Flixotide

Active material: Fluticasone
When ATH: R03BA05
CCF: GCS for inhalation
ICD-10 codes (testimony): J44, J45
When CSF: 04.03
Manufacturer: GlaxoSmithKline Trading Company (Russia)

DOSAGE FORM, STRUCTURE AND PACKAGING

Aerosol for inhalation dose in the form of a suspension of white or almost white.

Excipients: GR106642X propellant (does not contain freon).

60 doses – inhalers aluminum (1) with a metering device – cardboard boxes.
120 doses – inhalers aluminum (1) with a metering device – cardboard boxes.

Pharmacological action

SCS for inhalation use. In recommended doses, has expressed Antiinflammatory, and protiwallergicescoe effect, that reduces the severity of symptoms and reduce the frequency of exacerbations of disease, accompanied by airway obstruction (bronchial asthma, chronic bronchitis, эmfizema).

Fluticasone propionate ingibiruet proliferatiou fat cells, eozinofilov, lymphocytes, macrophages, neutrophil, reduces the production and release of mediators of inflammation and other biologically active substances (gistamina, prostaglandins, leukotrienes, Cytokine).

In chronic obstructive pulmonary disease (COPD) confirmed the efficiency of inhalation flutikazon propionata on lung function, that is characterized by a decrease in severity of symptoms, the frequency and severity of exacerbations, reduction in the need to assign additional courses GKS in pill form and improve the quality of life for patients.

System flutikazon expressed minimally: in therapeutic doses does not practically affect the hypothalamic-pituitary-suprarenal system.

The drug restores reaction to the patient bronchodilators, allowing to reduce the frequency of their use.

Therapeutic effects after inhalation use fluticasone begins within 24 no, reaches a peak during 1-2 weeks after the start of treatment and lasts for several days after cancellation.

Pharmacokinetics

Absorption

After inhalation flutikazon propionata absolute bioavailability is 10-30% Depending on the type of inhaler. Systemic absorption occurs primarily in the lungs. Part ingalirovanna doses can proglatyvatsja, but its minimal system operation due to weak drug solubility in water and intense metabolism when “first pass” through the liver (bioavailability of flutikazon propionata ingestion is less than 1%). There is a direct correlation between the size of ingalirovanna doses and systemic consequences fluticasone propionate.

Distribution

Plasma protein binding is 91%.

Flutikazon propionat has a big V_d – about 300 l.

Metabolism

Fluticasone propionate is metabolized in the liver, with the participation of CYP3A4, with the formation of inactive metabolite.

Deduction

Fluticasone propionate has a high plasma clearance – 1150 ml / min. T_1/2 is about 8 no. Renal clearance – less 0.2%. With less urine output 5% It saw in the metabolite.

Testimony

— basic anti-inflammatory therapy of bronchial asthma (incl. When severe illness and dependence on systemic CORTICOSTEROIDS) in adults and children 1 and older;

-treatment of chronic obstructive pulmonary disease in adults.

Dosage regimen

Fliksotid is only for inhalation use. Fliksotid is a tool for preventive therapy, the preparation should be applied regularly, even in the absence of symptoms.

At basic anti-inflammatory therapy of bronchial asthma therapeutic effect of Fliksotida comes through 4-7 days after treatment. Patients, previously not used inhaled CORTICOSTEROIDS, improvement can be observed already after 24 h after the beginning of drug.

To Adults and adolescents older 16 years the initial dose in bronchial asthma light flow – by 100-250 g 2 times / day, moderate – by 250-500 g 2 times / day, severe – by 500-1000 g 2 times / day. Then, Depending on the individual patient's response to treatment, the starting dose may be increased before the appearance of clinical effect or reduce to the minimum effective dose.

In older children 4 years It is recommended to apply aerosol, comprising 50 mcg flutikazon propionata in 1 dose. We recommend that you assign to 50-100 g 2 times / day. The initial dose of the drug depends on the severity of the disease. Then, Depending on the individual patient's response to treatment, the starting dose may be increased before the appearance of clinical effect or reduce to the minimum effective dose.

Children aged 1 Year to 4 years It is encouraged to nominate 100 g 2 times / day.

Young children require higher dose Fliksotida compared with older children due to the reduced revenue of the drug in inhalation introduction (less clearance bronchi, use spacer, intense nasal breathing in infants).

The drug is injected using the nebulizer through the spacer on the front mask (eg “Bebikhalyer”).

Dose aerosol Fliksotid especially showed young children with severe bronchial asthma.

For the treatment of chronic obstructive pulmonary disease adult It is encouraged to nominate for 500 g 2 times / day.

Patients with liver or kidney disease, as well as the elderly dose adjustment is not required.

Side effect

Local reactions: possible candidiasis mucous membranes of the oral cavity and pharynx, hoarseness, paradoxical bronchospasm.

Allergic reactions: in some cases – skin rash, angioedema, dyspnea or bronchospasm, anaphylactic reactions.

Systemic reactions: loss of function of the adrenal cortex, osteoporosis, growth retardation in children, Cataract, increased intraocular pressure, glaucoma, Cushing's syndrome, Cushingoid symptoms. There is also a very rare reports of hyperglycemia.

There are: mental disorders (anxiety, sleep disorders, behavioral changes, incl. hyperactivity and irritability/mostly in children/); often – bruising, pneumonia in patients with COPD.

Contraindications

— acute bronchospasm;

-Asthma status (as first);

is bronchitis neastmaticheskoj nature;

- Children up to age 1 year;

- Hypersensitivity to the drug.

FROM caution should designate product in liver cirrhosis, glaucoma, gipotireoze, systemic infections (bacterial, fungal, parasitic, Viral), osteoporosis, pulmonary tuberculosis, Pregnancy and lactation.

Pregnancy and lactation

Use of the drug during pregnancy is possible only in case, when the intended benefits to the mother outweighs the potential risk to the fetus.

Excretion of fluticasone with breast milk in humans is not known. However, after inhalation of the drug in the recommended doses, concentrations of fluticasone propionate in plasma low.

Cautions

Fliksotid intended for the long-term treatment of bronchial asthma, instead of cupping. For cupping patients should be prescribed a short-acting inhaled bronchodilators.

In the case of reducing the effectiveness of short-acting bronchodilators or need more frequent their application, the patient must consult a doctor.

Increased demand for use of inhaled beta agonists₂-adrenoretseptorov short indication of the deterioration of the disease. In such cases it is advisable to review the patient's treatment plan.

Sudden and progressive worsening of asthma can be life-threatening patient, Therefore, in these situations, there is an urgent need to address the issue of increasing the dose of CORTICOSTEROIDS.

Discontinue treatment abruptly Fliksotidom not recommended.

Be particularly careful in the treatment of inhaled corticosteroids in patients with active or inactive pulmonary tuberculosis.

In severe worsening of asthma or lack of effectiveness of therapy should increase the dose inhalation flutikazon propionata and, if necessary, assign the preparation of group systemic CORTICOSTEROIDS and/or antibiotic in development infection.

We recommend that you check, If the patient to use the inhaler.

Prolonged use of any inhaled GCS, especially in high doses, systemic effects may occur, However, the probability of their development is much lower, than when corticosteroids inside. Possible systemic effects include reduced function napochechnikov crust, osteoporosis, delayed growth in children, cataracts, glaucoma. It is therefore particularly important, to a therapeutic effect at the dose of inhaled corticosteroids has been reduced to the minimum effective dose, controlling the disease.

Transfer of patients, suffering from bronchial asthma, with systemic CORTICOSTEROIDS on fluticasone requires special attention, Since the recovery of adrenal function takes a long time. Should regularly monitor adrenal function and exercise caution when lowering the doses of systemic CORTICOSTEROIDS.

Gradual reduction of dose systemic CORTICOSTEROIDS can begin about a week after the appointment of fluticasone. In the maintenance dose of prednisolone (or other GCS in the equivalent doze) less 10 mg/day dose reduction should not exceed 1 mg/day and should take place at intervals of no less than 1 of the week. In the maintenance dose of prednisolone more 10 mg / day (in terms of day) – in high doses, also at intervals of not less than 1 of the week.

Some patients during dose reduction of systemic CORTICOSTEROIDS complain of malaise amid stabilizing or even improving respiratory function. If there are no objective signs of adrenal insufficiency, patients must be persuaded to continue the transition to inhaled CORTICOSTEROIDS and the gradual elimination of systemic CORTICOSTEROIDS.

In some cases there may be individual high sensitivity to inhalation GKS. The function of the adrenal cortex in the appointment of flutikazon propionata in recommended doses, usually, remains within the normal range. The benefits of inhalation flutikazon propionata minimize need for appointment of systemic CORTICOSTEROIDS. However, you may continue the likelihood of side effects in patients, had been receiving or host periodically GKS inside. When carrying out resuscitation or surgical interventions may need to consult a specialist to determine the degree of adrenal insufficiency. In such stressful situations you should always consider the suprarenal insufficiency and optionally assign additional GCS.

Due to possible adrenal insufficiency should be treated very carefully and regularly monitor the performance of the functions of the adrenal cortex when transferring patients, taking into GCS, for treatment of fluticasone propionate inhalation. The abolition of the system of the SCS amid inhalation flutikazon propionata should be gradually, and patients must carry the card, indicating, that they may require an additional intake of CORTICOSTEROIDS during stress.

In rare cases, the transfer of patients from systemic CORTICOSTEROIDS to receive an inhalation therapy can manifest State, accompanied by giperjeozinofiliej (eg, Churg-Strauss Syndrome). Usually, This occurs during dose reduction or withdrawal of systemic CORTICOSTEROIDS, However, the direct causal link is not installed.

The transfer of patients from receiving systemic CORTICOSTEROIDS on an inhalation therapy can also worsen related allergic diseases (eg, nasal allergy, eczema), which previously suppressed systemic drugs. In such situations, it is recommended to carry out symptomatic treatment with antihistamines and / or topical preparations, incl. SCS for local use.

To prevent the development of candidiasis you should rinse your mouth after you apply Fliksotida; If necessary, throughout the entire period of treatment, you can assign local protivogribkovu therapy.

To prevent hoarseness is recommended immediately after inhalation rinse mouth and throat with water.

In the case of paradoxical bronchospasm should immediately stop the introduction Fliksotida, assess the condition of the patient, carry out the necessary examination and, if necessary, appoint other medications. Bronhospazm paradoxical should immediately stop using the rapid inhalation bronhodilatatora.

There are very rare reports of increased blood glucose levels, and it should be remembered, assigning fluticasone propionate for patients with diabetes.

Like most other inhalation aerosol packages, This drug may be less efficient at cooling spray.

Use in Pediatrics

Should regularly monitor the growth of children, receiving inhaled corticosteroids for a long time.

Effects on ability to drive vehicles and management mechanisms

Influence of flutikazon propionata on ability to drive and work with the technique, it is unlikely.

Overdose

Acute overdose the drug can cause a temporary decrease in adrenal function, that usually does not require emergency therapy, tk. adrenocortical function is restored within a few days.

If Fliksotid is taken in high doses for a long time, possibly significant suppression of adrenal function. Were received very rare reports of the development of kriza adrenalovy in children, receiving flutikazon propionata dose 1 mg/day and above for months or years. These patients have marked hypoglycemia, oppression of consciousness and convulsive status.

Acute adrenalovy Kriz can develop against the background of the following States:: severe injury, surgical intervention, infection, the sharp decline dose fluticasone propionate.

In cases, When the patient gets a dose above recommended, You must gradually reduce the.

Drug Interactions

Because in inhalation route of Administration concentration flutikazon propionata plasma very low, interaction with other drugs is unlikely.

At the same time the application flutikazon propionata and CYP3A4 enzyme inhibitors (eg, ketoconazole, Ritonavir) may increase systemic action Fliksotida (use of the combination requires caution).

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children at or above 30 ° C; do not freeze or expose to direct sunlight. Shelf life – 2 year.