FORADIL COMBI

747 20 minutes read

Active material: Budesonide, Formoterol
When ATH: R03AK07
CCF: The drug is a bronchodilator and anti-inflammatory action
ICD-10 codes (testimony): J44, J45
When CSF: 12.01.05
Manufacturer: NOVARTIS PHARMA AG (Switzerland)

Pharmaceutical form, composition and packaging

Set capsules with powder for inhalations.

Capsule powder inhalations transparent colorless, size №3, labeled “CG” and on the lid “FXF” on the housing or “CG” on the body and “FXF” looked just like the black ink; contents of capsules – free flowing powder white.

	1 caps.
formoterol fumarate digidrat	12 g

Excipients: lactose monohydrate.

Ingredients of the capsule shell: gelatin.

Capsule powder inhalations solid gelatine, size №3, with Cap light pink colored and colorless transparent casing, with image and inscription “WILL BE 200”, contents of capsules – white powder.

	1 caps.
budesonide *	200 g

Excipients: lactose monohydrate.

Ingredients of the capsule shell: iron oxide red (E172), Titanium dioxide (E171), gelatin, water.

Ink composition: iron oxide black (E172), shellac, n-butanol, soy lecithin liquid, protivovspenivaûŝee connection dc 1510, Purified water.

40 PC. (10 PC. with formoterolom in 3 blisters and 10 PC. with budesonidom in 1 blister) – blisters (4) complete with a device for inhalation (aèrolajzerom) – packs cardboard.
60 PC. (10 PC. with formoterolom in 3 blisters and 10 PC. with budesonidom in 3 blisters) – blisters (6) complete with a device for inhalation (aèrolajzerom) – packs cardboard.
90 PC. (10 PC. with formoterolom in 3 blisters and 10 PC. with budesonidom in 6 blisters) – blisters (9) complete with a device for inhalation (aèrolajzerom) – packs cardboard.
150 PC. (10 PC. with formoterolom in 3 blisters and 10 PC. with budesonidom in 12 blisters) – blisters (15) complete with a device for inhalation (aèrolajzerom) – packs cardboard.
70 PC. (10 PC. with formoterolom in 6 blisters and 10 PC. with budesonidom in 1 blister) – blisters (7) complete with a device for inhalation (aèrolajzerom) – packs cardboard.
90 PC. (10 PC. with formoterolom in 6 blisters and 10 PC. with budesonidom in 3 blisters) – blisters (9) complete with a device for inhalation (aèrolajzerom) – packs cardboard.
120 PC. (10 PC. with formoterolom in 6 blisters and 10 PC. with budesonidom in 6 blisters) – blisters (12) complete with a device for inhalation (aèrolajzerom) – packs cardboard.
180 PC. (10 PC. with formoterolom in 6 blisters and 10 PC. with budesonidom in 12 blisters) – blisters (18) complete with a device for inhalation (aèrolajzerom) – packs cardboard.

Set capsules with powder for inhalations.

	1 caps.
formoterol fumarate digidrat	12 g

Excipients: lactose monohydrate.

Ingredients of the capsule shell: gelatin.

Capsule powder inhalations solid gelatine, size №3, with a cover of pink and colorless transparent casing, with image and inscription “THERE WILL BE 400”, contents of capsules – white powder.

	1 caps.
budesonide *	400 g

Excipients: lactose monohydrate.

Ingredients of the capsule shell: iron oxide red (E172), iron oxide black (E172), carmine dye (Ponceau 4R), Titanium dioxide (E171), gelatin, water.

Ink composition: iron oxide black (E172), shellac, n-butanol, soy lecithin liquid, protivovspenivaûŝee connection dc 1510, Purified water.

* international non-proprietary name, recommended by the WHO – ʙudezonid.

Pharmacological action

The drug is a bronchodilator and anti-inflammatory action.

Formoterol

Selective agonist β₂-adrenoreceptorov. Provides bronhorasshiratee effect in patients with both reversible, and irreversible airway obstruction. The product is quickly (within 1-3 m) and maintained for a 12 hours after inhalation. If you are using the drug in therapeutic doses, effect on the cardiovascular system is minimal and is celebrated only in rare cases.

It stops the release of histamine and leukotrienes of mast cells. In experiments on animals were showing some anti-inflammatory properties formoterola, such as the ability to prevent the development of edema and accumulation of cell inflammation.

Studies, conducted in humans, shows, that effectively prevents Combi Foradil bronchospasm, called by inhalable allergens, physical activity, cold air, gistaminom or methacholine challenge test. Since bronhorasširâûŝij effect Foradila Estate remains pronounced within 12 hours after inhalation, maintenance therapy, where Foradil Combi appoint 2 times / day, in most cases to ensure the necessary control bronchospasm of chronic lung diseases like during the day, and at night.

In patients with chronic obstructive pulmonary disease (COPD) a stable flow of formoterol causes rapid onset of effect and improvement of basic parameters of quality of life.

Budesonide

Budesonide is glûkokortikosteroidom (GCS) for inhalation use, practically do not have systemic consequences. Budesonide has anti-inflammatory, anti-allergic and immunosuppressive effect. Increases products lipokortina, the inhibitor of phospholipase A2, It stops the release of arachidonic acid, oppressing synthesis products metabolism arahidonova acid – cyclical endoperekisey and prostaglandins. It prevents the accumulation of neutrophils boundary, reduces inflammatory cytokine production and exudation, inhibits the migration of macrophages, reduces severity of infiltration and granulation processes, formation Substance chemotaxis (that explains the efficiency “later” Allergy reactions); It stops the release of mast cell mediators of inflammation (immediate allergic reaction). Increases the “Active” β-adrenoreceptor, restores the patient's response to bronchodilators, allowing to reduce the frequency of their use, reduces swelling of mucous membrane bronchi, mucus production, sputum and reduces giperreaguosti respiratory tract. Increases mukotiliarnyi transport.

Therapeutic effect of the drug in patients, needed to treat GKS, develops within an average of 10 days after the start of therapy. With regular use in patients with bronchial asthma budesonide reduces the severity of chronic inflammation in the lungs, and thus improves lung function, for bronchial asthma, reduces giperreaguosti bronchi and warn the aggravation of the disease.

Pharmacokinetics

Formoterol

Absorption

After a single inhalation of formoterola fumarate dose 120 mcg formoterol healthy volunteers quickly was absorbed into plasma, C_max formoterola in plasma was 266 pmol/l and was achieved within 5 minutes after inhalation. In patients with COPD, treated with formoterol in the dose 12 mcg or 24 g 2 times / day for 12 weeks, formoterola concentration in plasma, measured through 10 m, 2 and h 6 hours after inhalation, were in the ranges 11.5-25.7 pmol/l and 23.3-50.3 pmol respectively.

Studies, in which studied the total excretion of formoterola and its (R,R)- and (S,S)-enantiomers in urine has been shown, that the number of formoterola in systemic blood rises in proportion to the magnitude of the dose ingaliruemoj (12-96 g).

After inhalation of application formoterola the dose 12 mcg or 24 g 2 times / day for 12 weeks excretion of unchanged formoterola in the urine in patients with bronchial asthma increased on 63-73%, and in patients with COPD – on 19-38%. This indicates some formoterola cumulation in plasma after repeated inhalations. While there has been no greater cumulation of one of the enantiomers of formoterola compared to the other after repeated inhalations.

Same, as reported for other medicines, used in inhalations, a large part of the formoterola, applied using a nebulizer, will proglatyvat′sâ and then absorbed from the digestive tract. In appointing 80 mcg 3n-labelled formoterola inside two healthy volunteers after, at least, 65% formoterol.

Distribution

Linking plasma protein is formoterola 61-64% (albumin – 34%).

In the range of concentrations, celebrated after the use of the drug in therapeutic doses, saturation bonding is not achieved.

Metabolism

The main route of metabolism formoterola is direct glukuronizatia. Another way metabolism – O-demethylation with a follow-up glûkuronizaciej.

Unimportant way metabolism include kon″ûgaciû formoterola with sulphate with subsequent deformilirovaniem. Numerous isoenzymes involved in the glucuronidation (Ugt1a1, 1A3, 1A6, 1A7, 1A8, 1A9, 1A10, 2B7 and 2B15) and o-demethylation (CYP2D6, CYP2C19, CYP2C9, CYP2А6) formoterol, that implies a low probability of drug interaction through inhibition of any izofermenta, taking part in the metabolism of formoterola. Therapeutic concentrations of formoterol does not inhibit cytochrome P450 system Isoenzymes.

Deduction

In patients with bronchial asthma and COPD, treated with formoterola fumarate dose 12 mcg or 24 g 2 times / day for 12 weeks, about 10% or 7% Accordingly determined in the urine as unchanged formoterola. The calculated percentage (R,R)- and (S,S)-enantiomers unchanged formoterola in urine accounted for 40% and 60% Accordingly, after a single dose of formoterola (12-120 g) in healthy volunteers, and after a single and repeated doses of formoterola in patients with bronchial asthma.

An active substance and its metabolites is completely eliminated from the body; about 2/3 from the inside of the dose appears in the urine, from 1/3 – with feces. Kidney klirens formoterola is 150 ml / min.

In healthy volunteers end T_1/2 formoterola of plasma after a single Inhalation dose 120 mcg is 10 no; end T_1/2(R,R)- and (S,S)-enantiomers, calculated for excretion in the urine, were 13.9 and h 12.3 h, respectively.

Pharmacokinetics in special clinical situations

After adjusting for body weight pharmacokinetic parameters formoterola for men and women do not differ.

Pharmacokinetics formoterola in elderly patients 65 years and older was not studied.

In a clinical study in children aged 5-12 years with bronchial asthma, treated with formoterola fumarate dose 12 mcg or 24 g 2 times / day for 12 weeks, excretion unchanged with urine formoterola increased to 18-84% compared with the corresponding indicator, measured after the first dose.

In clinical studies in children in the urine was determined about 6% unmodified formoterola.

Formoterola pharmacokinetics in patients with impaired liver and/or kidney disease has not been studied.

Budesonide

Absorption

Budesonide rapidly and completely absorbed following inhalation, wherein C_max in the blood plasma is achieved immediately after use. After inhalation of budesonide in view of settling the drug on oropharyngeal mucosa absolute bioavailability of 73%. Absolute bioavailability when administered the drug inside is ± 10%.

Distribution

V_dis 3 l / kg. Plasma protein binding – 88%. In experimental studies budesonide accumulated spleen, lymph nodes, thymus, adrenal cortex, reproductive organs and bronchi, as well as pass through placental barrier. Systemic clearance inhalation drug entered – 0.5 l / min.

Metabolism

Budesonide is not metabolized in the lungs. After drug intake was almost completely (about 90%) metabolised in the liver with the formation of several inactive metabolites (Biological activity 100 times less compared to budesonidom), including 6β-gidroksibudesonid and 16α-gidroksiprednizolon (systemic clearance – 1.4 l / min). Budesonide has a high ground clearance system – 84 l/h and short T_1/2 – 2.8 no. The main route of metabolism in the liver using budesonide izofermenta CYP3A4 system R450 can change under the influence of inhibitors or inducers of CYP3A4 .

Deduction

T_1/2 – 2-2.8 no. Return via intestine in the form of metabolites – 10%, kidney – 70%.

Pharmacokinetics in special clinical situations

Concentration of budesonide in plasma is increased in patients with liver disease.

Testimony

Bronchial asthma:

is not sufficiently controlled by taking inhaled CORTICOSTEROIDS and beta₂-agonists short-acting as an on-demand therapy;

is adequately controlled inhalants GKS and beta₂-long-acting agonists.

Chronic obstructive pulmonary disease (COPD) (with the proven effectiveness of the application of GKS).

Dosage regimen

Formoterol and budesonide are intended for inhalation use. Drugs represent capsule powder inhalations, that should only be used with a special device – aèrolajzera, that included packaging.

Formoterol and budesonide should be appointed individually, the minimum effective dose.

When it reaches the control symptoms of bronchial asthma therapy on formoterolom, It is necessary to consider the possibility of progressively reducing the dosage. Lower doses formoterola are under regular medical supervision of the patient's condition. Against the backdrop of worsening asthma should not begin treatment formoterolom or change the dosage of the drug. Formoterol should not be used for cupping acute attack of bronchial asthma.

When you assign patient therapy through inhalation device, should gradually pick up (Titrate) dose of the drug to doses sufficient to maintain therapeutic effect.

Foradil is intended for inhalation use Adults and children 6 and older. The drug is a powder for inhalations, applied using a special device – aèrolajzera, that included packaging.

Budesonide + formoterol

Adult

Provisional inhalation beta-adrenostimulâtorov expands bronchi, improves the flow of inhaled budesonide and enhances its therapeutic effect. So for maintenance therapy of bronchial asthma and COPD is first inhalation formoterola, then – inhalation of budesonide.

1. Dose formoterola for regular maintenance therapy is 12-24 g (contents 1-2 capsules) 2 times / day. Do not exceed the maximum recommended dose for adults (48 mg / day).

Considering, the maximum daily dose is formoterola 48 g, If necessary, you can optionally apply 12-24 µg/day to relieve symptoms of bronchial asthma. If the need for additional doses of the drug ceases to be episodic (eg, It is becoming increasingly, than 2 days per week), the patient should be encouraged to consult with your doctor for review therapy, as this may indicate deterioration of the disease.

2. Supporting dose budesonide for adult patients is 400-800 mg / day 2 admission (by 200-400 g 2 times / day).

In acute bronchial asthma during transfer from oral CORTICOSTEROIDS to inhaled or when lower doses of oral CORTICOSTEROIDS can be prescribed in a dose of budesonide 1600 mg / day 2-4 admission.

If the dose of budesonide (divided into several times) is less than 400 mg / day, There is no need to use drugs.

Children ≥ 6 years

Provisional inhalation beta-adrenostimulâtorov expands bronchi, improves the flow of inhaled budesonide and enhances its therapeutic effect. So for maintenance therapy of bronchial asthma is first inhalation formoterola, then – inhalation of budesonide.

1. Dose formoterola for regular maintenance therapy is 12 g 2 times / day. The maximum recommended dose 24 mg / day.

2. Dose budesonide for regular maintenance therapy is 100-200 g 2 times / day. If necessary dose can be increased to a maximum of budesonide – 800 mg / day.

Rules for inhalations

In order to ensure the correct use of drugs, a doctor or other health worker must show a patient, How to use an inhaler; explain to the patient, that capsule powder inhalations should only be using aèrolajzera; warn the patient, that the capsules are intended only for inhalation use only and are not intended to be swallowed. In children and adolescents and budesonide inhalation formoterola should be under adult supervision. You must make sure, that the child correctly performs inhalation technique. Important, that the patient understood, that due to the destruction of gelatinous capsules small bits of gelatin as a result of inhalation can be caught in the mouth or throat. In order to bring this phenomenon to a minimum, should not Pierce capsule more 1 times.

Remove the capsule from the blister packaging immediately before use.

Rinsing the mouth with water after inhalation of budesonide may prevent irritation of mouth and pharynx, as well as reduce the risk of systemic adverse events.

Instructions for use aèrolajzera

1. Remove cap from aèrolajzera.

2. Hold aèrolajzer for the base and turn the mouthpiece in the direction of the arrow.

3. Place the capsule in cell, located at the base of the aèrolajzera (It has the form of a capsule). It should be remembered, that remove capsule from blister packs need to immediately before the inhalation.

4. Rotating mouthpiece, close aèrolajzer.

5. Holding aèrolajzer in strictly vertical position, Once pressure until the end of the blue buttons, available on the sides aèrolajzera. Then let them go.

At this stage, it can shatter capsule piercing, resulting in little bits of gelatin can be caught in the mouth or throat. Because gelatin edible, This is not harmless. In order to not totally destroyed capsule, should comply with the following requirements: do not perforate the capsule more than once; observe the storage rules; remove the capsule from blister just immediately before the inhalation.

6. Make a full exhalation.

7. Take the mouthpiece into your mouth and slightly tilt your head back. Tightly embrace the mouthpiece and do a quick, uniform, the maximum deep breath. In doing so, the patient must hear the characteristic sound of a jarring, generated by rotating the capsule and powder spray. If the characteristic of the sound was not, then open aèrolajzer and see, What happened to the capsule. Maybe, She is stuck in a cell. In this case, you must carefully extract capsule. In no case try to release capsule by repeated clicks on the buttons on the sides aèrolajzera.

8. If inhaled, hear a distinctive sound, You should hold your breath as long as possible. At the same time remove the mouthpiece from the mouth. Then exhale. Open aèrolajzer and look, does not stay in the capsule powder. If the capsule stayed powder, do the steps again, described in paragraphs 6-8.

9. After the end of the inhalation procedure open aèrolajzer, remove the empty capsule, close the nozzle and close the aèrolajzer Cap.

To remove residual powder should be wiped with a dry cloth to clean the cell and mouthpiece. You can also use a soft brush.

Side effect

Adverse reactions, observed in clinical trials, distributed in accordance with the frequency of. To assess the frequency used the following criteria: Often (≥ 1/10); often (of ≥ 1/100, < 1/10); sometimes (≥ 1/1000, < 1/100); rarely (≥ 1/10 000, < 1/1000); rarely (< 1/10 000), including isolated reports. Within each group the undesirable phenomena are distributed in decreasing order of importance.

Formoterol

Allergic reactions: rarely – hypersensitivity reactions, such as arterial gipotenzia, hives, angioedema, itch, rash.

CNS: often – headache, tremor; sometimes – ažitaciâ, anxiety, hypererethism, insomnia, dizziness.

Cardio-vascular system: often – palpitations; sometimes – tachycardia; rarely – peripheral edema.

The respiratory system: sometimes – bronchospasm, including the paradoxical, irritation of mucous membranes of pharynx and larynx.

From the digestive system: rarely – nausea, taste disturbances.

On the part of the musculoskeletal system: sometimes – muscle cramps, mialgii.

The following adverse reactions have been identified during the application of other dosage forms, which include formoterol: cough and a rash.

In applying formoterola in clinical practice there were following changes the results of laboratory research: kaliopenia, giperglikemiâ, QT prolongation (While conducting ECG).

Budesonide

On the part of the endocrine system: rarely – Suppression of adrenal function, Cushing's syndrome, giperkorticizm, growth retardation in children and adolescents.

On the part of the organ of vision: rarely – Cataract, glaucoma.

Allergic reactions: rarely – hypersensitivity reactions, rash, hives, angioedema, itch.

CNS: rarely – unusual behavior, including depression (described in children).

On the part of the musculoskeletal system: decrease in bone mineral density.

The respiratory system: often – cough; rarely – paradoxical bronchospasm, candidiasis mucous membranes of the oral cavity and larynx, throat irritation, disfonija, vanishing after cessation of therapy or reduction budesonidom dose.

In the three-year clinical study in the use of budesonide in patients with COPD noted increased the incidence of subcutaneous hemorrhage (10%) and pneumonia (6%) compared with the placebo group (4% and 3%, When r< 0.001 and p<0.01, respectively)

Contraindications

- Lactation (breast-feeding);

— active pulmonary tuberculosis;

- Hereditary galactose intolerance, severe deficiency of lactase and impaired glucose-Galactose malabsorption;

- Children up to age 6 years;

-hypersensitivity to formoterolu, budesonidu or any other component of the drug.

Formoterol

Compliance with special caution When applying formoterola (especially in terms of dose reduction) and careful observation of patients requires the following Comorbidities: CHD; Cardiac arrhythmia and conduction, especially AV-blokada III degree; expressed chronic heart failure; idiopathic podklapannyj aortic stenosis; gipertroficheskaya obstruktivnaya cardiomyopathy, aneurysm aortы; thyrotoxicosis; known or suspected elongation QT interval (QT korrigirovannyj > 0.44 sec), kaliopenia, hypocalcaemia and pheochromocytoma.

Given the giperglikemičeskij effect, typical beta-adrainomimetikam, including formoterol, diabetic patients are recommended to optional regular monitoring concentrations of glucose in the blood.

Budesonide

As budesonide is not effective for cupping acute bronchospasm, the drug should not be appointed as a primary therapy for astmaticescom status or other acute asthmatic conditions.

Observe caution When applying budesonide in patients with inactive pulmonary tuberculosis, fungal, bacterial and viral infections of the respiratory tract, cirrhosis of the liver, glaukomoj. Also, Bearing in mind the possibility of the development of fungal disease, should be cautious appoint drug bronhoèktazah and pneumoconiosis.

Formoterola and budesonide capsules contain lactose.

Pregnancy and lactation

Formoterol

The safety of the Foradila Estate in pregnancy and lactation has not been established so far.

Pregnancy may only, if the expected benefit to the mother outweighs the potential risk to the fetus. Formoterol, like other beta₂-adrenomimetiki, may slow the process of childbirth due to tokolitičeskogo actions (relaxing action on the smooth muscles of the uterus).

Unknown, does formoterol is excreted in breast milk in humans. During the reception, Foradila Combi breastfeeding should be discontinued.

Budesonide

IN experimental studies on animals revealed possible teratogenic effects on the fetus of the SCS. Data on the teratogennom action of budesonide or of the drug have reproductive toxicity in the application in person, no.

Pregnancy may only, if the expected benefit to the mother outweighs the potential risk to the fetus. When it is necessary to carry out therapy GKS during pregnancy their preferably assign of inhalations, tk. SCS for inhalation use have less systemic effect compared with oral CORTICOSTEROIDS.

Unknown, whether budesonide is excreted in breast milk in humans.

Cautions

Formoterol

Displaying, the formoterola improves the quality of life of patients with COPD.

Formoterol belongs to the class of beta₂-adrenomimetikov long-acting. Against the backdrop of another beta₂-long adrenomimetika, salmeterola, There was an increase in the frequency of deaths, associated with bronchial asthma (13 from 13 176 patients) compared to placebo (3 from 13 179 patients). Clinical studies to assess the incidence of deaths, associated with bronchial asthma, against the backdrop of formoterola has not been.

Anti-inflammatory therapy

Foradil Combi should not be used in conjunction with other agonists β₂-adrenoceptor long-acting.

In patients with bronchial asthma formoterol should only be used as a supplementary treatment with the ineffectiveness of other monitoring for disease medicines, eg, inhaled CORTICOSTEROIDS (in medium-sized and small doses) or with severe diseases, requiring the use of two supporting therapies, including formoterol. In appointing the drug to patients, not receiving anti-inflammatory therapy, It should start simultaneously with the application formoterola. In appointing formoterola, It is necessary to assess the condition of the patients in regard to the adequacy of the anti-inflammatory therapy, they receive. After the start of treatment formoterolom patients should be encouraged to continue to anti-inflammatory therapy without changes, even in the case, If it is improved.

For cupping acute attack of bronchial asthma should apply agonists β₂-adrenergic short-acting. The sudden deterioration of the patients should immediately seek medical care.

Severe exacerbation of asthma

In clinical studies when applying formoterola noted a slight increase in the incidence of severe exacerbations of asthma compared to placebo, incl. for children 5-12 years.

In placebo-controlled clinical trials in patients, treated with formoterol for 4 weeks, It was observed an increase in the frequency of development of severe exacerbations of asthma (0.9% When batching mode 10-12 g 2 times / day, 1.9% – at 24 g 2 times / day) compared with the placebo group (0.3%).

In two major controlled clinical trials, involving 1095 adult patients and adolescents from 12 and older, severe exacerbation of asthma, requiring hospitalization, were more frequent in patients, treated with formoterol in the dose 24 g 2 times / day (9/271, 3.3%), compared with groups formoterola the dose 12 g 2 times / day (1/275, 0.4%), placebo (2/277, 0.7%) and al′buterola (2/272, 0.7%).

In the application of formoterola during 16 weeks in another major clinical trial, which included 2085 adults and teenagers, There was no increase in the frequency of severe exacerbations of asthma depending on dose increases formoterola. However, in this study, the incidence of severe complications was higher in the Group formoterola (When batching mode 24 g 2 times / day – 2/527, 0.4%, at 12 g 2 times / day – 3/527, 0.6%) compared to placebo (1/517, 0.2%). In the open phase of this study when applying formoterola dose 12 g 2 times / day (If necessary, patients can use up to two additional doses of the drug) the frequency of severe exacerbations of asthma was 1/517, 0.2%.

In the 52-week a multicenter, randomized, double-blind clinical study, which included 518 children and adolescents between the ages of 5 to 12 years, the incidence of severe exacerbations of asthma was higher when applying formoterola in doses 24 g 2 times / day (11/171, 6.4%), 12 g 2 times / day (8/171, 4.7%) compared to placebo (0/176, 0.0%).

However, the results of the above clinical trials do not allow a quantitative assessment of the frequency
development of severe exacerbations of asthma in different groups.

Kaliopenia

Consequence of therapy beta₂-adrenomimetikami, including formoterol, can be potentially serious development gipokaliemii. Gipokaliemia may increase susceptibility to the development of arrhythmias.

Because this drug can be strengthened by hypoxia and related treatment, special caution should be exercised in patients with bronchial asthma heavy currents. In these cases, we recommend that you regularly monitor the concentration of potassium in serum.

Paradoxical bronchospasm

Just as with the other inhalation therapy, should take into account the possibility of paradoxical bronchospasm. If it occurs, You should immediately stop the drug and to appoint an alternative treatment.

Impact on the ability to drive vehicles and operate moving mechanisms

Patients, on the background of the drug formoterol occurs dizziness or other disorders of the central nervous system, should refrain from driving or using machinery during use of the drug.

Budesonide

To ensure receipt of budesonide in your lungs, it is important to instruct patients to properly drive inhalation preparation in accordance with instructions for use.

Patients should be informed, About, that the drug is not intended for cupping, and for regular daily use, even in the absence of symptoms of bronchial asthma.

With the development of paradoxical bronchospasm, you should immediately cease use of budesonide, assess the condition of the patient and, if necessary, appoint other drugs therapy. Bronhospazm paradoxical should immediately stop using the beta₂-adrenomimetic short-acting. Patients should always have a nebulizer with beta₂-adrenomimetikom short for short sharp exacerbations of asthma.

Patients should be informed, about the need for treatment to a doctor when the deterioration of the (increasing demand for short-acting bronhodilatatorah, strengthening attacks of breathlessness). In such cases, it is necessary to conduct a survey of the patient, and to consider the possibility of increasing the dose of inhaled or oral CORTICOSTEROIDS.

To reduce the risk of Candidal infections of the oral cavity and pharynx, the patient should rinse your mouth thoroughly with water after each inhalation medication. With the development of Candidal infections of the oral cavity and pharynx may conduct local antifungal therapy without termination of treatment budesonidom.

In acute bronchial asthma, you should increase the dose of budesonide or, if necessary, to undertake a short course of systemic CORTICOSTEROIDS and/or assign antibiotikoterapiiû in the development of infection.

There is a need to monitor the dynamics of growth of children and adolescents, receiving long-term therapy of inhaled GCS. If growth should consider the need to reduce the dose of inhaled CORTICOSTEROIDS (the appointment of the minimum effective dose) and referral to an allergist. Long-term effect of stunting (impact on final adult height) children, receiving therapy to inhaled CORTICOSTEROIDS, not investigated. Adequate study to compensate for a backlog in growth in children after the therapy with oral CORTICOSTEROIDS was conducted.

Budesonide usually has no effect on adrenal function. However, some patients with long-term use in the recommended daily doses may be a systemic effect of budesonide.

When prescribing inhaled CORTICOSTEROIDS in high doses or for a long period of time, Perhaps the development of systemic adverse events (However, less, than use of oral CORTICOSTEROIDS), such as suppressing the napochechnikov crust, gipercortitizm/Cushing Syndrome, growth retardation in children and adolescents, decrease in bone mineral density, hypersensitivity reactions, Cataract, glaucoma.

Patients with gormononezavisimoj asthma

In patients with bronchial asthma gormononezavisimoj therapeutic effect of budesonide develops on average during 10 days after treatment. At the beginning of therapy in patients with budesonidom increased bronchial secretion to drug ingalâciâm you can add oral CORTICOSTEROIDS short course (duration approx. 2 weeks).

Patients with bronchial asthma

When switching from oral ingestion of GKS to inhalation use budesonide patients should be in a relatively stable condition.

For the first 10 days prescribe high doses of budesonide in combination with previously oral CORTICOSTEROIDS in the previous dose. Then the daily dose of oral CORTICOSTEROIDS are beginning to gradually reduce the (by 2.5 mg each month in terms of prednisone) to the lowest possible level. Should not abruptly interrupt treatment GKS, including budesonide.

In the first months after the transition should carefully monitor the patient, While his hypothalamic-pituitary-adrenal system does not recover sufficiently, to provide an adequate response to stressful situations (eg, injury, surgery or severe infection). Should regularly monitor the performance of the function of the hypothalamic-pituitary-adrenal system.

In some cases, patients with decreased adrenal function may need supplemental oral CORTICOSTEROIDS during stressful situations. This category of patients, it is recommended that you always carry a warning card, which must be specified, that they are in stressful situations require additional systemic administration of corticosteroids.

The transfer of patients from systemic CORTICOSTEROIDS on an inhalation therapy such reactions may occur budesonidom, as allergic rhinitis, eczema, lethargy, pain in muscles and joints, sometimes nausea and vomiting, previously suppressed taking systemic CORTICOSTEROIDS. Treatment of these reactions should be antihistamines or local GCS.

Effects on ability to drive vehicles and management mechanisms

Data on effects of budesonide on the ability to drive vehicles and operate moving mechanisms no. The negative impact of the drug on the ability to drive vehicles and operate moving mechanisms, it is unlikely.

Overdose

Formoterol

Symptoms: formoterola suspected overdose can lead to phenomena, characteristic for excessive actions of other beta₂-adrenomimetikov, such as nausea, vomiting, headache, tremor, drowsiness, palpitations, tachycardia, ventricular arrhythmias, metabolic acidosis, kaliopenia, giperglikemiâ.

Treatment: shown holding a supportive and symptomatic therapy. In serious cases require hospitalization. Can be considered the use of beta blockers, but only subject to emergency care and under careful medical supervision, tk. the use of such means may cause bronchospasm.

Budesonide

Budesonide has low acute toxicity. Single inhalation of large quantities of the drug can cause temporary suppression function of the hypothalamic-pituitary-adrenal system, that does not require emergency treatment. Budesonidom overdose treatment can be continued in doses, sufficient to maintain therapeutic effect.

Drug Interactions

Formoterol

Formoterol (Like other beta₂-adrenostimulyatorov) should be cautious appoint patients, receiving such medicines, as quinidine, disopyramide, prokaynamyd, fenotiazinы, antihistamines, MAO inhibitors, tricyclic antidepressants, as well as other drugs, known, They lengthened QT interval, tk. in these cases, the effect of adrenostimulâtorov on cardiovascular system can increase. When using drugs, capable of lengthened QT interval, increased risk of ventricular arrhythmias.

The simultaneous use of other simpatomimeticakih funds can lead to aggravation of the side effects of formoterola.

Simultaneous application of Xanthine derivatives, CORTICOSTEROIDS or diuretics may exacerbate the potential action of beta gipokaliemičeskoe₂-adrenomimetikov. Gipokaliemia may increase the propensity for development of cardiac arrhythmias in patients, receiving digitalis preparations.

Beta-adrenoblokatora may weaken the effect formoterola. Therefore, you should not use formoterola in conjunction with beta-adrenoblokatorami (including eye drops), unless the use of such a combination of drugs does not compel any extraordinary reasons.

Budesonide

Use of the drug in conjunction with CYP3A4 inhibitors (eg, itraconazole, ketoconazole, ritonavirom, nelfinavirom, amiodarone, clarithromycin) can lower metabolism and improve systemic budesonide concentrations. When assigning budesonida CYP3A4 inhibitors together should regularly monitor the function of the adrenal cortex, and optionally change the dose budesonide.

When applied together with budesonide, induciruûŝimi CYP3A4 (eg, rifampicin, fenoʙarʙitalom, phenytoin), possibly increasing metabolism and decrease its systemic budesonide concentrations.

Methandrostenolone, estrogens increase the effect of budesonide.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored in a dry, inaccessible to children at temperature not exceeding 25 ° C. Shelf life – 2 year.

Vladimir Andreevich Didenko

747 20 minutes read