Flixotide analogues and prices. Pharmacological characteristics of the drug
pharmachologic effect
Fluticasone propionate belongs to the group of corticosteroids local action and when inhaled in recommended doses, has a pronounced anti-inflammatory and antiallergic effect, which leads to a decrease in the severity of symptoms and a decrease in the frequency of exacerbations of diseases accompanied by obstruction respiratory tract(bronchial asthma, Chronical bronchitis, emphysema).
Fluticasone propionate inhibits proliferation mast cells, eosinophils, lymphocytes, macrophages, neutrophils, reduces the production and release of inflammatory mediators and other biological active substances- histamine, prostaglandins, leukotrienes, cytokines.
In COPD, the effectiveness of inhaled fluticasone propionate on lung function has been 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 tableted corticosteroids and an increase in the quality of life of patients.
The systemic effect of fluticasone is minimally expressed: in therapeutic doses has virtually no effect on the hypothalamic-pituitary-adrenal system.
The drug restores the patient's response to bronchodilators, making it possible to reduce the frequency of their use.
Therapeutic effect after inhalation use 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 administration, the absolute bioavailability of fluticasone propionate ranges from 7.8% to 10.9% in healthy volunteers, depending on the drug delivery system. In patients with chronic obstructive pulmonary disease (COPD) or bronchial asthma, systemic exposure to the drug is less than in healthy volunteers.
Systemic absorption occurs primarily in the lungs, with absorption initially rapid and then slowing down. Part of the inhaled dose can be swallowed, but its systemic effect is minimal due to the drug's poor solubility in water and intensive first-pass metabolism 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
Plasma protein binding is moderately high, 91%.
Fluticasone propionate has a large volume of distribution in equilibrium state- about 300 l.
Metabolism
Fluticasone propionate is metabolized in the liver with the participation of CYP3A4, forming an inactive metabolite.
Removal
Fluticasone propionate has a high plasma clearance of 1150 ml/min. T 1/2 is about 8 hours. Renal clearance- less than 0.2%. Less than 5% is excreted in the urine as a metabolite.
Indications
- basic anti-inflammatory therapy bronchial asthma(including when severe course diseases and addictions systemic GCS) in adults and children 1 year and older;
- treatment of chronic obstructive pulmonary disease in adults as additional means to bronchodilator therapy long acting/for example, to long-acting beta-agonists LABA).
Dosage regimen
Flixotide metered dose aerosol is intended for oral inhalation only. Treatment with Flixotide aerosol refers to methods preventive therapy, the drug must be used regularly, even in the absence of symptoms of the disease. For patients in whom the use of metered dose aerosol for inhalation is difficult, it is recommended to use a spacer.
Persons elderly and patients with liver or kidney diseases special selection no dose required.
Bronchial asthma
The therapeutic effect after using the drug Flixotide occurs 4-7 days after the start of treatment. In patients who have not previously used inhaled corticosteroids, improvement can be observed within 24 hours after starting the drug.
If the patient believes that treatment with bronchodilators fast action becomes less effective or needs larger number inhalations than usual, the doctor should pay special attention to this.
Adults and teenagers over 16 years of age: The recommended dose is 100-1000 mcg 2 times a day. The initial dose of the drug depends on the severity of the disease: for bronchial asthma mild degree severity - 100-250 mcg 2 times a day, for bronchial asthma medium degree severity - 250-500 mcg 2 times/day, for severe bronchial asthma - 500-1000 mcg 2 times/day. Depending on the patient's individual response, the initial dose of the drug can be increased until the disease is controlled or reduced to the minimum effective dose.
Children aged 4 years and older It is recommended to use the drug Flixotide ® containing 50 mcg of fluticasone propionate in one dose. The recommended dose is 50-200 mcg 2 times a day. In most children, asthma control can be achieved using doses of 50-100 mcg 2 times a day. In children with insufficiently controlled bronchial asthma, the dose may be increased to 200 mcg 2 times a day. The initial dose of the drug depends on the severity of the disease. Then, depending on the patient's individual response, the initial dose of the drug can be increased until the disease is controlled or reduced to the minimum effective dose.
Children aged 1 to 4 years: The recommended dose is 100 mcg 2 times/day. The drug is administered using an inhaler through a spacer with a face mask, for example, Babyhaler. Flixotide ® dosed aerosol is especially indicated for children younger age with frequent and prolonged attacks of bronchial asthma.
Diagnosis and treatment of bronchial asthma should be carried out during regular examination of the patient by a doctor.
Chronic obstructive pulmonary disease
For adults The recommended dose is 500 mcg 2 times / day as an additional agent to therapy with long-acting bronchodilators (for example, LABA). It is recommended to use Flixotide ® metered aerosol containing 250 mcg per dose.
To achieve optimal effect, it is recommended to use the drug daily for 3-6 months. If there is no clinical improvement after 3-6 months, a medical examination is necessary.
Side effect
Adverse reactions are listed according to damage to organs and systems and frequency of occurrence. Frequency of occurrence determined in the following way: very often >1/10, often >1/100 and<1/10, нечасто >1/1000 and<1/100, редко >1/10000 and<1/1000 и очень редко <1/10000, включая отдельные случаи. Категории частоты были сформированы на основании клинических исследований препарата и пострегистрационного наблюдения.
From the immune system(hypersensitivity reactions with the following manifestations have been described): uncommon - skin hypersensitivity reactions; very rarely - angioedema (mainly swelling of the face and oropharynx), respiratory disorders (shortness of breath and/or bronchospasm) and anaphylactic reactions.
From the endocrine system(systemic effects are possible): very rarely - Cushing's syndrome, Cushingoid symptoms, suppression of adrenal cortex function, growth retardation, decreased bone mineralization, cataracts, glaucoma.
Metabolism and nutrition: very rarely - hyperglycemia.
From the mental side: very rarely - anxiety, sleep and behavior disorders, including hyperactivity and irritability (mainly in children).
From the respiratory system, chest and mediastinal organs: often - hoarseness of voice (some patients may experience hoarseness; it is recommended to rinse your mouth and throat with water immediately after inhalation); very rarely - paradoxical bronchospasm.
For the skin and subcutaneous fat: often - bruising.
Contraindications for use
- hypersensitivity to any component of the drug;
- acute bronchospasm;
- status asthmaticus (as a first-line remedy);
- children's age (up to 1 year).
Use during pregnancy and breastfeeding
Controlled clinical studies on the use of fluticasone propionate in pregnant women have not been conducted. The effect of fluticasone propionate on pregnancy has not been studied. Preclinical studies of the effect of fluticasone propionate on reproductive function have shown that at systemic exposure values exceeding those observed when using recommended therapeutic inhalation doses, only effects characteristic of GCS are observed. Genotoxicity studies have shown no mutagenic potential.
However, as with the use of other drugs, the use of fluticasone propionate during pregnancy is only possible if the expected benefit to the mother outweighs any potential risk to the fetus.
It has not yet been established whether fluticasone propionate passes into breast milk. Measurable concentrations of fluticasone propionate in the blood plasma of lactating laboratory rats after subcutaneous administration of the drug indicate the presence of fluticasone propionate in breast milk. However, following inhaled use of fluticasone propionate at recommended doses, plasma concentrations are expected to be low.
Use in children
Contraindication: children under 1 year of age.
U children over 4 years old It is recommended to use an aerosol containing 50 mcg of fluticasone propionate in 1 dose. It is recommended to prescribe 50-100 mcg 2 times a day. The initial dose of the drug depends on the severity of the disease. Then, depending on the patient's individual response to treatment, the initial dose can be increased until clinical effect occurs or reduced to the minimum effective dose.
Children aged 1 to 4 years It is recommended to prescribe 100 mcg 2 times a day.
Young children require higher doses of Flixotide compared to older children due to reduced drug intake during inhalation (smaller bronchial lumen, use of a spacer, intense nasal breathing in young children).
The drug is administered using an inhaler through a spacer with a face mask (for example, Babyhaler).
Flixotide dosed aerosol is especially indicated for young children with severe bronchial asthma.
Overdose
Symptoms: An acute overdose of the drug can lead to temporary inhibition of the function of the hypothalamic-pituitary-adrenal system, which usually does not require emergency treatment, since the function of the adrenal cortex is restored within a few days. With long-term use of doses of the drug exceeding the recommended ones, significant suppression of the function of the adrenal cortex is possible. Very rare reports have been received of the development of acute adrenal crisis in children who received a dose of fluticasone propionate of 1000 mcg/day or higher for several months or years. Such patients experienced hypoglycemia, depression of consciousness and seizures. Acute adrenal crisis can develop against the background of the following conditions: severe trauma, surgery, infections, a sharp reduction in the dose of fluticasone propionate.
Treatment: It is necessary to monitor patients receiving high doses and gradually reduce the dose of fluticasone propionate.
Drug interactions
When fluticasone propionate is administered by inhalation, its concentrations in the blood plasma are very low due to active first-pass metabolism and high systemic clearance in the intestines and liver, with the participation of enzymes of the cytochrome P450 3A4 system. Therefore, clinically significant drug interactions with fluticasone propionate are unlikely.
A drug interaction study in healthy volunteers showed that ritonavir (a highly active cytochrome P450 3A4 inhibitor) can significantly increase plasma concentrations of fluticasone propionate, which consequently leads to a decrease in serum cortisol concentrations. During post-marketing use, clinically significant drug interactions have been observed in patients receiving intranasal or inhaled fluticasone propionate with ritonavir, resulting in systemic corticosteroid effects. including Cushing's syndrome and adrenal suppression. Therefore, concomitant use of ritonavir and fluticasone propionate should be avoided unless the potential benefit to the patient outweighs the possible risk of systemic side effects of GCS.
Studies with other cytochrome P450 3A4 inhibitors have demonstrated small (erythromycin) and small (ketoconazole) increases in systemic exposure of fluticasone propionate without any significant decrease in serum cortisol concentrations. However, caution should be exercised when concomitantly administering potent cytochrome P450 3A4 inhibitors (eg, ketoconazole), as there is a possibility of increased plasma concentrations of fluticasone propionate.
Conditions for dispensing from pharmacies
The drug is available with a prescription.
Storage conditions and periods
The drug should be stored out of the reach of children at a temperature not exceeding 30°C; Do not freeze or expose to direct sunlight. Shelf life - 2 years.
Use for liver dysfunction
Patients with liver dysfunction no dose adjustment is required.
Use for renal impairment
Patients with renal dysfunction no dose adjustment is required.Use in elderly patients
Elderly people no dose adjustment is required.special instructions
An increase in the frequency of use of short-acting inhaled beta 2 agonists to control the symptoms of bronchial asthma indicates a deterioration in control over the course of the disease. In this case, the patient's treatment plan requires revision.
A sudden and progressive deterioration in control over the course of bronchial asthma represents a potential danger to the patient's life and requires an increase in the dose of GCS. Patients at risk may be prescribed daily peak flow measurements.
Abruptly stopping treatment with Flixotide ® is not recommended.
Particular care should be taken when treating patients with active or inactive forms of pulmonary tuberculosis with inhaled corticosteroids.
It is recommended to check the patient's ability to use the inhaler correctly to ensure that the inhaler is activated in sync with inhalation to ensure optimal delivery of the active substance to the lungs.
With long-term use of any inhaled corticosteroids, especially in high doses, systemic effects may be observed, but the likelihood of their development is much lower than when taking corticosteroids orally. Possible systemic effects include Cushing's syndrome, Cushingoid symptoms, adrenal suppression, decreased bone mineral density, growth retardation in children and adolescents, cataracts, glaucoma. Therefore, it is especially important that when a therapeutic effect is achieved, the dose of inhaled corticosteroids is reduced to the minimum effective dose to control the course of the disease.
It is always necessary to consider the possibility of adrenal insufficiency in emergency situations (including surgery), as well as during planned interventions, which can cause stress, especially in patients taking high doses of corticosteroids for a long time. In this case, the issue of the need for additional administration of GCS should be decided depending on the clinical situation.
Due to possible adrenal insufficiency, special care should be taken and regular monitoring of adrenal function indicators when transferring patients who have taken oral corticosteroids to treatment with fluticasone propionate in the form of an inhalation aerosol. Discontinuation of systemic corticosteroids while taking fluticasone propionate inhaled aerosol should be done gradually, and patients should carry a card indicating that they may require additional corticosteroids during periods of stress.
When transferring patients from taking systemic corticosteroids to inhalation 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 carry out symptomatic treatment with antihistamines and/or topical drugs, incl. GCS for local use.
As with other inhalation therapy, there is a possibility of developing paradoxical bronchospasm with an immediate increase in shortness of breath after inhalation. To stop this attack, immediate use of a fast and short-acting inhaled bronchodilator is necessary. Fluticasone propionate inhalation should be discontinued immediately, the patient's condition should be assessed and, if necessary, alternative therapy should be prescribed.
As with most inhalation products in aerosol packages, the effect decreases as the can cools.
There are very rare reports of increased blood glucose levels, and this should be kept in mind when prescribing fluticasone propionate to patients with diabetes.
An increase in cases of pneumonia has been reported in patients with COPD receiving fluticasone propionate 500 mcg. One should be aware of the possibility of pneumonia in such patients, since the clinical signs of pneumonia and exacerbation of the underlying disease may often coincide.
Impact on the ability to drive vehicles and operate machinery
The effect of fluticasone propionate on the ability to drive a car and operate machinery that requires increased concentration is unlikely.
Flixotide is a drug from the group of glucocorticosteroids.
What is the composition and release form of the drug Flixotide?
The product is produced in a dosed aerosol for inhalation, which contains a white suspension. The drug in a metal inhaler is equipped with a nebulizer. The active substance is fluticasone propionate in the so-called micronized form. Auxiliary component – tetrafluoroethane.
The inhaler with the medicine Flixotide contains a different number of doses: 120 and 60. You can buy the medicine with a prescription. The implementation period is two years. Do not freeze the aerosol or expose it to direct sunlight.
What is the effect of Flixotide suspension?
The glucocorticosteroid Flixotide is intended for local use; the drug has a pronounced anti-inflammatory effect, in addition, it has an antiallergic effect. As a result, the severity of symptoms of diseases that occur with airway obstruction (emphysema, bronchial asthma, and chronic bronchitis) decreases.
The active component, fluticasone propionate, suppresses the proliferation of lymphocytes, mast cells, neutrophils, as well as eosinophils, macrophages, and also reduces the production of inflammatory mediators. The systemic effect of the drug is minimal.
The therapeutic effect of the drug Flixotide begins within 24 hours after inhalation use, reaching a maximum within one, two weeks or more from the start of therapeutic measures. Bioavailability is 10%.
Systemic absorption occurs predominantly in the lung tissue. Binding to blood proteins is 91 percent. Metabolized in the liver through the participation of CYP3A4. The half-life is eight hours. Excreted in urine.
What are the indications for use of the Flixotide inhaler?
The instructions for use of the drug Flixotide are prescribed for the treatment of bronchial asthma as a basic therapy, in addition, the medication is prescribed for chronic obstructive pulmonary disease as an additional drug.
What are the contraindications for use of Flixotide aerosol?
Among the contraindications to the use of the drug Flixotide (aerosol), the instructions for use include children under one year of age, hypersensitivity to the drug component, asthmatic status, and the presence of acute bronchospasm.
The medication is used with caution for osteoporosis, liver cirrhosis, pulmonary tuberculosis, glaucoma, pregnancy, hypothyroidism, during the lactation period, as well as for systemic infections (viral, bacterial, mycotic, fungal).
What are the uses and dosage of Flixotide?
Metered aerosol is used for inhalation through the mouth. For bronchial asthma, the therapeutic effect occurs approximately a week after the start of treatment procedures. Typically the recommended dose ranges from 100 to 1000 mcg twice daily.
For mild asthma, the dose is 100-250 mcg, for moderate asthma, 250-500 mcg, for severe asthma, 500-1000 mcg. Depending on the patient's condition, the dosage can be increased according to the doctor's recommendation.
Overdose from Flixotide
Symptoms of an overdose of the drug Flixotide: depression of the hypothalamic-pituitary-adrenal system, especially with prolonged use of the drug; sometimes an acute adrenal crisis may develop, which will manifest itself as convulsions, depression of consciousness, and hypoglycemia will also occur. In this situation, the dose of the drug is gradually reduced and symptomatic treatment is carried out.
What are the side effects of Flixotide?
Among other side effects, hypersensitivity reactions can be noted; angioedema is possible, which is mainly localized in the oropharynx, as well as on the face; in addition, respiratory disorders in the form of bronchospasm or shortness of breath; in more severe situations, an anaphylactic reaction occurs.
Other negative manifestations are expressed in the form of Cushing's syndrome, which is characterized by a slowdown in growth, suppression of the function of the adrenal cortex, a decrease in the mineralization of the obliques is observed, in addition, changes in vision occur in the form of cataracts and glaucoma.
In addition to the listed side effects, the following manifestations may be observed: hyperglycemia is noted, anxiety occurs, bruising may be observed on the skin, sleep disturbance occurs, behavior changes, including irritability and some hyperactivity, mainly in children.
In addition, a patient using the drug Flixotide may experience changes in the respiratory system in the form of hoarseness. To prevent the development of this symptom, it is necessary to rinse the mouth with running water after each inhalation. Sometimes so-called paradoxical bronchospasm may occur.
special instructions
It is worth noting that abrupt discontinuation of Flixotide is not recommended. As with most inhalation agents, cooling the canister may reduce the therapeutic effect of the drug.
How to replace Flixotide, what analogues should I use?
Flixonase, Fluticasone, as well as Fluticasone propionate, Cutivate, Nazarel.
Conclusion
Flixotide should be used on the recommendation of a qualified specialist.
Flixotide is a drug from the group of glucocorticosteroid hormones used in the form of inhalations.
1 dose of Flixotide Discus 50/100/250 contains microionized fluticasone propionate 50/100/250 µg, respectively.
1 dose of Flixotide Evohaler 50/100/250 contains microionized fluticasone propionate 50/100/250 µg, respectively.
1 nebula (2 ml) of Flixotide contains microionized fluticasone propionate 0.5 or 2 mg.
Flixotide is an inhaled drug that has a pronounced anti-inflammatory effect on lung tissue. The active substance is fluticasone propionate, a glucocorticosteroid that helps reduce the frequency of bronchial asthma attacks, reduces bronchial obstruction in patients with CLD, and improves lung function. When using Flixotide according to the instructions, a pronounced therapeutic effect is achieved already on days 4-6, and a subjective improvement in the condition is observed within a day. Thanks to this, reviews of Flixotide are positive both from pulmonologists and from patients using this drug.
The bioavailability of Flixotide ranges from 10 to 30%. When administered by inhalation, some of the drug enters the digestive system, but this does not play a significant role, since when administered orally, the bioavailability of fluticasone propionate does not exceed 1%. Systemic absorption of the drug through the inhalation route is directly proportional to the administered dose. Part of the drug that enters the bloodstream is quickly metabolized in the liver, and the drug is excreted by the kidneys. The half-life of Flixotide is 8 hours.
Flixotide: indications for use
The instructions for Flixotide describe the following indications for use:
- therapy for patients suffering from severe or moderate bronchial asthma (including those taking systemic glucocorticosteroids) to prevent attacks;
- therapy of patients with CLD to reduce bronchial obstruction and improve ventilation function of the lungs.
Flixotide: instructions for use
Flixotide Discus
Used for inhalation. To achieve the desired effect, Flixotide Discus must be used regularly, even during remission. The duration of treatment and dosage in each clinical situation is selected by the attending physician.
For adult patients, depending on the severity of pulmonary pathology, the dosage of Flixotide Discus is 100-1000 mcg twice a day. The use of the drug begins with minimal doses that cause a therapeutic effect. If necessary, the dosage is increased.
For patients taking beclamethasone dipropionate, the dosage of Flixotide is half the dose of beclamethasone.
The maximum daily dosage of Flixotide according to the instructions is 2000 mcg.
For children over 4 years old suffering from bronchial asthma, Flixotide Discus is prescribed at a dose of 50-100 mcg twice a day. If necessary, the dosage can be gradually increased to 400 mcg per day.
For adult patients suffering from CLD, Flixotide Discus is prescribed 500 mcg twice a day.
Flixotide Evohaler
Before using Flixotide Evohaler for the first time, as well as in cases where the drug has not been used for more than a week, it is necessary to spray several doses. This ensures uniform dosing of the active substance. The mouthpiece should be cleaned at least once a week. Before use, the bottle with the drug must be shaken thoroughly. The aerosol should be sprayed while inhaling slowly. When determining the dosage of the drug, it must be taken into account that a single dose must correspond to the dose of two sprays of Flixotide Evohaler.
For children aged 1-4 years, inhalation is carried out using a special delivery device - the Babyhaler spacer.
Flixotide Nebula
This form of the drug is used for inhalation using a mouthpiece or face mask. The drug can also be delivered using a jet (not ultrasonic!) nebulizer. If it is necessary to carry out inhalation for a long time, as well as to achieve a small dosage, diluting the drug in saline solution is permissible.
Contraindications to the use of Flixotide
The instructions for Flixotide indicate the following contraindications for its use:
- individual intolerance to the active substance or auxiliary components;
- not used to relieve attacks of bronchial asthma.
Flixotide and drug analogues should be prescribed with extreme caution to children, taking into account possible hormonal disorders. Also, special care should be taken when prescribing the drug to patients suffering from pulmonary tuberculosis and diabetes mellitus.
Side effects of the drug Flixotide
When using the drug, the following side effects may occur:
- from the respiratory system: paradoxical bronchospasm (if this symptom occurs, it is necessary to use fast-acting bronchodilators), hoarseness,
- from the metabolic and endocrine system: impaired mineralization of bone tissue, in children - growth retardation, increased concentration of glucose in the blood, glaucoma, cataracts,
- from the central nervous system: increased excitability, anxiety, sleep disturbance,
- allergic reactions: bronchospasm, urticaria, angioedema, anaphylaxis.
special instructions
After each use of the drug, you must rinse your mouth thoroughly with water. If this rule is not followed, oral candidiasis may develop, which is often the reason for negative reviews of Flixotide.
Use of Flixotide during pregnancy
The use of the drug during pregnancy is possible only in cases where the benefit to the mother significantly outweighs the risk of possible pathology in the fetus. 
Storage conditions
Flixotide and drug analogues should be stored at room temperature away from sunlight. Open nebulas are stored for no more than 12 hours in a vertical position. It is strictly forbidden to freeze the drug.
Flixotide: drug analogues
The following analogues of Flixotide are found: Cutivate, Nazarel, Flixonase, Fluticasone.
3D images
Composition and release form
in inhalers (with a metering device); 1 set in a cardboard box.
Description of the dosage form
A metal inhaler with a concave base and a metering device, equipped with a nebulizer. The contents of the inhaler are a white or almost white suspension.
Characteristic
GCS of local action.
pharmachologic effect
pharmachologic effect- antiallergic, local anti-inflammatory, glucocorticoid.Inhibits the proliferation of mast cells, eosinophils, lymphocytes, macrophages, neutrophils, reduces the production and release of inflammatory mediators and other biologically active substances (histamine, PG, leukotrienes, cytokines).
Pharmacodynamics
Reduces the severity of symptoms and reduces the frequency of exacerbations of diseases accompanied by airway obstruction, reduces the need to prescribe additional courses of tableted GCS, and is characterized by an increase in the patient’s quality of life. Restores the patient's response to bronchodilators, allowing to reduce the frequency of their use. The therapeutic effect appears within 24 hours after inhalation use, reaches a maximum within 1-2 weeks or more after the start of treatment and persists for several days after discontinuation of the drug.
Pharmacokinetics
After inhalation administration, absolute bioavailability is 10-30% (depending on the drug delivery system). Absorbed primarily in the lungs. When part of an inhaled dose is swallowed, the systemic effect is minimal due to the low solubility of the drug in water and intensive metabolism during the “first pass” through the liver. The bioavailability of fluticasone propionate when absorbed from the gastrointestinal tract is less than 1%. There is a direct relationship between the inhaled dose and the systemic effect of fluticasone propionate. Plasma protein binding is 91%. Has a large distribution volume (about 300 l). Metabolized in the liver with the participation of the CYP3A4 enzyme of the cytochrome P450 system to form an inactive metabolite. Renal clearance is insignificant (less than 0.2%). Has a high plasma Cl - 1150 ml/min. T1/2 is 8 hours. Excreted in the urine as a metabolite (less than 5%).
Indications of the drug Flixotide ®
Bronchial asthma (basic anti-inflammatory therapy) in adults and children 1 year and older (including those with severe disease, with dependence on systemic corticosteroids), chronic obstructive pulmonary disease in adults.
Contraindications
Hypersensitivity, acute bronchospasm, status asthmaticus (as a first-line remedy), bronchitis of non-asthmatic nature, children's age (up to 1 year).
Use caution only if the expected effect of therapy outweighs the potential risk to the fetus or child.
Side effects
Candidiasis of the oral cavity and pharynx, hoarseness (after inhalation it is necessary to rinse the mouth and throat with water), paradoxical bronchospasm (requires discontinuation of the drug and continuation of therapy with other means); rarely - the development of allergic reactions (skin rash, angioedema, dyspnea or bronchospasm, anaphylactic reactions); Possible decreased function of the adrenal cortex, osteoporosis, growth retardation in children, cataracts, increased intraocular pressure.
Interaction
When co-administered with CYP3A4 inhibitors (ketoconazole, ritonavir), the systemic effect of fluticasone propionate may increase (caution should be exercised).
Directions for use and doses
Inhalation, after inhalation you should 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 form of asthma - 100-250 mcg, moderate form - 250-500 mcg, severe form - 500-1000 mcg. Depending on the patient's individual response, the initial dose is either increased until clinical effect appears or reduced to the minimum effective dose.
Children over 4 years of age (only in the form of an inhalation aerosol dosed at 50 mcg of fluticasone in one dose): the recommended dose is 50-100 mcg 2 times a day.
Children from 1 year to 4 years: (only in the form of an inhalation aerosol dosed at 50 mcg of fluticasone per dose): 100 mcg 2 times a day. Young children require higher doses compared to older children due to reduced drug intake during inhalation (use of a spacer, smaller bronchial lumen, intense nasal breathing). The drug 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
Symptoms: acute - temporary decrease in the function of the adrenal cortex; chronic - suppression of the function of the adrenal cortex.
Treatment: chronic overdose - monitoring the reserve function of the adrenal cortex (treatment with the drug can be continued in doses sufficient to maintain the therapeutic effect).
Precautionary measures
If there is no effect or a sharp exacerbation of bronchial asthma, the dose of the drug should be increased and, if necessary, oral steroids and/or antibiotics should be prescribed if infection develops. In patients taking systemic steroids, the transition to inhalation should take place against the background of gradual withdrawal of systemic drugs. A gradual reduction in the dose of systemic glucocorticoids should begin one week after starting fluticasone. When the maintenance dose of prednisolone (or other glucocorticoids in equivalent doses) is less than 10 mg/day, dose reduction should not exceed 1 mg/day and should be carried out at intervals of at least 1 week. With a maintenance dose of prednisolone over 10 mg/day - in large doses at intervals of 1 week.
Treatment with Flixotide should not be stopped abruptly. Use with caution for pulmonary tuberculosis. The growth dynamics of children receiving the drug for a long time should be regularly monitored.
In rare cases, when transferring patients from taking systemic glucocorticoids to inhaled therapy, conditions accompanied by hypereosinophilia may develop; Concomitant allergic diseases (allergic rhinitis, eczema), which were previously suppressed by systemic drugs, may also worsen. In these cases, symptomatic treatment with antihistamines and/or topical medications is necessary. If necessary, local antifungal therapy can be prescribed throughout the course of treatment.
special instructions
Not intended for relieving attacks of bronchial asthma.
The drug must be taken regularly throughout the course of treatment, even in the absence of symptoms of the disease.
The effect decreases as the can cools.
Manufacturer
GlaxoSmithKline Pharmaceuticals SA, Poland.
Storage conditions for the drug Flixotide ®
At a temperature not exceeding 30 °C. Do not freeze or expose to direct sunlight.Keep out of the reach of children.
Shelf life of the drug Flixotide ®
2 years.Do not use after the expiration date stated on the package.
Synonyms of nosological groups
| Category ICD-10 | Synonyms of diseases according to ICD-10 |
|---|---|
| J42 Chronic bronchitis, unspecified | Allergic bronchitis |
| Asthmoid bronchitis | |
| Allergic bronchitis | |
| Asthmatic bronchitis | |
| Chronic bronchitis | |
| Inflammatory disease of the respiratory tract | |
| Bronchial disease | |
| Qatar smoker | |
| Cough due to inflammatory diseases of the lungs and bronchi | |
| Exacerbation of chronic bronchitis | |
| Recurrent bronchitis | |
| Chronic bronchitis | |
| Chronic obstructive pulmonary diseases | |
| Chronical bronchitis | |
| Chronic bronchitis of smokers | |
| Chronic spastic bronchitis | |
| J45 Asthma | Exercise asthma |
| Asthmatic conditions | |
| Bronchial asthma | |
| Mild bronchial asthma | |
| Bronchial asthma with difficulty in sputum discharge | |
| Severe bronchial asthma | |
| Bronchial asthma of physical exertion | |
| Hypersecretory asthma | |
| Hormone-dependent form of bronchial asthma | |
| Cough with bronchial asthma | |
| Relief of asthma attacks in bronchial asthma | |
| Non-allergic bronchial asthma | |
| Nocturnal asthma | |
| Nocturnal asthma attacks | |
| Exacerbation of bronchial asthma | |
| Attack of bronchial asthma | |
| Endogenous forms of asthma |
Analogs of the drug flixotide are presented, in accordance with medical terminology, called “synonyms” - drugs that are interchangeable in their effects on the body, containing one or more identical active ingredients. When selecting synonyms, consider not only their cost, but also the country of production and the reputation of the manufacturer.
Description of the drug
Flixotide- Fluticasone propionate belongs to the group of topical corticosteroids and, when inhaled in recommended doses, has a pronounced anti-inflammatory and antiallergic 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 COPD, the effectiveness of inhaled fluticasone propionate (when used in combination with long-acting bronchodilators) on lung function has been 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 tableted corticosteroids and an increase in the quality of life of patients compared with placebo .
At therapeutic doses, the effect on the hypothalamic-pituitary-adrenal axis is insignificant, and this effect is not considered clinically significant.
The therapeutic effect after inhaled use of 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.
List of analogues
Note! The list contains synonyms for Flixotide that have a similar composition, so you can choose a replacement yourself, taking into account the form and dose of the medicine prescribed by your doctor. Give preference to manufacturers from the USA, Japan, Western Europe, as well as well-known companies from Eastern Europe: KRKA, Gedeon Richter, Actavis, Egis, Lek, Hexal, Teva, Zentiva.
| Release form(by popularity) | price, rub. |
| Flixotide | |
| Aerosol 50 mcg 120 doses (GlaxoSmithKline Pharmaceuticals (Poland) | 630.20 |
| Aerosol 125 mcg 60 doses (GlaxoSmithKline Pharmaceuticals (Poland) | 927.90 |
| Aerosol 250 µg 60 doses (GlaxoSmithKline Pharmaceuticals (Poland) | 1321.10 |
| Cutivate | |
| Cream 15g (GlaxoSmithKline Pharmaceuticals (Poland) | 319.50 |
| Ointment 15g (GlaxoSmithKline Pharmaceuticals (Poland) | 327.50 |
| Nazarel | |
| Nasal spray 50 mcg 120 doses (Ivex Pharmaceuticals s.r.o. (Czech Republic) | 367.50 |
| Sinoflurin | |
| Flixonase | |
| 50mcg/dose 120doses nasal spray (Glaxo Wellcome S.A. (Spain) | 791.10 |
| Nasal aerosol 50 mcg 120 doses (GlaxoSmithKline Pharmaceuticals (Poland) | 811.60 |
| Fluticasone* | |
| Fluticasone propionate | |
Reviews
Below are the results of surveys of site visitors about the drug flixotide. They reflect the personal feelings of the respondents and cannot be used as an official recommendation for treatment with this drug. We strongly recommend that you consult a qualified healthcare professional to determine a personalized course of treatment.Visitor survey results
Three visitors reported effectiveness
Four visitors reported frequency of intake per day
How often should I take Flixotide?Most respondents most often take this drug 2 times a day. The report shows how often other survey participants take this drug.
Visitor start date report
Visitor report on reception time
Information has not yet been provided24 visitors reported the patient's age
Visitor reviews
There are no reviews |
Official instructions for use
There are contraindications! Read the instructions before useNazarel
NazarelRegistration number:
LSR-005468/08-150708Tradename: NAZAREL
International nonproprietary name:
FlixotideChemical name: 6a,9-Difluoro-17-[[(fluoromethyl)sulfanyl]carbonyl]-11 b-hydroxy-16a-methyl-3-oxoandrosta-1,4-dien-17a-yl propionate
Dosage form:
dosed nasal sprayCompound:
Each dose contains:
active substance: fluticasone propionate 50 mcg;
Excipients: polysorbate-80, microcrystalline cellulose + sodium carmellose (dispersed cellulose), dextrose, benzalkonium chloride (50% solution), phenylethanol, water.
Description:
White or almost white opaque, homogeneous suspension placed in a dark glass bottle (type 1) with a dosing device and a protective cap for 60, 120, 150 doses, containing 50 mcg of fluticasone propiont per dose.
Pharmacotherapeutic group:
glucocorticosteroid for local use.ATX code:
Pharmacological properties
PharmacodynamicsGlucocorticosteroid drug (GCS) for local use. In recommended doses it has a pronounced anti-inflammatory, anti-edematous and anti-allergic effect. The anti-inflammatory effect is realized as a result of the interaction of the drug with glucocorticosteroid receptors. Suppresses the proliferation of mast cells, eosinophils, lymphocytes, macrophages, neutrophils, reduces the production and release of inflammatory mediators and other biologically active substances (including histamine, prostaglandins, leukotrienes, cytokines) during the early and late phases of the allergic reaction. The antiallergic effect appears within 2-4 hours after the first use. Reduces nasal itching, sneezing, runny nose, nasal congestion, discomfort in the sinuses and pressure around the nose and eyes. Relieves eye symptoms associated with allergic rhinitis. The effect of the drug lasts for 24 hours after a single use. When used in therapeutic doses, Flixotide does not exhibit systemic effects and has virtually no effect on the hypothalamic-pituitary-adrenal system.
Pharmacokinetics
Absorption:
After intranasal administration of fluticasone (200 mcg/day), the maximum concentration in the blood plasma in most patients is below the detection level (Flixotide in a stable state has a significant volume of distribution - about 318 l. Plasma protein binding is 91%.
Metabolism:
Has a “first pass” effect through the liver. Metabolized in the liver with the participation of the CYP3A4 isoenzyme of the cytochrome P450 system with the formation of an inactive carboxyl metabolite. Removal:
The half-life (T1/2) is 3 hours. It is excreted mainly through the intestines. Renal clearance of fluticasone is less than 0.2%, renal clearance of the metabolite containing a carboxyl group is less than 5%.
Indications for use
Contraindications
CAREFULLY
Pregnancy and lactation
Not recommended for use during pregnancy. If necessary, the expected benefit of therapy for the mother and the potential risk to the fetus should be taken into account.The passage of fluticasone into breast milk is unlikely. However, it is recommended to stop breastfeeding while using the drug.
Directions for use and doses
Intranasally.Adults and children 12 years and older: 2 doses (100 mcg) in each nasal passage 1 time per day, preferably in the morning. In some cases, it is necessary to administer 2 doses into each nasal passage 2 times a day (maximum daily dose 400 mcg). After achieving a therapeutic effect, a maintenance dose of 50 mcg per day can be administered into each nasal passage (100 mcg). The maximum daily dose should not exceed 400 mcg (4 doses in each nasal passage).
Elderly patients no dose adjustment required. Children aged 4 to 12 years: one dose (50 mcg) once a day in each nasal passage, preferably in the morning. The maximum daily dose should not exceed 200 mcg in each nasal passage. It is necessary to use the minimum dosage that ensures effective relief of symptoms.
To achieve the full therapeutic effect, the drug should be used regularly.
INSTRUCTIONS FOR USE
The nasal spray bottle is equipped with a protective cap that protects the tip from dust and contamination.
When using for the first time, you need to prepare the bottle: press the dispenser 6 times. The spray mechanism is unlocked. If you have not used the drug for more than one week, you should prepare the bottle again and unlock the spray mechanism. Next you need:
Next, inject the drug into the other nasal passage in the same way. After use, blot the tip with a clean napkin or handkerchief and close it with the cap. The sprayer should be washed at least once a week. To do this, remove the tip, rinse it in warm water, dry it and then carefully install it in the upper part of the bottle. Put on the protective cap. If the tip hole becomes clogged, the tip should be removed and left in warm water for a while. Then rinse under running water, dry and put back on the bottle. Do not clean the hole with a pin or other sharp objects.
Use for no more than 3 months after the first use of the spray.
Side effects
Local reactions. Headaches, dryness and irritation of the nasopharynx, unpleasant taste and smell, burning, nasal congestion, nosebleeds are often observed; very rarely, perforation of the nasal septum (usually in patients who have previously undergone surgery in the nasal cavity).Allergic reactions. Possible skin rash, very rarely anaphylactic reactions and bronchospasm, angioedema (mainly swelling of the face, mouth and pharynx).
With long-term use in high doses, concomitant or previous use of systemic glucocorticosteroids, in rare cases, decreased function of the adrenal cortex, osteoporosis, growth retardation in children, cataracts, and increased intraocular pressure are observed.
Overdose
No symptoms of acute or chronic overdose have been recorded. When intranasally administered to volunteers 2 mg of fluticasone 2 times a day for 7 days, no effect on the hypothalamic-pituitary-adrenal system was found.Interaction with other drugs
Interaction with other drugs is unlikely, since fluticasone plasma concentrations are very low when administered intranasally. When used simultaneously with strong inhibitors of the CYP3A4 isoenzyme of the cytochrome P450 system (ritonavir), the systemic effect of fluticasone may be enhanced and side effects may develop (Cushing's syndrome, suppression of adrenal function). When used simultaneously with other inhibitors of the cytochrome P450 system (erythromycin, ketoconazole), a slight increase in the concentration of fluticasone in the blood is observed, which has virtually no effect on cortisol levels.special instructions
Combined use with inhibitors of the CYP3A4 isoenzyme of the cytochrome P450 system (ritonavir, ketonazole) requires careful monitoring of the patient's condition, since these drugs can cause an increase in the concentration of fluticasone in plasma.Systemic effects of nasal corticosteroids may occur, especially if they are prescribed for a long period of time and in large doses. Therefore, with long-term use of the drug, regular monitoring of the function of the adrenal cortex is necessary. Since nasal glucocorticosteroids, even when used in permitted doses, can cause a slowdown in the growth of children during long-term therapy, it is necessary to regularly monitor the child’s growth and promptly adjust the dose of the drug.
In the treatment of seasonal allergic rhinitis, Nazarel is quite effective, however, in the case of particularly high concentrations of allergens in the air in the summer, additional treatment may be required.
Release form
Nasal spray dosed 50 mcg/dose.60, 120 or 150 doses in a dark glass bottle (type 1) with a dosing device and a protective cap. Each bottle, along with instructions for use, is placed in a cardboard box.
Storage conditions
At a temperature not exceeding 25° C. Keep out of the reach of children!Best before date
3 years.Do not use after the expiration date indicated on the package!
Vacation conditions
On prescription.Manufacturer
Ivax Pharmaceuticals s.r.o., Czech Republic Opava-Komarov, Ostravska 29, 74770 IVAX Pharmaceuticals s.r.o., Czech Republic, Opava-Komarov, Ostravska 29, 747 70Address for receiving complaints:
119049, Moscow, st. Shabolovka, 10, building 2, Concord Business Center
The information on the page was verified by physician-therapist E.I. Vasilyeva.
