Foradyl - instructions for use, analogs, reviews and release forms (capsules with powder for inhalation of 12 mcg, 12 mcg + 200 mcg or 400 mcg Combi with budesonide) for the treatment of bronchial asthma in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Foradyl. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Foradil in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Foradil in the presence of existing structural analogues. Use for the treatment of bronchial asthma, chronic obstructive pulmonary disease or COPD in adults, children,as well as during pregnancy and lactation. Composition of the preparation.

Foradyl - beta-adrenomimetic. Acts primarily on beta2-adrenergic receptors. It has a bronchodilator effect, it stops and prevents bronchospasm. Inhibits the release of histamine, leukotrienes and prostaglandin D2 from mast cells, basophils and sensitized bronchoalveolar tree cells.

Formoterol

Selective beta2-adrenergic receptor agonist. It has a bronchodilator effect in patients with both reversible and irreversible airway obstruction. The effect of the drug occurs quickly (within 1-3 minutes) and persists for 12 hours after inhalation. When the drug is used in therapeutic doses, the effect on the cardiovascular system is minimal and is noted only in rare cases.

It 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.

Clinical studies have shown that the drug effectively prevents bronchospasm caused by inhaled allergens, physical activity, cold air, histamine or methacholine.As the bronchodilator effect of formoterol remains pronounced within 12 hours after inhalation, the administration of the drug 2 times a day for prolonged maintenance therapy allows in most cases to provide the necessary control of bronchospasm in chronic lung diseases both during the day and at night.

In patients with COPD of stable course, formoterol causes a rapid onset of bronchodilator effect and improvement of quality of life parameters.

Budesonide

Budesonide is a glucocorticosteroid (GCS) for inhalation, with little or no systemic effect. Like other inhaled corticosteroids, Budesonide exerts pharmacological effects through interaction with intracellular glucocorticoid receptors.

Budesonide has anti-inflammatory, anti-allergic and immunosuppressive effects. Increases the production of lipocortin, which is an inhibitor of phospholipase A2, inhibits the release of arachidonic acid, inhibits the synthesis of metabolic products of arachidonic acid-cyclic endoperoxides and prostaglandins.It prevents the accumulation of neutrophils, reduces inflammation and cytokine production, inhibits the migration of macrophages, reduces the intensity of infiltration and granulation processes, the formation of a chemotaxis substance (which explains the effectiveness of "late" allergy reactions); inhibits the release of mast cells from inflammatory mediators (immediate allergic reaction). Increases the number of "active" beta-adrenergic receptors, restores the patient's response to bronchodilators, reducing the frequency of their use, reduces edema of the bronchial mucosa, mucus production, sputum formation and reduces airway hyperreactivity. Increases mucociliary transport.

The therapeutic effect of the drug in patients requiring treatment with GCS, develops on average within 10 days after the initiation of therapy. With regular use in patients with bronchial asthma budesonide reduces the severity of chronic inflammation in the lungs, and thus improves pulmonary function, the course of bronchial asthma, reduces the hyperreactivity of the bronchi and prevents exacerbations of the disease.

Composition

Formoterol fumarate dihydrate + excipients (foradyl).

Formoterol fumarate dihydrate + budesonide + excipients (Foradyl Combi).

Pharmacokinetics

Formoterol

In studies that studied the total excretion of formoterol and its (R, R) - and (S, S) enantiomers in urine, 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 application of formoterol at a dose of 12 μg or 24 μg twice a day for 12 weeks, the 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 accumulation of one of the enantiomers of formoterol compared to others after repeated inhalations. Just as it was reported for other drugs used as inhalants, most of the formoterol used with the inhaler will be swallowed and then absorbed from the digestive tract. When 80 μg of 3H-labeled formoterol was administered to the two healthy volunteers, at least 65% of formoterol was absorbed.formoterol Binding to plasma proteins is 61-64% (Albumin - 34%). In the range of concentrations observed after application of the drug in therapeutic doses, saturation of binding sites is not achieved.

The main route of metabolism is formoterol direct conjugation with glucuronic acid. Another way of metabolism is O-demethylation followed by glucuronization.

The secondary metabolic pathway include conjugation formoterol sulphate, followed by deformylation. The set of isozymes involved in the glucuronidation (UGT1A1, 1A3, 1A6, 1A7, 1A8, 1A9, 1A10, 2B7 and 2B15) and O-demethylation (CYP2D6, CYP2C19, CYP2C9, CYP2A6) formoterol, which involves a low probability of drug-drug interactions by inhibiting kakogo- or isoenzyme, taking part in the metabolism of formoterol. In therapeutic concentrations, formoterol does not inhibit the isoenzymes of the cytochrome P450 system.

Patients with bronchial asthma and COPD is treated with formoterol fumarate in a dose of 12 mg or 24 mg 2 times a day for 12 weeks, about 10% or 7%, respectively, determined in the urine as unchanged formoterol. Calculated shares(R, R) - and (S, S) -enantiomers of formoterol unchanged in urine are 40% and 60%, respectively, after a single dose of formoterol (12-120 .mu.g) in healthy volunteers after single and repeated doses of formoterol in asthmatic patients.

The active substance and its metabolites are completely eliminated from the body: 70% by the kidneys, 30% through the intestine.

After correction for body weight, the pharmacokinetic parameters of formoterol in men and women do not differ significantly.

The pharmacokinetics of formoterol in elderly patients aged 65 years and older have not been studied.

In a clinical trial in children aged 5-12 years with asthma treated with formoterol fumarate at a dose of 12 mg or 24 mg 2 times a day for 12 weeks, urinary excretion of unchanged formoterol increased by 18-84% compared with the corresponding indicator , measured after the first dose.

In clinical studies in children in urine was determined about 6% of unchanged formoterol.

Budesonide

Budesonide is quickly and completely absorbed after inhalation. After inhalation budesonide taking into account the sedimentation of the drug on the mucous membrane of the oropharynx absolute bioavailability is 73%. Binding to plasma proteins - 88%.In experimental studies, budesonide accumulated in the spleen, lymph nodes, thymus gland, adrenal cortex, reproductive organs and bronchi, and also penetrated the placental barrier.

Budesonide is not metabolized in the lungs. After absorption, the drug is almost completely (about 90%) metabolized in the liver with the formation of several inactive metabolites (biological activity is 100 times less than budesonide), including 6-hydroxybudesonide and 16alpha-hydroxy-prednisolone. The main pathway of budesonide metabolism in the liver with the CYP3A4 isoenzyme of the P450 system can be altered by inhibitors or inducers of CYP3A4.

Output through the intestine in the form of metabolites - 10%, kidneys - 70%.

The concentration of budesonide in the blood plasma is increased in patients with liver disease.

The pharmacokinetics of budesonide in children and adolescents has not been studied. However, data on other inhaled drugs containing budesonide suggest that budesonide clearance in children over 3 years is approximately 50% higher than in adult patients.

Indications

Bronchial asthma:

insufficiently controlled by the intake of inhaled glucocorticosteroids (GCS) and beta2-agonists of short action as therapy on demand;
adequately controlled by inhaled GCS and long-acting beta2-agonists;
prevention and treatment of bronchospasm in patients with obstructive bronchitis, bronchial asthma.

Chronic obstructive pulmonary disease (COPD) (with proven efficacy of GCS).

Forms of release

Capsules with powder for inhalation 12 mcg with device for inhalation (aerolaser).

A set of capsules with powder for inhalation 12 μg + 200 μg, 12 μg + 400 μg with device for inhalation (airlaser) (Foradyl Combi).

Instructions for use and dosing regimen

Foradyl

Inhalation.

It is intended for inhalation in adults and children 5 years and older. The drug is not intended for oral administration.

The dose of the drug is selected individually, depending on the needs of the patient. Use the smallest dose that provides a therapeutic effect. When you reach the control of symptoms of bronchial asthma on the background of therapy with the drug Foradil, you should consider the possibility of a gradual decrease in the dose of the drug. Dose reduction is carried out under regular medical supervision of the patient's condition.

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

Adults

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

Foradyl should be used only as an adjunct to inhaled glucocorticosteroids.

Do not exceed the maximum recommended dose of the drug for adults (48 mcg per day). Considering that the maximum daily dose of Foradyl is 48 mcg, if necessary, 12-24 mcg per day can be used additionally to relieve the symptoms of bronchial asthma.

If the need to apply additional doses of the drug ceases to be episodic (for example, it becomes more frequent than 2 days a week), the patient should be advised to consult a doctor for revision of therapy, this may indicate a worsening of the course of bronchial asthma.

Against the background of exacerbation of bronchial asthma, do not start treatment with Foradyl or change the dosage. The drug Foradil should not be used to stop acute attacks of bronchial asthma.

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

Patients with severe bronchospasm in the history for prevention may need to inhalate the contents of 2 capsules (24 μg).

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

Children 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, the use of combined drugs containing inhaled glucocorticosteroids and a long-acting beta2-adrenoreceptor agonist is recommended, with the exception of cases of their separate use.

Instructions for inhalation

In order to ensure proper use of the drug, the doctor or other health care provider should show the patient how to use the inhaler; explain to the patient that it is necessary to use capsules with powder for inhalations only with the help of an air-conditioner; warn the patient that the capsules are for inhalation use only and are not intended for ingestion.

Children should use the drug under the supervision of adults.

It is important that the patient understands that, due to the destruction of the gelatin capsule, small pieces of gelatin can be inhaled into the mouth or throat. In order to minimize this phenomenon to a minimum, you should not pierce the capsule more than 1 time. Remove the capsule from the blister pack immediately before use. 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 apply the medication correctly, especially if the patient does not get better breathing after inhalations.

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.

Instruction for the use of an air-conditioner

1. Remove the cap from the air conditioner.

2. Hold the airlighter firmly by the base and rotate the mouthpiece in the direction of the arrow.

3. Place the capsule in the cell located at the base of the airlighter (it has the shape of a capsule). It must be remembered that you need to remove the capsule from the blister pack immediately before the inhalation.

4. Turn the mouthpiece and close the air conditioner.

5. Holding the airlighter in a strictly vertical position, press the end of the blue buttons one after the other on the blue buttons on the sides of the airlighter. Then let them go.

Note. At this stage, when piercing the capsule, it can collapse, causing small pieces of gelatin to enter the mouth or throat. Since gelatin is edible, it will not do any harm. To ensure that the capsule does not completely break down, the following requirements should be met: do not puncture the capsule more than 1 time; observe the rules of storage; Remove the capsule from the blister just before the inhalation.

6. It is necessary to make a full exhalation.

7.You should take the mouthpiece in your mouth and throw your head back slightly. Tightly grasp the mouthpiece with your lips and make a quick, uniform, maximum deep breath. There must be a characteristic rattling sound created by rotating the capsule and spraying the powder. If there is no characteristic sound, then you should open the air-lift and see what happened to the capsule. Perhaps she was stuck in the cell. In this case, you need to carefully remove the capsule. In no case should you try to release the capsule by repeatedly pressing the buttons on the sides of the airlighter.

8. If a characteristic sound has arisen upon inhalation, it is necessary to hold your breath as long as possible. At the same time, you should take the mouthpiece out of your mouth. Then exhale. Open the air conditioner and see if the powder remained in the capsule. If the powder remains in the capsule, repeat the actions described in paragraphs 6-8.

9. After the end of the inhalation procedure, it is necessary to open the air-lift, take out the empty capsule, close the mouthpiece and air-cap with a cap.

Care of the air-conditioning device: to remove powder residues, wipe the mouthpiece and cell with a dry cloth. You can also use a soft brush.

Foradil Combi

Formoterol and budesonide are intended for inhalation use. Preparations are capsules with powder for inhalation, which should be used only with the help of a special device - the air-bottle, which is included in the package.

Formoterol and budesonide should be administered individually, at the lowest effective dose.

When you reach the control of symptoms of bronchial asthma on the background of therapy with formoterol, you should consider the possibility of a gradual decrease in the dose of the drug. Reduction of the dose of formoterol is carried out under regular medical supervision of the patient's condition. Against the background of exacerbation of bronchial asthma should not begin treatment with formoterol or change the dosage of the drug. Formoterol should not be used to stop acute attacks of bronchial asthma.

When a patient is prescribed therapy with an inhalation device, the dose of the drug should be gradually selected (titrated) to a dose sufficient to maintain a therapeutic effect.

Budesonide + formoterol

Adults

Preliminary inhalation of beta-adrenostimulants expands bronchi, improves the flow of budesonide into the respiratory tract and enhances its therapeutic effect.Therefore, for maintenance therapy of bronchial asthma and COPD, first inhalation of formoterol, then - inhalation budesonide.

1. The dose of formoterol for regular maintenance therapy is 12-24 μg (1-2 capsules) 2 times a day. Do not exceed the maximum recommended dose of the drug for adults (48 mcg per day).

Given that the maximum daily dose of formoterol is 48 μg, if necessary, you can additionally apply 12-24 μg per day to alleviate the symptoms of bronchial asthma. If the need to apply additional doses of the drug ceases to be episodic (for example, it becomes more frequent than 2 days a week), the patient should be advised to consult a doctor for revision of therapy, this may indicate a worsening of the course of the disease.

2. The minimum dosage of budesonide in one capsule is 200 μg. The drug is not prescribed if a single dose of less than 200 μg is required. In adults with mild bronchial asthma, treatment with a minimum effective dose of 200 μg per day can be started.

The maintenance dose of budesonide for adult patients is 400-800 μg per day in 2 divided doses (200-400 μg twice a day).

With exacerbation of bronchial asthma during the transfer from oral GCS to inhaled or with a decrease in the dose of oral GCS, budesonide can be administered at a dose of 1600 μg per day in 2-4 doses.

Children aged 6 years and over

Preliminary inhalation of beta-adrenostimulants expands bronchi, improves the flow of budesonide into the respiratory tract and enhances its therapeutic effect. Therefore, for maintenance therapy of bronchial asthma, first inhalation of formoterol, then - inhalation budesonide.

1. The dose of formoterol for regular maintenance therapy is 12 μg 2 times a day. The maximum recommended dose of the drug is 24 μg per day.

2. Treatment of children with mild bronchial asthma begins with a dose of 200 mcg per day. The dose of budesonide for regular maintenance therapy is 100-200 μg 2 times a day. If necessary, the dose of budesonide can be increased to a maximum of 800 μg per day.

Due to the lack of clinical experience in children younger than 6 years of age, budesonide should not be used in this age group.

Patients with impaired renal function

Data on the need for dose adjustment in patients with impaired renal function have not been obtained.Based on the pharmacokinetics of budesonide for oral administration, it is unlikely that a clinically significant systemic effect of the drug is possible in such patients.

Patients with impaired hepatic function

Data on the need for dose adjustment in patients with impaired liver function was not obtained. But budesonide is metabolized mainly in the liver. Therefore, the drug should be used with caution in patients with severe impairment of liver function. In patients with mild or moderate impairment of liver function, a significant change in the effect of the drug, taking into account the pharmacokinetic parameters for budesonide for oral administration, is unlikely.

Patients of advanced age (over 65 years)

Data on the need for dose adjustment in patients older than 65 years, compared with younger patients, is not obtained.

Rules of inhalation

In order to ensure the correct use of drugs, the doctor or other health care provider should show the patient how to use the inhaler; explain to the patient that it is necessary to use capsules with powder for inhalations only with the help of an air-conditioner; warn the patient that the capsules are for inhalation use only and are not intended for ingestion.In children and adolescents inhalation budesonide and formoterol should be carried out under the supervision of adults. It is necessary to make sure that the child correctly performs the technique of inhalation.

It is important that the patient understands that, due to the destruction of the gelatin capsule, small pieces of gelatin can be inhaled into the mouth or throat. In order to reduce this phenomenon to a minimum, do not pierce the capsule more than 1 time.

Remove the capsule from the blister pack immediately before use.

Rinsing the oral cavity with water after inhalation budesonide can prevent irritation of the oral and pharyngeal mucosa, as well as reduce the risk of developing systemic adverse events.

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 apply the medication correctly, especially if the patient does not get better breathing after inhalations.

Side effect

Formoterol

hypersensitivity reactions, such as arterial hypotension, urticaria, angioedema, itching, rash;
sense of anxiety;
increased excitability;
insomnia;
headache;
tremor;
dizziness;
violation of taste;
a feeling of palpitations;
tachycardia;
peripheral edema;
bronchospasm, including paradoxical;
irritation of the mucous membrane of the pharynx and larynx;
dryness of the oral mucosa;
nausea;
muscular spasm;
myalgia;
cough;
hypokalemia, hyperglycemia;
prolongation of the QT interval (during ECG);
increased blood pressure (including arterial hypertension);
angina pectoris;
heart rhythm disturbances, incl. Atrial fibrillation, ventricular extrasystoles, tachyarrhythmia.

Budesonide

suppression of adrenal cortex function;
Cushing's syndrome;
hypercorticism;
growth retardation in children and adolescents;
cataract;
glaucoma;
hypersensitivity reaction including rash, urticaria, angioedema, pruritus, contact dermatitis;
psychomotor hyperactivity;
sleep disorders;
anxiety;
depression;
aggressive behavior;
behavioral disorders (especially in children);
decrease in bone mineral density;
cough;
paradoxical bronchospasm;
Candidiasis of the mucous membrane of the mouth and larynx;
irritation of pharynx;
dysphonia, disappearing after discontinuing therapy with budesonide or reducing the dose of the drug;
pneumonia.

Contraindications

lactation period (breastfeeding);
active pulmonary tuberculosis;
hereditary intolerance to galactose, severe lactase deficiency, and impaired glucose-galactose absorption syndrome;
children's age under 5 years (Foradil) and up to 6 years (Foradil Kombi);
hypersensitivity to formoterol, budesonide or any other component of the drug.

Application in pregnancy and lactation

In pregnancy and lactation, Foradil is used with caution, only in cases where the expected therapeutic effect for the mother exceeds the potential risk of side effects to the fetus or child.

The safety of Foradyl Combi use during pregnancy and lactation has not been established to date.

Use during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus. Formoterol, as well as other beta2-adrenomimetics, can slow the process of labor due to tocolytic action (a relaxing effect on the smooth muscles of the uterus).

It is not known whether formoterol is excreted in human breast milk. When taking Foradyla Combi, breastfeeding should be discontinued.

Fertility

There are no data on the effect of the drug on fertility. In experimental animal studies, there was no effect on fertility in oral administration of formoterol and subcutaneous administration of budesonide.

Use in children

Foradyl is contraindicated in children under 5 years of age. Foradyl Combi is contraindicated in children younger than 6 years.

special instructions

Particular caution and careful observation is required when it is necessary to use formoterol in patients with the following concomitant diseases: IHD; heart rhythm disturbances and conduction, especially AV blockade of the 3rd degree; severe heart failure; idiopathic subvalvular aortic stenosis; hypertrophic obstructive cardiomyopathy; thyrotoxicosis; known or suspected prolongation of the QT interval (QT adjusted more than 0.44 s).

Use with caution in patients with diabetes mellitus, myoma of the uterus.

Impact on the ability to drive vehicles and manage mechanisms

Tremor, or anxiety that occur during treatment with beta-agonists, may affect the patient's ability to drive a car, so the application of formoterol is not recommended to engage in potentially hazardous activities that require attention, rapid psychomotor reactions.

Data on the influence of budesonide on the ability to drive vehicles and work with mechanisms there. The negative effect of the drug on the ability to drive vehicles and work with mechanisms is unlikely.

Drug Interactions

Formoterol

Formoterol (as well as other beta2-adrenostimulyatorov) should be used with caution in patients taking drugs such as quinidine, disopyramide, procainamide, phenothiazines, antihistamines, macrolides, MAO inhibitors, tricyclic antidepressants, and other drugs which are known that they extend the QT interval, because 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 formoterol.

The simultaneous use of xanthine derivatives, GCS or diuretics can enhance the potential hypokalemic effects of beta2-adrenostimulants.

In patients receiving anesthesia using halogenated hydrocarbons, the risk of arrhythmia increases.

Beta-adrenoblockers can weaken the action of formoterol. In this regard, do not prescribe formoterol together with beta-blockers (including eye drops), unless the use of this combination of drugs is not forced for any extraordinary reasons.

Budesonide

The use of the drug together with CYP3A4 inhibitors (for example, itraconazole, ketoconazole, ritonavir, nelfinavir, amiodarone, clarithromycin) can lead to a decrease in budesonide metabolism and an increase in its systemic concentration. When budesonide is prescribed together with CYP3A4 inhibitors, the function of the adrenal cortex should be monitored regularly and, if necessary, the dose of budesonide should be changed.

When budesonide is used together with drugs inducing CYP3A4 (for example, rifampicin, phenobarbital, phenytoin),it is possible to increase the metabolism of budesonide and reduce its systemic concentration.

Methandrostenolone, estrogens strengthen the action of budesonide.

Analogues of the drug Foradil

Structural analogs for the active substance:

Atimos;
Oxys Turbuhaler;
Foradil Combi;
Formotherol Ishihler;
Formoterol native;
Formoterol fumarate;
Formoterol fumarate dihydrate.

Analogues on the curative effect (funds for the treatment of bronchial asthma):

Aldecin;
Aminophylline;
Arthromax;
Ascoril;
Asthmopent;
Atrovent;
Beklazone;
Beclomethasone aeronaut;
Benacorte;
Berlikort;
Berodual;
Berotek;
Bronal;
Bronchalamine;
Broncholitin;
Bronhosan;
Budesonide;
Ventolin;
Hydrocortisone;
Glycyrs;
Decortin;
Dexamethasone;
Diprospan;
Zaditen;
Intal;
Ipratropium bromide;
Kenakorth;
Kenalog;
Clenbuterol;
Cromogen;
Cromoglyn;
Xidifon;
Methylprednisolone;
Mistabrone;
Montelar;
Platyphylline;
Plibékot;
Polcortolone;
Prednisolone;
Pulmicort;
Pulmicort Turbuhaler;
Salbutamol;
Salmecort;
Salmeter;
Seretid;
Seredid Multidisk;
Symbicort Turbuhaler;
Taileed;
Theostat;
Theotard;
Triamcinolone;
Fenoterol;
Fliksotid;
Fortecortin;
Celeston;
Eladon;
Erespal;
Erispirus;
Eufillin;
Eufilong.

If there are no analogues of the medication for the active substance, you can go to the links below for diseases, from which the corresponding drug helps, and to look at the available analogs for therapeutic effects.

Used for the treatment of diseases: asthma, chronic obstructive pulmonary disease, bronchospasm, bronchial asthma, wretched