Oxus Turbuhaler - instructions for use, dose, side effects, contraindications

Plastic inhaler. The color of the rotating disk for a dosage of 4.5 μg / dose is light greenish-blue, for a dosage of 9 μg / dose - a dark greenish-blue. The contents of the inhaler are rounded granules from white to almost white, decaying into a fine powder at low pressure. The content of the powder fraction is possible.

Pharmacotherapeutic group:Bronchodilator-beta2-adrenergic selective

ATX: & nbsp

R.03.A.C Selective beta-2-adrenomimetics

R.03.A.C.13 Formoterol

Pharmacodynamics:

Formoterol refers to selective beta2-adrenomimetic drugs, which exert a bronchodilating effect in patients with reversible airway obstruction.The therapeutic effect (bronchodilator effect) is achieved quickly, after 1 -3 min after taking the drug, and lasts an average of 12 hours after the application of a single dose.

Pharmacokinetics:

Absorption

Formoterol after inhalation quickly absorbed. The maximum concentration in the plasma is noted 10 min after the inhalation of the drug.

The average proportion of the drug that enters the lungs after inhalation with 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 participating in the O-demygylation, not installed. The total plasma clearance and volume of distribution is not established.

Excretion from the body

The bulk of formoterol is excreted as a result of metabolism. After inhalation, 8-13% of the delivered dose of formoterol (corresponding to 6-10% of the inhaled dose) is excreted unchanged in the urine.The half-life of the drug with inhalation administration is an average of 17 hours.

Indications:

Oxus® Turbuhaler® is shown in addition to corticosteroid therapy for regular maintenance of bronchial asthma, for the relief of bronchospasm attacks, for the prevention of bouts caused by physical exertion.

In chronic obstructive pulmonary disease (COPD) for the prevention and treatment of bronchial obstructive symptoms.

Contraindications:

Hypersensitivity to formoterol or lactose.
Children under 6 years.

Carefully:

With care, prescribe the drug to patients with thyrotoxicosis, pheochromocytoma, diabetes, hypertrophic obstructive cardiomyopathy, idiopathic podvalvannym aortal stenosis, severe hypertension, aneurysm or other severe cardiovascular diseases, for example, ischemic disease, tachyarrhythmias or severe heart failure.

It is necessary to prescribe with caution the drug to patients who determine the lengthening of the interval QTc, as well as patients taking medications that can affect the duration QTc-Interval (seesection "Interaction with other drugs and other forms of interaction").

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 in pregnant women is limited. Experimental animals showed rejection of the implant, as well as a decrease in the life span 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.

Bronchial asthma is a potentially dangerous disease, and therefore, during pregnancy, control over its symptoms should be exercised. If it is necessary to control the bronchial asthma, Oxys® Turbuhaler® can be used at all times of pregnancy (see section "Dosing and Administration"). However, as for any other drugs, the decision to prescribe the drug during pregnancy can be taken only in the event that,when the expected effect for the mother exceeds any possible risk to the fetus.

It is not known whether formoterol in the breast milk of women.

In experiments on laboratory animals (rats), small amounts of formoterol in breast milk were shown.

The decision to prescribe Oxys® Turbuhaler® to women during lactation is taken when the expected benefit to the mother exceeds any possible risk to the child.

Dosing and Administration:Inhalation

4.5 mcg / dose

Adults:

Normal dosage; 1 or 2 inhalations once or twice a day. The dose of the drug can be inhaled in the morning and / or in the evening. Some patients may need 4 inhalations once or twice a day. The maximum daily dose for regular maintenance therapy is 8 inhalations. If necessary, additional inhalations, more than those recommended for regular maintenance therapy, may be taken by the patient for relief of bronchospasm attacks to a maximum daily dose of 12 inhalations (maintenance dosage plus doses taken as needed).It is not recommended to take more than 6 doses (inhalations) of the drug to stop one attack. The need to use the drug more than 2 times a day, and / or use of dosages exceeding those recommended as normal maintenance therapy more than 2 days a week, is a criterion of insufficient disease control, and the treatment regimen should be reviewed.

In the presence of nocturnal symptoms of bronchial asthma, the recommended dose of the drug can be taken once a night. The duration of the drug is about 12 hours.

When selecting the dosage, it is necessary to strive to prescribe the minimum effective dose.

Chronic obstructive pulmonary disease:

Normal dosage: 2 inhalations once or twice a day. 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 relieve bronchial obstructive symptoms, up to a maximum total daily dose of 8 inhalations (maintenance dosage plus doses taken as needed). It is not recommended to inhale more than 4 doses of the drug in a single dose.The need to use the drug more than 2 times a day, and / or use of dosages exceeding those recommended as normal maintenance therapy more than 2 days a week, is a criterion of insufficient disease control, and the treatment regimen should be reviewed.

Prevention of asthma attacks caused by physical exertion:

2 inhalations before exercise. Do not exceed the maximum daily dose.

Children 6 years and older:

Normal dosage; 2 inhalations once or twice a day. Do not take more than 4 inhalations a day.

Prevention of asthma attacks caused by physical exertion:

2 inhalation before exercise. Do not exceed the maximum daily dose.

9 μg / dose

Adults

Normal dosage; 1 inhalation once or twice a day. The dose (inhalation) of the drug can be taken in the morning or in the evening. Some patients may need 2 inhalations once or twice a day. The daily dose for regular maintenance therapy is 4 inhalations. If necessary, additional inhalations, more than those recommended for regular maintenance therapy,can be performed by the patient for the relief of bronchospasm attacks to a maximum daily dose of 6 inhalations (maintenance dosage plus doses taken as needed). It is not recommended to take more than 3 doses (inhalations) of the drug to stop one attack. The need to use the drug more than 2 times a day, and / or use of dosages exceeding those recommended as normal maintenance therapy more than 2 days a week, is a criterion of insufficient disease control, and the treatment regimen should be reviewed.

In the presence of nocturnal symptoms of bronchial asthma, the necessary dose of the drug can be taken at one time at night. The duration of the drug is about 12 hours.

When selecting the dosage, it is necessary to strive to prescribe the minimum effective dose.

Chronic obstructive pulmonary disease:

Normal dosage: 1 inhalation once or twice a 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 dosage plus doses taken as needed). It is not recommended to inhale more than 2 doses of the drug in a single dose. 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 an insufficient control of the disease and the need to revise the treatment regimen.

Preventing attacks of bronchial asthma, caused by physical activity:

1 inhalation before exercise. Do not exceed the maximum daily dose.

Children 6 years and older:

Normal dosage: 1 inhalation once or twice a day. Do not take more than 2 inhalations a day.

Prevention of asthma attacks caused by physical exertion:

1 inhalation before exercise. Do not exceed the maximum daily dose.

Special patient groups: No special dose selection is required in elderly patients, as well as in patients with impaired renal or hepatic function in the appointmentrecommended normal dosages of the drug (see section "Special instructions").

Instructions on the use of turbuhaler

Turbuhaler is a multi-dose inhaler that allows to dose and inhale the drug in very small doses (Figure 1). When you inhale, the powder from Turbuhaler is delivered to the lungs. Therefore, it is important that you take a deep and deep breath through the mouthpiece.

Preparing the Turbuhaler for first use:

Before the first use of Turbuhaler it must be prepared for work.

1. Unscrew and remove the lid.

2. Hold the inhaler vertically with the dispenser down (Fig. 2). Do not hold the inhaler for the mouthpiece when you turn dispenser.

Turn the dispenser all the way in one direction (no matter, clockwise or counterclockwise), and then also against the stop in the opposite direction. During the rotation of the dispenser, you will hear a click. Follow the procedure twice.

Now the inhaler is ready for use, and you should not repeat this procedure of preparing Turbuhaler for work before each use. In order to take the drug, follow the instructions below.

How to use Oxys® Turbuhaler®

For taking one dose of the drug follow the procedure described below.

1. Unscrew and remove cover.

2. Hold the inhaler vertically dispenser down (Figure 2). Do not hold the inhaler for the mouthpiece, when turn the dispenser. For in order to measure the dose drug, turn the dispenser up to the stop in one direction (it does not matter, clockwise or counterclockwise), and then also to the the opposite direction. During turning the dispenser you hear a click.

3. Do not hold the inhaler at the mouth. Exhale. Do not exhale through the mouthpiece.

4. Carefully place mouthpiece between teeth, Squeeze your lips and do strong and deep breath through an inhaler (Figure 3). The mouthpiece is not chewed and not clench your teeth.

5. Before exhaling, remove the inhaler from the mouth.

6. If inhalation is required more than one dose, repeat steps 2-5.

7. Close the inhaler cover, check that the cover of the inhaler was carefully screwed.

IMPORTANT!

Never exhale through the mouthpiece.

Always close the inhaler tightly cover after use.

Do not attempt to remove the mouthpiece, as it is fixed to the inhaler and is not removed.

The Turbuhaler's mouthpiece rotates, but do not turn it unnecessarily.

Since the amount of inhaled powder very little, you probably will not feel taste of powder after inhalation. But, If you followed the instructions, you can be sure that they inhaled the necessary dose of the drug.

Cleaning

Regularly (once a week), cleanse mouthpiece from the outside with a dry cloth.

Do not use water or other liquids to clean the mouthpiece.

How do you know that the inhaler is empty?

The appearance in the window of the indicator of doses of red mark means that there is left in the inhaler approximately 20 doses (Figure 4). When the red mark will reach the bottom edge the window of the dose indicator (Fig. 5), the inhaler is empty and should be replaced by a new one.

Note that even when the inhaler is empty, the dispenser continues to turn. The sound that you hear, shaking the inhaler, is made by the dehumidifier agent, not a medicine.

Recycling

Be careful with the inhaler used, remember that some amount of the drug may remain inside the inhaler.

Side effects:

Frequently encountered (> 1/100)

Central nervous system: headache.

Cardiovascular system: heart palpitations.

Musculoskeletal system: tremor.

Rarely occurring (<1/100)

Central nervous system: agitation, anxiety, sleep disturbance.

Musculoskeletal system: muscle cramps.

Cardiovascular system: tachycardia, changes in blood pressure.

Very rare (<1/1000)

Skin: rash, hives, itching.

Cardiovascular system: atrial fibrillation, supraventricular tachycardia, extrasystole.

Metabolic disorders: hypokalemia / hyperkalemia. Respiratory tract: bronchospasm.

Tremor and heart palpitations are temporary and go through the process of treatment. As with any inhalation therapy, in very rare cases, it is possible to develop paradoxical bronchospasm.

Single cases of development of the following side effects are described: nausea, taste disturbance, dizziness, angina pectoris, lengthening of the interval QTc, hypersensitivity reactions, changes in blood pressure and hyperglycemia. The use of beta2-sympathomimetics can lead to an increase in the blood levels of insulin, free fatty acids, glycerol and ketone.

Overdose:

Clinical experience of treatment in case of an overdose is absent. Most likely, with an overdose, symptoms typical of other beta2-adrenomimetics will be observed: tremor, headache, heart palpitations. In some cases, the development of tachycardia, hyperglycemia, hypokalemia, lengthening of the interval QTc, arrhythmias, nausea and vomiting. Symptomatic and supportive treatment is shown.

Possible appointment of cardioselective beta-blockers, but this should be done with great caution, since the appointment of beta2 blockers- adrenergic receptors can trigger the development of bronchospasm. It is necessary to control the potassium level in the blood serum.

Interaction:

Special studies to study the interaction of Oxys® Turbuhaler® with other drugs have not been conducted.

Joint use with other sympathomimetics, such as beta2-adrenomimetics or ephedrine, can lead to the development of side effects of Oxis® Turbuhaler® and may require dose selection.

Co-administration with xanthine derivatives, steroids or diuretics, such as thiazides and loop diuretics, can provoke the development of such a rare side effect beta2-adrenomimetics, like hypokalemia.Hypokalemia may increase the predisposition to arrhythmia in patients receiving cardiac glycosides.

There is a possibility of increasing the risk of ventricular arrhythmia due to pharmacodynamic interaction in the joint appointment of formoterol with other drugs that extend QTc interval. These drugs include antihistamines, such as terfenadine, astemizole, mizolastine, some antiarrhythmic drugs (for example, quinidine, disopyramide, procainamide), erythromycin and tricyclic antidepressants. There is an increased risk of arrhythmia in patients on the background of simultaneous anesthesia with halogenated hydrocarbons.

Beta-adrenoblockers can weaken or inhibit the pharmacological action of Oxys® Turbuhaler®. In this connection, it is not recommended to use the drug together with adrenergic receptor blockers (including eye drops), except for the extreme need for joint application.

Special instructions:

Formoterol, contained in the preparation, enters the patient's airways along with the air streams when performing an active inspiration through the turbuhaler mouthpiece.

It is important to clearly instruct the patient to take a strong and deep breath through the Turbuhaler mouthpiece to ensure that the optimal dose of the drug reaches the respiratory tract.

It is also important to instruct the patient never to chew or chew on 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 Oxis® Turbuhaler®, which is due to a small amount of the substance being delivered.

Patients suffering from bronchial asthma and regularly taking beta2-adrenomimetics should receive optimal anti-inflammatory therapy with corticosteroids. Patients should be advised to continue anti-inflammatory therapy even when after Oxys® Turbuhaler® it is improved. Preservation of symptoms or occurrence the need to increase the dosage of beta2-adrenomimetics is a sign of worsening of the patient's condition and requires a revision of anti-asthma therapy. Do not start treatment with the drug and increase its dose in severe exacerbation of the disease.

Do not exceed the maximum daily dose of the drug. There is no safety data for prolonged continuous use of the drug at higher doses, such as 36 μg per day in adults and 18 μg per day in children with bronchial asthma, and 18 μg per 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 during one week against the background of adequate maintenance therapy (glucocorticosteroids and beta2-long-acting adrenomimetics), then a review of the current treatment regimen by a specialist is necessary.

In patients with diabetes, at the beginning of treatment should be additionally monitored blood glucose, as beta2-adrenomimetics have a hyperglycemic effect.

As a result of applying beta2-adrenomimetics potentially severe hypokalemia may develop. Special care should be taken when exacerbating severe bronchial asthma, as the risk of hypokalemia may be exacerbated by hypoxia. Hypokalemia can be aggravated with concomitant therapy with xanthine derivatives, steroids and diuretics. In these 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.

Children under 6 years of age should not receive treatment with the drug, since there is insufficient information for this age group.

Impaired liver and kidney function: Influence on the pharmacokinetics of formoterol reduced renal or hepatic function, as well as pharmacokinetics in elderly patients are not described. Because the formoterol is excreted from the body as a result of metabolism, in patients with severe cirrhosis of the liver should be expected to slow the withdrawal of the drug.

The delivered dose of the drug contains 450 μg of lactose (corresponding to 600 μg in the measured dose). This amount, as a rule, does not cause problems in people with lactose intolerance.

Effect on the ability to drive transp. cf. and fur:Oxus® Turbuhaler® does not affect the ability to drive a car and work with complex machinery.

Form release / dosage:

The powder for inhalation is dosed at 4.5 μg / dose and 9 μg / dose.

Packaging:A plastic inhaler with a first opening control (protective film indicating the location of the opening) containing 60 doses of the preparation consisting of a dispensing device, a powder storage tank, a desiccant tank, a mouthpiece, a screw cap, a lower turning colored disc. The inhaler is packed in a cardboard box with instructions for use.

Storage conditions:

Store at temperatures below 30 ° C out of the reach of children.

After use, store the turbohealer with the lid closed tightly.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N013937 / 01

Date of registration:31.05.2007

Expiration Date:Unlimited

The owner of the registration certificate:AstraZeneca ABAstraZeneca AB Sweden

Manufacturer: & nbsp

ASTRAZENECA, AB Sweden