Index of drugs

Bronchial asthma. Systematic treatment of bronchial asthma when simultaneous use of long-acting β is recommended₂-mimetic and inhaled corticosteroid: in patients whose asthma symptoms can not be controlled despite using an inhaled corticosteroid and a short-acting β₂-mimetic used temporarily; in patients whose asthma symptoms can be controlled with an inhaled and long-acting β corticosteroid₂agonists. Note: The preparation in the dose: 100 μg + 50 μg is not intended for use in severe asthma in adults and children.Chronic obstructive pulmonary disease (COPD). The 500 μg + 50 μg dose is indicated for the symptomatic treatment of COPD patients with COPD₁ <60% of the amount due (before administration of a bronchodilator), with repeated exacerbations in the past, in which significant symptoms persist despite regular treatment with bronchodilators.

1 dose contains: 100 μg, 250 μg or 500 μg of micronized fluticasone propionate and 50 μg of micronized salmeterol (in the form of salmeterol xinafoate). The preparation contains lactose.

The product contains salmeterol and fluticasone propionate, substances with different mechanisms of action. Salmeterol is a selective, long-acting (12 h) β-agonist₂-renergic, with a long side chain, which is associated with an extra-cardiac site. Fluticasone propionate administered by inhalation at the recommended doses exerts an anti-inflammatory effect in the lungs, which results in a decrease in the severity of symptoms and the frequency of asthma exacerbations. When using fluticasone propionate and salmeterol, good asthma control was achieved faster than with inhaled corticosteroid monotherapy. During the concomitant administration of fluticasone propionate and salmeterol, the pharmacokinetic properties of the individual active substances of the preparation remain unchanged compared to the administration of the active substances separately. The absolute bioavailability of fluticasone propionate after a single inhalation administration in healthy people is approximately 5-11% of the nominal dose, depending on the type of inhaler used. Lower systemic exposure was observed in patients with asthma or COPD. Systemic absorption takes place mainly from the lungs and is initially rapid and then slow. The remainder of the inhaled dose is swallowed and enters the gastrointestinal tract, but the systemic exposure is minimal (<1%). Plasma protein binding is 91%. T_0,5 is about 8 hours. Fluticasone propionate is rapidly removed from the systemic circulation. The main route is metabolism to an inactive carboxylic acid derivative; this reaction is catalyzed by CYP3A4. Less than 5% of the dose is excreted in the urine, mainly in the form of metabolites. Most of the dose is excreted in the faeces as metabolites and unchanged drug. Salmeterol works locally in the lungs.

Hypersensitivity to any active substance or excipient.

The preparation should not be used to treat acute asthma symptoms. Do not start treatment with patients during an exacerbation of asthma or if there is a significant or acute worsening of the course of the disease. If asthma symptoms deteriorate during treatment or are not properly controlled, treatment should be continued and medical advice should be sought. For patients treated for asthma or COPD, additional use of corticosteroids should be considered. The preparation should be used with caution in patients with pulmonary tuberculosis. Due to the risk of arrhythmias and transient decreases in serum potassium (high doses), the preparation should be used with caution in patients with severe cardiovascular disorders including heart rhythm disturbances, diabetes mellitus, hyperthyroidism and untreated hypokalaemia, or patients prone to low concentrations of potassium ions in the serum. There have been very rare cases of increased blood Glucose - this should be taken into account when prescribing to patients with a history of diabetes.If paradoxical bronchoconstriction occurs, the preparation should be immediately discontinued, the condition of the patient should be assessed and other treatment should be necessary. Caution should be exercised when changing the treatment with steroids that are systemically active to treatment with the preparation, especially in patients who are suspected of adrenal insufficiency due to prior systemic steroid treatment. Long-term treatment with high doses of inhaled corticosteroids may cause adrenal suppression and acute adrenal crisis. Situations in which acute adrenal crisis may occur are associated with such conditions as: trauma, surgery, infection or rapid dose reduction. At the time of exposure to stress or prior to planned surgery, additional oral corticosteroids should be considered. In patients who have previously been switched to oral treatment with oral propionate fluticasone propionate, there is a risk of experiencing symptoms of adrenocortical insufficiency for a longer period of time. This risk may also apply to patients who have been given high doses of steroids in the past. The possibility of adrenocortical dysfunction should always be considered in emergency and stress-related situations, and consideration should be given to administering an appropriate complementary dose of corticosteroids. Before the planned surgical procedures, specialist consultations may be necessary to assess the degree of adrenal insufficiency. The concomitant use of fluticasone propionate with ritonavir should be avoided unless the potential benefit to the patient outweighs the risk of systemic adverse reactions of corticosteroids. The concomitant use of other potent CYP3A inhibitors may also increase the risk of systemic side effects. During treatment with the preparation in patients with COPD there is an increased risk of lower respiratory tract infections (especially pneumonia and bronchitis). This is especially true for elderly patients with a low BMI (<25 kg / m²pc.) and patients with very severe disease (FEV₁ <30% of the value due); particular attention should be paid to patients for symptoms of lower respiratory tract infections, because the symptoms of these infections and the exacerbation of COPD often overlap. If pneumonia is diagnosed in a patient with severe COPD, the treatment should be reassessed. In patients with African-American origins treated with salmeterol, there is an increased risk of serious respiratory symptoms or death - if a patient with African or Afrocaranic origin develops asthma symptoms or is not properly controlled during treatment, treatment should be continued and medical advice should be sought . The simultaneous use of salmeterol with ketoconazole or other strong CYP3A4 inhibitors should be avoided, unless the benefits outweigh the potential increased risk of systemic side effects of salmeterol. In children and adolescents under 16 years taking high doses of fluticasone (usually ≥1000 μg / day) there is a special risk of systemic effects (especially when using high doses over a long period). It is recommended that the inhaled corticosteroid be regularly monitored for growth in children during long-term treatment. The dose of inhaled corticosteroid should be reduced to the lowest dose that provides effective control of asthma symptoms. There are no data on the use of the preparation in children under the age of 4 years. The preparation contains lactose in an amount that usually does not cause any problems in patients with lactose intolerance.

The use of the preparation in pregnant women should be limited to cases where the expected benefit to the mother outweighs the potential risk to the fetus. In pregnant women, the lowest effective dose of fluticasone propionate should be used to ensure adequate control of asthma symptoms. It is not known if the active substances in the preparation or their metabolites are excreted in human milk. The risk for newborns and breastfed infants can not be excluded. A decision should be made whether to discontinue breast-feeding or discontinue treatment with the preparation, taking into account the benefits for the baby resulting from breastfeeding and the benefits for the mother resulting from the treatment with the preparation.

Very common: headache, nasopharyngitis.Common: oral and pharyngeal candidiasis, pneumonia, bronchitis, hypokalaemia, hoarseness, noises, sinusitis, easier bruising, post-traumatic fractures, arthralgia, muscle pain. Uncommon: respiratory symptoms (shortness of breath), anxiety, tremors, palpitations, tachycardia, throat irritation, muscle spasms. Rarely: hypersensitivity reactions (including skin hypersensitivity reactions), angioneurotic edema (mainly swelling of the face, mouth and throat), respiratory symptoms (bronchospasm), anaphylactic reactions (including anaphylactic shock), Cushing's syndrome, curingoid facial features , adrenal suppression, slower growth in children and adolescents, reduction in bone mineral density, sleep disturbances and changes in behavior (including: attention deficit hyperactivity disorder and irritability, mainly in children), cataracts, glaucoma, arrhythmias (including atrial fibrillation, supraventricular tachycardia and additional contractions), paradoxical bronchospasm. Frequency unknown: depression, aggression (mainly in children).

Inhalation. The dose of the preparation is determined individually for each patient depending on the severity of the disease, including the dose of fluticasone propionate contained in the preparation. In patients with asthma, the dose of fluticasone propionate is approximately as effective as 2 doses of another inhaled corticosteroid (eg: 100 μg of fluticasone propionate corresponds to approximately 200 μg of beclometasone dipropionate (containing Freon or Budesonide). in doses that can not be administered with the preparation, the appropriate doses of β-agonist and / or corticosteroid should be prescribed, the preparation should be used every day, even if the symptoms are not present, the patient should be subjected to regular medical check-up. symptom control After an improvement in the patient with the lowest dose administered twice a day, an attempt should be made to continue treatment with an inhaled corticosteroid only as an alternative to patients requiring long-term treatment. with β₂-mimetic, the preparation can be used once a day, if in the doctor's opinion it will allow to maintain adequate control of the symptoms of the disease. In the case of data from an interview indicating that the patient has nocturnal complaints, the dose should be administered in the evening, and in the case of ailments occurring mainly during the day, the dose should be administered in the morning.Bronchial asthma. Adults and adolescents from 12 years: 1 inhalation of the preparation (100 μg + 50 μg) twice a day or 1 inhalation of the preparation (250 μg + 50 μg) twice a day or 1 inhalation of the preparation (500 μg + 50 μg) twice a day day. Short-term use of the preparation may be considered as an initial maintenance treatment in adults and adolescents with chronic, moderate asthma (patients with symptoms occurring during the day, using the drug when needed, with moderate to severe airway congestion) who have rapid asthma control important. In these cases, the recommended starting dose is 1 inhalation of 50 μg salmeterol and 100 μg fluticasone propionate twice daily. If only asthma control is achieved, the treatment should be reviewed and considered if the patient can only use an inhaled corticosteroid. It is important to regularly assess the patient's condition after initiation of corticosteroid use only in inhalation form. There were no clear benefits compared to the use of fluticasone inhaled propionate as initial maintenance therapy if 1 or 2 symptoms of the severity criteria are absent. Typically, the majority of patients with inhaled corticosteroids are "first line" medicines, the preparation is not intended for use in the initial treatment of mild asthma .The 100 μg + 50 μg formulation is not suitable for use in adult patients and children with severe asthma; with severe asthma, it is recommended to determine the appropriate dose of inhaled corticosteroid before the combination treatment Children 4 years: 1 inhalation of the preparation (100 μg + 50 μg) twice daily Maximum allowed for use in children the dose of fluticasone propionate administered with the preparation is 100 μg 2 times a day.COPD. Adults: 1 inhalation of the preparation (500 μg + 50 μg) twice a day.
No dose adjustment is necessary in elderly patients or in patients with impaired renal function.There are no data on use in patients with hepatic impairment.