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Seretide, 1 piece, 25 mcg+125 mcg/dose, dosed aerosol for inhalation

Seretide has anti-asthmatic, bronchodilator, anti-inflammatory effects.

Pharmacodynamics The drug Seretide is a combination drug containing salmeterol and fluticasone propionate, which have different mechanisms of action. Salmeterol prevents the occurrence of bronchospasm, fluticasone propionate improves pulmonary function and prevents exacerbations. The drugs may be an alternative for patients who simultaneously receive a β 2 -adrenergic receptor agonist and inhaled corticosteroids.

Salmeterol is a selective, long-acting (up to 12 hours) β 2 -adrenergic receptor agonist, which has a long side chain that binds to the outer domain of the receptor.

The pharmacological properties of salmeterol provide protection against histamine-induced bronchoconstriction and longer bronchodilation (lasting at least 12 hours) than short-acting β2-adrenergic receptor agonists. The onset of the bronchodilator effect is within 10–20 minutes. Salmeterol is a strong and long-acting inhibitor of the release of mast cell mediators such as histamine, LT and PG D2 from human lung tissue.

Salmeterol inhibits the early and late phases of the response to inhaled allergens; the latter lasts more than 30 hours after administration of 1 dose, i.e. at a time when the bronchodilator effect is no longer present. A single administration of salmeterol weakens the hyperreactivity of the bronchial tree. This indicates that salmeterol, in addition to its bronchodilator activity, has an additional effect, the clinical significance of which has not been fully established. This mechanism of action differs from the anti-inflammatory effect of GCS. At therapeutic doses, salmeterol has no effect on CCC.

Fluticasone propionate belongs to the group of corticosteroids for topical use and, when inhaled in recommended doses, has a pronounced anti-inflammatory and antiallergic effect in the lungs, which leads to a decrease in clinical symptoms and a decrease in the frequency of exacerbations of diseases accompanied by airway obstruction. Restores the patient's response to bronchodilators, allowing to reduce the frequency of their use. The effect of fluticasone propionate is not accompanied by adverse reactions characteristic of systemic corticosteroids.

With long-term use of inhaled fluticasone propionate in the maximum recommended doses, the daily secretion of adrenal hormones remains within normal limits in both adults and children. After switching patients receiving other inhaled corticosteroids to fluticasone propionate, the daily secretion of adrenal hormones gradually improves, despite previous and current intermittent use of oral steroids. This indicates restoration of adrenal function with inhaled use of fluticasone propionate. With long-term use of fluticasone propionate, the reserve function of the adrenal cortex also remains within normal limits, 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).

A study conducted among 318 adult patients with persistent bronchial asthma showed that when using a double dose of Seretide and Seretide Multidisc for 14 days (regardless of the dose of the components in the drug), there was a slight increase in the incidence of adverse events associated with the action of β-adrenergic agonists ( tremor - 1 patient (1%), 0 patients - at the usual dose; rapid heartbeat - 6 patients (6%), 1 patient (

Pharmacokinetics When administered together by inhalation, salmeterol and fluticasone propionate do not affect each other's pharmacokinetics, therefore the pharmacokinetic characteristics of each component of Seretide preparations can be considered separately.

Even despite the very low plasma concentrations of salmeterol and fluticasone propionate, interactions with other substrates and inhibitors of the CYP3A4 isoenzyme cannot be excluded.

Salmeterol: acts locally in the lung tissue, so its plasma levels do not correlate with the therapeutic effect. Data on its pharmacokinetics are very limited due to technical problems: when inhaled in therapeutic doses, its Cmax in plasma is extremely low (about 200 pg/ml and below). After repeated inhalations of salmeterol xinafoate, hydroxynaphthoic acid can be detected in the blood, the C ss of which is about 10 pg/ml. These concentrations are 1000 times lower than equilibrium levels observed in toxicity studies.

Fluticasone propionate: The absolute bioavailability of inhaled fluticasone propionate in healthy subjects varies depending on the inhaler used (when using salmeterol/fluticasone propionate using a metered dose inhalation aerosol, it is 5.3% of the nominal dose). In patients with bronchial asthma and COPD, lower plasma concentrations of fluticasone propionate are observed. Systemic absorption occurs primarily through the lungs, and is initially faster but then slows down.

Part of the inhalation dose may be swallowed, but this part makes a minimal contribution to systemic absorption due to the low solubility of the drug in water and due to its first-pass metabolism. Bioavailability from the gastrointestinal tract is less than 1%. As the inhalation dose increases, a linear increase in the plasma concentration of fluticasone propionate is observed. The distribution of fluticasone propionate is characterized by rapid clearance from plasma (1150 ml/min), a large V ss (about 300 l) and a final half-life of approximately 8 hours. Fluticasone propionate has a relatively high degree of binding to plasma proteins (91%). It is rapidly eliminated from the blood, mainly as a result of metabolism under the action of the CYP3A4 isoenzyme to an inactive carboxyl metabolite.

The renal clearance of unchanged fluticasone propionate is negligible (

It is excreted through the gastrointestinal tract, mainly in the form of a hydroxylated metabolite.

Drug interactions Seretide™

Non-selective and selective β2-adrenergic blockers should be avoided in patients with reversible bronchial obstruction, unless absolutely necessary. Under normal conditions, after inhaled use of the drug, low plasma concentrations of fluticasone are achieved due to extensive first-pass metabolism and high systemic clearance of the drug mediated by cytochrome P450 3A4 in the liver and intestines. Therefore, clinically significant interactions due to fluticasone propionate are unlikely. Based on drug interaction studies in healthy volunteers, it has been shown that rinatavir (a strong inhibitor of cytochrome P450 3A4) can significantly increase plasma concentrations of fluticasone propionate, which can lead to a significant decrease in plasma cortisol concentrations. According to post-marketing data from the use of the drug, clinically significant drug interactions were reported in patients who were treated with inhaled or intranasal administration of fluticasone propionate and ritanavir, which was the cause of the systemic effects of GCS, including Cuschiig's syndrome and suppression of adrenal function. Therefore, the simultaneous use of fluticasone propionate and ritanavir should be avoided, unless the benefit of use will outweigh the risk of systemic effects of GCS. Based on studies of other cytochrome P450 3A4 inhibitors, it has been proven that other cytochrome P450 3A4 inhibitors have a very minor (erythromycin) or small (ketoconazole) effect on increasing the systemic concentration of fluticasone propionate in the blood plasma, without leading to a significant decrease in cortisol concentrations. However, strong inhibitors of cytochrome P450 3A4 (for example, ketoconazole) should be used with caution, given the possibility of systemic effects of fluticasone propionate. The combined use of ketoconazole and salmeterol causes a significant increase in the concentration of salmeterol in the blood plasma (maximum plasma concentration 1.4 times and 15 times the AUC), which may cause a prolongation of the QT (see SPECIAL INSTRUCTIONS ).

Side effects of Seretide™

Since Seretide contains salmeterol and fluticasone propionate, adverse reactions of the type and severity that are characteristic of each component can be expected. No additional side effects were noted with the simultaneous use of 2 components of the drug. As with other inhaled drugs, paradoxical bronchospasm may occur with an immediate increase in the severity of shortness of breath after inhalation. If such a condition develops, a rapid and short-acting inhaled bronchodilator should be immediately used. Seretide should be discontinued immediately, the patient examined and, if necessary, alternative therapy prescribed. Data from clinical studies Salmeterol-fluticasone propionate Isolated cases of hematomas have been reported. Commonly reported side effects included hoarseness/dysphonia, throat irritation, headache, oral and throat candidiasis, and palpitations. Patients with COPD may develop pneumonia. Post-licensing data Salmeterol-fluticasone propionate Infrequent skin hypersensitivity reactions have been described. There are isolated reports of hypersensitivity reactions that manifest as angioedema (mainly swelling of the face and oropharynx), respiratory symptoms (shortness of breath and/or bronchospasm) and very rarely anaphylactic reactions. There have been isolated cases of anxiety, sleep disturbances and behavioral changes, including hyperactivity and agitation (mainly in children), as well as isolated cases of hyperglycemia. Salmeterol There are reports of pharmacological side effects of treatment with β2-agonists, such as tremor, palpitations, headache (usually transient, the severity of which decreases with regular use of the drug). In patients with higher sensitivity, cardiac arrhythmia (including atrial fibrillation, supraventricular tachycardia and extrasystole) is noted. Rarely - arthralgia and very rarely - hypersensitivity reactions and anaphylaxis, including edema and angioedema, bronchospasm and anaphylactic shock. There are reports of irritation of the mucous membranes of the mouth and throat. Uncommon: rash; common: muscle spasm. There are isolated reports of the development of hyperglycemia. Fluticasone propionate Some patients experienced hoarseness and candidiasis of the mucous membrane of the mouth and throat. Skin hypersensitivity reactions have been described, in isolated cases - angioedema of the face and oropharynx, the development of respiratory symptoms - shortness of breath and bronchospasm, and extremely rarely - anaphylactic reactions. Rinsing the mouth and throat with water after inhaling the drug can help reduce the incidence of dysphonia and candidiasis. Symptomatic candidiasis can be treated with topical antifungals while continuing to take Seretide. Possible systemic effects include adrenal suppression, Cushing's syndrome, Cushingoid signs, growth retardation in children and adolescents, decreased bone mineralization, cataracts and glaucoma. There are isolated reports of the development of hyperglycemia. There are anecdotal reports of anxiety, sleep disturbances and behavioral disturbances, including hyperactivity and agitation (mainly in children).

Seretide™ overdose, symptoms and treatment

Symptoms of salmeterol overdose that can be expected are typical of excessive β2-adrenergic receptor stimulation and include tremor, headache, tachycardia, increased systolic blood pressure and hypokalemia. Cardioselective beta-adrenergic blockers are used as optimal antidotes, which should be used with caution when treating patients with a history of bronchospasm. If treatment with Seretide must be discontinued due to an overdose of the β2-agonist included in the drug, the patient should be prescribed appropriate corticosteroid replacement therapy. Inhalation of fluticasone propionate in doses higher than recommended may lead to temporary depression of the hypothalamic-pituitary-adrenal axis. This condition does not require immediate attention as adrenal function returns within a few days. However, when doses higher than recommended are used over a long period of time, significant suppression of adrenal function is possible. Cases of acute adrenal crises have been reported rarely, mainly in children receiving higher than recommended doses of the drug over a long period (several months or years). Hypoglycemia may occur, accompanied by impaired consciousness and/or convulsions. Factors that trigger acute adrenal crisis include trauma, surgery, infection, or a sharp reduction in the dose of inhaled fluticasone propionate. Therefore, Seretide should not be used in doses higher than recommended. The dosage regimen should be regularly reviewed and the dose reduced to the minimum level sufficient to effectively control the disease.