Active substanceFormoterolFormoterol
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  • Dosage form: & nbsppowder for inhalation dosed
    Composition:

    active substance: formoterol fumarate dihydrate - 0.012 mg; auxiliary substance: lactose monohydrate - 7.988 mg.

    Description:

    inhaler from a polymeric material. At the dosing part of the device is put on the lid with a lock. On the front side of the device there is an inscription "Easyhaler®". Side is the counter of the number of remaining doses. The contents of the inhaler are a homogeneous powder of white or yellowish white color.

    Pharmacotherapeutic group:bronchodilator means - beta2-adrenomimetic selective.
    ATX: & nbsp

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

    R.03.A.C.13   Formoterol

    Pharmacodynamics:

    Formoterol - a potent selective stimulator of beta2-adrenergic receptors. In patients with reversible airway obstruction, he has a bronchodilator effect. This action develops rapidly (within 1-3 minutes) and remains quite pronounced 12 hours after inhalation of the drug.

    It is shown that in humans formoterol prevents the development of bronchospasm, induced by physical exertion and methacholine.

    Pharmacokinetics:

    Suction

    About 80% of formoterol when administered through the Ishidler inhaler swallowed and subsequently absorbed in the gastrointestinal tract. Therefore, data on the pharmacokinetic properties obtained for oral dosage forms are largely applicable to the inhalation dosage form. After inhalation of therapeutic doses of the drug formoterol It is not detected in plasma using existing analytical methods.

    Absorption occurs rapidly and with high intensity at doses exceeding therapeutic (120 mcg), the maximum concentration of the drug in the plasma is observed 5 minutes after inhalation, while ingestion of 80 mcg absorbs not less than 65%, and intake of the drug inside, in doses up to 300 mcg is accompanied by its rapid absorption with reaching a maximum concentration within 0.5-1 hours.

    Pharmacokinetics of formoterol in the studied range of doses, i.e. 20-300 μg, is linear in nature. With repeated oral administration at a dose of 40-160 μg / day, significant accumulation of the drug was not observed.The maximum rate of excretion after administration of 12-96 μg is reached within 1-2 hours after inhalation.

    In studies of cumulative excretion of formoterol and / or its (R, R) and (S, S) -enantiomers with urine after inhalation of dry powder (12-96 μg) or aerosol dosage forms (12-96 μg), it was found that the absorption increases linearly with increasing dose.

    The connection with plasma proteins for formoterol is 61-64 (34% with albumin). Saturation of binding sites in the range of concentrations achieved with the administration of therapeutic doses of the drug does not occur.

    Biotransformation

    The main pathway of biotransformation is glucuronidation, in another way G-detylation with further conjugation with glucuronic acid. The process catalyzes a large number of isozymes of the system ~ CYP450r (2D6; 2C19; 2C9, 2A6), so the possibility of metabolic drug interactions is low. The kinetics of formoterol after a single and repeated administration is similar, indicating that there is no autoinduction or suppression of metabolism.

    Excretion from the body

    The process of removing formoterol from the circulatory system is multiphase; the elimination half-life depends on the time interval under consideration.Based on the data on plasma concentrations of the drug in the period up to 6, 8 or 12 hours after ingestion, the elimination half-life is about 2-3 hours. According to the urinary excretion rate in the period from 3 to 16 hours after inhalation, the elimination half-life is about 5 hours.

    After a single intake of formoterol. 59-62% is excreted in the urine, and 32-34% % with feces. The renal clearance of formoterol is 150 ml / min.

    Indications:Treatment and prevention of bronchospasm caused by physical stress; cold air or inhaled allergens, in patients with bronchial asthma as a supplement to therapy with inhaled glucocorticosteroids.
    Contraindications:

    Hypersensitivity reactions to formoterol or lactose, children under 6 years of age, lactation period, rare hereditary diseases; such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption;

    Carefully:

    severe heart failure, coronary heart disease, cardiac rhythm disturbances, tachyarrhythmia, atrioventricular blockade of III stage, Q-T interval prolongation (Q-T adjusted 0.44s), hypertrophic obstructive cardiomyopathy, aneurysm, arterial hypertension, pheochromocytoma, diabetes mellitus, thyrotoxicosis.

    Pregnancy and lactation:

    Pregnancy and lactemia

    Necessary data on the use of formoterol for the treatment of pregnant women are absent.

    Teratogenic effects of the drug in animal studies have not been identified, however, in animal studies formoterol led to the rejection of the implanted egg, as well as to a decrease in the level of postnatal survival and to a decrease in the weight of the newborn. These effects, apparently, are due to a stronger systemic effect than that observed with the clinical use of formoterol. Before the accumulation of more extensive experience Formoterol Ishihler is not recommended for use during pregnancy (especially at the end of pregnancy or during childbirth), unless there are no other proven alternatives to treatment. As with any type of drug therapy, the use of this drug during pregnancy should be considered only if the expected benefit for the mother is higher than the risk from this type of treatment for the fetus.

    In studies on rats, small amounts of formoterol were found in breast milk. There is no data on whether the formoterol in breast milk in humans, so mothers during lactation, using an inhaler Formoterol Ishihler, it is recommended to refrain from breastfeeding.


    Dosing and Administration:

    Inhalation.

    Adults (including the elderly)

    Bronchial asthma

    Permanent maintenance therapy: 1 inhalation (12 mcg) 2 times a day; some patients may require 2 inhalations (24 μg) 2 times a day. The maximum daily dose with constant use is 4 inhalations.

    If necessary, the use of additional doses, in addition to those prescribed for permanent maintenance therapy, for relief of symptoms to the maximum total daily dose of 6 inhalations (supporting plus taken as required). Do not take more than 3 inhalations at a time. However, frequent (more than twice a day and / or more than 2 days a week) application, or use in doses exceeding those recommended for permanent maintenance therapy, is a sign of suboptimal control of the course of bronchial asthma and requires revision of the treatment regimen.

    Prevention of bronchospasm caused by physical stress:

    1 inhalation (12 μg) approximately 15 minutes before exercise.In severe bronchial asthma may require 2 inhalations (24 mcg). Do not exceed the maximum total daily dose (6 inhalations).

    Children aged 6 years and over

    Bronchial asthma

    Constant, maintenance therapy: 1 inhalation (12 mcg) 2 times a day. Do not take more than 2 inhalations a day.


    INSTRUCTIONS on the use of the inhaler and administration of the drug

    "Easyhaler" [Ishihler] inhaler, powered by a flow of inhaled air; this means that when inhaled through the mouthpiece, the drug along with the air stream enters the respiratory tract.

    Carefully read the instructions for using the inhaler!

    1. Remove the protective cap from the Ishiheiler mouthpiece

    2. Shake the inhaler 3 ~ 5 times vertically

    3. To release 1 pill of medicine, place Isichaeler between the thumb and index finger and press the inhaler once. -You will hear a click

    4. Take a full breath, tightly grasp the mouthpiece and take a deep breath, hold your breath for 5-10 seconds

    5. If you are prescribed more than 1 dose, repeat steps 2, 3 and 4

    6. Close the Ishiheyler's mouthpiece with a protective cap

    7. The dose counter will help you to know the number of remaining doses of the drug.The counter switches every 5 doses. The red zone on the counter means that there are 20 doses left in your Ishihler.

    The inhaler is recommended to be stored in a rigid case to protect it from shocks and ensure reliable operation of the device.

    Do not exhale through the mouthpiece, as this will result in a decrease in the dose received.

    If the patient inadvertently exhales through the mouthpiece, it is necessary to tap the inhaler on a hard surface or on the palm of the hand to extract the powder from the mouthpiece, and then repeat the procedure for taking the drug. In the same way, if the patient unintentionally turned on the inhaler without a subsequent inhalation.

    After using the inhaler, you must always wear a protective cap on it to avoid accidental switching on the device, which can lead to either an overdose or a dose reduction with the next use of the inhaler.

    The mouthpiece should be cleaned regularly with a dry cloth. To clean it, you can not use water, because the powder inside is hygroscopic.

    Whenever the counter shows zero, it is necessary to replace the drug, despite the fact that inside the inhaler there may remain a powder


    Side effects:
    The most commonly reported adverse side effects of beta2-adrenomimetic therapy, such as tremor and palpitation, tend to mild and disappear after a few days after starting treatment.

    Metabolic and nutritional disorders


    Rarely (> 1/10000 - < 1/1000)

    Hypokalemia, hyperkalemia

    Very rarely, including individual cases (<1/100 00)

    Hyperglycaemia

    Diseases of the nervous system

    Often (>1/100 - < 1/10)

    Headache

    Infrequently (> 1/1000 <1/100)

    Excitation, anxiety, dizziness,

    anxiety, nervousness, insomnia, sleep disorders

    Heart Disease

    Often (> 1/100 <1/10)

    Heart rhythm disturbances

    Infrequently (>

    1/1000 < 1/100 )

    Tachycardia

    Rarely (> 1/10000

    < 1/1000 )

    Atrial fibrillation, supraventricular tachycardia, extrasystole

    Very rarely, including individual cases (<1/10000)

    Angina pectoris, an increase in the duration of the interval QT

    Diseases of blood vessels

    Very rarely, including isolated cases

    (< 1/10000)

    Oscillations arterial pressures

    Diseases respiratory tract, bodies thoracic cells and mediastinum

    Rarely

    (> 1/10000-<1/1000)

    Strengthening of bronchospasm, irritation of the mouth and pharynx,

    paradoxical bronchospasm

    Gastrointestinal diseases

    Rarely, including

    individual cases

    (< 1/10000)

    Disorders of taste, nausea

    Diseases of the musculoskeletal system, connective and bone tissue

    Often (>1/100 - < 1/10)

    Tremor

    Infrequently (>1/1000 - <1/100)


    Muscular convulsions,

    myalgia

    Common diseases and diseases developing in the site of drug administration

    Very rarely, including

    individual cases

    (< 1/10000)

    Reactions hypersensitivity, incl.

    Bronchospasm, marked decrease in blood pressure, urticaria, angioedema, itching, rashes, peripheral edema.


    Treatment with beta2-adrenomimetics can lead to an increase in blood concentrations of insulin, free fatty acids, glycerol, ketone bodies.
    As with any inhalation means,
    paradoxical bronchospasm is observed in very rare cases.

    Overdose:
    Symptoms
    Clinical experience in the treatment of overdose has not been accumulated to date, but it is assumed that the overdose of the drug substance Formoterol Ishihler will be accompanied by symptoms commonly observed with an overdose of beta2-agonists: nausea, vomiting, headaches, tremor, drowsiness, palpitations, tachycardia, ventricular arrhythmias, increased / decreased blood pressure, metabolic acidosis, hypokalemia, hyperglycaemia.
    In a limited number of cases of overdose such symptoms as tachycardia, hyperglycaemia, hypokalemia, QT interval prolongation, arrhythmia, nausea and vomiting have been documented. Supporting and symptomatic therapy. In severe cases, the patient should be hospitalized. It is possible to use cardioselective beta-blockers, which requires extreme caution, since the use of beta-blockers can provoke the development of bronchospasm.
    It should be monitored the concentration of potassium in the blood serum.

    Interaction:
    Studies of specific interactions of the inhaler Formoterol Ishihler were not performed.
    An increase in the duration of the QT interval and an increased risk of developing ventricular arrhythmias can be observed with a number of QT prolonging drugs with eg quinidine, disopyramide, procainamide, sotalol, amiodarone, phenothiazines, some antihistamines (for example, terfenadine, astemizole, mizolastin), monoamine oxidase inhibitors, tricyclic antidepressants, erythromycin. Simultaneous use of other sympathomimetic drugs may increase the side effects of Formoterol Ishihler. The intake of levodopa, levothyroxine sodium, oxytocin and alkaloids can increase the side effect of beta2-adrenomimetics on the heart.
    In patients receiving monoamine oxidase inhibitors or tricyclic antidepressants, Formoterol Ishihler should be used with caution, since the effect of beta2-adrenomimetics on the cardiovascular system can be enhanced. Do not use Formoterol Ishihler for patients receiving monoamine oxidase inhibitors and for 14 days after discontinuation. Simultaneous reception of xanthine derivatives, glucocorticosteroids, diuretics can enhance the possible hypokalemic effects of beta2-adrenomimetics. Hypokalemia may increase the risk of cardiac arrhythmias on the background of treatment with digitalis preparations. The risk of arrhythmias increases with general anesthesia with halocarbons.Beta-blockers can weaken or eliminate the action of Formoterol Ishihler. Therefore, the drug should not be used simultaneously with beta-blockers (including in the eye drops), unless their use is justified by life indications. The simultaneous use of formoterol and glucocorticosteroids can lead to an increase in the hyperglycemic effect observed when taking these drugs.
    The broncholytic effect of formoterol can be enhanced by taking anticholinergic drugs.
    Special instructions:In patients with bronchial asthma, Formoterol Ishihler should be used only as an additional treatment for inadequate efficacy of inhaled glucocorticosteroids (in medium and small doses) or in severe form of the disease requiring the use of two maintenance therapies, including Formoterol Ishihler. When the drug is prescribed patients, not receiving anti-inflammatory therapy, it should be started simultaneously with the use of Formoterol Ishihler.
    Lesion of the kidneys and liver
    Data on the need to adjust the dose of the drug Formoterol Ishihler in patients with impaired renal or hepatic function.
    The duration of formoterol is about 12 hours. Treatment in all cases should be carried out with minimally effective doses of the drug.
    The current recommendations for the treatment of bronchial asthma indicate the need to use long-acting beta2-adrenomimetics for maintenance bronchodilator therapy in addition to therapy with glucocorticosteroids. In addition, they recommend the use of short-acting beta2-adrenomimetics in the event of an attack of bronchial asthma.
    Patients should be advised for the period of inclusion in the treatment regimen Formoterol Ishihler not to stop taking and not change the regimen of treatment with glucocorticosteroids, even if the symptoms of bronchial asthma have decreased.
    If the symptoms of the disease persist or worsen, or if the recommended dosages of Formoterol Ishihler do not allow them to be controlled (providing relief of seizures), this condition is usually a sign of worsening of the course of bronchial asthma and the need to revise the treatment regimen.
    The frequent need for medicines (ie preventive care, for example, glucocorticosteroids and beta2-adrenomimetics of prolonged action) to prevent bronchospasm during exercise several times a week, despite adequate supportive therapy may be a sign of inadequate control of asthma symptoms and requires a review of anti-asthmatic treatment and an assessment of its compliance. When transferring patients to therapy with inhaler Formoterol Ishihler from other inhalers, the treatment regimen should be selected individually. In this case, it is necessary to take into account the features of the previously used drug, treatment regimens, methods of application drug substance.
    In patients with cirrhosis of the liver, an increase in excretion is expected; formoterol initially eliminated through hepatic metabolism.
    The Ishidler inhaler is controlled by the flow of air formed on the inhalation, which means that when the patient inhales air through the mouthpiece, the drug enters the respiratory tract along with the inhaled air.
    Note: it is important to teach the patient to inhale through the mouthpiece quite actively and deeply, in order to ensure the optimal dose of the drug in the bronchial tissue.
    If a patient needs regular admission of prolonged beta2-adrenomimetics, he should also receive regular and sufficient doses systematic anti-inflammatory treatment (inhalation or oral glucocorticosteroids). Formoterol Ishihler should be used only in patients who require prolonged therapy with bronchodilators. In the case of an attack of bronchial asthma, it is recommended that short-range beta2-adrenomimetics.
    When prescribing the drug, it is necessary to assess whether the activity of the anti-inflammatory therapy administered to the patient is sufficient.
    During an exacerbation of a current of a bronchial asthma therapy
    inhaler should not be started. Care should be taken when use of Formoterol Ishiheler and theophylline to patients with heart disease.
    Given the ability of beta2-adrenomimetics to cause
    hyperglycaemia, in patients with diabetes it is recommended to carry out additional control of the concentration of glucose in the blood.
    With therapy beta2-adrenomimetics can lead to life-threatening hypokalemia. Particular caution should be exercised in severe exacerbations of bronchial asthma, since the risk of hypokalemia at This increases against the background of the developing hypoxia.
    Hypokalemic action can be enhanced by simultaneous therapy with xanthine derivatives, glucocorticosteroids and diuretics. In these cases, it is recommended to monitor the potassium concentration in the blood serum.
    As with other types of inhalation therapy, one should not forget about the risk of developing paradoxical bronchospasm. If such bronchospasm develops, the drug should be stopped immediately, replacing it with an alternative treatment. Each dose of Formoterol Ishihler contains about 8 mg of lactose. Usually, this amount of lactose in individuals suffering from lactose intolerance does not cause clinical manifestations.
    The drug should not be used for persons with lactase deficiency, lactose intolerance and glucose-galactose malabsorption.

    Effect on the ability to drive transp. cf. and fur:

    Tremor or anxiety arising during treatment with beta-adrenostimulants can affect a patient's ability to drive.

    Form release / dosage:

    Powder for inhalation dosed. 12 mcg - 120 doses.


    Packaging:1.7 g of the powder of the preparation is placed in an inhaler from a polymeric material. Each inhaler, hermetically packed in a foil bag of aluminum laminated, together with the instruction for use, is placed in a pack of cardboard
    Storage conditions:

    Store at a temperature not exceeding 30 ° C, in a dry place inaccessible to children.

    Shelf life:

    2 years.

    After opening the aluminum bag, use it for 4 months.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-002226
    Date of registration:30.09.2011
    The owner of the registration certificate:Orion Corporation Orion Pharma Orion Corporation Orion Pharma Finland
    Manufacturer: & nbsp
    Information update date: & nbsp27.10.2015
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