

Combined bronchodilator (beta2-adrenergic selective + local glucocorticosteroid).
Saltikazon® - native is a combined preparation containing 2 active ingredients: salmeterol xinafoate and fluticasone propionate, which have different mechanisms of action. Salmeterol prevents the occurrence of bronchospasm symptoms, fluticasone improves pulmonary function and prevents exacerbation. Saltikazon®- A native, due to a convenient dosing regimen, can be an alternative for patients who simultaneously receive a beta2-adrenoreceptor agonist and an inhaled glucocorticosteroid (GCS) using different inhalers.
Salmeterol is a selective, long-acting (up to 12 hours) beta2-adrenoreceptor agonist, having in its structure 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 beta2-adrenoreceptor agonists.
Salmeterol is a potent and long-acting inhibitor of mast cell mediators, such as histamine, leukotrienes and prostaglandin D2, from human lung tissue.
Salmeterol inhibits the early and late phases of the 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 bronchial tree hyperreactivity.
This suggests that in addition to the bronchodilator activity, salmeterol has an additional effect not related to 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 belongs to the group of corticosteroids for topical administration 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 asthma. Fluticasone does not cause adverse effects that are observed with systemic glucocorticosteroids.
With prolonged use of inhaled fluticasone, the daily secretion of adrenal cortex hormones remains within the normal range, both in adults and in children, even when using the maximum recommended doses. After transferring patients receiving other inhaled corticosteroids, the fluticone daily secretion of adrenal cortex hormones gradually improves, despite the previous and current intermittent use of oral steroids. This indicates the restoration of adrenal function in the background of inhaled fluticasone. With prolonged use of fluticasone, the reserve function of the adrenal cortex also remains within the normal range, as evidenced by a normal increase in cortisol production in response to appropriate stimulation (it must be borne in mind that the residual decrease in adrenal reserve caused by prior therapy may persist for a long time).
PharmacokineticsSaltikazon® - the native is intended for regular treatment of bronchial asthma, if combination therapy with long-acting beta2-adrenomimetic and inhaled glucocorticosteroid is indicated:
• in patients with insufficient disease control against the background of continuous monotherapy with inhaled glucocorticosteroids with occasional use of beta2-adrenergic short-acting;
• in patients with adequate disease control during therapy with an inhaled glucocorticosteroid and long-acting beta2-adrenergic mimic;
• as a starting maintenance therapy in patients with persistent bronchial asthma in the presence of indications for the appointment of glucocorticosteroids to achieve control of the disease.
Saltikazon® - the native is intended for maintenance therapy in COPD in patients with a forced expiratory volume (FEV1) <60% of the proper values (before inhalation of the bronchodilator) and repeated exacerbations in history, in which the symptoms of the disease persist despite regular bronchodilator therapy.
The composition of one capsule: |
|
Active substance: |
50 mcg + 500 mcg |
Salmeterol Xinafoat |
72.5 mcg |
(in terms of salmeterol) |
50 mcg |
Fluticasone Propionate Excipients: |
500 mcg |
Sodium benzoate |
2.0 mg |
Lactose monohydrate |
up to 12.0 mg |
Capsules gelatin capsule body: - Azorubine |
0,0016 % |
- brilliant black |
0,0958 % |
- patented blue |
0,1643 % |
- quinoline yellow |
1,1496 % |
- titanium dioxide |
1,3333 % |
- gelatin |
up to 100% |
capsule cap: - indigotin - |
- |
- iron oxide yellow - |
- |
- Azorubine - |
0,0016 % |
- brilliant black - |
0,0958 % |
- patented blue - |
0,1642 % |
- quinoline yellow - |
1,1496 % |
- titanium dioxide 2% |
1,3333 % |
- gelatin to 100% |
up to 100% |
Salmeterol, Fluticasone is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Salticazone native | Nativa | Russia | powder |
Seretide | GlaxoSmithKline | France, France, Poland | inhalation spray |
Seretide Multidisk | GlaxoSmithKline | UK, UK, France | powder |
Seretide Multidisk | GlaxoSmithKline | UK | powder |
No customer reviews for the moment.
Seretide is intended for inhalation only.
To obtain the 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 be prescribed the drug in a dosage form that contains a dose of fluticasone propionate, corresponding to the severity of the disease.
The recommended doses for adults and children aged 12 years and older are 2 inhalations (25 mcg salmeterol and 50 mcg fluticasone propionate) 2 times / day, or 2 inhalations (25 mcg salmeterol and 125 mcg fluticasone propionate) 2 times / day, or 2 inhalation (25 mcg salmeterol and 250 mcg fluticasone propionate) 2 times / day.
For children aged 4 years and older, 2 inhalations are recommended (25 mcg salmeterol and 50 mcg fluticasone propionate) 2 times / day.
The dose of Seretide should be reduced to the minimum effective dose.
WithCOPD for adults, the maximum recommended dose is 2 inhalations (25 mcg salmeterol and 250 mcg fluticasone propionate) 2 times / day.
Elderly patients and patients with impaired liver or kidney function dose reduction is not required.
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.
Salmeterol
Since the cardiovascular system: palpitations, headache (as a rule, transient, decrease with the continuation of therapy salmeterol); usually in predisposed patients - cardiac arrhythmias (including atrial fibrillation, supraventricular tachycardia, extrasystole).
From the digestive system: rarely - abdominal pain, nausea, vomiting; in some cases - a violation of taste.
Allergic reactions: rash, angioedema.
Other: tremor, hypokalemia (as a rule, transient, decrease with the continuation of therapy salmeterol); rarely - arthralgia, nervousness, peripheral edema; in some cases - irritation of the mucous membrane of the oropharynx, 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), bronchospasm, anaphylactic reactions.
Systemic reactions: It is theoretically possible to suppress adrenal function, growth retardation in children and adolescents, a decrease in bone mineral density, cataracts and glaucoma.
- children's age up to 4 years;
- Hypersensitivity to the drug.
WITHcaution should be prescribed for the treatment of pulmonary tuberculosis, fungal, viral or bacterial infections of the respiratory system, thyroxemia , glaucoma, hypothyroidism, osteoporosis, pregnancy, in the period of lactation.
The use of selective and non-selective beta-blockers should be avoided, unless it is really necessary and justified.
Even despite the very low concentration of salmeterol in the blood plasma, its interaction with other substrates and inhibitors of the CYP3A4 isoenzyme cannot be ruled out.
When using fluticasone propionate in the form of inhalations, its plasma concentration is low due to intensive metabolism during the "first pass" through the liver under the influence of the CYP3A4 isoenzyme and high systemic clearance.Due to this, clinically significant interaction with fluticasone propionate is unlikely.
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.
Ritonavir (a highly active inhibitor of the isoenzyme CYP3A4) can cause a significant increase in the concentration of fluticasone propionate in the blood plasma, as a result of which serum cortisol concentrations are significantly reduced. There are reports of clinically significant drug interactions in patients who simultaneously received fluticasone propionate and ritonavir, which was manifested by the development of Itsenko-Cushing's syndrome and adrenal suppression. With this in mind, the simultaneous use of fluticasone propionate and ritonavir should be avoided, except in cases where the potential benefit of combination therapy for the patient exceeds the risk of developing systemic side effects of GCS.
Other inhibitors of the isoenzyme CYP3A4 cause a negligible (erythromycin) and a slight (ketoconazole) increase in the content of fluticasone propionate in the plasma, at which the concentration of serum cortisol remains practically unchanged. Despite this, caution is advised when using fluticasone propionate and strong CYP3A4 inhibitors (for example, ketoconazole) at the same time, since such combinations do not exclude the likelihood of increasing plasma concentrations of fluticasone propionate.
With simultaneous use of Seretide, xanthine derivatives, GCS and diuretics increase the risk of hypokalemia (especially in patients with exacerbation of bronchial asthma, with hypoxia); MAO inhibitors and tricyclic antidepressants increase the risk of cardiovascular side effects.
Seretide is compatible with cromoglicic acid.
During pregnancy and lactation (breastfeeding) Seretide can be prescribed only if the intended benefit to the mother outweighs any possible risk to the fetus or child.
Seretide is intended for long-term treatment of the disease, and not for the relief of seizures. To relieve seizures, patients should be prescribed inhaled short-acting bronchodilators (for example, salbutamol), which patients are advised to always carry with them.
With the development of paradoxical bronchospasm, you should immediately apply a short-acting inhaled bronchodilator, cancel Seretide and begin, if indicated, alternative therapy.
Treatment of bronchial asthma is recommended in stages, controlling the patient's clinical response to treatment and lung function. The patient must be taught to use the inhaler correctly.
The severity and frequency of coarsening of voice and candidiasis can be reduced by rinsing the mouth with water after Seretide inhalation. When candidiasis is prescribed antifungal drugs for local use, continuing therapy with Seretide.
More frequent use of short-acting bronchodilators to relieve symptoms indicates a deterioration in the control of the disease, in such situations the patient should consult a doctor.
A sudden and progressive deterioration in the control of the bronchospastic syndrome represents a potential threat to life. In such situations, the need to control the doctor. If the applied dose of Seretide does not provide adequate control of the disease, then an additional administration of GCS may be required, and if the exacerbation is caused by an infection, then antibiotics are prescribed.
Because of the danger of aggravation, the sudden discontinuation of seretide should be avoided, the dose should be reduced gradually under the supervision of a physician.
When using any inhaled corticosteroids, it is possible to develop systemic effects (suppression of adrenal function, growth retardation in children and adolescents, decrease in bone mineral density, cataracts and glaucoma), especially with long-term use in high doses, but the likelihood of such effects is much lower than with treatment of oral forms of corticosteroids. Given this, the dose of inhaled corticosteroids should be titrated to the minimum, which ensures the maintenance of effective control.
In emergency and planned stressful situations, it is always necessary to remember about the possibility of suppressing the function of the adrenal glands and the emergence of the need to use GCS.
When resuscitation or surgical interventions are performed, determination of the degree of adrenal insufficiency is required.
In some patients, individual sensitivity to GCS for inhalation may be noted.
In connection with possible adrenal insufficiency, special care should be taken and the indicators of the function of the adrenal cortex should be regularly monitored when transferring patients taking GCS orally to fluticone propionate for inhalation. When transferring patients from taking systemic corticosteroids to inhalation therapy, allergic reactions can occur (for example, allergic rhinitis, eczema), which were previously suppressed by systemic corticosteroids. In such situations, it is recommended to carry out symptomatic treatment with antihistamines and / or topical preparations (including GCS for local use).
The abolition of systemic corticosteroids against the background of inhaled fluticasone propionate should be carried out gradually. Patients should carry with them a card indicating that they may need additional administration of GCS in various stressful situations.
Symptoms: tremor, headache and tachycardia caused by the action of salmeterol; temporary suppression of the hypothalamic-pituitary-adrenal system, due to the action of fluticasone.
With prolonged inhalation of Seretide in excessively high doses, a marked inhibition of adrenal function is possible. There are rare reports of acute adrenal crisis, which occurs predominantly in children who receive Seretide in excessively high doses for a long time (several months or years). 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 a rapid decrease in the dose of fluticasone propionate, which is part of Seretide.
Treatment: symptoms caused by the action of salmeterol, should be stopped by the introduction of an antidote - a cardioselective beta-blocker. In those cases when it is necessary to discontinue Seretide due to an overdose of its salmeterol, the patient should be given an appropriate replacement GCS.
Symptoms caused by the action of fluticasone propionate, usually do not require emergency treatment, since in most cases the normal function of the adrenal glands is restored within a few days. In chronic overdose, it is recommended to monitor the reserve function of the adrenal cortex.
To avoid overdose, patients should not take Seretide at doses higher than recommended. It is important to regularly evaluate the effectiveness of therapy and reduce the dose of Seretide to the minimum level that provides effective control of the symptoms of the disease.
Studies and clinical trials of Salmeterol, Fluticasone (Click to expand)