Formoterol fumarate dihydrate,
Foradil Combi is a combined bronchodilator containing topical corticosteroids for local use and selective beta2-adrenostimulator, which exhibit an additive effect in reducing the frequency of exacerbations of bronchial asthma.
Budesonide is an inhaled GCS, at the recommended doses it has an anti-inflammatory effect (has a lower frequency of side effects than systemic GCS). Formoterol is a selective beta2-adrenergic receptor agonist that causes relaxation of the smooth muscles of the bronchi in patients with reversible airway obstruction.
The bronchodilator effect occurs quickly, within 1-3 minutes after inhalation, and persists for 12 hours after single dose inhalation.
The addition of formoterol to budesonide reduces the severity of symptoms of bronchial asthma, improves bronchial function and reduces the frequency of exacerbations of the disease.
The effect on the function of the bronchi corresponds to that of a combination of the single drugs budesonide and formoterol and exceeds the effect of one budesonide. The drug has good tolerance.
Bronchial asthma: - insufficiently controlled by inhaled corticosteroids and beta 2 -agonists of short action as therapy on demand; - adequately controlled by inhaled corticosteroids and beta 2 long-acting agonists.
Chronic obstructive pulmonary disease (COPD) (with proven efficacy of GCS).
-period of lactation (breastfeeding);
active pulmonary tuberculosis;
- hereditary galactose intolerance, severe lactase deficiency and impaired glucose-galactose absorption syndrome;
- children under 6 years old;
- Increased sensitivity to formoterol, budesonide or any other component of the drug.
Adverse reactions observed in clinical trials are distributed according to frequency of occurrence. The following criteria were used to evaluate the frequency: very often (≥ 1/10); often (from ≥ 1/100, <1/10); sometimes (≥ 1/1000, <1/100); rarely (≥ 1/10 000, <1/1000); very rarely (<1/10 000), including single messages.
Within each group, adverse events are distributed in decreasing order of importance. - Formoterol Allergic reactions: very rarely - hypersensitivity reactions, such as arterial hypotension, urticaria, angioedema, itching, exanthema.
From the side of the central nervous system: often - headache, tremor; sometimes - agitation, anxiety, irritability, insomnia, dizziness.
From the cardiovascular system: often - a feeling of palpitations; sometimes tachycardia; very rarely - peripheral edema.
From the respiratory system: sometimes - bronchospasm, including paradoxical, irritation of the mucous membrane of the pharynx and larynx.
From the digestive system: very rarely - nausea, taste disturbances.
From the musculoskeletal system: sometimes - cramps in the muscles, myalgia.
The following side effects were identified with the use of other dosage forms, which include formoterol: cough and rash. When using formoterol in clinical practice, the following changes in laboratory results were noted: hypokalemia, hyperglycemia, lengthening of the QT interval (during ECG). - budesonide
From the endocrine system: rarely - suppression of adrenal cortex function, Cushing's syndrome, hypercorticism, growth retardation in children and adolescents.
From the side of the organ of vision: rarely - cataract, glaucoma. Allergic reactions: rarely - hypersensitivity reactions, rash, urticaria, angioedema, itching.
From the side of the central nervous system: rarely - unusual behavior, including depression (described in children).
From the musculoskeletal system: a decrease in the mineral density of bone tissue.
From the respiratory system: often - cough; rarely - paradoxical bronchospasm, candidiasis of the mucous membrane of the oral cavity and larynx, pharyngeal irritation, dysphonia, disappearing after discontinuation of budesonide therapy or a decrease in the dose of the drug.
In a three-year clinical study using budesonide in patients with COPD, an increase in the incidence of subcutaneous hematomas (10%) and pneumonia (6%) was observed compared with the placebo group (4% and 3%)
- Formoterol Formoterol (like other beta2-adrenostimulants) should be used with caution in patients receiving drugs such as quinidine, disopyramide, procainamide, phenothiazines, antihistamines, MAO inhibitors, tricyclic antidepressants, as well as other drugs known to be they lengthen the QT interval, because in these cases, the effect of adrenostimulants on the cardiovascular system may be enhanced.
When using drugs that can extend the QT interval, the risk of ventricular arrhythmias increases. The simultaneous use of other sympathomimetic agents can lead to aggravation of side effects of formoterol. The simultaneous use of xanthine derivatives, corticosteroids, or diuretics can enhance the potential hypokalemic effect of beta2-adrenergic agonists. Hypokalemia may increase the predisposition to the development of cardiac arrhythmias in patients receiving digitalis preparations. Beta-blockers can weaken the effect of formoterol.
In this regard, formoterol should not be used in conjunction with beta-adrenergic blocking agents (including eye drops), unless any emergency causes are required to use such a combination of drugs. - Budesonide The use of the drug together with CYP3A4 inhibitors (for example, itraconazole, ketoconazole, ritonavir, nelfinavir, amiodarone, clarithromycin) can lead to a decrease in the metabolism of budesonide and an increase in its systemic concentration.
When prescribing budesonide along with CYP3A4 inhibitors, adrenal cortex function should be regularly monitored and, if necessary, change the dose of budesonide. When using budesonide together with drugs that induce CYP3A4 (for example, rifampicin, phenobarbital, phenytoin), an increase in the metabolism of budesonide and a decrease in its systemic concentration are possible. Methandrostenolone, estrogens enhance the effect of budesonide.
How to take, course of administration and dosage
Formoterol and budesonide are intended for inhalation use. The preparations are capsules with powder for inhalation, which should be used only with the help of a special device - an aerolizer, which is included in the package. Formoterol and budesonide should be administered individually at the minimum effective dose. When achieving control of symptoms of bronchial asthma during therapy with formoterol, it is necessary to consider the possibility of a gradual reduction in the dose of the drug.
Formoterol dose reduction is carried out under regular medical supervision of the patient. Against the background of exacerbation of bronchial asthma, one should not start treatment with formoterol or change the dosage of the drug. Formoterol should not be used to relieve acute attacks of bronchial asthma. When prescribing therapy to a patient using an inhalation device, a dose of the drug should be gradually selected (titrated) to doses sufficient to maintain a therapeutic effect.
Foradil is intended for inhalation use in adults and children aged 6 years and older. The drug is a powder for inhalation, used with a special device - an aerolizer, which is included in the package. Budesonide + formoterol Adults Pre-inhalation of beta-adrenostimulants expands the bronchi, improves the intake of budesonide in the respiratory tract and enhances its therapeutic effect.
Therefore, for maintenance treatment of bronchial asthma and COPD, formoterol is first inhaled, then budesonide is inhaled. 1. The dose of formoterol for regular maintenance therapy is 12-24 mcg (contents of 1-2 capsules) 2 times / day. Do not exceed the maximum recommended dose for adults (48 mcg / day). Given that the maximum daily dose of formoterol is 48 μg, if necessary, you can additionally apply 12-24 μg / day. to relieve symptoms of bronchial asthma. If the need for 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, as this may indicate a worsening of the disease. 2. The maintenance dose of budesonide for adult patients is 400-800 mcg / day. in 2 doses (200-400 mcg 2 times / day.). In case of exacerbation of bronchial asthma during the transfer from oral GCS to inhalation or when the dose of oral GCS is reduced, budesonide can be prescribed at a dose of 1600 mcg / day. in 2-4 doses.
If the dose of budesonide (divided into several doses) is less than 400 mcg / day., There is no need to use the drug. Children 6 years of age and older Pre-inhalation of beta-adrenostimulants expands the bronchi, improves the intake of budesonide in the respiratory tract and enhances its therapeutic effect. Therefore, for maintenance therapy of bronchial asthma, formoterol is first inhaled, then budesonide is inhaled. 1. The dose of formoterol for regular maintenance therapy is 12 mcg 2 times / day. The maximum recommended dose of the drug is 24 mcg / day. 2. The dose of budesonide for regular maintenance therapy is 100-200 mcg 2 times / day.
If necessary, the dose of budesonide can be increased to a maximum of 800 mcg / day. Rules for inhalation In order to ensure the correct use of drugs, the doctor or other medical professional must show the patient how to use the inhaler; explain to the patient that capsules with powder for inhalation should be used only with the help of an aerolizer; warn the patient that the capsules are for inhalation use only and are not intended to be swallowed. In children and adolescents, inhalation of budesonide and formoterol should be carried out under the supervision of adults.
You must make sure that the child performs the inhalation technique correctly. It is important that the patient understands that, because of the destruction of the gelatin capsule, small pieces of gelatin may get into the mouth or throat as a result of inhalation.
In order to minimize this phenomenon, do not puncture the capsule more than 1 time. Remove the capsule from the blister pack immediately before use. Rinsing the mouth with water after inhalation of budesonide can prevent irritation of the oral mucosa and pharynx, as well as reduce the risk of developing systemic adverse events.
Instructions for use of the aerolizer.
1. Remove the cap from the aerolizer.
2. Hold the aerolizer firmly by the base and turn the mouthpiece in the direction of the arrow.
3. Place the capsule in the cell located at the base of the aerolizer (it has the shape of a capsule). It should be remembered that you need to remove the capsule from the blister pack immediately before inhalation.
4. Turning the mouthpiece, close the aerolizer.
5. While holding the aerolizer in a strictly vertical position, once fully push the blue buttons on the sides of the aerolizer. Then let them go. At this stage, when a capsule is punctured, it can break down, as a result of which small pieces of gelatin can enter the mouth or throat. Since gelatin is edible, it does no harm. In order for the capsule not to collapse completely, the following requirements should be met: do not pierce the capsule more than once; comply with storage rules; Take the capsule out of the blister just before inhalation.
6. Exhale completely.
7. Take the mouthpiece into your mouth and slightly lean your head back. Grasp the mouthpiece tightly with your lips and take a quick, uniform, deepest breath. In this case, the patient should hear a characteristic rattling sound created by the rotation of the capsule and the spraying of the powder. If there was no characteristic sound, then you need to open the aerolizer and see what happened to the capsule. It may be stuck in the cell, in which 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 aerolizer.
8. If you hear a characteristic sound when you inhale, hold your breath for as long as possible. At the same time, remove the mouthpiece from the mouth. Then exhale. Open the aerolizer and see if the powder remains in the capsule. If powder remains in the capsule, repeat the steps described in paragraphs 6-8.
9. After the end of the inhalation procedure, open the aerolizer, take out the empty capsule, close the mouthpiece and close the aerolizer with a cap. To remove powder residue, wipe the mouthpiece and cell with a dry cloth. You can also use a soft brush.
Symptoms: an overdose of formoterol can presumably lead to the phenomena characteristic of the excessive action of other beta 2 -adrenomimetics, such as nausea, vomiting, headache, tremor, drowsiness, palpitations, tachycardia, ventricular arrhythmias, metabolic acidosis, hypokalemia, hyperglycemia.
Treatment: supportive and symptomatic therapy is indicated. In severe cases, hospitalization is required. The use of beta-blockers may be considered, but only subject to extreme caution and under close medical supervision, as the use of such drugs can cause bronchospasm. Budesonide.
Budesonide has low acute toxicity. A single inhalation of a large amount of the drug can lead to a temporary suppression of the function of the hypothalamic-pituitary-adrenal system, which does not require emergency therapy. In case of an overdose of budesonide, treatment can be continued in doses sufficient to maintain a therapeutic effect.
An inhalation powder containing budesonide and formoterol in a ratio of 80 / 4.5 μg / dose is not indicated for patients with severe bronchial asthma. Not intended for the initial selection of therapy in the early stages of treatment of bronchial asthma. A gradual reduction in the dose of the drug before stopping treatment is recommended.
An increase in the frequency of taking bronchodilators for emergency care indicates a deterioration in the course of the underlying disease and serves as a basis for reviewing the tactics of treating bronchial asthma. To minimize the possibility of developing a fungal infection of the oropharynx, it is necessary to rinse the mouth with water after each inhalation. There is no data on the use of the drug for the relief of acute attacks of bronchial asthma. Patients should be strictly advised to have medicines for emergency care at all times. Treatment should not be started during an exacerbation of bronchial asthma.
As with any other inhalation therapy, paradoxical bronchospasm may occur (in this case, treatment tactics should be reviewed and alternative therapy should be prescribed if necessary). The manifestation of a systemic effect during inhalation therapy is less likely than when using oral corticosteroids. However, it can occur when taking any inhaled GCS, especially when using high doses for a long period of time (it is very important to use the lowest effective dose of inhaled GCS, which provides optimal control of symptoms of bronchial asthma).
Doctors need to carefully monitor the growth of children and adolescents who take GCS in any dosage form for a long time, and evaluate the ratio of the benefits of GCS therapy and the possible risk of stunting. In the event that adrenal function was impaired against the background of previous systemic therapy for corticosteroids, precautions should be taken when transferring patients to inhaled treatment with the drug (patients who discontinue therapy with oral corticosteroids may have insufficient adrenal function for a long time).
In stressful situations, it is always necessary to remember the possibility of residual dysfunction of the adrenal gland in such patients. There are no clinical data on the use of the drug or the combined use of formoterol and budesonide during pregnancy. In pregnant women, the drug should only be used if the intended benefit to the mother outweighs the potential risk to the fetus, while the lowest effective dose of budesonide necessary to maintain adequate control of symptoms of bronchial asthma should be used. It is not known whether formoterol or budesonide passes into breast milk of women (the drug can be prescribed to nursing women only if the expected benefit to the mother is greater than any possible risk to the baby).
During the treatment period, it is recommended to control the concentration of K + in the blood serum, as well as glucose in patients with diabetes mellitus. Contains lactose (less than 1 mg / dose). Typically, this amount does not cause problems in patients with lactose intolerance.
A set of capsules with powder for inhalation.