Foradyl (Foradil®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceFormoterolFormoterol
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    • Dosage form: & nbspcapsules with powder for inhalation
    Composition:

    1 capsule contains: active substance - formoterol fumarate 0.012 mg; adjuvant - lactose up to 25 mg.

    Description:

    Description: transparent colorless capsules, labeled CG on the lid and FXF on the body or CG on the body and FXF on the lid with black ink. The size capsule number 3. Contents of the capsule: white easily free-flowing powder.

    Pharmacotherapeutic group:bronchodilator - beta2-adrenergic selective
    ATX: & nbsp

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

    R.03.A.C.13   Formoterol

    Pharmacodynamics:
    Formoterol is a selective beta2 receptor agonist. It has a bronchodilator effect in patients with reversible airway obstruction. The effect of the drug occurs quickly (within 1-3 minutes) and persists for 12 hours after inhalation. With the use of therapeutic doses, the effect on the cardiovascular system is minimal and is noted only in rare cases.
    Foradyl inhibits the release of histamine and leukotrienes from mast cells. In animal experiments, some of the anti-inflammatory properties of formoterol have been shown, such as the ability to inhibit the development of edema and the accumulation of inflammatory cells.
    In experimental animal studies in vitro, it was shown that racemic formoterol and its (R, R) and (S, S) enantiomers are highly selective beta2 receptor agonists. (S, S) enantiomer was 800-1000 times less active than the (R, R) enantiomer and did not adversely affect the activity of the (R, R) enantiomer with respect to the effect on the smooth muscle of the trachea. No pharmacological evidence has been obtained for the advantage of using one of these two enantiomers, as compared to the racemic mixture.
    In studies conducted in humans, Foradil is shown to effectively prevent bronchospasm caused by inhaled allergens, physical activity, cold air, histamine or methacholine. Since the bronchodilator effect of Foradil remains expressed within 12 hours after inhalation, the administration of the drug 2 times a day for prolonged maintenance therapyallows in most cases to provide the necessary control of bronchospasm in chronic lung diseases both during the day and at night.
    In patients with chronic obstructive pulmonary disease (COPD) of stable course formoterol, used in the form of inhalations from the Aerolaser in doses of 12 or 24 μg 2 times a day, causes a rapid onset of bronchodilator effect, which lasts for at least 12 hours and is accompanied by an improvement in the quality of life parameters.

    Pharmacokinetics:
    The therapeutic dosage range of formoterol is from 12 μg to 24 μg 2 times a day. Data on pharmacokinetics of formoterol were obtained in healthy volunteers after inhalation of formoterol in doses above the recommended range and in COPD patients after inhalation of formoterol in therapeutic doses.
    Suction.
    After a single inhalation of formoterol fumarate at a dose of 120 μg to healthy volunteers formoterol quickly absorbed into the plasma, the maximum concentration of formoterol in plasma (Cmax) was 266 pmol / L and was reached within 5 minutes after inhalation.
    In patients with COPD who received formoterol in a dose of 12 or 24 μg twice a day for 12 weeks, the concentrations of formoterol in the plasma, measured after 10 minutes, 2 hours and 6 hours after inhalation, were in the ranges 11.5-25.7 pmol / L and 23.3-50.3 pmol / L, respectively.
    In studies in which the total excretion of formoterol and its (R, R) and (S, S) enantiomers in the urine was studied, it was shown that the amount of formoterol in the systemic blood flow increases in proportion to the amount of inhaled dose (12-96 μg).
    After inhalation of formoterol 12 or 24 μg twice a day for 12 weeks, excretion of unchanged formoterol in urine in patients with bronchial asthma increased by 63-73%, and in COPD patients - by 19-38%. This indicates a certain cumulation of formoterol in the plasma after multiple inhalations. At the same time, there was no greater cumulation of one of the enantiomers of formoterol compared to another after repeated inhalations.
    As was also reported for other drugs used as inhalants, most of the formoterol used with the inhaler will be swallowed and then absorbed from the gastrointestinal tract (GI tract).When 80 μg of 3H-labeled formoterol was administered, at least 65% of formoterol was absorbed into two healthy volunteers.
    Binding to blood plasma proteins and distribution.
    The binding of formoterol to plasma proteins is 61-64%, binding to serum albumin is 34%.
    In the range of concentrations noted after the application of therapeutic doses of the preparation, saturation of binding sites is not achieved.
    Metabolism.
    The main route of metabolism is formoterol direct conjugation with glucuronic acid. Another way of metabolism is O-demethylation followed by conjugation with glucuronic acid (glucuronidation).
    Low-value metabolic pathways include conjugation of formoterol with sulfate, followed by deforming. A variety of isoenzymes participate in the glucuronidation processes (UGT1A1, 1AZ, 1A6, 1A7, 1A8, 1A9, 1A10, 2B7 and 2B15) and O-demethylation of formoterol (CYP2D6, 2C19, 2C9 and 2A6), which implies a low probability of drug interaction, or isoenzyme, taking part in the metabolism of formoterol. In therapeutic concentrations formoterol It does not inhibit the isoenzymes of the cytochrome P450 system.
    Excretion.
    In patients with bronchial asthma and COPD who received formoterol fumarate at a dose of 12 or 24 μg twice daily for 12 weeks, approximately 10% or 7% of the dose, respectively, was determined in the urine as unchanged formoterol. The calculated proportions of (R, R) and (S, S) enantiomers of unchanged formoterol in urine are 40% and 60%, respectively, after a single dose of formoterol (12-120 μg) in healthy volunteers and after single and repeated doses of formoterol in patients with bronchial asthma.
    The active substance and its metabolites are completely eliminated from the body; about 2/3 of the applied dose is excreted in the urine, 1/3 - with feces. The renal clearance of formoterol is 150 ml / min.
    In healthy volunteers, the final half-life of formoterol from plasma after a single inhalation of formoterol fumarate at a dose of 120 μg is 10 hours; the final half-lives of the (R, R) and (S, S) enantiomers calculated from excretion in the urine were 13.9 and 12.3 hours, respectively.
    Pharmacokinetics in selected patient groups
    Floor
    After adjusting for body weight, the pharmacokinetic parameters of formoterol in men and women do not differ significantly.
    Elderly patients
    The pharmacokinetics of formoterol in elderly patients have not been studied.
    Pediatrics
    In a clinical study in children aged 5-12 years with bronchial asthma who received formoterol fumarate at a dose of 12 or 24 μg twice a day for 12 weeks, the excretion of unchanged formoterol with urine increased by 18-84% compared with the corresponding index, measured after the first dose.
    In clinical studies in children in urine was determined about 6% of unchanged formoterol.
    Patients with impaired hepatic and / or renal function
    The pharmacokinetics of formoterol in patients with impaired hepatic and / or renal function have not been studied.

    Indications:
    • Prevention and treatment of violations of bronchial patency in patients with bronchial asthma as a supplement to therapy with inhaled glucocorticosteroids.
    • Prevention of bronchospasm caused by physical exertion, cold air or inhalation of allergens as a supplement to therapy with inhaled glucocorticosteroids
    • Prevention and treatment of bronchial obstruction in patients with chronic obstructive pulmonary disease (COPD), with both reversible and irreversible bronchial obstruction, chronic bronchitis and emphysema
    Contraindications:
    • Hypersensitivity to any of the components of the drug.
    • Children under 5 years.
    • Lactation.
    Carefully:
    If you have one of these diseases, always consult a doctor before using the drug.
    Accompanying illnesses
    Observance of extreme caution in the use of Foradil (especially in terms of dose reduction) and careful monitoring of patients is required in the presence of the following concomitant diseases: coronary heart disease; heart rhythm and conduction disorders, especially atrioventricular blockade III degree; severe heart failure; idiopathic hypertrophic subaortic stenosis; severe degree of arterial hypertension; aneurysm; pheochromocytoma; hypertrophic obstructive cardiomyopathy; thyrotoxicosis; known or
    suspected elongation of the QTc interval (QT corrected> 0.44 sec).
    Considering the hyperglycemic effect, characteristic of beta2-adrenomimetics, in patients sugar diabetes, taking Foradyl, additional regular monitoring of the concentration of glucose in the blood is recommended.


    Pregnancy and lactation:
    The safety of the use of formoterol in pregnancy and during breastfeeding has not been established to date.
    The use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus. Foradyl, as well as other beta2-adrenomimetics, can slow down the process of labor due to tocolytic action (a relaxing effect on the smooth muscles of the uterus).
    It is not known whether the formoterol in breast milk. Therefore, if you need to use Foradyl, breastfeeding should be stopped.
    There are no data on the effect of the drug on fertility. Studies on experimental animals showed no effect on fertility in oral administration of formoterol

    Dosing and Administration:

    Foradyl is intended for inhalation in adults and children aged 5 years and over. A drug not intended for oral administration. Dose preparation is selected individually in depending on the needs of the patient. The lowest dose should be used, providing a therapeutic effect. When you reach the control of symptoms bronchial asthma on the background of therapy Foradyl is necessary consider the possibility of a graduallowering the dose of the drug. Dose reduction Foradyl is administered regular medical supervision patient's condition.

    The preparation is a powder for inhalation, which should be used only with the help of a special device - the air-conditioner, which enters in the package.

    Adults

    When bronchial asthma drug dose for regular maintenance therapy is 12-24 μg (the contents of 1-2 capsules) 2 times a day.

    Foradyl should be used only as an adjunctive therapy to inhaled glucocorticosteroids. Do not exceed the maximum recommended dose of the drug for adults (48 mcg per day).

    Given that the maximum daily dose Foradyl is 48 μg, If necessary, you can additionally apply 12-24 mcg per day for relief of symptoms of bronchial asthma asthma. If the need for application additional doses of the drug ceases be episodic (for example, it becomes more often than 2 days a week), should recommend to the patient consult your doctor for revision of therapy, as this may point to a deterioration in the course bronchial asthma.

    Na background of exacerbation of bronchial asthma do not start drug treatment Foradyl or change the dose of the drug. Foradyl should not be used for relief of acute attacks of bronchial asthma.

    In order to prevent bronchospasm, caused by physical exertion or inevitable impact of the well-known allergen, 15 minutes before the alleged contact with the allergen or before the load should be inhaled 12 μg drug (the contents of 1 capsule). Patients with severe bronchospasm in the history for prevention may need to inhalate the contents of 2 capsules (24 mcg).

    With COPD, the dose of the drug for regular maintenance therapy is 12-24 μg (1-2 capsules) twice a day.

    Children aged 5 years and over

    The maximum recommended dose of the drug is 24 μg per day.

    With bronchial asthma, the dose of the drug for regular maintenance therapy is 12 μg 2 times a day. Foradyl should be used only as an adjunct to inhaled glucocorticosteroids.

    In children from 5 to 12 years of age, the use of combination medicines containing inhalation

    a glucocorticosteroid and a long-acting beta2-adrenergic agonist, with the exception of the cases of their separate use.

    For the prevention of bronchospasm caused by physical exertion or the inevitable action of a known allergen, 15 capsules of the contents of 1 capsule (12 μg) should be inhaled 15 minutes before supposed contact with the allergen or before loading.

    Instructions for inhalation

    In order to ensure the correct use of the drug, a doctor or other the medical worker must show patient, how to use the inhaler; explain to the patient what to apply capsules with powder for inhalation It is only with the help of the Airlighter; warn the patient that capsules intended only for inhalation application, and are not designed for swallowing.

    Children should use the drug for supervision of adults.

    Elderly patients (over 65 years of age) Data in favor of the need to use the drug in a different dose in patients older than 65 years compared with younger patients is not obtained.

    It is important that the patient understands that because of destruction of the gelatin capsule small pieces of gelatin as a result of Inhalation can get into the mouth or throat.

    In order to reduce this phenomenon to minimum should not be pierced capsule more than 1 time.

    Remove the capsule from the blister pack follows immediately before application. (See also the application of the air-conditioner).

    There are separate reports of accidental ingestion of whole capsules by the patients. Most of these cases are not associated with the development of adverse events. The health worker should explain to the patient how to correctly apply the medication, especially if after inhalation the patient does not have an improvement in breathing.


    Side effects:

    Unwanted reactions (N / A) distributed according to frequency occurrence. To estimate the frequency the following criteria were used: very often (> 1/10); often (from> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10000, <1/1000); very rarely (<1/10000), including individual messages.

    Disorders from the immune system system: very rarely - reactions increased sensitivity, such as lowering blood pressure, urticaria, angioedema, itching, rash.

    Disorders of the psyche: rarely - agitation, anxiety, increased excitability, insomnia.

    Impaired nervous system: often - headache, tremor; infrequently - dizziness; very rarely - violations taste.

    Heart Disease: often - a feeling of palpitations; infrequently - tachycardia; very rarely - peripheral edema.

    Disturbances from respiratory system, chest organs and mediastinum: infrequently - bronchospasm, including paradoxical.

    General disorders and disorders in place introduction: infrequent - irritation of the mucosa the pharynx and larynx.

    Disorders from the gastro-intestinal tract: infrequent - dryness of the oral mucosa; very rarely - nausea.

    Disorders from the side of the skeletal-muscular and connective tissue: infrequently - muscle spasm, myalgia.

    According to post-marketing observations when prescribing the drug Foradyl, the following AEs were noted, frequency of which due to a small number of patients was regarded as "frequency unknown":

    Laboratory and instrumental data: hypokalemia and hyperglycemia, interval lengthening QT on electrocardiogram, increase blood pressure (including arterial hypertension).

    Disturbances from respiratory system, chest organs and mediastinum: cough.

    Disturbances from the skin and subcutaneous fabrics: rash.

    Heart Disease: angina, disturbance of the heart rhythm (including atrial fibrillation, ventricular extrasystoles, tachyarrhythmia).

    In clinical studies with the use of formoterol, there was a slight increase in the incidence of serious exacerbations of bronchial asthma compared with placebo. However, the results of the above clinical studies do not allow a quantitative assessment of the incidence of serious exacerbations of bronchial asthma in various groups.

    If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.


    Overdose:
    Symptoms. An overdose of Foradyl can probably lead to the development of phenomena characteristic of an overdose of beta2-adrenomimetics or an increase in the manifestations of side effects: chest pain, nausea, vomiting, headache, tremor,drowsiness, palpitations, tachycardia up to 200 beats / min, ventricular arrhythmias, metabolic acidosis, hypokalemia, hyperglycemia, increased or decreased blood pressure, nervousness, convulsions, muscle cramps, dry mouth, dizziness, weakness, anxiety. As for all inhalation sympathomimetics, with an overdose of the drug Foradil, cardiac arrest and fatal outcome are possible.
    Treatment. Showing supportive and symptomatic therapy. Serious cases require hospitalization.
    Cardioselective beta-blockers may be considered, but only under careful medical supervision, provided extreme caution is observed, since the use of such drugs can cause bronchospasm.
    Recommended control of cardiac activity.

    Interaction:
    Foradyl, as well as other beta2-adrenomimetics, should be administered with caution to patients receiving such medicines as quinidine, disopyramide, procainamide, phenothiazines, antihistamines, macrolides, monoamine oxidase inhibitors (MAO), tricyclic antidepressants,as well as other drugs that are known to prolong the QT interval, since in these cases the action of adrenostimulators on the cardiovascular system can be enhanced. When using drugs that can extend the QT interval, the risk of ventricular arrhythmias increases.
    Simultaneous use of other sympathomimetic drugs can lead to aggravation of side effects of Foradil.
    Simultaneous use of xanthine derivatives, glucocorticosteroids or diuretics can strengthen the potential hypokalemic effects of beta2-adrenomimetics.
    In patients receiving anesthesia using halogenated hydrocarbons, the risk of arrhythmia increases.
    Beta-adrenoblockers can weaken the effect of Foradil. In this regard, do not use Foradyl together with beta-blockers (including eye drops), unless the use of this combination of drugs is not forced to any extraordinary reasons.


    Special instructions:

    Patients with increased sensitivity to lactose should consider that the preparation contains lactose.

    Foradyl belongs to the class of beta2-adrenergic agonists of long-acting.Against the background of other beta2-adrenergic agonist is a long-acting (salmeterol) showed an increase in the frequency of deaths associated with bronchial asthma (13 of the 13 176 patients) compared to placebo (3 patients from the 13179). Clinical studies to assess the incidence of lethal outcomes associated with bronchial asthma, against the background of the use of Foradil was not carried out.

    It is shown that the quality of life of COPD patients improves with the use of Foradil.

    Anti-inflammatory therapy in patients with bronchial asthma Foradil should only be used as an additional treatment for the symptoms of lack of control on monotherapy with inhaled corticosteroids or severe diseases, requiring

    the use of a combination of an inhaled glucocorticosteroid and a long-acting beta2-adrenoreceptor agonist. Do not use the drug with other agonists beta2-adrenergic receptors of long-acting.

    When administering Foradyl, it is necessary to assess the condition of patients with regard to the adequacy of the anti-inflammatory therapy that they receive.After starting treatment with Foradil, patients should be advised to continue the anti-inflammatory therapy without changes, even if improvement is noted.

    For relief of an acute attack of bronchial asthma should be applied agonists of beta2-adrenergic receptors. When sudden worsening of the condition patients must immediately apply for medical care.

    Severe exacerbations of bronchial asthma

    In clinical trials with application of formoterol was noted a slight increase in the frequency of development severe exacerbations of bronchial asthma compared with placebo, especially in children 5-12 years.

    In placebo-controlled clinical studies in patients who received formoterol for 4 weeks, increased frequency of development severe exacerbations of bronchial asthma (0.9% with the dosing regimen of 10-12 μg 2 once a day, 1.9% - at 24 μg 2 times in day) compared with the placebo group (0.3%), especially in children 5-12 years old.

    Hypokalemia

    The consequence of beta2-adrenomimetics, including Foradyl, can be the development of a potentially severe hypokalemia. Hypokalemia may increase the risk of arrhythmias.

    Since this action of the drug may hypoxia and associated treatment, extra care should be taken observe patients with bronchial asthma heavy current. In these cases regular monitoring is recommended concentration of potassium in the blood serum.

    Paradoxical bronchospasm

    As well as in the conduct of another Inhalation therapy should be considered the possibility of developing a paradoxical bronchospasm. If it occurs, it should be immediately cancel the drug and appoint alternative treatment.

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

    Patients who experience dizziness or other disturbances from the central nervous system, should refrain from driving or working with machinery during the period of application of the drug against the background of Foradyl.

    Form release / dosage:
    Capsules with powder for inhalation, 12 μg
    Packaging:
    10 capsules in a blister pack. 3 or 6 blisters together with the instructions for use and the device for inhalation of the air conditioner in a cardboard box.

    Storage conditions:
    At a temperature of no higher than 25 ° C. Protect from moisture.
    Keep out of the reach of children.

    Shelf life:
    2 years
    The drug should not be used after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:P N008952
    Date of registration:02.04.2010
    The owner of the registration certificate:Novartis Pharma AGNovartis Pharma AG Switzerland
    Manufacturer: & nbsp
    Information update date: & nbsp28.10.2015
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