Active substanceSalmeterol + FluticasoneSalmeterol + Fluticasone
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  • Dosage form: & nbspAerosol for inhalation dosed.
    Composition:
    Aerosol for inhalation dosage 1 dose
    (in terms of salmethrol 25 μg)
    Salmeterol xinafoate 36.3 μg
    Fluticasone propionate 50 μg
    125 μg
    250 mcg
    Excipients:
    1,1,1,2-tetrafluoroethane (HFA-134a) 73.099 mg (for a dosage of 25 + 50 μg)
    73,024 mg (for a dosage of 25 + 125 μg)
    72,900 mg (for a dosage of 25 + 250 μg)
    Polyethylene glycol 1000 0.01464 mg
    Description:A white or almost white suspension placed under pressure into an aerosol aluminum can with a metering valve.
    Pharmacotherapeutic group:Bronchodilator (beta2-adrenomimetic selective + glucocorticosteroid local).
    ATX: & nbsp

    R.03.A.K   Sympathomimetics in combination with corticosteroids or other drugs, excluding anticholinergic drugs

    R.03.A.K.06   Salmeterol and fluticasone

    Pharmacodynamics:Salmecort is a combined bronchodilator (contains salmeterol and fluticasone propionate). Salmeterol - selective agonist of beta2-adrenoreceptors of long-term action (not less than 12 hours). The salmeterol molecule has a long side chain that binds to the outer domain of the receptor. Due to these pharmacological properties salmeterol is more effective for the prevention of histamine-induced bronchospasm and causes longer bronchodilation in comparison with the usual short-acting beta2-receptor agonists. Effective and prolonged inhibition of the release in the lung tissues of mediators of mast cells, such as histamine, leukotrienes and PgD2. Suppresses early and late stage of allergic reaction; after the introduction of a single dose, the hyperreactivity of the bronchi decreases, the inhibition of the late stage persists for more than 30 hours after a single dose, when the bronchodilator effect is no longer present.
    Fluticasone propionate-glucocorticosteroid (GCS) topical. When inhaled in the 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. With prolonged use of inhalation fluticasone propionate at the maximum doses, the daily and reserve secretion of adrenal cortex hormones remains within the normal range in adults and children. The residual reduction in the reserve function of the adrenal gland can persist for a long time after the therapy.
    Pharmacokinetics:
    There is no evidence that joint inhalation administration of salmeterol and fluticasone propionate affects the pharmacokinetics of each of these substances. Salmeterol: after inhalation at therapeutic doses, very low concentrations of the drug in the blood plasma are created (200 pg / ml or less). With regular use of inhaled salmeterol in the systemic blood stream, hydroxynaphthoic acid is determined in concentrations up to 100 ng / ml.
    Fluticasone propionate: after inhalation, the relative bioavailability is 10 to 30%, depending on the drug delivery system. Systemic absorption occurs predominantly in the lungs.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 when "first passed" through the liver. The bioavailability of fluticasone upon ingestion is less than 1%. There is a direct relationship between the magnitude of the inhaled dose and the systemic effect of fluticasone, the volume of distribution is about 300 liters. Metabolized in the liver to an inactive metabolite involving the CYP3A4 cytochrome P450 system. Less than 5% of the metabolite is excreted in the urine. Plasma clearance is 1.15 l / min. Half-life T1/2 about 8 hours.

    Indications:
    The drug Salmecort is designed for regular treatment of bronchial asthma in patients who are shown combined therapy with long-acting beta2-adrenomimetic and inhaled glucocorticosteroid:
    in patients with insufficient control of the disease against a background of continuous monotherapy with inhaled glucocorticosteroids with the periodic use of short-acting beta2-adrenomimetics;
    in patients with adequate disease control on the background of therapy with inhaled glucocorticosteroid and long-acting beta2-adrenomimetic;
    as a starting maintenance therapy in patients with persistent asthma (daily occurrence of symptoms, daily use of funds for rapid relief of symptoms) in the presence of indications for the appointment of glucocorticosteroids to achieve control of the disease;
    supportive therapy in patients with COPD who have a forced expiratory volume (FEV1) value of <60% of the required values ​​(prior to bronchodilator inhalation) with repeated exacerbations in the anamnesis, and whose severe symptoms persist despite regular therapy with bronchodilators.
    Contraindications:
    - hypersensitivity to one or more of the components of the drug,
    - children's age (up to 4 years).
    Carefully:
    Like all other inhaled preparations containing glucocorticosteroids, Salmecort should be used with caution in patients with acute or latent pulmonary tuberculosis, fungal, viral or bacterial infections of the respiratory system, with thyrotoxicosis.
    When taking any drugs group of sympathomimetics, especially when the therapeutic dose is exceeded, it is possible to develop cardiovascular events such as an increase in systolic blood pressure and heart rate.For this reason, Salmecort should be administered with caution to patients suffering from cardiovascular diseases, including arrhythmias such as supranventicular tachycardia and extrasystole, ventricular extrasystole, atrial fibrillation.
    All simpatomimeticheskie drugs in dosages exceeding the therapeutic, can cause tranzitonos lower serum potassium levels, so the drug Salmecort should be used with caution in patients with hypokalemia. Any inhaled GCS can cause systemic effects, especially with prolonged use in high doses, so the drug should be used with caution in glaucoma, cataracts, and osteoporosis (see section "Special instructions and precautions for use").
    There are very few reports of an increase in blood glucose, so patients with diabetes should use Salmecort with caution (see section "Side effect").
    Pregnancy and lactation:
    Pregnant women and women during lactation should be prescribed a drug only in the event that,if the expected benefit for the mother exceeds any possible risk to the fetus or child.
    There is insufficient data on the use of salmeterol and fluticasone propionate in pregnancy and lactation.
    Pregnancy
    Excessive systemic concentration of active beta2-adrenomimetic and GCS affects the fetus.
    The extensive clinical experience of using this class of drugs indicates that when using therapeutic doses, the described effects are not clinically significant. Salmeterol and fluticasone propionate do not possess genotoxicity.
    Lactation
    The concentration of salmeterol and fluticasone propionate in blood plasma after inhaling the drug in therapeutic doses is extremely low, so their concentration in breast milk should be the same low. There is no data on the concentration of salmeterol and fluticasone propionate in breast milk of women during lactation.
    Dosing and Administration:
    Inhalation. Only for inhalation.
    The patient should be informed about that. that to obtain the optimal effect the drug should be used regularly, even in the absence of clinical symptoms of bronchial asthma and COPD.
    The physician should regularly evaluate the effectiveness of the patient's treatment.
    Determining the duration of the course of therapy and changing the dose of the drug is possible only on the advice of a doctor.
    The initial dose of the drug is determined based on the dose of fluticasone, which is recommended for the treatment of a disease of a given severity. Then the initial dose should be gradually reduced to the lowest effective dose. During treatment should be observed regularly with a doctor in order to select the optimal dose. The patient should not independently change the dose prescribed by the doctor.
    Bronchial asthma
    If taking Salmecort twice a day provides control over the symptoms, within the dose reduction to minimally effective it is possible to reduce the frequency of taking the drug to 1 time per day.
    The patient should be prescribed a form of Salmecort, which contains a dose of fluticasone propionate, corresponding to the severity of his disease. If therapy with inhaled glucocorticosteroids does not provide adequate control over the disease, then their replacement with Salmecort at a dose therapeutically equivalent to the dose administered by GCS can improve the control of asthma.In patients who can monitor the course of asthma exclusively with the help of inhaled GCS. their replacement with Salmecort can help reduce the dose of GCS necessary to control the course of asthma.
    Recommended doses:
    Adults and children aged 12 years and over:
    two inhalations (25 μg salmeterol and 50 μg fluticasone propionate) 2 times a day, or
    two inhalations (25 μg salmeterol and 125 μg fluticasone propionate) 2 times a day, or
    two inhalations (25 μg salmeterol and 250 μg fluticasone propionate) 2 times a day.
    Children aged 4 years and over:
    two inhalations (25 μg salmeterol and 50 μg fluticasone propionate) 2 times a day.
    All patients taking the drug as maintenance therapy should undergo a doctor's consultation 6-12 weeks after the initial admission.
    Chronic obstructive pulmonary disease
    For adult patients, the maximum recommended dose is 2 inhalations (25 μg salmeterol and 250 μg fluticasone propionate) 2 times a day.
    Special patient groups
    There is no need to reduce the dose of Salmecort in elderly patients, as well as in patients with impaired renal or hepatic function.

    INSTRUCTIONS FOR USING THE INHIBITOR
    Before each use, the inhaler should be shaken.
    Checking the inhaler
    1. Before the first application or if the inhaler has not been used for 2 days or more, it is necessary to check the inhaler. To do this, press 4 (inhalation) into the air (see Figure 1).

    Use of an inhaler
    2. Remove the protective cover from the mouthpiece. In doing so, the mouthpiece must remain tightly attached to the vial (inhaler) (see Figure 2); If the inhaler was stored without a protective cover, it is necessary to check the mouthpiece for contamination.


    3. Take the inhaler in the hands of the mouthpiece downwards so that one finger is on the bottom of the inhaler and the other finger or two on the upper end of the inhaler. Exhale and place the mouthpiece between the teeth (see Figure 3).

    4. Tightly grasp the mouthpiece with your lips and slightly tilt your head back. Slowly start inhaling and simultaneously press the bottom of the can. Continue inhaling to the end (see Figure 4).


    5. Remove the inhaler from the mouth and hold your breath for 10 seconds or as long as it is comfortable. Slowly exhale (see Figure 5).



    Note:
    After each inhalation, rinse mouth and / or throat with water. This will help reduce the dryness associated with taking the drug.The interval between inhalations should be at least 1 minute. When re-inhalation is repeated, repeat steps 2-5.

    After use, it is necessary to close the mouthpiece with a protective cap (see Figure 6).


    The first few inhalations are recommended to be carried out, controlling yourself in front of the mirror. If you see a "leakage" of the drug through the mouth or out of the hole between the mouthpiece and the body of the inhaler, this indicates an incorrect inhalation technique (see Figure 7).

    Inhalations to young children should be carried out under the supervision of an adult (see Figure 8).

    Older children and adults with weak arms should hold the inhaler with both hands. Thus both index fingers should settle down on the top part of an inhaler, and both greater fingers - on the basis below a mouthpiece.


    Cleaning the inhaler
    Cleaning of the inhaler should be carried out at least once a day.
    1. Remove the metal can from the body of the inhaler. Remove the spray tip;
    2. Wash the mouthpiece and body of the inhaler under warm running water;
    3. Wipe thoroughly with a dry cloth or cotton swab. Do not overheat;
    4. Collect the inhaler.

    After using all the doses indicated on the package, the metal canister should be discarded.


    Side effects:
    All the undesirable reactions presented below are characteristic for the active substances - salmeterol and fluticasone propionate alone. The safety profile of Salmecort does not differ from the profile of undesirable reactions of its active ingredients.
    The undesirable reactions presented below are listed in accordance with the damage to organs and organ systems and frequency of occurrence. Frequency of occurrence is defined as follows: very often (>1/10), often (>1/100 and <1/10), infrequently (>1/1000 and <1/100), rarely (>1/10000 and <1/1000), very rarely (<1/10000, including individual cases).
    Infections and infestations:
    often: candidiasis of the mouth and pharynx, pneumonia (in patients with COPD).
    Immune system disorders:
    infrequently: skin reactions of hypersensitivity;
    rarely: anaphylactic reactions, angioedema, mainly edema of the face and oropharynx, bronchospasm;
    Disorders from the endocrine system:
    Possible systemic effects include (see the sections "With caution" and "Special instructions")
    rarely: Cushing's syndrome, Cushingoid symptoms, suppression of adrenal function, growth retardation in children and adolescents, reduction of bone mineral density;
    Disorders from the organs of vision:
    infrequently: cataract; rarely: glaucoma;
    Disorders from the metabolism and nutrition:
    infrequently: hyperglycemia;
    very rarely: hypokalemia:
    Disorders of the psyche:
    infrequently: anxiety, sleep disturbances;
    rarely: changes in behavior, including increased activity and irritability (especially in children);
    Impaired nervous system:
    very often: headache (see section "Special instructions"); infrequently: tremor (see section "Special instructions");
    Heart Disease:
    infrequent: palpitations (see "With caution" and "Special instructions"), tachycardia, atrial fibrillation;
    rarely: arrhythmia, including ventricular extrasystole, supraventricular tachycardia, extrasystole;
    Disturbances from the respiratory system, chest and mediastinal organs:
    often: hoarseness of voice and / or dysphonia; infrequently: irritation of pharynx;
    rarely: paradoxical bronchospasm (see section "Special instructions");
    Disturbances from the skin and subcutaneous tissues:
    infrequently: bruising;
    Disorders from the musculoskeletal system and connective tissues:
    often: muscle spasms, arthralgia;
    Disorders from the gastrointestinal tract:
    very rarely: indigestion, nausea.
    Children and teens
    It is theoretically possible to develop systemic reactions involving Cushing syndrome, Cushingoid symptoms, suppression of adrenal function, growth retardation in children and adolescents. Very rarely there may be anxiety, sleep disorders and behavioral disorders, including hyperactivity and irritability.
    Overdose:
    It is not recommended to administer the drug at doses exceeding those specified in the section "Method of administration and dose". It is very important to regularly review the patient's dosage regimen and reduce the dose to the lowest recommended dose, which provides effective control of the disease ("Mode of administration and dose").
    Symptoms
    The expected symptoms and signs of an overdose of salmeterol are typical for excessive beta2-adrenergic stimulation, and include tremor, headache, tachycardia, increased systolic blood pressure, and hypokalemia.Acute overdose of fluticasone propionate with inhalation can provoke a temporary suppression of the hypothalamic-pituitary-adrenal system. Usually this does not require taking any emergency measures, since the normal function of the adrenal glands is restored within a few days. When taking the drug in doses above the recommended for a long period of time, a significant suppression of the function of the adrenal cortex is possible. Rare cases of acute adrenal crisis, which occurred mainly in children who received doses of the drug above recommended for a long time (several months or years), are described. Acute adrenaline crisis is manifested by hypoglycemia, accompanied by confusion and / or convulsions. Situations that can serve as triggers for an acute adrenal crisis include trauma, surgery, infection, or any rapid reduction in the dose of inhaled fluticasone propionate, which is part of the Salmecort.
    Treatment
    There is no specific treatment for an overdose of salmeterol and fluticasone propionate.In case of an overdose, supportive therapy should be followed and the patient's condition monitored.
    When applying the drug in doses exceeding the instructions specified for a long time, suppression of the function of the adrenal cortex may be observed.
    Interaction:
    Because of the risk of developing bronchospasm, selective and nonselective beta-blockers should be avoided, unless they are extremely necessary for the patient.
    Salmeterol
    Combined use with ketoconazole should be avoided if the benefit from the application does not exceed the potential risk of systemic adverse reactions in the treatment with salmeterol. There is a similar risk of interaction with other strong inhibitors of CYP3A4 (itraconazole, telithromycin, ritonavir).
    Fluticasone propionate
    In usual situations, inhalations of fluticasone propionate are accompanied by low plasma concentrations due to intensive metabolism in the "first" passage and high systemic clearance under the influence of the CYP3A4 isoenzyme of the cytochrome P-450 system in the intestine and liver. Due to this, clinically significant interactions involving fluticasone propionate are unlikely.
    Ritonavir, as a highly active inhibitor of the enzyme CYP3A4, can cause a dramatic increase in the concentration of fluticasone propionate in plasma, resulting in a significant decrease in serum cortisol concentrations.
    Joint application with ritanovir causes such side effects as Cushing's syndrome and suppression of adrenal function. Given this, simultaneous use of fluticasone propionate and ritanavir should be avoided, unless the potential benefit to the patient exceeds the risk of systemic side effects of GCS.
    Other inhibitors of the isoenzyme CYP3A4 cause negligible (erythromycin) and insignificant (ketoconazole) an increase in the content of fluticasone propionate in plasma, in which the concentrations of serum cortisol are practically not reduced. Despite this, caution should be exercised while using strong inhibitors of CYP3A4 (for example, ketoconazole), since such combinations do not exclude an increase in the concentration of fluticasone propionate in plasma.
    The derivatives of xanthine, GCS (glucocorticosteroids) and diuretics increase the risk of hypokalemia (especially in patients with exacerbation of bronchial asthma, hypoxia).Monoamine oxidase inhibitors and tricyclic antidepressants increase the risk of developing side effects from the cardiovascular system. Compatible with cromoglicic acid.
    Special instructions:
    Salmecort is not intended to alleviate acute symptoms, because in such cases, a rapid and short-acting inhaled bronchodilator should be used (for example, salbutamol). Patients should be informed that they always have at hand a drug to stop acute symptoms. The combination of salmeterol and fluticasone propionate can be used for initial maintenance therapy in patients with persistent asthma (daily occurrence of symptoms or daily use of an agent for arresting seizures), if there is evidence of SCS administration and when determining their approximate dosage.
    The more frequent use of short-acting bronchodilators to relieve symptoms indicates a worsening of control over the disease, and in such situations the patient should consult a doctor.
    The sudden and increasing deterioration in the control of bronchial asthma poses a potential threat to life, and in such situations, the patient should also consult a doctor.The doctor should consider the possibility of a higher dose of GCS. If the dose of Salmecort used does not provide adequate control over the disease, the patient should also consult a doctor.
    Patients with asthma can not dramatically reduce the treatment with Salmecort because of the danger of aggravation, the dose of the drug should be reduced gradually under the supervision of a doctor. In patients with COPD, the withdrawal of the drug may be accompanied by symptoms of decompensation and requires the supervision of a physician.
    In patients with COPD receiving Salmecort, an increase in the incidence of pneumonia is possible (see section "Side effect"). Doctors should be aware of the possibility of developing pneumonia in patients with COPD, as the clinical picture of exacerbation of COPD and pneumonia is often similar.
    Any inhaled GCS can cause systemic reactions, especially with prolonged use in high doses; but the likelihood of such symptoms is much lower than when treated with oral GCS (see the section "Overdose"). Possible systemic reactions include Cushing's syndrome, cushingoid features, suppression of adrenal function, growth retardation in children and adolescents, reduction of bone mineral density, cataract and glaucoma.
    Therefore, in the treatment of 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 the possibility of suppressing the function of the adrenal gland and be ready for use by the GCS (see section "Overdose").
    When carrying out resuscitation measures or surgical interventions, it is required to determine the degree of adrenal insufficiency. It is recommended to regularly measure the growth of children who receive prolonged therapy with inhaled glucocorticosteroids.
    Because of the possibility of adrenal suppression, patients transferred from oral corticosteroids to inhalation of fluticasone propionate therapy should be treated with extreme caution and regular monitoring of their function of the adrenal cortex. When transferring patients from taking systemic GCS to inhalation therapy, allergic reactions (for example, allergic rhinitis, eczema), which were suppressed by systemic GCS, may appear. In such situations it is recommended to carry out symptomatic treatment with antihistamines and / or topical preparations, including SCS for topical application.
    After initiation of treatment with inhaled fluticasone propionate, systemic GCS should be discontinued gradually, and such patients should carry a special patient card containing an indication of the possible need for additional administration of SCS in stressful situations.
    In patients with exacerbation of bronchial asthma, hypoxia, it is necessary to monitor the concentration of potassium K + ions in the plasma.
    There are very rare reports of an increase in blood glucose levels, and this should be borne in mind when appointing a combination of salmeterol with fluticasone propionate in patients with diabetes mellitus (see section "Side effect").
    Because of the potential for systemic effects of GCS, including Cushing's syndrome and suppression of adrenal function, fluticasone propionate and ritonavir should be avoided, unless the potential benefit to the patient exceeds the risk associated with systemic SCS effects (see "Interaction with other medicinal products ").
    When taking salmeterol, the risk of serious unwanted reactions from the respiratory system or death in patients of African-American origin is presumably higher,than in other patients. The importance of pharmacogenetic factors or other causes is unknown. The effect of concomitant use of inhaled glucocorticosteroids on the risk of lethal outcomes in patients with asthma has not been studied.
    Like other inhaled drugs, Salmecort can cause a paradoxical bronchospasm, manifested by the increase in dyspnea immediately after use. In this case, rapid and short-acting inhalation bronchodilator should be immediately applied, Salmecort should be canceled and, if necessary, alternative therapy should be started (see "Side effect" section).
    There may be adverse reactions associated with the pharmacological action of beta2-antagonists, such as tremor, subjective palpitation and headache. However, these reactions are of a short-term nature, and their severity decreases with regular therapy (see section "Side effect").
    Effect on the ability to drive transp. cf. and fur:In clinical trials, no evidence of the effect of the drug on the ability to drive vehicles and other mechanisms has been obtained, but side effects that the drug may cause should be considered.
    Form release / dosage:
    The aerosol for inhalation is dosed with 25 μg + 50 μg / dose, 25 μg + 125 μg / dose, 25 μg + 250 μg / dose.
    Packaging:For 120 doses in an aerosol canister with a dosing valve and a mouthpiece with a protective cap. A balloon with the instruction but application is placed in a cardboard pack.
    Storage conditions:At a temperature of no higher than 25 ° C, do not freeze. Keep out of the reach of children.
    Shelf life:2 years. Do not use the drug after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-002852
    Date of registration:06.02.2015
    The owner of the registration certificate:Glenmark Pharmaceuticals Co., Ltd.Glenmark Pharmaceuticals Co., Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspGLENMARK PHARMACEUTICALS LTD. GLENMARK PHARMACEUTICALS LTD. India
    Information update date: & nbsp16.08.2015
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