronchial asthma   moderate to severe (grade 3 and 4 respectively).

The dose during maintenance therapy is chosen, focusing on the severity of the disease and the clinical response to the designated patient treatment. After reaching control   asthma , The dose was reduced to minimum, in which is stored the desired clinical effect.

When dosing the drug twice a day maintenance job dose is from 200 to 400 mg for adult patients diagnosed bronchial asthma   mild (not higher than stage 2), including the elderly and adolescents over the age of twelve.

According to the testimony of the doctor during periods of exacerbation of the disease is allowed to increase the daily dose up to 1,600 mg per day. It is divided into two stages and lower after the stabilization of the patient's condition.

The dosage regimen of the drug once a day in the appointment of maintenance therapy involves the use of adult patients diagnosed with bronchial asthma   mild (not higher than stage 2), including the elderly and adolescents over the age of twelve:

• 200-400 mg once a day, if they have not previously glucocorticosteroid medications ;
• 800 mg once a day, if earlier the disease was controlled glucocorticosteroid   inhaled drugs prescribed for admission twice a day.

Children from six to twelve years with a diagnosis of " bronchial asthma   mild or moderately severe "as maintenance daily dose administered of from 200 to 400 g of budesonide when:

• This category of patients have not previously received therapy steroids ;
• previously assigned to receive twice daily inhaled glucocorticosteroid medications allow fully to control the disease.

After transferring the patient to a one-time use of a daily dose, which varies from 200 to 400 mg, the dose is reduced to the minimum possible, in which will be maintained effective control of the disease.

The optimum is considered the drug once a day at the same time in the evening. It is important that in this case it was regular.

To date sufficient data to generate the optimum scheme of transfer of patients who do not pass the course before inhalation therapy glucocorticosteroid medications On Easyhaler budesonide once a day no.

During exacerbation of the disease and the deterioration of the patient to take the drug once a day, guide recommends increasing the daily dose by half by transferring the patient to inhalation twice a day while maintaining the previously established single dose.

At the same time patients advised to immediately call to your doctor.

Also, patients are advised to keep on hand bronchodilators   short-term actions that are designed to relieve symptoms of acute attacks asthma .

Patients with chronic obstructive pulmonary disease   (COPD) dose of budesonide is selected individually based on the severity of the disease. The initial dose, which recommends the preparation instructions, is 100 to 400 micrograms twice daily matter.

Maximum permissible dose - 800 micrograms of budesonide twice daily.

Overdose

The incidence of acute toxic reactions to receiving budesonide characterized as rare. Long-term use of high doses of the drug can trigger the development of systemic reactions glucocorticosteroid medications Including:

• increased susceptibility to various infections;
• the occurrence of symptoms Hyper - Or hypocorticoidism ;
• suppression of normal function   adrenal .

In rare cases, the patient can begin the process of atrophying   adrenocortical .

When symptoms of an acute overdose of any specific treatment is needed. Budesonide treatment continues with therapeutic doses recommended for the control of the disease.

Typically, the recovery of the function hypothalamus . pituitary   and adrenocortical   It takes a few days.

In stressful situations, it may be necessary as a preventive measure systemic administration glucocorticosteroids   (e.g., high dose hydrocortisone ).

Patients who developed symptoms of atrophy adrenocortical , Classified as steroid-dependent and up to the full stabilization of their condition translate into adequate maintenance therapy with the use of the system glucocorticosteroids .

Cooperation

Simultaneous with the appointment of budesonide drugs interact with isoenzymes of cytochrome P450 3A4 Including itraconazole .   ketoconazole , Nelfinavir, ethinyl estradiol, etc., leads to disruption of the metabolic conversion of budesonide and provokes increase of its plasma concentrations.

With short-term treatment with budesonide (no more than 1-2 weeks), plasma concentrations of such a change is not anything significant. However, if necessary, its long course of treatment should be considered mandatory.

In the absence of data to provide the necessary dosage in such cases, the above combination of drugs is not recommended.

Effectiveness g phenobarbital   or rifampicin ).

methandrostenolone   or .

Estrogens   and . oral contraceptives   It noted.

adrenal    

Terms of sale

Storage conditions

Shelf life

Cautions

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antibiotics . glucocorticosteroids  

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Synonyms

pregnancy

pregnant  

Reviews

asthma  

Asthma .

 

glucocorticosteroids   pregnancy .