Asmaneks Tvistkheyle

General characteristics. Structure:

Active agent: mometazona furoate of 200 mkg; 
Auxiliary a veshchestva:laktoza anhydrous - 1.161 mg. 240 mg (30 doses or 60 doses) - the inhalers dosing Tvistkheyler (1) - the aluminum foil laminated by a film polymeric (1) - a pack cardboard.

Pharmacological properties:

Pharmacodynamics. Asmaneks Tvistkheyler (a mometazona furoate) - the glucocorticosteroid (GKS) drug for inhalations having local antiinflammatory effect.
 
The mechanism of antiallergic and antiinflammatory action of a mometazon of furoate is caused by its ability to inhibit release of mediators of an inflammation. In vitro of a mometazon furoate significantly inhibits release of leukotrienes from leukocytes. In cultures of cells of a mometazon furoate showed high ability to inhibit synthesis and release of interleykin of 1,5 and 6 (IL-1,IL-5, IL-6), and also a tumor necrosis factor an alpha (ФНО-α); it is also inhibitor of products of LT (leukotrienes), and also extremely powerful Th2-tsitokinov inhibitor, interleykin 4 and 5, CD4+ T-cells of the person.
 
At a mometazon of furoate affinity and ability to linkng with GKS receptors of the person are 16 times higher, than at dexamethasone, is 7 times higher, than at Triamcinolonum of acetonide, 5 times are higher, than at a budesonid and 1,5 times above, than at a flutikazon. Asmaneks Tvistkheyler's use in doses from 200 to 800 mkg/days improves function of external respiration (on indicators of a peak expiratory rate and volume of the forced exhalation for I mines), leads to more complete control of symptoms of bronchial asthma, and reduced the need for use of inhalation betag-adrenostimulyator. Improvement of function of breath is observed at some patients already in 24 h after the beginning of therapy, however the maximum effect is usually reached not earlier than in 1-2 weeks. Improvement of function of breath remains throughout the entire period of treatment.
 
At patients with bronchial asthma at regular use of Asmaneks Tvistkheyler within 4 weeks in doses from 200 mkg 2 times a day to 1200 mkg do not come to light suppression signs гипоталамо - pituitary and adrenal system, and system effects are shown only at use in a dose of 1600 mkg/days.

Pharmacokinetics. At inhalation use of a mometazon furoate has low system bioavailability (less than 1%). At use concentration of drug in plasma is in the recommended doses about or below a definition threshold (50 pg/ml). Thereof it is impossible to define neither an elimination half-life, nor volume of distribution of a mometazon of furoate after inhalation.

Indications to use:

- The Bronchial Asthma (BA) of any severity (including at the patients applying earlier both inhalation, and system GKS and also at insufficient efficiency of the therapy applied earlier without use of GKS);
- the chronic obstructive pulmonary disease (COPD) - from moderate severity to very heavy.

Route of administration and doses:

In the form of inhalations. The recommended doses depend on disease severity.
 
At a stable current OH easy and moderate severity the recommended initial dose of Asmaneks Tvistkheyler makes 400 mkg of 1 times a day. Inhalation is recommended to be carried out in the evening. At some patients (for example, GKS receiving before inhalation in high doses) more adequate control of a course of a disease is reached when the daily dose of 400 mkg is divided into 2 inhalations. At a number of patients when carrying out a maintenance therapy decrease in a daily dose to 200 mkg of 1 times a day is effective in the evening. In these cases it is necessary to use Asmaneks Tvistkheyler with the maintenance of a mometazon of furoate 200 mkg in 1 dose.
 
The dose should be selected individually (before achievement of the minimum dose providing adequate control of the course of asthma).
 
At a severe form OH the initial recommended dose makes 400 mkg 2 times a day that corresponds to the maximum daily dose of 800 mkg. After achievement of effective control of symptoms of asthma it is necessary to reduce Asmaneks Tvistkheyler's dose to the minimum effective gradually.
 
Upon transition from oral administration of GKS to therapy by Asmaneks Tvistkheyler in an initiation of treatment both drugs apply at the same time. Approximately in a week of combined use begin to cancel gradually peroral GKS, reducing its daily dose or missing one reception. The following dose decline is carried out in 1 or 2 weeks, depending on a condition of the patient. It is not necessary to reduce a dose more than by 2,5 mg of Prednisolonum a day (or its equivalent). Cancellation should be carried out surely gradually. At the same time careful control of a condition of the patient, including breath function indicators is necessary (not to miss the moment of deterioration in a course of bronchial asthma) and functions of adrenal glands (for an exception of insufficiency of function of bark of adrenal glands).
 
At HOBL the recommended dose of 800 mkg/days. Most of patients can accept all dose once a day - in the evening. At some patients reception on 400 mkg 2 times a day is more effective.
 
Instructions for use inhaler Tvistkheyler
 
Before opening Tvistkheylsr, it is necessary to be convinced that the counter and the index on a cover are combined. Tvistkheyler open, shifting a white cover counterclockwise, at the same time holding Tvistkheyler's basis in the fixed situation. The counter of doses at the same time notes use of 1 dose. Further Tvistkheyler it is necessary to place in an oral cavity and, having clasped with lips a mouthpiece, quickly and deeply to inhale. Then to take out a mouthpiece from a mouth and to hold the breath on 10 sec. or so for a long time as far as it is convenient to the patient. The patient should not exhale through Tvistkheyler.
 
To close Tvistkheyler, it is necessary to return a cover to the place of right after inhalation and to load the following dose, having turned a cover clockwise at the same time softly pressing it down, the click will not sound yet and the cover completely will not be closed. The arrow on a cover at the same time completely to be combined with a counter window.
 
The patient should advise to rinse a mouth after each inhalation. It reduces risk of development of candidiasis.
 
The display of the counter will show when the last dose is loaded. After a dose 01 on the counter it will be highlighted 00 and the cover will be blocked. After that performing inhalations is impossible and Tvistkheyler it is necessary to throw out.
 
Tvistkheyler it is necessary to contain dry and pure. The mouthpiece outside can be cleaned a dry gauze or fabric. Tvistkheyler it is impossible to wash with water.

Features of use:

Asmaneks Tvistkheyler is not intended for bystry stopping of a bronchospasm. The patient should be warned that for this purpose it is necessary to use high-speed inhalation bronchial spasmolytics.
 
The patient should be warned also about need of the immediate address to the doctor if against the background of therapy by Asmaneks Tvistkheyler attacks of a bronchospasm do not manage to be stopped use of bronchial spasmolytics. In these cases increase in a dose of Asmaneks Tvistkheyler (can be required up to the maximum recommended daily) or/and purpose of GKS for system use.
 
It is necessary to explain to the patient need of constant use of Asmaneks Tvistkheyler (even in the absence of disease symptoms) and inadmissibility of the sharp termination of inhalations.
 
Upon transition from GKS system use on Asmaneks Tvistkheyler's inhalation requires extra care because of possible risk of development of adrenal insufficiency. After cancellation of system GKS function recovery гипоталамо - pituitary and adrenal system requires several months.
 
During stressful situations, including injuries, surgical interventions, infectious diseases or a heavy attack of bronchial asthma, the patients who were earlier receiving GKS for system use need additional purpose of a short course of system GKS which then, in process of subsiding of symptoms, gradually cancel. Such patients should recommend to carry at themselves a small amount of GKS for intake together with the warning card. On it it is necessary to designate need of use at stressful situations of system GKS and their recommended doses. At this category of patients it is regularly necessary to control function of adrenal glands (in particular, the morning maintenance of cortisol in a blood plasma).
 
Upon transition from system GKS on Asmaneks Tvistkheyler display of the accompanying allergic diseases which symptoms were suppressed with corticosteroid system therapy earlier is possible. During this period at some patients emergence of signs of cancellation of system GKS, including muscle pain and/or joints, a depression, feeling of fatigue is possible in spite of the fact that indicators of function of lungs at the same time are stable or even improve. Such patients should be convinced of need of continuation of therapy by Asmaneks Tvistkheyler, but at the same time carefully to control their state in connection with possible development of insufficiency of bark of adrenal glands. If there are signs of insufficiency of adrenal glands, it is necessary to increase temporarily GKS dose for system use, and further to carry out their cancellation more smoothly.
 
As well as when using other inhalation drugs, after Asmaneks Tvistkheyler's use development of a paradoxical bronchospasm is possible. In this case immediate use of inhalation high-speed bronchodilators with the subsequent cancellation of Asmaneks Tvistkheyler and purpose of alternative therapy is required.
 
The patients receiving GKS or other immunodepressants should advise to avoid contacts with sick some infections (chicken pox, measles) and it is obligatory to consult with the doctor if such contact happened (especially important at use for teenagers 12 years are more senior).
 
For maintenance of low potential of suppression гипоталамо - pituitary and adrenal system it is not necessary to exceed the recommended doses, and at each patient Asmaneks Tvistkheyler's dose should be titrated, trying to obtain the minimum effective. At Asmaneks Tvistkheyler's appointment the doctor should consider that impact of drug on products of cortisol can vary at various patients.
 
Data that Asmaneks Tvistkheyler's use in the doses exceeding recommended leads to strengthening of its therapeutic effect are not available. Developing of candidiasis can demand performing the corresponding antifungal therapy or phase-out of Asmaneks Tvistkheyler.
 
Use in pediatric practice
 
Safety and efficiency of use of Asmaneks Tvistkheyler for children up to 12 years are up to the end not studied.
 
Recommend to control regularly growth of the teenagers receiving long therapy of GKS for inhalations. At delay of growth it is necessary to reconsider the carried-out therapy for the purpose of a dose decline of inhalation GKS to minimum at which effective control behind disease symptoms is achievable.

Use during pregnancy

Adequate and well controlled drug use studies during pregnancy were not conducted. However after inhalation use concentration of a mometazon of furoate in a blood plasma is very low; impact on a fruit is probably not enough, the probability of toxic impact on reproductibility is very low.
 
Asmaneks Tvistkheyler's use (as well as other inhalation GKS) during pregnancy and at nursing mothers perhaps only if the estimated advantage for mother exceeds potential risk for a fruit or the child.
 
Newborns whose mothers received GKS during pregnancy demand observation for identification of signs of insufficiency of function of bark of adrenal glands.

Side effects:

Most often: oral cavity candidiasis, pharyngitis, dysphonia, headache.
 
Seldom: dryness in a mouth and a throat, dyspepsia, a body weight increase, heartbeat.
 
In some cases at predisposed patients: emergence of hypersensitivity reactions, including rash, urticaria, an itch, an erythema, and also an eye, persons, lips and a throat swelled.
 
At use of inhalation GKS for treatment of asthma development of a bronchospasm and increase in number of rattles in lungs right after inhalation is possible. At use of inhalation GKS there can be, also, system side effects (especially at use in high doses and for an appreciable length of time). These effects include oppression of function of bark of adrenal glands, a growth inhibition at children and teenagers, demineralization of a bone tissue, glaucoma, increase in intraocular pressure, development of a cataract.

Interaction with other medicines:

At simultaneous use of Asmaneks Tvistkheyler and inhibitor of CYP3A4 enzyme of a ketokonazol decrease in AUC0-24 of cortisol is noted small (on limit of the statistical importance). However it is improbable that these changes have clinical value.

Contraindications:

— children's age (up to 12 years);
— the established hypersensitivity to drug components.

With care: active or latent pulmonary tuberculosis, fungal, bacterial or system viral infections, herpetic damage of eyes (Herpes simplex), pregnancy, lactation period.

Overdose:

Due to the low system bioavailability of Asmaneks Tvistkheyler at acute overdose special therapy, except control of a condition of the patient is not required. Then it is necessary to resume use of drug in a therapeutic dose. It is necessary to consider that prolonged use of GKS for inhalations in the raised doses can lead to function suppression гипоталамо - pituitary and adrenal system. In such cases carry out symptomatic therapy, gradual drug withdrawal, correction of electrolytic disturbances.

Storage conditions:

In original packaging from a foil at a temperature of 2-30 °C. Not to cool, not to freeze. To use for 3 months after opening of packaging from a foil. To avoid contact with water.

Issue conditions:

According to the recipe

Packaging:

powder for inhalations dosed 200 mkg / a dose; an inhaler dosing Tvistkheyler, a package (bag) from the aluminum foil laminated by polyethylene 1, a pack cardboard 1;
 powder for inhalations dosed 400 mkg / a dose; an inhaler dosing Tvistkheyler, a package (bag) from the aluminum foil laminated by polyethylene 1, a pack cardboard 1;