Composition, form of production and packaging
Powder for inhalation in the form of round granules from white to almost white, decaying into a fine powder at low pressure; the content of the powder fraction is possible.
1 dose (1 inhalation)
formoterol fumarate dihydrate 4.5 Ојg
Excipients: lactose monohydrate - 450 mcg.
60 doses - plastic inhalers (1) consist of a metering device, a powder storage tank, a desiccant tank, a mouthpiece, a screw cap, a lower rotating disk of light greenish-blue color - packs of cardboard.
Powder for inhalation in the form of round granules from white to almost white, decaying into a fine powder at low pressure; the content of the powder fraction is possible.
1 dose (1 inhalation)
formoterol fumarate dihydrate 9 Ојg
Excipients: lactose monohydrate - 450 mcg.
60 doses - plastic inhalers (1) consist of a metering device, a powder storage tank, a desiccant tank, a mouthpiece, a screw cap, a lower turning disc of a dark greenish-blue color - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
Selective beta 2 -adrenomimetic. Has a bronchodilator effect in patients with reversible airway obstruction.
After applying the drug in a single dose, the therapeutic effect is achieved quickly (after 1-3 min) and lasts an average of 12 hours.
PHARMACOKINETICS
Suction
After inhalation, formoterol is rapidly absorbed. C max in plasma is observed after 10 min. The average proportion of the drug that enters the lungs after inhalation with a turbuhaler is 28-49% of the delivered dose (corresponding to 21-37% of the inhaled dose). At higher concentrations in the lungs, the overall systemic bioavailability of the drug is 61% of the delivered dose (corresponding to 46% of the inhaled dose).
Distribution and Metabolism
Binding to plasma proteins is approximately 50%.
The drug is metabolized by direct addition of a glucuronic acid residue and O-demethylation. The enzyme involved in the O-demethylation reaction is not established.The total plasma clearance and V d are not established.
Excretion
The bulk of formoterol is excreted from the systemic blood stream in the form of metabolites. After inhalation, 8-13% of the delivered dose (corresponding to 6-10% of the inhaled dose) is excreted unchanged in the urine. T 1/2 is an average of 17 hours.
Pharmacokinetics in special clinical cases
Influence on pharmacokinetics of formoterol reduced renal or hepatic function, as well as pharmacokinetics in elderly patients are not described.
Since formoterol is excreted from the body as a result of metabolism, in patients with severe cirrhosis of the liver should be expected delay in excretion preparation.
INDICATIONS
In bronchial asthma in addition to therapy with GCS:
- for regular maintenance therapy;
- for relief of bronchospasm attacks;
- for the prevention of attacks caused by physical exertion.
In chronic obstructive pulmonary disease for the prevention and treatment of bronchial obstructive symptoms.
DOSING MODE
The drug at a dose of 4.5 mcg / 1 dose is prescribed for adults 1-2 inhalations 1-2 times / day (in the morning and / or in the evening). If necessary, appoint 4 inhalations 1-2 times / day. The maximum daily dose for regular maintenance therapy is 8 inhalations. If necessary, additional inhalations, more than those recommended for regular maintenance therapy, can be performed by the patient to stop bronchospasm attacks up to a maximum daily dose of 12 inhalations (maintenance dose + doses taken if necessary). It is not recommended to use more than 6 doses (inhalations) to stop one attack. The need for the use of the drug more than 2 times a day and / or the use of larger doses than is necessary for maintenance therapy more than 2 days a week is a criterion of insufficient control of the disease and therapy of the disease should be reviewed.
In the presence of nocturnal attacks of bronchial asthma, the recommended dose of the drug can be taken 1 time per night (the duration of the drug is about 12 hours).
When choosing a dose, it is necessary to strive for the appointment of a minimum effective dose.
In chronic obstructive pulmonary disease 2 inhalations 1-2 times / day are prescribed. The maximum daily dose for regular maintenance therapy is 4 inhalations. If necessary, additional inhalations, more than those recommended for regular maintenance therapy, may be performed by the patient to alleviate bronchial obstructive symptoms, up to a maximum total daily dose of 8 inhalations (maintenance dose + doses taken as needed). Do not use more than 4 doses per 1 reception. Frequent use of the drug (more than 2 times a day and / or more often 2 days a week), more than recommended for regular maintenance therapy, indicates inadequate control of the disease and the need to revise the treatment regimen.
Children aged 6 years and older are prescribed 2 inhalations 1-2 times / day. The maximum daily dose is 4 inhalations.
To prevent attacks of bronchial asthma caused by physical exertion, adults and children aged 6 years and older are prescribed 2 inhalations before physical exertion. Do not exceed the maximum daily dose.
The drug in a dose of 9 mcg / 1 dose is prescribed for adults 1 inhalation 1-2 times / day (in the morning and / or in the evening). If necessary, appoint 2 inhalations 1-2 times / day. The daily dose of regular maintenance therapy is 4 inhalations. If necessary, additional inhalations, more than those recommended for regular maintenance therapy, can be performed by the patient to stop bronchospasm attacks up to a maximum daily dose of 6 inhalations (maintenance dose + doses taken as needed). It is not recommended to use more than 3 doses (inhalations) to stop one attack. Frequent use of the drug (more than 2 times a day and / or 2 days a week), more than recommended for regular maintenance therapy, indicates an insufficient control of the disease and the need to revise the treatment regimen.
In the presence of nocturnal attacks of bronchial asthma, the recommended dose of the drug can be taken 1 time per night (the duration of the drug is about 12 hours).
When selecting a dose, it is necessary to prescribe the minimum effective dose.
In chronic obstructive pulmonary disease, 1 inhalation is prescribed 1-2 times / day. The maximum daily dose for regular maintenance therapy is 2 inhalations. If necessary, additional inhalations (more than those recommended for regular maintenance therapy) may be taken by the patient to stop bronchial obstructive symptoms up to a maximum total daily dose of 4 inhalations (maintenance dose + doses taken as needed). Do not use more than 2 doses of the drug for 1 reception. Frequent use of the drug (more than 2 times / day and / or more often 2 days a week), more than recommended for regular maintenance therapy, indicates insufficient control of the disease and the need to review the treatment regimen.
Children aged 6 years and older are prescribed 1 inhalation 1-2 times / day. The maximum daily dose is 2 inhalations.
To prevent attacks of bronchial asthma caused by physical exertion, adults and children aged 6 years and older are prescribed 1 inhalation before exercise. Do not exceed the maximum daily dose.
No special dose selection is necessary for elderly patients, as well as patients with impaired renal or hepatic function when prescribing the recommended doses of the drug.
SIDE EFFECT
From the side of the central nervous system: often (> 1/100) - headache; rarely (<1/100) - agitation, anxiety, sleep disturbance.
From the cardiovascular system: often (> 1/100) - heart palpitations; rarely (<1/100) - tachycardia, change in blood pressure; Very rarely (<1/1000) - atrial fibrillation, supraventricular tachycardia, extrasystole.
From the musculoskeletal system: often (> 1/100) - tremor; rarely (<1/100) - muscle cramps.
Dermatological reactions: very rarely (<1/1000) - rash, hives, itching.
Metabolic disorders: very rare (<1/1000) - hypokalemia, hyperkalemia.
From the respiratory system: very rarely (<1/1000) - bronchospasm.
Tremor and heart palpitations are temporary and go through the process of treatment. As with any inhalation therapy, in very rare cases, the development of paradoxical bronchospasm is possible.
Single cases of development of the following side effects are described: nausea, taste disturbance, dizziness, angina pectoris, lengthening of the QT c interval, hypersensitivity reactions, change in blood pressure and hyperglycemia. Application? 2- cimpathomimetics can lead to an increase in the blood levels of insulin, free fatty acids, glycerol and ketone.
CONTRAINDICATIONS
- children's age till 6 years;
- Hypersensitivity to formoterol or lactose.
Caution should be given to patients with thyrotoxicosis, pheochromocytoma, diabetes mellitus, hypertrophic obstructive cardiomyopathy, idiopathic subaortal stenosis, severe arterial hypertension, aneurysm and severe cardiovascular diseases (including IHD, tachyarrhythmia or severe heart failure).
It is necessary to carefully prescribe the drug to patients who determine the prolongation of the QT interval on the ECG, as well as patients taking medications that can affect the duration of the QT c interval.
Special care should be taken when exacerbating severe bronchial asthma, as the risk of hypokalemia may be exacerbated by hypoxia.
PREGNANCY AND LACTATION
The clinical experience of using the drug Oxys Turbuhaler during pregnancy is limited.
During pregnancy, the symptoms of bronchial asthma should be monitored, for this purpose Oxus Turbuhaler can be used at all times of pregnancy. However, as with any other drug, the decision to prescribe the drug during pregnancy should be taken only if the expected benefit for the mother exceeds any possible risk to the fetus.
In experimental studies on laboratory animals, implant rejection was noted, as well as a decrease in the life expectancy of the offspring in the early postnatal period and a decrease in body weight at birth. These effects were observed with systemic exposures significantly exceeding the exposure achieved with the application of clinical doses of the drug.
It is not known whether formoterol is excreted in breast milk.
In experimental studies on laboratory animals (rats), the presence of small amounts of formoterol in human milk was shown.
The decision to prescribe the drug during lactation is only accepted if the expected benefit for the mother exceeds any possible risk to the child.
APPLICATION FOR FUNCTIONS OF THE LIVER
No special dose selection is required for patients with impaired renal function when prescribing the recommended doses of the drug.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
It is not necessary to select a special dose for patients with impaired liver function when prescribing the recommended doses of the drug.
SPECIAL INSTRUCTIONS
Formoterol contained in the preparation enters the patient's airways along with air streams when performing an active inspiration through the Turbuhaler mouthpiece.It is important to clearly instruct the patient to take a deep and strong breath through the mouthpiece to ensure that the optimal dose of the drug reaches the respiratory tract.
Also, the patient should be instructed never to chew or chew the mouthpiece, do not use Turbuhaler in case of damage to the mouthpiece or detachment of the mouthpiece from the turbuhaler body.
The patient may not feel a taste or feel the drug after using the Oxus Turbuhaler, which is due to a small amount of the delivered substance.
It should be borne in mind that patients with bronchial asthma who regularly take beta 2 -adrenomimetics should receive optimal anti-inflammatory therapy with corticosteroids. Patients should be advised to continue anti-inflammatory therapy even in cases where improvement of the Oxus Turbuhaler administration occurs.Preservation of symptoms or the need to increase the dose of beta 2 -adrenomimetics is a sign of worsening of the patient's condition and requires revision of anti-asthmatic therapy.
Do not start treatment with Oxys Turbuhalerom and increase its dose in an exacerbation of the disease.
Do not exceed the maximum daily dose of the drug. There are no safety data for prolonged continuous use of the drug at higher doses, such as 36 Ојg / day in adults and 18 Ојg / day in children with bronchial asthma, and 18 Ојg / day in patients with COPD.
Frequent use of the drug to prevent symptoms of asthma caused by physical exertion can indicate an inadequate control of the course of the disease and cause a review of the treatment regimen used, as well as an assessment of the patient's commitment to adherence to the regimen. If the need to prevent symptoms of bronchial asthma caused by physical exertion occurs several times within one week against the background of adequate maintenance therapy (GCS, beta 2 -adrenomimetics long-acting), then a review of the current treatment regimen by a specialist is necessary.
With diabetes mellitus, the concentration of glucose in the blood should be monitored at the beginning of the treatment, since beta 2 -adrenomimetics have a hyperglycemic effect.
As a result of the use of beta 2 -adrenomimetics, potentially severe hypokalemia can develop. Special care should be taken when exacerbating severe bronchial asthma, because The risk of developing hypokalemia may be enhanced by hypoxia. Hypokalemia can be aggravated with concomitant therapy with xanthine derivatives, steroids, diuretics. In such cases, it is necessary to monitor the potassium level in the blood serum.
As well as with the use of other inhalation therapy, it is necessary to take into account the possibility of developing paradoxical bronchospasm.
The delivered dose of the drug contains 450 Ојg lactose in (corresponds to 600 Ојg in the measured dose). This amount, as a rule, does not cause problems in people with lactose intolerance.
Use in Pediatrics
Children under the age of 6 years should not prescribe the drug, since there is insufficient information for this age group.
Impact on the ability to drive vehicles and manage mechanisms
Oxus Turbuhaler does not affect the ability to concentrate attention and the speed of psychomotor reactions.
OVERDOSE
Clinical experience of treatment in case of an overdose is absent.
Symptoms: the most likely symptoms are typical of other beta 2 -adrenomimetics, - tremor, headache, heart palpitations; in some cases - tachycardia, hyperglycemia, hypokalemia, lengthening of the interval QT c , arrhythmia, nausea, vomiting.
Treatment: conduct symptomatic and supportive therapy. Perhaps the appointment of cardioselective beta-blockers, but this should be done with great caution, since the appointment of blockers? -adrenoceptors can trigger the development of bronchospasm. This also shows the monitoring of potassium in the blood serum.
DRUG INTERACTION
Special studies on the study of drug interaction Oxys Turbuhaler with other drugs have not been conducted.
When used simultaneously with other sympathomimetics (ephedrine) Oxys Turbuhaler it is possible to increase the side effects of the latter.
When used simultaneously with xanthine derivatives, GCS or diuretics (thiazide and "loop" diuretics), hypokalemia may be increased. Hypokalemia may increase the risk of arrhythmias in patients receiving cardiac glycosides.
With the simultaneous use of Oxys Turbuhaler with drugs that extend the QTc interval (including antihistamines such as terfenadine, astemizole, misolastine, antiarrhythmics: quinidine, disopyramide, procainamide, erythromycin and tricyclic antidepressants), the risk of developing ventricular arrhythmias may increase.
There is a risk of arrhythmias in patients receiving Oxygen Turbuhaler and concomitant anesthesia with halogenated hydrocarbons.
Beta-blockers can partially or completely block the action of the drug (especially when non-selective ОІ-adrenoceptors are used). In this connection, it is not necessary to prescribe Oxys Turbuhaler together with beta-blockers (including eye drops), except for the extreme need for joint application.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children at a temperature of no higher than 30 В° C. The turbo-chiller should be kept tightly closed after use. Shelf life - 2 years.
