Flixotide Nebules, suspension for inhalation 2mg/2ml, 10 nebules — Made in Australia — Free Delivery

Pharmacological properties

Pharmacodynamics. GCS fluticasone propionate in recommended doses for inhalation has a pronounced anti-inflammatory effect on the lungs, which helps to reduce the severity of symptoms and reduce the frequency of BA attacks.

Pharmacokinetics. As a result of inhalation use, the systemic availability of nebulized fluticasone propionate in healthy volunteers is expected to be 8%, compared with 26% when using the preparation in the form of a metered-dose inhaler. Systemic absorption is carried out mainly through the respiratory system, at first quickly, then over a long time. The remainder of the inhalation dose may be swallowed in the mouth.

The absolute oral bioavailability is very low (1%) due to the combination of incomplete absorption in the digestive tract and extensive first-pass metabolism. 87-100% of an oral dose is excreted in the feces, 75% - as a primary component, as well as an inactive main metabolite.

The safety of the preparation. Toxicological studies have shown the presence of effects typical of strong GCS, but at doses many times higher than those shown for therapeutic use. In studies to study the effect of the preparation on reproductive function and the presence of teratogenic properties, no new data have been identified. Fluticasone propionate has no mutagenic activity in vitro and in vivo. Animal studies have shown that the preparation has no carcinogenic potential. It also has no irritating or sensitizing properties.

Indications

Children and adolescents over the age of 16. prophylactic use in severe BA in patients who need inhalation or oral corticosteroids in high doses. to patients who take high doses of oral corticosteroids, to reduce or eliminate the use of corticosteroids inside.

Children and adolescents aged 4-16 years. Treatment of asthma exacerbation. Appropriate supportive care can be complemented by the use of a metered-dose aerosol or powder inhaler.

Inhaled fluticasone propionate has a potent glucocorticoid anti-inflammatory effect in the lungs. It reduces symptoms and exacerbations of asthma in patients who were previously treated with bronchodilators alone or in combination with other prophylactic preparations. Brief symptomatic episodes of exacerbation can generally be alleviated with the use of fast-acting bronchodilators, but prolonged exacerbations require the addition of GCS as early as possible to control inflammation.

Application

The preparation is intended for inhalation use only.

Flixotide Nebula should be administered as an aerosol from a jet nebulizer. Since the delivery of the preparation is influenced by numerous factors, it is necessary to adhere to the recommendations of the manufacturer that produces nebulizers.

The use of Flixotide Nebula with ultrasonic nebulizers is generally not recommended.

Patients should be warned that treatment with inhaled fluticasone propionate is prophylactic, so it must be used regularly even in the absence of symptoms.

In the event of a decrease in the effectiveness of short-acting bronchodilators or the need for their frequent use, the patient should consult a doctor.

The starting dose of the preparation should correspond to the severity of the disease. The dose can be increased until control is achieved or decreased to the minimum effective dose that allows for adequate control of the disease.

Adults and adolescents over the age of 16: 0.5–2.0 mg 2 times a day.

Fluticasone propionate is effective at a dose that is half the dose of other inhaled corticosteroids. For example, 100 mcg of fluticasone propionate is roughly equivalent to a 200 mcg dose of beclomethasone dipropionate (containing Freon) or budesonide.

There is always a risk of systemic effects when using high doses of GCS (see SPECIAL INSTRUCTIONS and SIDE EFFECTS).

Children and adolescents aged 4-16 years: 1.0 mg 2 times a day.

Separate groups of patients. There is no need to change the dose for elderly patients or with impaired liver and kidney function.

Transfer of patients who used oral corticosteroids to inhalation use. The gradual withdrawal of systemic steroids begins after about a week. Dose reduction should be consistent with the maintenance level of systemic steroids and occur at intervals of at least a week. In total, for a maintenance dose of prednisolone (or analogs) of 10 mg per day or less, the dose reduction should not be more than 1 mg per day at intervals of at least a week. To maintain a dose of prednisolone in excess of 10 mg per day, it is allowed to reduce the dose by more than 1 mg per day with an interval of at least a week, with extreme caution.

Flixotide Nebula should not be injected.

It is useful to use the preparation through a mouthpiece in order to avoid the development of atrophic changes in the skin of the face, which can be noted with prolonged use of the face mask.

When using a face mask, skin that is exposed to the preparation should be protected with a cream or thorough washing after the procedure.

Instructions for the use of Flixotide Nebula. Before use, make sure that the contents of the nebula are well mixed. Holding the nebula horizontally by the edge where the marking is located, shake it several times. Repeat this process several times until the contents are completely mixed. To open the nebula, rotate the top cap.

If necessary, the preparation can be diluted with sodium chloride solution. An unused solution from the nebulizer container cannot be reused. It should be disposed of.

Contraindications

History of hypersensitivity to any component of the preparation.

Side effects

The following side effects are classified by organs, systems and frequency of occurrence: very often (≥1 / 10), often (≥1 / 100 and 1/10), infrequently (≥ / 1000 and 1/100), rarely (≥1 / 10 000 and 1/1000) and very rarely (1/10 000) and the frequency is unknown (if data is available, the frequency cannot be determined), including individual messages. data on side effects that occur very often, often and infrequently, are mainly based on clinical studies. data on side effects, which are rare and very rare, are obtained mainly from episodic reports.

Infections and invasions: very often - candidiasis of the oral cavity and pharynx.

In some patients, candidiasis of the oral cavity and pharynx may develop. In order to prevent this phenomenon, after using Flixotide in the form of inhalation through a nebulizer, it is necessary to rinse the oral cavity. If necessary, during the entire period of treatment, a topically antifungal preparation is prescribed, while continuing the use of Nebula Flixotide.

Often: Patients with chronic obstructive pulmonary disease (COPD) may develop pneumonia.

In clinical studies involving patients with COPD, who used fluticasone propionate at a dose of 500 mcg, an increase in the incidence of pneumonia was reported. Physicians should be careful about the possible development of pneumonia in patients with COPD, since the clinical symptoms of pneumonia and exacerbation of COPD often coincide.

Rarely: esophageal candidiasis.

From the immune system: hypersensitivity reactions have been reported with the following manifestations: infrequently - skin hypersensitivity reactions; very rarely - angioedema (mainly of the face and oropharynx), respiratory symptoms (shortness of breath and / or bronchospasm) and anaphylactic reactions.

On the part of the endocrine system: a systemic effect is possible, which includes: very rarely - Cushing's syndrome, cushingoid symptoms, suppression of adrenal function, growth retardation in children and adolescents, decreased bone mineralization, development of cataracts and glaucoma (see SPECIAL INSTRUCTIONS).

Metabolism and digestive disorders: very rarely - hyperglycemia (see SPECIAL INSTRUCTIONS).

Digestive system: very rarely - dyspepsia.

Musculoskeletal system and connective tissue: very rarely - arthralgia.

Mental disorders: very rarely - a feeling of anxiety, sleep disturbances, changes in behavior, including hyperactivity and irritability (mainly in children).

The frequency is unknown - depression, aggression (mainly in children).

From the respiratory system and chest: often - hoarseness. In some patients, the use of an inhaled form of fluticasone propionate may cause hoarseness. In this case, it is helpful to gargle with water immediately after inhalation. Very rarely - paradoxical bronchospasm.

As with other inhaled preparations, paradoxical bronchospasm may develop with rapidly increasing shortness of breath after inhalation. In this case, quick-acting inhaled bronchodilators are immediately used, the inhalation of Flixotide is immediately stopped, the patient is examined and, if necessary, alternative therapy is carried out. Frequency unknown - epistaxis.

On the part of the skin and subcutaneous tissues: often - bruising.

special instructions

BA treatment should be carried out according to a step-by-step program, the patient's condition should be regularly monitored both clinically and by determining the parameters of the external respiration function.

A sudden and progressive deterioration in asthma control is a potentially life-threatening condition in which the issue of increasing the GCS dose should be addressed. In the event of such a risk, the patient should be monitored daily for peakfluometry.

Flixotide Nebula is not intended to reduce the severity of acute asthma attacks, in which it is necessary to use fast and short-acting inhaled bronchodilators. Patients should be warned about the need to carry such medicines with them. Flixotide Nebula should be prescribed for long-term prophylactic treatment.

Flixotide Nebula is not a preparation that can replace the injection or oral administration of GCS in emergency conditions (for example, in severe exacerbation of asthma, which is life-threatening).

Severe asthma requires constant medical monitoring, including the determination of indicators of respiratory function, since there is a risk of acute asthma attacks and even death in such patients.

An increase in the frequency of use and dose of short-acting inhaled β2-agonists signals a gradual loss of control over asthma. If the effectiveness of short-acting bronchodilators is reduced or the need for their more frequent use, the patient should consult a doctor. In such situations, patients are advised to undergo additional examination to determine the need to strengthen anti-inflammatory therapy (for example, increasing the doses of inhaled corticosteroids or prescribing a course of oral corticosteroids). In severe exacerbation of asthma, the usual therapy for this condition should be prescribed.

There are isolated reports of an increase in blood glucose levels both in patients with diagnosed diabetes mellitus and in patients without diabetes mellitus (see SIDE EFFECTS). This should be taken into account when prescribing Flixotide Nebula to patients with diabetes mellitus.

As with the treatment with other inhaled preparations, it is possible to develop paradoxical bronchospasm with rapidly increasing shortness of breath after inhalation. In this case, inhalation of Flixotide is immediately stopped, the patient is examined and, if necessary, alternative therapy is prescribed.

When using inhaled GCS in high doses and for a long time, a systemic effect may occur, but the likelihood of this is much less than when using oral steroids. Systemic action can manifest as Cushing's syndrome, cushingoid symptoms, suppression of adrenal function, stunted growth in children and adolescents, decreased bone mineralization, cataracts and glaucoma, and, in rare cases, mental disorders, behavioral changes, including psychomotor hyperactivity, sleep disorders, anxiety , depressive and aggressive states (mainly in children). Therefore, the dose of inhaled corticosteroids should be regularly checked, it should be reduced to the minimum possible to maintain effective control of asthma symptoms.

Long-term use of inhaled corticosteroids in high doses can cause suppression of adrenal function and an acute adrenal crisis. Children under 16 years of age, when using fluticasone doses exceeding the approved ones (usually ≥1000 mcg / day), are at particular risk. The development of an acute adrenal crisis can be triggered by trauma, surgery, infections, or a sharp decrease in the dose of the preparation. Symptoms are usually mild and may present with anorexia, abdominal pain, weight loss, fatigue, headache, nausea, vomiting, decreased consciousness, hypoglycemia, and seizures. In case of stress or surgery, additional use of systemic corticosteroids is possible.

It is recommended to regularly check the growth of children undergoing long-term treatment with inhaled GCS. If growth has slowed down, therapy should be revised in order to reduce the dose of inhaled corticosteroids, if possible, to the minimum dose that maintains effective control of asthma symptoms. Additionally, the child should be consulted with a pediatric pulmonologist.

Some patients may have a higher sensitivity to inhaled GCS than most patients.

The effect of inhaled fluticasone propionate should reduce the need for oral steroids. But when switching from oral steroids to inhaled fluticasone propionate, patients remain at risk of adrenal suppression. The possibility of side reactions persists for some time. Such patients may need to stay in specialized consultations to determine the degree of negative effect on the adrenal glands before undergoing certain procedures. It should be borne in mind the possibility of residual dysfunction of the adrenal glands in emergency situations, including surgery and other stressful situations, and take into account the need to prescribe appropriate treatment with GCS.

Patients should receive doses of inhaled fluticasone propionate appropriate for the severity of the disease. The dose should be reduced to the lowest effective dose that allows effective control of the disease. Systemic steroids and / or antibiotics may be necessary if effective disease control is not established.

Replacing systemic steroid therapy with inhaled therapy can sometimes unmask allergic diseases, such as allergic rhinitis or eczema, that were previously controlled by systemic steroid use. These allergic manifestations should be symptomatically relieved with antihistamines and / or topical preparations, including topical corticosteroids.

As with all inhaled corticosteroids, patients with active or latent pulmonary tuberculosis require special attention.

Treatment with Nebula Flixotide should not be discontinued abruptly.

Transfer of patients treated with oral corticosteroids to inhalation use. The transfer of patients who are treated with oral steroids to the inhaled use of Flixotide Nebula and their further treatment require special attention, since the restoration of adrenal function weakened due to prolonged systemic steroid therapy may take a long time.

Long-term use of inhaled corticosteroids in high doses can cause suppression of adrenal function. The adrenal function of such patients should be monitored regularly. Systemic steroid doses should be reduced with caution (see APPLICATION).

Some patients experience non-specific deterioration during the transition period despite maintaining or even improving respiratory function. They should continue to switch from systemic steroids to inhaled fluticasone propionate unless objective symptoms of adrenal insufficiency appear.

Patients who discontinue treatment with oral steroids, in whom adrenal function remains reduced, should have a special card with a warning about the need for additional administration of a systemic steroid in stressful situations, such as an acute attack of asthma, respiratory tract infections, significant intercurrent diseases, surgery, trauma ...

Ritonavir can significantly increase plasma concentrations of fluticasone propionate. Therefore, the simultaneous use of fluticasone propionate and ritonavir should be avoided, unless the benefits of such use outweigh the risk of systemic effects of GCS. There is also an increased risk of systemic effects of fluticasone propionate when used concomitantly with CYP 3A4 inhibitors (see INTERACTIONS).

Use during pregnancy and lactation. Experience with use during pregnancy in humans is limited. When deciding on the appointment of the preparation during this period, it is necessary to weigh the expected benefit to the mother and the potential risk to the fetus. The results of a retrospective epidemiological study indicated the absence of an increased risk of major congenital malformations after exposure to fluticasone propionate in the first trimester of pregnancy compared with other inhaled corticosteroids.

It is currently not established whether fluticasone propionate passes into breast milk, however, based on the pharmacological profile of the preparation, this is unlikely. The preparation can be used during breastfeeding only when the expected benefit to the mother outweighs the potential risk to the fetus.

Children. For use in children over 4 years of age.

The ability to influence the reaction rate when driving or operating other mechanisms. Impact is unlikely.

Interactions

Under normal conditions, after inhalation, a low plasma concentration of fluticasone propionate is achieved due to extensive first-pass metabolism and high systemic clearance of the preparation mediated by cytochrome p450 3a4 in the liver and intestines. therefore, the likelihood of clinically significant preparation interactions mediated by fluticasone propionate is very low.

The results of studies on the study of preparation interactions in healthy volunteers showed that ritonavir (a strong inhibitor of cytochrome P450 3A4), when applied 100 μg 2 times a day, can increase the concentration of fluticasone propionate in the blood plasma hundreds of times, which leads to a significant decrease in the concentration of cortisol in the blood plasma ... There is not enough information about such interactions with inhaled fluticasone propionate, but the indicated increase in the concentration of fluticasone propionate in blood plasma may be observed. There have also been reports of the development of Cushing's syndrome and adrenal suppression. The simultaneous use of fluticasone propionate and ritonavir should be avoided, unless the benefits of such use outweigh the risk of systemic effects of GCS.

In a small study in healthy volunteers, the less potent CYP 3A4 inhibitor ketocanosol increased the concentration of fluticasone propionate after one inhalation to 150%, which led to a significant decrease in the concentration of cortisol in the blood serum compared with the use of fluticasone propionate alone. When used simultaneously with other potent inhibitors of CYP 3A, such as itraconazole, an increase in the concentration of systemic fluticasone propionate and the risk of systemic effects are also expected. Care should be taken and, if possible, long-term use of such a combination of preparations should be avoided.

In studies of interaction with other inhibitors of cytochrome P450 3A4, it was proved that these inhibitors have a very insignificant (erythromycin) or insignificant (ketoconazole) effect on increasing the systemic concentration of fluticasone propionate in blood plasma without a significant decrease in the concentration of cortisol. Nevertheless, the simultaneous use of strong inhibitors of cytochrome P450 3A4 (for example, ketoconazole) should be used with caution, given the possibility of an increase in the systemic effect of fluticasone propionate.

Overdose

As a result of the use of flixotide nebula in doses exceeding the recommended ones, temporary inhibition of adrenal function may occur. this condition does not require urgent care, since the function of the adrenal cortex is restored after a few days, which is confirmed by the determination of the level of cortisol in the blood plasma. but when using doses exceeding the recommended ones, for a long period, some suppression of the function of the adrenal cortex is possible, therefore, it may be necessary to control the adrenal reserve.

In case of overdose, therapy can be prolonged in doses necessary to control asthma symptoms. Patients who use doses exceeding the recommended ones should be under the special supervision of a physician, and the dose of the preparation for them should be reduced gradually.

Storage conditions

At temperatures below 30 ° C in an upright position. protect from direct sunlight. do not freeze. Nebula removed from aluminum foil bag should be stored protected from light and used within 28 days. opened nebules should be stored upright in the refrigerator and used within 12 hours after opening.