Flixotide aerosol 125mcg dose 60dose
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Active ingredients
Fluticasone
Release form
Spray
Composition
Active ingredient: Fluticasone Concentration of active ingredient (mcg): 125 mcg
Pharmacological effect
Fluticasone propionate belongs to the group of local 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 obstruction of the respiratory tract (bronchial asthma, chronic bronchitis, emphysema). inhibits the proliferation of mast cells, eosinophils, lymphocytes, macrophages, neutrophils, reduces the production and release of media ditch of inflammation and other biologically active substances - histamine, prostaglandins, leukotrienes, cytokines. When COPD confirmed the effectiveness of inhaled fluticasone propionate (when used in combination with long-acting bronchodilators) for lung function, which is characterized by a decrease in the severity of symptoms of the disease, frequency and severity of exacerbations reducing the need for additional courses of preformed GCS and improving the quality of life of patients compared with placebo. In therapeutic In these doses, the effect on the hypothalamic-pituitary-adrenal system is insignificant, and this effect is not considered clinically significant. The therapeutic effect after inhaled fluticasone starts within 24 hours, reaches a maximum within 1-2 weeks or more after the start of treatment and lasts for several days after cancellation.
Pharmacokinetics
Absorption The absolute bioavailability of fluticasone propionate when used as a metered-dose aerosol for inhalation in healthy volunteers is approximately 10.9%. In patients with chronic obstructive pulmonary disease (COPD) or bronchial asthma, the systemic exposure of the drug is lower than in healthy volunteers. Systemic absorption occurs mainly in the lungs, while initially rapid absorption with subsequent slowdown. Part of the inhaled dose may be swallowed, but its systemic effect is minimal due to the poor solubility of the drug in water and intensive metabolism during the first passage through the liver (the bioavailability of fluticasone propionate when ingested is less than 1%).There is a direct relationship between the value of the inhaled dose and the systemic effect of fluticasone propionate. Distribution Plasma protein binding is moderately high, 91%. Fluticone propionate has a large Vd in the equilibrium state - about 300 l. Metabolism metabolism to an inactive carboxylic acid metabolite under the action of CYP3A4 isoenzyme of the cytochrome P450 system. Since there is a possibility of increasing the systemic exposure of fluticasone propionate, caution should be exercised when used together with known inhibitors of CYP3A4. Introduction Fluticonone propionate pharmacokinetics is characterized by a high plasma clearance (1150 ml / min). T1 / 2 is about 8 hours. Renal clearance is less than 0.2%. With urine less than 5% is excreted as a metabolite.
Indications
- basic anti-inflammatory therapy of bronchial asthma (including with severe disease and dependence on systemic corticosteroids) in adults and children 1 year and older; - treatment of chronic obstructive pulmonary disease in adults.
Contraindications
- acute bronchospasm; - asthmatic status (as a primary means); - bronchitis of non-asthmatic nature; - children's age up to 1 year; - hypersensitivity to the drug. Precautions should be prescribed in case of liver cirrhosis, glaucoma, hypothyroidism, systemic infections (bacterial, fungal, parasitic, viral), osteoporosis, pulmonary tuberculosis, pregnancy and lactation.
Precautionary measures
The drug should be used with caution in case of liver cirrhosis, glaucoma, hypothyroidism, systemic infections (bacterial, fungal, parasitic, viral), osteoporosis, pulmonary tuberculosis, pregnancy and lactation.
Use during pregnancy and lactation
Fertility There are no data on the effect on fertility in humans. In animal studies, no effect of fluticasone propionate on the fertility of males or females was detected. Pregnancy Data on the use of the drug in pregnant women is limited. The use of fluticasone propionate during pregnancy is permissible only in the caseif the potential benefit to the mother outweighs the possible risk to the fetus. Results of a retrospective epidemiological study did not reveal an increased risk of serious congenital malformations (CAD) after fluticasone propionate compared with other inhaled corticosteroids during the first trimester of pregnancy. at values of systemic exposure exceeding those observed when using the recommended therapeutic inhalation to , only the effects characteristic of GCS are observed. Breastfeeding Period The isolation of fluticasone propionate with breast milk in humans has not been studied. When, after n / a administration of the drug, laboratory concentrations of lactation were measured in the blood plasma, fluticasone propionate was also found in breast milk. However, after inhaled fluticasone propionate at the recommended doses, its plasma concentrations in patients are likely to be low. Use of the drug during breastfeeding is permissible only if the potential benefit to the mother exceeds the potential risk to the baby.
Dosage and administration
Flixotide is intended for inhalation use only. Flixotide is a means of preventive therapy, the drug must be used regularly, even in the absence of symptoms of the disease. With the basic anti-inflammatory therapy of asthma, therapeutic effect of Flixotide occurs 4-7 days after the start of treatment. In patients who have not previously used inhaled corticosteroids, improvement may be noted as early as 24 h after the start of the drug. For adults and adolescents over the age of 16, the initial dose for bronchial asthma of the mild course is 100-250 mcg 2 times / day, moderate severity is 250-500 mcg 2 times / day, severe course is 500-1000 mcg 2 times / days Then, depending on the patient's individual response to treatment, the initial dose can be increased until a clinical effect appears or reduced to the minimum effective dose. In children older than 4 years, it is recommended to use an aerosol containing 50 mcg of fluticasone propionate in 1 dose. It is recommended to appoint 50-100 mcg 2 times / 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 a clinical effect appears or reduced to the minimum effective dose. Children aged 1 to 4 years are advised to prescribe 100 μg 2 times / day. Younger children require higher doses of Flixotide compared with older children due to reduced intake of the drug during inhalation (a smaller lumen of the bronchi, the use of a spacer, intensive nasal breathing in young children). The drug is administered using an inhaler through a spacer with a face mask (for example, Bebihaler). Flixotide dosed aerosol is especially indicated for young children with severe bronchial asthma. For the treatment of chronic obstructive pulmonary disease, adults are recommended to prescribe 500 μg 2 times / day. Patients with impaired liver or kidney function, as well as the elderly are not required to adjust the dose.
Side effects
Local reactions: possible candidiasis of the mucous membrane of the oral cavity and pharynx, hoarseness, paradoxical bronchospasm. Allergic reactions: in some cases - skin rash, angioedema, dyspnea or bronchospasm, anaphylactic reactions. Systemic reactions: reduced function of the adrenal cortex, osteoporosis, growth retardation in children, cataracts, increased intraocular pressure, glaucoma, Cushing's syndrome, cushingoid symptoms. There are also very rare reports of hyperglycemia. There are possible: mental disorders (anxiety, sleep disorders, changes in behavior, including hyperactivity and irritability / mainly in children /); often - bruising, pneumonia in patients with COPD.
Overdose
Symptoms: An acute overdose of the drug can lead to a temporary inhibition of the function of the hypothalamic-pituitary-adrenal system, which usually does not require emergency therapy, since the function of the adrenal cortex is restored within a few days. With prolonged doses of the drug in excess of the recommended, possibly significant suppression of the function of the adrenal cortex. Very rare reports have been received of the development of acute adrenal crisis in children who received a dose of fluticasone propionate 1000 mcg / day and higher for several months or years. In such patients, hypoglycemia, depression of consciousness and convulsions were noted.Acute adrenal crisis may develop on the background of the following conditions: severe trauma, surgery, infection, a sharp decrease in the dose of fluticasone propionate. Treatment: it is necessary to monitor patients receiving high doses, and a gradual decrease in the dose of fluticasone propionate.
Interaction with other drugs
During the inhalation route of administration of fluticasone propionate, its plasma concentrations are very low due to the active first-pass metabolism and high systemic clearance in the intestine and liver, with the participation of cytochrome P450 3A4 enzymes. Thus, clinically significant drug interactions of fluticasone propionate are unlikely. A study of drug interactions in healthy volunteers showed that ritonavir (a highly active inhibitor of cytochrome P450 3A4) can significantly increase the concentration of fluticasone propionate in plasma, which accordingly leads to a decrease in serum cortisol concentration. In the framework of post-registration use, clinically significant drug interactions were observed in patients receiving fluticasone propionate intranasally or inhalation with ritonavir, which led to systemic effects of corticosteroids. including Cushing's syndrome and adrenal suppression. Thus, the concomitant use of ritonavir and fluticasone propionate should be avoided, unless the potential benefit for the patient outweighs the possible risk of systemic side effects of GCS. Studies of other cytochrome P450 3A4 inhibitors showed a slight (erythromycin) and small (ketoconazole) increase in systemic exposure fluticasone propionate without any noticeable decrease in serum cortisol concentration. However, care must be taken with the concomitant prescription of potent inhibitors of cytochrome P450 3A4 (for example, ketoconazole), since there is a possibility of increasing the concentration of fluticasone propionate in plasma.
special instructions
An increase in the frequency of use of short-acting inhaled beta2-agonists to control symptoms of bronchial asthma indicates a worsening of control over the course of the disease.In this case, the patient's treatment plan requires revision. The sudden and progressive deterioration of control over the course of bronchial asthma is 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. It is not recommended to stop treatment with Flixotide. Special care should be taken when treating inhaled GCS patients with active or inactive forms of pulmonary tuberculosis. It is recommended to check whether the patient is able to use the inhaler correctly, so that make sure that the actuation of the inhaler is carried out synchronously with the inhale to ensure optimal delivery of the active substance to the lungs. Mr. applying any inhaled corticosteroids, especially in high doses, may experience systemic effects, but the probability of their development is much lower than when receiving corticosteroids inside. Possible systemic effects include Cushing's syndrome, cushing-like symptoms, suppression of adrenal function, decrease in bone mineral density, growth retardation in children and adolescents, cataracts, glaucoma. Therefore, it is especially important that when the therapeutic effect is achieved, the dose of inhaled GCS is reduced to the minimum effective dose that allows you to control the course of the disease. It is recommended to regularly monitor the growth of children receiving inhaled GCS for a long time. Always consider the probability of adrenal insufficiency in emergency situations ( including surgery), as well as with planned intervention, which can cause stress, especially in patients s taking high doses of corticosteroids for a long time. At the same time, it is necessary to decide on the need for additional prescription of GCS depending on the clinical situation (see section Overdose). In connection with possible adrenal insufficiency, special care should be taken and to regularly monitor indicators of the function of the adrenal cortex when fluticone is treated propionate in the form of an aerosol for inhalation.The abolition of systemic corticosteroids against the background of fluticasone propionate in the form of an aerosol for inhalation should be carried out gradually, and patients should carry a card indicating that they may need additional intake of GCS during stress. When transferring patients from receiving systemic corticosteroids for inhalation therapy concomitant allergic diseases (for example, allergic rhinitis, eczema), which were previously suppressed by systemic drugs. In such situations, it is recommended to carry out symptomatic treatment with antihistamines and / or topical preparations, including GCS for local use. As with other inhalation therapy, there is a possibility of the development of paradoxical bronchospasm with an immediate increase in shortness of breath after inhalation. For relief of this attack, immediate use of inhaled bronchodilator of quick and short action is necessary. Fluticasone propionate inhalation should be stopped immediately, then the patient’s condition should be evaluated and alternative therapy should be prescribed if necessary. As with most inhalants in aerosol packs, the effect decreases when the can is cooled. There are very rare reports of an increase in blood glucose concentration, and this It should be remembered when prescribing fluticasone propionate to patients with diabetes mellitus. An increase in cases of pneumonia in patients with COPD who received fluticasone propionate in doses was recorded. 500 micrograms. One should be aware of the possibility of pneumonia in these patients, since the clinical signs of pneumonia and exacerbation of the underlying disease can often coincide. Impact on the ability to drive vehicles and control mechanisms The effect of fluticasone propionate on the ability to drive and work with mechanisms that require increased concentration of attention is unlikely.