Zenhale aerosol for inhalation 200mkg + 5mkg/dose 120doz

Packaging

Bottle of 120 doses.

Mechanism of action

Zenheyl - the combined drug.

Formoterol is a strong selective beta2-adrenergic agonist. On average, the bronchodilatory effect in patients with reversible bronchial obstruction lasts 12 hours. Formoterol inhibits the release of histamine and leukotrienes into lung tissue. In preclinical studies, some anti-inflammatory properties have been shown, such as inhibiting the development of edema and the accumulation of inflammatory cells.

Mometasone furoate - GCS, which has a local anti-inflammatory effect. The anti-inflammatory effect of corticosteroids is realized through glucocorticosteroid receptors (HRS). After the addition of the GCS, the GKH heterocomplex dissociates, and the part activated by the ligand passes from the cytoplasm to the nucleus, where it enhances the expression of anti-inflammatory genes by joining special DNA segments, the so-called "elements of the GCS response". At the same time, it is believed that the main way of implementing anti-inflammatory activity is the suppression of gene transcription. In this case, activated HRS interacts with transcription factors apolipoprotein 1 (AP1) or nuclear kappa B factor (NF-kV) to reduce gene expression. In addition, the corticosteroids enhance the expression of the gene responsible for the synthesis of the NF-kV inhibitor.

Indications and usage

The drug Senhale shown as a drug for continuous use for maintenance therapy of bronchial asthma, including to reduce the severity of asthma exacerbations in adults and children over the age of 12 years.

The drug Senhale shown:

• patients who cannot control the course of the disease, using only inhaled GCS and inhaled short-acting beta2-adrenomimetics for relief of seizures (in the "on demand" mode);
• patients whose severity of the disease requires the appointment of two types of maintenance therapy.

The drug Senhale can also be assigned to patients in whom the disease is adequately controlled by the use of inhaled GCS and long-acting beta2-adrenomimetics.

Contraindications

• children up to 12 years;
• Hypersensitivity to mometasone furoate, formoterol fumarate, or other components of the drug.

Pregnancy and Breastfeeding

Properly controlled studies of the use of the drug Zenheyl in pregnant women were not performed. Preclinical studies of mometasone revealed its toxicity to the reproductive system, similar to that for the entire GCS group; however, the potential risk to humans is unknown.Zenheyl drug should not be used during pregnancy, except in cases where the expected therapeutic effect for the mother far exceeds the potential risk to the fetus.

All newborns whose mothers took GCS during pregnancy should be carefully examined for adrenal dysfunction.

Formoterol, as a beta2-adrenomimetic, has a tocolytic effect (a relaxing effect on the smooth muscles of the uterus) and can suppress labor activity.

Properly controlled studies of the drug Zenheyl in nursing mothers were not performed. It has been established that formoterol is excreted in milk in rats, GCS is excreted in human milk. The decision to cancel or continue treatment should be made individually and based on a comparison of the benefits of breastfeeding for the baby and the use of the drug Zenheyl for the mother.

Dosage and administration

The drug Senhale should be used in the form of inhalation, 2 doses 2 times / day (morning and evening).

Selection of the optimal dose of the drug is based on the previously used therapy.

For patients who have not previously received inhaled GCS, but the severity of the condition requires two-component therapy, the starting dose of the drug depends on the severity of bronchial asthma and may be 50 mcg + 5 mcg / dose, 100 mcg + 5 mcg / dose or 200 mcg + 5 mcg / dose, 2 inhalations 2 times / day.

Forpatients aged 12 and overThe maximum recommended daily dose is 2 inhalations of the drug 200 mcg + 5 mcg / dose 2 times / day. If bronchial asthma symptoms occur between doses of the drug, a short-acting inhaled beta2-adrenergic mimic should be used to relieve symptoms immediately.

After achieving optimal control of asthma, it is recommended to titrate the dose of the drug to the minimum effective.

Adverse reactions

The side effects that were observed during the clinical trials of the use of the drug Zenhale in patients with bronchial asthma, are given depending on the frequency of their occurrence: very often (≥ 1/10); often (≥ 1/100, <1/10); infrequently (≥ 1/1000, <1/100); rarely (≥ 1/10 000, <1/1000).

Infection: often - oral candidiasis; infrequently pharyngitis.

Immune system: hypersensitivity reactions with the following manifestations: bronchospasm (rare), atopic dermatitis (rare), urticaria (infrequently).

Nervous system: often - headache; infrequently - insomnia, tremor, dizziness; rarely - neurosis.

Special senses: infrequently - lesion of the lens (defined as a change ≥ 1 point according to the lens opacification classification system, version III (LOCS III). Not a single case of posterior subcapsular cataract was registered); rarely, increased intraocular pressure.

Cardiovascular: infrequently - tachycardia, palpitations, increased blood pressure.

Respiratory: often - dysphonia; infrequently - pain in the oropharynx, irritation of the pharynx.

Gastrointestinal: infrequently - nausea, dry mouth.

Musculoskeletal system: infrequently - muscle spasms.

Screening: rarely - prolonged QT interval.

Special notes

Patients should be trained by a doctor or medical staff on how to use the drug.

Exacerbation of the disease

With the use of the drug Senhale, serious side effects and complications associated with bronchial asthma can develop. Patients should not interrupt the course of treatment, however, in the absence of control of the disease or amplification of symptoms, consult a doctor immediately.

You should not start treatment with Zenhale in patients with a sharp increase in symptoms of bronchial asthma, as well as with life-threatening exacerbations. The use of the drug Senhale has not been studied in patients with rapidly advancing exacerbations of bronchial asthma.

The physician should review asthma therapy if the symptoms of bronchial asthma persist, if a constant dose increase is required to achieve disease control, if bronchodilators no longer stop bronchial asthma attacks or if the peak expiratory rate decreases, these symptoms usually indicate a worsening asthma course. In the above cases, you should consider the use of additional therapy of GCS.

Bronchial Asthma Attacks

The drug Senhale is not a drug for the rapid relief of bronchospasm or any other manifestations of an attack of asthma. In such cases, short-acting beta2-adrenomimetics should be used. In addition, the patient should be informed of the need for immediate treatment to the doctor in case of worsening of the course of bronchial asthma.

An overdose of the drug Senhale and its use with other prolonged beta2-adrenomimetikami

Zenheyl should not be used with other prolonged beta2-adrenomimetics.

For the treatment of bronchial asthma, the dose of Zenhale should be chosen individually for each patient, the dose should be minimal to achieve the desired therapeutic effect. The dose should also not exceed the maximum recommended dose. Information confirming the increase in the effectiveness of the drug with an increase in its dose higher than the recommended, no.

Oral pharyngeal candidiasis

During the clinical trials of the drug Zenhale in some patients, the development of oropharyngeal candidiasis was noted, associated with taking GCS. This kind of complication usually requires a special course of treatment with antifungal drugs, and in some cases, drug withdrawal. The patient should be advised to rinse the mouth after applying the drug.

Systemic effect of GCS

The systemic effect of inhaled GCS may manifest itself, in particular, with long-term use of the drug in high doses. However, the probability of its occurrence is much lower than when taking GCS orally.Among the potential systemic effects, there is an inhibition of adrenal function, growth retardation in children and adolescents, a decrease in bone mineral density, cataracts and glaucoma. It is important to titrate doses of the drug Senhale to the minimum effective dose.

Cases of development of cataracts and glaucoma with mometasone furoate are rarely described.

Suppression of adrenal function

As a rule, the dose of the drug Zenheyl, necessary for complete control of asthma, causes significantly less suppression of the function of the hypothalamic-pituitary-adrenal system than the equivalent efficacy of the oral dose of prednisolone.

The probability of suppression of adrenal function when using the drug Zenheyl exists, especially in the case of the use of doses of the drug that exceed the recommended. Particular attention to the suppression of adrenal function should be paid in stressful situations or before planned operations, when patients will receive additional therapy of SCS. However, during clinical trials, no clinically significant effect of Zenhale (at a dose of mometasone fumarate of 800 mcg / day) on plasma cortisol level was detected.

Inhalation bronchospasm

As with any other inhaled drug, it is necessary to take into account the possibility of the development of bronchospasm caused by inhalation. In the case of its development, you should immediately cancel the drug and choose an alternative method of treatment.

Hypokalemia and Hyperglycemia

Against the background of the use of beta2-adrenomimetics, serious hypokalemia may develop.Hypokalemia may increase the likelihood of developing arrhythmias.

Patients with severe bronchial asthma should be treated with caution, since the development of hypokalemia can be potentiated by hypoxia and concomitant treatment. In such situations, it is recommended to continuously monitor the level of serum potassium.

Beta2-adrenomimetics, including and formoterol, have a hyperglycemic effect, therefore, patients with diabetes mellitus are recommended additional monitoring of blood glucose.

Influence on ability to drive motor transport and control mechanisms

With the development of side effects from the nervous system should refrain from driving or working with mechanisms during the period of taking the drug.

In clinical studies, the use of the drug Zenhale together withbeta2 adrenomimetics short actions and intranasal corticosteroids did not lead to the development of any undesirable interaction.

A special study of drug interactions drug Zenheyl not conducted. It is assumed that the list of effects of drug interactions for a given combination drug will be a summary list of interaction effects known for each of its active ingredients.

The simultaneous use of mometasone furoate inhalation with a potent inhibitor of the CYP3A4 enzyme,ketoconazole, leads to a significant increase in the concentration of mometasone in the blood plasma.

Simultaneous use withsympathomimeticsmay increase the incidence of side effects of formoterol.

Simultaneous use withxanthine derivatives and with non-calcium-saving diuretics may enhance the hypokalemic effect of beta2-adrenomimetics.

Formoterol, like other beta2-adrenomimetics, should be used with caution in patients takingquinidine, disopyramide, procainamide, phenothiazines, terfenadine, astemizole, MAO inhibitors , tricyclic antidepressants, or any drugs that prolong the QT interval, because These drugs can enhance the adrenergic effect of Zenhale on the cardiovascular system. Drugs that prolong the QT interval increase the risk of developing ventricular arrhythmias.

Beta blockers may weaken the effect or completely block the effect of formoterol. Therefore, drugs of these groups (including eye drops) should not be administered at the same time, unless there are undeniable reasons for this.

Mometasone furoate:overdose of GCS with inhalation or ingestion can lead to suppression of the function of the hypothalamic-pituitary-adrenal system.

Formoterol fumarate:overdose can lead to the development of symptoms characteristic of beta2-adrenergic mimics (nausea, vomiting, headache, tremor, lethargy, feeling of heartbeat, tachycardia, ventricular arrhythmia, metabolic acidosis, hypokalemia, hyperglycemia, increased blood pressure).

Treatment:symptomatic and supportive care is indicated, hospitalization if necessary. In some cases, it will be reasonable to use beta-blockers, but only under medical supervision and with great caution, because they can cause bronchospasm. Monitoring of the adrenal function is also required.

The drug should be stored out of the reach of children at a temperature not higher than 25 ° C. Do not freeze.