Seretide aerosol 25mcg 50mcg 120dose
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Active ingredients
Salmeterol + Fluticasone
Release form
Spray
Composition
Active ingredient: salmeterol 25 mcg, fluticasone 50 mcg Concentration of the active substance (mcg): 75 mcg
Pharmacological effect
Mechanism of action Seretide is a combination drug that contains salmeterol and fluticasone propionate, which have different mechanisms of action. Salmeterol prevents the occurrence of symptoms of bronchospasm, fluticasone propionate improves pulmonary function and prevents exacerbation of the disease. Due to a more convenient dosing regimen, Seretide may be an alternative for patients who simultaneously receive a β2-adrenoreceptor agonist and inhaled GCS from different inhalers. Salmeterol is a selective long-acting (up to 12 h) β2-adrenoreceptor agonist, which has a long side chain, which binds to the outer domain of the receptor. The pharmacological properties of salmeterol provide more effective protection against histamine-induced bronchoconstriction and more prolonged bronchodilation (prolonged not more than 12 hours) than short-acting β2-adrenoreceptor agonists. In vitro studies have shown that salmeterol is a potent inhibitor of mast cell mediators such as histamine, leukotrienes and prostaglandin D2 from the human lung, and has a prolonged period of action. Salmeterol inhibits early and late phases of response to inhaled allergens. Inhibition of the late phase of the response persists for more than 30 hours after taking a single dose, while the bronchodilating effect is already absent. A single administration of salmeterol reduces the hyper-reactivity of the bronchial tree. This suggests that in addition to the bronchodilator activity, salmeterol has an additional effect that is not associated with the expansion of the bronchi, the clinical significance of which has not been fully established. This mechanism of action differs from the anti-inflammatory effect of GCS. Fluticasone propionate belongs to the GCS group for topical use and, when inhaled in recommended doses, has a pronounced anti-inflammatory and antiallergic effect in the lungs, which reduces the clinical symptoms and decreases the frequency of exacerbations of asthma.Fluticasone propionate does not cause undesirable effects that are observed with systemic corticosteroids. With prolonged use of inhaled fluticasone propionate, the daily secretion of adrenal cortex hormones remains within the normal range in both adults and children, even when used at the maximum recommended doses. After the transfer of patients receiving other inhaled corticosteroids, the admission of fluticasone propionate to the daily secretion of adrenal cortex hormones gradually improves, despite the previous and current periodic use of oral steroids. This indicates restoration of adrenal function in the background of inhaled fluticasone propionate. With long-term use of fluticasone propionate, the reserve function of the adrenal cortex also remains within the normal range, as evidenced by the normal increase in cortisol production in response to appropriate stimulation (it must be taken into account that the residual decrease in adrenal reserve caused by previous therapy may persist for a long time).
Pharmacokinetics
There is no evidence that, with co-administration of inhalation, salmeterol and fluticasone propionate affect each other’s pharmacokinetics, and therefore the pharmacokinetic characteristics of each component of Seretide can be considered separately. A study conducted with 15 healthy volunteers who also received salmeterol (inhalation administration 50 mcg 2 times / day) and CYP3A4 isoenzyme inhibitor - ketoconazole (oral administration of 400 mg 1 time / day) for 7 days, showed a significant increase in late Plasma salmeterol counts (Cmax increase 1.4 times and AUC 15 times). There was no increase in salmeterol accumulation when receiving repeated doses. In three patients, treatment was canceled due to prolongation of the QTc interval or rapid heartbeat with sinus tachycardia. In the remaining 12 patients, the simultaneous use of salmeterol and ketoconazole did not have a clinically significant effect on heart rate, blood potassium level, or QTc interval duration (see sections With caution, Special instructions and precautions for use, Interaction with other drugs). Absorption Salmeterol acts locally in the lung tissues, so its content in the blood plasma is not an indicator of therapeutic effects.The data on its pharmacokinetics are very limited due to technical problems: during inhalation at therapeutic doses, its Cmax in plasma is extremely low (about 200 pg / ml and lower). After regular inhalations with salmeterol, hydroxynaphthoic acid can be detected in blood, the Css of which is about 100 ng / ml. These concentrations are 1000 times lower than the Css observed in toxicity studies. No adverse effects were observed with prolonged regular use of the drug (for more than 12 months) in patients with airway obstruction. Fluticasone propionate: the absolute bioavailability of inhaled fluticasone propionate in healthy people varies depending on the inhaler used, with the introduction of a combination of salmeterol and fluticasone propionate using metered aerosol for inhalation, it is 5.3%. Patients with asthma and COPD have lower plasma levels of fluticasone propionate. Systemic absorption occurs predominantly through the lungs. At first, it is faster, but then its speed slows down. A part of the inhalation dose may be swallowed, but this part makes a minimal contribution to systemic absorption due to the low solubility of fluticasone propionate in water and because of its presystemic metabolism; GIT bioavailability is less than 1%. As the inhalation dose increases, a linear increase in plasma concentration of fluticasone propionate is observed. Distribution There is no data on the distribution of salmeterol. Fluticasone propionate has a large Vd in the equilibrium state (about 300 l) and has a relatively high degree of binding to plasma proteins (91%). MetabolismResults of the study In vitro showed that salmeterol is extensively metabolized by the cytochrome P450 system CYP3A4 isoenzyme to α-hydroxysalmeterol by aliphatic oxidation. In a study with repeated dosing of salmeterol and erythromycin in healthy volunteers, there were no clinically significant changes in pharmacodynamic effects when taking 500 mg of erythromycin 3 times / day. However, a study of the interaction of salmeterol and ketoconazole showed a significant increase in the concentration of salmeterol in the blood plasma (seesections Special instructions and precautions for use, Interaction with other drugs). Fluticasone propionate is rapidly eliminated from the blood, mainly as a result of metabolism under the action of the cytochrome P450 isoenzyme CYP3A4 to an inactive carboxyl metabolite. Care must be taken with the simultaneous use of known inhibitors of CYP3A4 and fluticasone propionate, since in such situations it is possible to increase the content of the latter in plasma. Output There is no data on the elimination of salmeterol. The distribution of fluticasone propionate is characterized by rapid plasma clearance (1150 ml / min) and final T1 / 2, equal to about 8 hours. Renal clearance of unchanged fluticasone propionate is negligible (less than 0.2%), less than 5% of the dose is excreted as a metabolite with urine.
Indications
The drug is intended for the treatment of bronchial asthma in patients who have been shown combination therapy with beta2-adrenergic long-acting and inhaled corticosteroids: - in patients with insufficient disease control against the background of continuous monotherapy with inhaled corticosteroids with occasional use of short-acting beta2-adrenomimetica - in patients with adequate control diseases during therapy with inhaled corticosteroids and long-acting beta2-adrenergic mimic; - as starting maintenance therapy in patients with persian isting asthma (daily occurrence of symptoms, daily use of funds for rapid relief of symptoms) with indications for the appointment of the GCS to achieve control of the disease. Supportive therapy for COPD and a FEV1 value less than 60% of proper values (before inhalation of a bronchodilator) and repeated exacerbations in history , in which the symptoms of the disease are pronounced, despite regular therapy with bronchodilators.
Contraindications
- Children under 4 years of age - hypersensitivity to the preparata.S Precautions should be prescribed the drug for pulmonary tuberculosis, fungal, viral or bacterial infections of the respiratory system, thyrotoxicosis, pheochromocytoma, diabetes, uncontrolled hypokalemia, idiopathic hypertrophic subaortic stenosis, uncontrolled hypertension , arrhythmias, prolongation of the QT interval on ECG, IHD, hypoxia of various genesis, cataract, glaucoma, hypothyroidism, osteoporosis, pregnancy, in the period of lacquer tation.
Precautionary measures
With caution As with all other inhalation drugs containing GCS, Seretide should be used with caution in patients with acute or latent pulmonary tuberculosis. Seretide should be administered with caution when thyrotoxicosis. Seretide should be used with caution in case of fungal, viral or bacterial respiratory infections .When taking any drugs of the sympathomimetic group, especially when therapeutic doses are exceeded, the development of such cardiovascular events as an increase in isstolic blood pressure and heart rate. For this reason, the drug Seretide should be used with caution in patients with cardiovascular diseases, including arrhythmias such as supraventricular tachycardia and premature beats, ventricular premature beats, atrial fibrillation. All sympathomimetic drugs in dosages exceeding therapeutic may cause a transient decrease in serum potassium. Therefore, the drug Seretide should be used with caution in patients with hypokalemia. Any inhalation GCS can cause systemic effects, especially with long-term use in high doses. Therefore, the drug should be used with caution in glaucoma, cataracts, osteoporosis (see section Special instructions and precautions for use). There are very rare reports of an increase in blood glucose, therefore, patients with diabetes should use Seretide with caution (see section Side effect).
Use during pregnancy and lactation
Fertility There are no data on the effect on fertility in humans. In animal studies, fluticasone propionate or salmeterol xinafoate had no effect on the fertility of males or females. Pregnancy Data on the use of the drug in pregnant women is limited. Use during pregnancy is permissible only if the potential benefit to the mother outweighs the possible risk to the fetus. According to the results of a retrospective study, there is no increased risk of serious congenital malformations (GPR) after exposure to fluticasone propionate during the first trimester of pregnancy compared to other inhaled corticosteroids. When conducting reproductive toxicity studies in animals with the introduction of both each component of the drug separately, and their combinations,The effect on the fetus of excessive systemic concentrations of active beta2-adrenergic and GCS has been revealed. Extensive clinical experience with this class of drugs suggests that using therapeutic doses, the effects described are not clinically significant. Breast-feeding period: Salmeterol and fluticasone propionate concentration in plasma after inhalation of the drug in therapeutic doses are extremely low, so their concentration in breast milk should be equally low. This is confirmed by studies on animals in whose milk low concentrations of the drug were determined. Associated data on breast milk of women are not. The use of the drug during breastfeeding is permissible only if the potential benefit to the mother outweighs the possible risk to the baby.
Dosage and administration
Seretide is intended only for inhalation. To obtain an optimal effect, the drug should be used regularly, even in the absence of clinical symptoms of bronchial asthma and COPD. The doctor sets the course of treatment and dose change individually. The patient should prescribe the drug in a dosage form that contains a dose of fluticasone propionate corresponding to severity of the disease. The recommended dose for adults and children aged 12 years and older - 2 inhalations (25 mcg salmeterol and 50 mcg fluticasone propionate) 2 times / day, or 2 inhalation (25 µg salmeterol and 125 µg fluticasone propionate) 2 times / day, or 2 inhalations (25 µg salmeterol and 250 µg fluticasone propionate) 2 times / day. For children aged 4 years and older, 2 inhalations are recommended (25 µg salmeterol and 50 µg of fluticasone propionate) 2 times / day. The dose of Seretide should be reduced to the minimum effective dose. If symptom control is provided by 2 Seretide inhalations per day, the minimum effective dose may be 1 inhalation per day. For adults with COPD, the maximum recommended dose is 2 inhalations (25 µg salmeterol and 250 µg fluticasone propionate) 2 times / day. Elderly patients and Patients with impaired liver or kidney function do not need a dose reduction. Method of administration and dose Before using the inhaler for the first time or if the inhaler has not been used for a week or longer, remove the cap from the mouthpiece by slightly squeezing the cap ok sides, shake the inhaler well and release one jet in the air to make sure it rabotaet.Ispolzovanie ingalyatora1.Remove the cap from the mouthpiece, slightly squeezing the cap from the sides, and inspect the mouthpiece inside and outside to make sure that it is clean. Shake the inhaler well. Hold the inhaler between the index finger and thumb in a vertical position, bottom up, with the thumb should be located on the base under the mouthpiece. Make the maximum exhalation, put the mouthpiece in the mouth between the teeth and clasp it with your lips, without clenching your teeth. At the moment of inhalation through the mouth, they press on the upper part of the inhaler to release the dose of Seretide, while continuing to take a deep breath. After holding the breath, remove the mouthpiece from the mouth and remove the finger from the top of the inhaler. Continue to hold your breath for as long as possible. To receive the second dose, holding the inhaler in a vertical position, wait about 30 seconds and then repeat stages 2-6.8. The mouthpiece is tightly closed with a protective cap. The preparation can also be applied through a spacer (for example, Volumatics). It should be borne in mind that stages 4, 5 and 6 should be carried out slowly, observing all requirements. Inhale as slowly as possible, immediately before pressing the inhaler valve. The first few times it is recommended to practice in front of a mirror. If there is a fog coming out of the upper part of the inhaler or from the corners of the mouth, then you should start all over again from stage 2. The patient should follow the doctor's recommendations on using the inhaler, if difficulties arise, consult a doctor. Adults should help young children use the inhaler. It should wait until the child makes the exhalation and put the inhaler into action at the moment of inhalation. It is recommended to practice using the inhaler with the child. Older children and adults with weak hands should hold the inhaler with both hands. In this case, both index fingers should be located on the upper part of the inhaler, and both thumbs - on the base below the mouthpiece. For children, the drug is injected with an inhaler through a spacer with a face mask (for example, Bebihaler). Inhaler cleaning The inhaler must be cleaned at least once a week. Remove the protective cap from the mouthpiece. Do not remove the metal can from the plastic housing.Use a dry cloth or cotton swab to wipe the mouthpiece inside and out and the plastic cover on the outside. Close the mouthpiece with a protective cap. Do not immerse the metal can in water.
Side effects
Since Seretide contains salmeterol and fluticasone propionate, its side effects are characteristic of each of these drugs. Their simultaneous use does not cause additional side effects. Seretide may cause paradoxical bronchospasm. In clinical studies using Seretide, sometimes bruises were reported, as well as frequent cases of pneumonia (in patients with COPD). The following data on undesirable effects were obtained in the post-marketing surveillance SeretidIt has sometimes been reported about hypersensitivity reactions, including manifested as skin reactions, angioedema (mainly edema of the face and oropharynx), respiratory disorders (shortness of breath and / or bronchospasm), and in very rare cases - anaphylactic reactions. Anxiety, behavioral disorders (including hyperactivity and irritability mainly in children), sleep disturbances, hyperglycemia. Salmeterol On the side of the cardiovascular system: heartbeat, headache (usually transient, diminished as therapy with salmeterol continues); in predisposed patients, cardiac rhythm disturbances are possible (including atrial fibrillation, supraventricular tachycardia, extrasystole). On the part of the digestive system: rarely - abdominal pain, nausea, vomiting; in some cases - a violation of taste, irritation of the mucous membranes of the oropharynx. Allergic reactions: rash, angioedema, local edema. Others: tremor, hypokalemia (usually transient, decrease with the continuation of salmeterol therapy); rarely - arthralgia, nervousness; very rarely - hyperglycemia; in some cases, painful muscle spasms. Fluticasone propionate On the part of the respiratory system: hoarseness, candidiasis of the mouth and pharynx. Allergic reactions: skin manifestations, angioedema (mainly of the face and oropharynx), respiratory symptoms (shortness of breath and / or bronchospasm), anaphylactic reactions. System reactions: it is theoretically possible to develop systemic reactions,including Cushing's syndrome, cushingoid symptoms, adrenal suppression, growth retardation in children and adolescents, reduced bone mineral density, cataracts and glaucoma. Anxiety, sleep disorders and behavioral disorders, including hyperactivity and irritability (mostly in children) ) hyperglycemia.
Overdose
It is not recommended to administer the drug in doses exceeding those indicated in the section Dosing regimen. It is very important to regularly review the patient dosing regimen and reduce the dose to the lowest recommended dose, providing effective control over the disease. Symptoms Expected symptoms and signs of overdose of salmeterol are typical for excessive beta2-adrenergic stimulation, and include tremor, headache, tachycardia, increased systolic blood pressure and Hypopotassemia. Acute overdose of fluticasone propionate with inhalation may provoke temporary suppression of the hypothalamic-pituitary-adrenal th system. Usually, this does not require any emergency measures, since the normal function of the adrenal glands is restored within a few days. When taking the drug in doses higher than those recommended for a long period of time, it is possible to significantly suppress the function of the adrenal cortex. Rare cases of acute adrenal crisis, which occurred mainly in children who received doses higher than recommended for a long time (several months or years), are described. Acute adrenal crisis is manifested by hypoglycemia, accompanied by confusion and / or convulsions. The situations that can serve as triggering factors for acute adrenal crisis include trauma, surgery, infection, or any rapid dose reduction of inhaled fluticasone propionate, which is part of Seretide. Treatment There is no specific treatment for overdose of salmeterol and fluticasone propionate. In case of overdose, maintenance therapy should be carried out and the patient’s condition monitored. In chronic overdose, it is recommended to monitor the reserve function of the adrenal cortex.
Interaction with other drugs
Because of the danger of developing bronchospasm, the use of selective and non-selective beta-adrenergic blockers should be avoided, unless they are urgently needed by the patient. In normal situations, inhalation of fluticasone propionate is accompanied by low plasma concentrations due to intensive metabolism during the first passage and high systemic clearance under the influence of the CYP3A4 isoenzyme of the cytochrome P450 system in the intestine and liver. Because of this, clinically significant interactions involving fluticasone propionate are unlikely. A study of drug interactions has shown that ritonavir, a highly active inhibitor of the CYP3A4 isoenzyme, can cause a sharp increase in plasma concentrations of fluticasone propionate, resulting in significantly reduced serum cortisol concentrations. During the period of post-registration observations, there were reports of clinically significant drug interactions in patients who simultaneously received fluticasone propionate (intranasal or inhalation) and ritonavir. These interactions caused systemic side effects inherent in SCS, such as Cushing's syndrome and adrenal suppression. With this in mind, the simultaneous use of fluticasone propionate and ritonavir should be avoided, except when the potential benefit to the patient exceeds the risk of systemic side effects of GCS. Studies have shown that other CYP3A4 isoenzyme inhibitors cause a negligible (erythromycin) and a slight (ketoconazole) increase in fluticasone plasma propionate, in which the concentration of serum cortisol is practically not reduced. Despite this, caution is advised when using fluticasone propionate and strong CYP3A4 inhibitors (such as ketoconazole) at the same time, since such combinations do not exclude the likelihood of increasing plasma concentration of fluticasone propionate, which can potentially increase the systemic effects of fluticasone propionate. it was found that using ketoconazole as a concomitant systemic therapy significantly increases the salme concentration Erol in plasma (Cmax increase by 1.4 times and AUC is 15 times).This can lead to a prolongation of the QTc interval. Caution should be exercised in the joint appointment of strong inhibitors of CYP3A4 (for example, ketoconazole) and salmeterol. Xanthine derivatives, GCS and diuretics increase the risk of hypokalemia (especially in patients with exacerbation of asthma, with hypoxia). MAO inhibitors and tricyclic antidepressants may increase on the part of the cardiovascular system. The drug Seretide is compatible with cromoglicic acid.
special instructions
The drug Seretide is not intended to relieve acute symptoms, since in such cases a fast and short-acting inhaled bronchodilator should be used (for example, salbutamol). Patients should be informed that they always have on hand a drug to relieve acute symptoms. The combination of salmeterol and fluticasone propionate can be used for initial maintenance therapy in patients with persistent bronchial asthma (the daily occurrence of symptoms or the daily use of remedies for treating attacks) when indicated to the purpose of the GCS and in the determination of their approximate dosage. More frequent use of short-acting bronchodilators to facilitate Impediments indicate a deterioration in the control of the disease, and in such situations the patient must consult a doctor. A sudden and increasing deterioration in the control of the bronchospastic syndrome poses a potential threat to life, and in such situations the patient must also consult a doctor. The physician should consider the possibility of prescribing a higher dose of corticosteroids. If the used dose of Seretide does not provide adequate control of the disease, the patient should also consult a doctor. Patients with asthma should not abruptly stop treatment with Seretide due to the risk of exacerbation, the dose should be reduced gradually under medical supervision. In patients with COPD, drug withdrawal may be accompanied by symptoms of decompensation and requires medical supervision. In clinical studies, data have been obtained on the increase in the frequency of pneumonia in patients with COPD who receive Seretide (see the Adverse Effects section).Doctors should be aware of the possibility of developing pneumonia in COPD, since the clinical picture of pneumonia and exacerbations of COPD are often similar. Any inhaled GCS can cause systemic effects, especially with long-term use in high doses; however, the likelihood of such symptoms is much lower than in the treatment of oral GCS (see section Overdose). Possible systemic reactions include Cushing syndrome, cushingoid features, adrenal suppression, growth retardation in children and adolescents, reduced bone mineral density, cataracts and glaucoma. Therefore, in the treatment of bronchial asthma, it is important to reduce the dose to the lowest dose, which provides effective control over the disease. In emergency and planned situations that can cause stress, it is always necessary to remember about the possibility of suppression of the adrenal glands and be ready to use GCS (see Overdose). During resuscitation or surgical interventions, determination of the degree of adrenal insufficiency is required. It is recommended to regularly measure the growth of children who receive long-term therapy and Inhalation GCS. Due to the possibility of suppression of the adrenal glands, patients transferred from oral GCS to inhaled fluticasone propionate should be treated with extreme caution and their adrenal cortical function should be regularly monitored. Such patients should be discontinued carry a special patient card containing an indication of the possible need for additional administration of GCS in stressful situations. Since asthma, hypoxia, it is necessary to control the concentration of K + ions in plasma. There are very rare reports of an increase in blood glucose levels, and this should be remembered when prescribing a combination of salmeterol and fluticasone propionate for diabetes mellitus (see section Side Effects. During the post-registration period, there were reports of clinically significant drug interactions between fluticasone propionate and ritonavir, leading to systemic effects of GCS, including Cushing's syndrome and adrenal suppression.Therefore, it is recommended to avoid the combined use of fluticasone propionate and ritonavir, except when the potential benefit to the patient exceeds the risk associated with the systemic effects of GCS (see section Drug Interactions). A clinical study of the safety of salmeterol added to the asthma therapy compared with placebo, it was shown that the incidence of deaths due to bronchial asthma was significantly higher in the salmeterol group. When taking salmeterol compared with placebo, the risk of serious adverse reactions from the respiratory system or death in patients of African-American origin, presumably, is higher than in other patients. The significance of pharmacogenetic factors or other causes is unknown. The effect associated with the use of SCS on the risk of death in patients with asthma has not been studied in this study. As with other inhalants, Seretide may cause paradoxical bronchospasm, manifested by an increase in shortness of breath immediately after administration. In this case, you should immediately apply a fast and short-range inhalation bronchodilator, discontinue Seretide, examine the patient and start alternative therapy, if necessary (see the Side Effects section). There are reports of adverse reactions related to the pharmacological action of beta-antagonists such like tremor, subjective feeling of heartbeat and headache. However, these reactions are short-lived, and their severity decreases with regular therapy (see section Side Effects). Effect on ability to drive vehicles and control mechanisms In clinical studies, no data on the effect of the drug on the ability to drive vehicles and other mechanisms, but should consider side effects that may cause the drug.