Flixotide, inhalation aerosol 125 µg/dose, 60 doses

Composition

1 dose contains:  

fluticasone 125 mcg,

excipients:

propellant tetrafluoroethane GR106642X (the preparation does not contain freon).

Pharmacological action

Pharmaceutical group:

glucocorticosteroid for topical use.

Pharmaceutical action:  

Flixotide-corticosteroids for inhalation use. In recommended doses, it has a pronounced anti-inflammatory and anti-allergic effect, which leads to a decrease in the severity of symptoms and a decrease in the frequency of exacerbations of diseases accompanied by airway obstruction (bronchial asthma, chronic bronchitis, emphysema).

Fluticasone propionate inhibits the proliferation of mast cells, eosinophils, lymphocytes, macrophages, neutrophils, reduces the production and release of inflammatory mediators and other biologically active substances (histamine, prostaglandins, leukotrienes, cytokines).

In chronic obstructive pulmonary disease (COPD), the effectiveness of inhaled fluticasone propionate on lung function was confirmed, which is characterized by a decrease in the severity of symptoms of the disease, the frequency and severity of exacerbations, a decrease in the need for additional courses of corticosteroids in the form of tablets, and an increase in the quality of life of patients.

The systemic effect of fluticasone is minimal: in therapeutic doses, it has practically no effect on the hypothalamic-pituitary-adrenal system.

The drug Flixotide restores the patient’s response to bronchodilators, allowing to reduce the frequency of their use. The therapeutic effect after inhaled fluticasone begins within 24 hours, reaches a maximum within 1-2 weeks or more after the start of treatment, and persists for several days after discontinuation.

Pharmacokinetics:  

Suction

After inhalation, the absolute bioavailability of fluticasone propionate is 10-30%, depending on the type of inhaler.

Systemic absorption occurs mainly in the lungs. Part of the inhaled dose can be swallowed, but its systemic effect is minimal due to the weak solubility of the drug in water and intensive metabolism during the” first pass ” through the liver (the bioavailability of fluticasone propionate when taken orally is less than 1%).

There is a direct relationship between the inhaled dose and the systemic effect of fluticasone propionate.

Distribution

Binding to plasma proteins is 91%.

Fluticasone propionate has a large Vd-about 300 l.

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

Elimination

of Fluticasone propionate has a high plasma clearance of 1150 ml / min. T1 / 2 is about 8 hours. Renal clearance is less than 0.2%. Less than 5% is excreted in the urine as a metabolite.

Indications

Bronchial asthma (basic anti-inflammatory therapy) in adults and children 1 year and older (including those with a severe course of the disease, with dependence on systemic corticosteroids), chronic obstructive pulmonary disease in adults.

Contraindications

Hypersensitivity, acute bronchospasm, asthmatic status (as a priority remedy), non-asthmatic bronchitis, children (up to 1 year).

With caution — for cirrhosis of the liver, glaucoma, hypothyroidism, systemic infections (bacterial, fungal, parasitic, viral), osteoporosis, pulmonary tuberculosis, pregnancy and lactation.

Side effects

Candidiasis of the mouth and throat, hoarseness (after inhalation, rinse the mouth and throat with water), paradoxical bronchospasm (requires discontinuation of the drug, and continuation of therapy by other means);

rarely — allergic reactions (skin rash, angioedema, dyspnoea or bronchospasm, anaphylactic reactions) may decrease in the function of the adrenal cortex, osteoporosis, growth retardation in children, cataract, increased intraocular pressure.

Interaction

Since plasma concentrations of fluticasone propionate are very low in the inhaled route of use, interaction with other drugs is unlikely.

Simultaneous use of fluticasone propionate and CYP3A4 inhibitors (for example, ketoconazole, ritonavir) may increase the systemic effect of Flixotide (the use of such a combination requires caution).

How to take, course of use and dosage

of Flixotide is used by inhalation, after inhalation, rinse your mouth with water.

Bronchial asthma. Adults and adolescents over 16 years of age: 100-1000 mcg 2 times a day, depending on the severity of the disease: mild asthma — 100-250 mcg, medium form-250-500 mcg, severe form-500-1000 mcg. Depending on the individual response of the patient, the initial dose of Flixotide is either increased until the clinical effect appears, or reduced to the minimum effective dose.

Children over 4 years of age (only in the form of an aerosol for inhalation, dosed with 50 mcg of fluticasone in one dose): the recommended dose is 50-100 mcg 2 times a day.

Children from 1 to 4 years of age: (only in the form of an aerosol for inhalation dosed with 50 mcg of fluticasone in one dose): 100 mcg 2 times a day. Younger children require higher doses compared to older children due to reduced intake of the drug during inhalation (use of a spacer, smaller bronchial lumen, intensive nasal breathing).

Flixotide is administered using an inhaler through a spacer with a face mask (“Babyhaler”). Chronic obstructive pulmonary disease. Adults,500 mcg 2 times a day.

Overdose

Acute overdose of the drug can lead to a temporary decrease in the function of the adrenal cortex, which usually does not require emergency therapy, since the function of the adrenal cortex is restored within a few days.

If Flixotide is taken in high doses for a long time, significant suppression of the function of the adrenal cortex is possible. There have been very rare reports of an adrenal crisis in children treated with fluticasone propionate at a dose of 1 mg / day. and higher for several months or years. Hypoglycemia, depression of consciousness and convulsive states were observed in such patients.

Acute adrenal crisis can develop against the background of the following conditions: severe trauma, surgery, infection, a sharp decrease in the dose of fluticasone propionate.

In cases where the patient receives a dose higher than the recommended one, it should be gradually reduced.

Special instructions

Flixotide is intended for the long-term treatment of bronchial asthma, and not for the relief of seizures. Short-acting inhaled bronchodilators should be given to patients to relieve seizures.

If the effectiveness of short-acting bronchodilators decreases or the patient needs to use them more frequently, the patient should consult a doctor.

An increase in the need for short-acting inhaled beta-2-adrenergic agonists indicates a worsening of the disease. In such cases, it is recommended to review the patient’s treatment plan.

Sudden and progressive deterioration of bronchial asthma can pose a threat to the patient’s life, so in such situations, it is necessary to urgently decide whether to increase the dose of corticosteroids.

Abruptly discontinue treatment with Flixotide is not recommended.

Special care should be taken when treating inhaled corticosteroids in patients with active or inactive forms of pulmonary tuberculosis. In case of severe exacerbation of bronchial asthma or insufficient effectiveness of the therapy, the dose of inhaled fluticasone propionate should be increased and, if necessary, a drug from the group of systemic corticosteroids and/or an antibiotic should be prescribed if infection develops. It is recommended to check whether the patient knows how to use the inhaler correctly.

With prolonged use of any inhaled corticosteroids, especially in high doses, systemic effects may occur, but the likelihood of their development is much lower than with oral corticosteroids. Possible systemic effects include decreased adrenal cortex function, osteoporosis, growth retardation in children, cataracts, and glaucoma. Therefore, it is especially important that when the therapeutic effect is achieved, the dose of inhaled corticosteroids is reduced to the minimum effective dose that controls the course of the disease.

The transfer of patients suffering from hormone-dependent bronchial asthma from systemic corticosteroids to fluticasone inhalation requires special attention, since the restoration of adrenal function requires a long time. Adrenal cortex function should be monitored regularly and caution should be exercised when reducing the dose of systemic corticosteroids.

A gradual reduction in the dose of systemic corticosteroids can be initiated approximately one week after the appointment of fluticasone. When the maintenance dose of prednisone (or other corticosteroids in an equivalent dose) is less than 10 mg / day. the dose reduction should not exceed 1 mg / day. It should be performed at intervals of at least 1 week. When the maintenance dose of prednisone is more than 10 mg / day. (in terms of day) – in high doses also at intervals of at least 1 week.

Some patients during the period of reducing the dose of systemic corticosteroids complain of general malaise against the background of stabilization or even improvement in the indicators of external respiratory function. If there are no objective signs of adrenal insufficiency, patients should be encouraged to continue switching to inhaled corticosteroids and gradually discontinue systemic corticosteroids.

In some cases, individual high sensitivity to inhaled corticosteroids may occur. The function of the adrenal cortex when prescribed fluticasone propionate in the recommended doses, as a rule, remains within the normal range.The benefits of inhaled fluticasone propionate minimize the need for systemic corticosteroids. However, there may still be a chance of side effects in patients who have previously received or periodically take corticosteroids orally. When performing resuscitation measures or surgical interventions, you may need to consult a specialist to determine the degree of adrenal insufficiency. In such stressful situations, you should always take into account possible adrenal insufficiency and, if necessary, additionally prescribe corticosteroids.

Due to possible adrenal insufficiency, special care should be taken and the function of the adrenal cortex should be regularly monitored when transferring patients who have taken corticosteroids orally to treatment with inhaled fluticasone propionate. Discontinuation of systemic corticosteroids with inhaled fluticasone propionate should be carried out gradually, and patients should carry a card indicating that they may need additional corticosteroid use during periods of stress.

In rare cases, when patients are transferred from taking systemic corticosteroids to inhaled therapy, conditions accompanied by hypereosinophilia may occur (for example, Churge-Strauss syndrome). As a rule, this occurs during dose reduction or discontinuation of systemic corticosteroids, but a direct causal relationship has not been established.

When patients are transferred from taking systemic corticosteroids to inhaled therapy, concomitant allergic diseases (for example, allergic rhinitis, eczema), which were previously suppressed by systemic drugs, may also worsen. In such situations, it is recommended to conduct symptomatic treatment with antihistamines and / or topical medications, including topical corticosteroids.

To prevent the development of candidiasis, you should rinse your mouth after using Flixotide; if necessary, local antifungal therapy can be prescribed throughout the entire treatment period.

To prevent hoarseness of the voice, it is recommended to rinse the mouth and throat with water immediately after inhalation.

If paradoxical bronchospasm develops, the use of Flixotide should be stopped immediately, the patient’s condition should be evaluated, the necessary examination should be performed, and other medications should be prescribed if necessary. Paradoxical bronchospasm should be immediately stopped with a fast-acting inhaled bronchodilator.

There are very rare reports of elevated blood glucose levels, and this should be borne in mind when prescribing fluticasone propionate to patients with diabetes mellitus.

Like most other aerosol inhalation products, this product may be less effective when cooling the canister.

Use in pediatrics

The growth dynamics of children receiving inhaled corticosteroids for a long time should be regularly monitored.

Influence on the ability to drive motor vehicles and manage mechanisms

The effect of fluticasone propionate on the ability to drive a car and work with machinery is unlikely.

Form of production

Metered-dose inhalation aerosol.

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

2 years

Active ingredient

of Fluticasone furoate

Conditions of release from pharmacies

By prescription

Dosage form

aerosol for inhalation

Purpose

For adults as prescribed by a doctor, Children over 1 year old, Children as prescribed by a doctor

Indications

Bronchitis, Bronchial asthma, Chronic Obstructive pulmonary Disease