Active ingredients: Budesonide
AIRCORT 0.25 mg / ml suspension to be nebulised
AIRCORT 0.5 mg / ml suspension to be nebulised
Aircort package inserts are available for pack sizes: - AIRCORT 0.25 mg / ml suspension for nebulization, AIRCORT 0.5 mg / ml suspension for nebulization
- AIRCORT 100 micrograms Nasal Spray, suspension, AIRCORT 50 micrograms Nasal Spray, suspension
- AIRCORT 200 micrograms / act, Pressurized inhalation suspension, AIRCORT 400 micrograms / act, Pressurized inhalation suspension
Why is Aircort used? What is it for?
Pharmacotherapeutic group
Inhaled asthmatics - glucocorticoids.
THERAPEUTIC INDICATIONS
AIRCORT suspension to be nebulized is indicated in the treatment of bronchial asthma.
AIRCORT suspension for nebulisation is also indicated in the treatment of very severe subglottic laryngitis (pseudocroup) in which hospitalization is indicated.
Contraindications When Aircort should not be used
Hypersensitivity to the active substance or to any of the excipients.
Precautions for use What you need to know before taking Aircort
AIRCORT Nebuliser Suspension is not intended for the rapid improvement of acute episodes of asthma, for which a short-acting bronchodilator is required.
The physician must carefully evaluate the cases of patients who do not benefit from the use of short-acting bronchodilators or who increase the number of inhalations compared to the usual one. In these cases, the physician should evaluate the need for increased therapy with anti-inflammatory drugs, for example by increasing the dose of inhaled budesonide or by starting a course of oral glucocorticosteroid therapy.
Particular attention should be paid to transferring patients from oral steroid therapy as the risk of adrenal compromise may remain for a long period of time. Patients who have required emergency therapy with high doses of corticosteroids or prolonged treatment with high doses of inhaled corticosteroids may also be at risk. Such patients may show signs and symptoms of adrenal insufficiency when exposed to severe stress. In times of stress or in the case of elective surgery, additional coverage with systemic corticosteroids should be considered.
During the suppression phase of systemic glucocorticosteroid therapy some patients may experience general malaise such as muscle and joint pain. General glucocorticosteroid insufficiency should be suspected in the rare cases of onset of symptoms such as fatigue, headache, nausea and vomiting. In these cases, a temporary increase in the oral glucocorticosteroid dose may sometimes be necessary.
Some patients may experience symptoms of systemic glucocorticosteroid suppression such as joint and / or muscle pain, fatigue and depression despite the maintenance or even improvement of lung function during the period of withdrawal of oral steroid treatment. Such patients should be encouraged to continue therapy with AIRCORT Nebuliser Suspension but should be monitored for objective signs of adrenal insufficiency. If there is evidence of adrenal insufficiency, the dose of systemic corticosteroid should be temporarily increased and the transfer to AIRCORT Nebuliser Suspension may be continued later, more slowly. During times of stress or during a severe asthma attack, patients who are replacing systemic steroid treatment with inhaled therapy may need additional systemic corticosteroid treatment.
Replacing systemic steroid treatment with inhaled therapy can sometimes manifest allergies, such as rhinitis and eczema, previously controlled by systemic steroid treatment. These allergic manifestations should be symptomatically controlled with antihistamine drugs and / or topical preparations.
Reduced liver function affects the elimination of glucocorticosteroids, resulting in a reduced rate of elimination and higher systemic exposure. This may be clinically relevant in patients with severely impaired liver function.
You need to be aware of possible systemic side effects. The concomitant use of ketoconazole, HIV protease inhibitors or other potent CYP3A4 inhibitors should be avoided. If this is not possible, the time period between the two treatments should be as long as possible (see also "Interactions").
Particular caution is required in the case of patients with active or quiescent pulmonary tuberculosis and in patients with fungal or viral infections of the respiratory tract. AIRCORT should be used with caution in patients with fungal and viral infections (such as measles and chickenpox) and in those with glaucoma and cataracts.
Oral candidiasis may occur during inhaled corticosteroid therapy. This infection may require treatment with appropriate antifungal therapy and treatment may need to be stopped in some patients (see also Dose, method and time of administration).
In long-term treatment with high doses of Aircort, local and systemic effects may occur in humans. Systemic effects with inhaled corticosteroids occur less frequently than with oral corticosteroids.
Systemic effects may occur with inhaled corticosteroids, particularly when prescribed in high doses for prolonged periods. These effects are less likely to occur than with oral corticosteroid treatment. Possible systemic effects include Cushing's syndrome, Cushingoid aspect, adrenal suppression, growth retardation in children and adolescents, decreased bone mineral density, cataracts, glaucoma.
Rarely, a range of psychological and behavioral effects may occur, including psychomotor hyperactivity, sleep disturbances, anxiety, depression, aggression, behavioral disturbances (predominantly in children).
Therefore, on the basis of the above, once asthma control has been achieved, the dose to be used in maintenance treatment should be the least effective.
It is important to take the dose as directed in the package leaflet or as prescribed by your doctor.
You should not increase or decrease the dose without first consulting your doctor. AIRCORT should be used with caution in children.
As with other inhaled therapies, paradoxical bronchospasm may arise with an immediate increase in wheezing after administration. In this case, inhaled budesonide should be discontinued immediately, the patient should be evaluated and alternative therapy initiated if necessary.
Influence on growth
It is recommended that the height of children on prolonged treatment with inhaled corticosteroids is periodically monitored. If growth is slowed, therapy should be re-evaluated in order to reduce the dose of inhaled corticosteroids. The benefits of therapy with corticosteroids. and the possible risk of growth suppression should be carefully considered, and consideration should be given to referring the patient to a pediatric pulmonologist specialist.
Interactions Which medications or foods may change the effect of Aircort
Tell your doctor or pharmacist if you have recently taken any other medicines, even those without a prescription. No interactions of budesonide have been observed with any other drug used in the treatment of asthma.
The metabolism of budesonide is mainly mediated by CYP3A4, the cytochrome p450 isoenzyme. Inhibitors of this enzyme, such as ketoconazole and itraconazole, can therefore increase systemic exposure to budesonide by several fold (see Precautions for use).
As no data is available to support a dosage recommendation, the combination of these drugs should be avoided. If this is not possible, the longest possible time should elapse between the two treatments and a reduction in the dose of budesonide may be considered.
Based on a limited amount of data regarding this interaction for high doses of budesonide administered by the inhaled route, substantial increases in plasma levels (on average four-fold) may occur when itraconazole 200 mg once daily is administered. concomitantly with inhaled budesonide (single dose equal to 1000 µg).
Increased plasma concentrations and enhanced effects of corticosteroids were observed in women also treated with estrogen and contraceptive steroids, while no effect was observed with the use of budesonide and the concomitant intake of low-dose oral contraceptives.
Since the function of the adrenal glands can be inhibited, an ACTH stimulation test to diagnose "pituitary insufficiency may give false results (low values)."
At recommended doses cimetidine has a slight effect on the pharmacokinetics of orally administered budesonide not clinically relevant.
Warnings It is important to know that:
Pregnancy and breastfeeding
Ask your doctor or pharmacist for advice before taking any medicine.
The results from large prospective epidemiological studies and post-marketing experience on a worldwide scale do not indicate any adverse effects on the health of the fetus / neonate with the use of inhaled budesonide during pregnancy.
As with other drugs, the expected benefits to the mother should be weighed against the risks to the fetus when administering budesonide during pregnancy.
Budesonide is excreted in breast milk. However, at therapeutic doses of AIRCORT no effects on the suckling child are expected. Budesonide can be used during breastfeeding.
Maintenance therapy with inhaled budesonide (200 or 400 micrograms twice daily) in breastfeeding asthmatic women results in negligible systemic exposure to budesonide in breastfed infants.
In a pharmacokinetic study, the estimated daily dose for the infant was 0.3% of the daily dose taken by the mother for both dose levels and the mean plasma concentrations in the infant were estimated to be 1/600 of the concentrations observed in maternal plasma, assuming complete oral bioavailability for the infant. Budesonide concentrations found in infant plasma samples were always found to be below the limit of quantification.
Based on data obtained with the use of inhaled budesonide and on the fact that budesonide exhibits a linear pharmacokinetic profile within the therapeutic dose range after nasal, inhaled, oral and rectal administration at the therapeutic doses of budesonide, l " infant exposure is presumably low.
Effects on ability to drive and use machines
AIRCORT Nebuliser Suspension does not affect the ability to drive and use machines.
For those who carry out sporting activities: the use of the drug without therapeutic necessity constitutes doping, and can in any case determine positive anti-doping tests.
Dosage and method of use How to use Aircort: Dosage
Bronchial asthma
Initial dose: the dosage of AIRCORT suspension to be nebulized is individual.
Recommended starting dose:
CHILDREN from 6 months to 12 years: total daily dose 0.25 - 0.5 mg. In patients on oral steroid therapy, it is possible to start with a higher initial total daily dose, for example 1 mg. The higher dose (2 mg per day) should only be considered in children with severe asthma and for limited periods.
ADULTS AND ELDERLY: 0.5-1 mg twice daily. If necessary, the dose can be further increased.
In cases where a greater therapeutic effect is required, it is possible to administer higher doses of AIRCORT suspension to be nebulized; in fact the risks of systemic effects are low, if compared with those detectable following a treatment in combination with oral steroids.
Maintenance dose: the maintenance dose is individual. Once the desired clinical results are achieved, the maintenance dose should be gradually reduced until the minimum amount necessary to control symptoms is achieved.
Onset of effect: Improvement in asthma control and following administration of AIRCORT inhaled nebuliser suspension may occur within three days of starting treatment, although maximum benefit is obtained after 2 - 4 weeks.
Patients treated with oral steroids (see also Precautions for use)
AIRCORT suspension to be nebulized, can allow the replacement or significant reduction of the dosage of oral steroids, maintaining control of asthma.
When initiating the transfer from oral corticosteroid therapy to AIRCORT Nebuliser Suspension, the patient should be in a relatively stable phase. A high dose of AIRCORT is then administered in combination with the previously used oral dose for approximately 10 days. After that, the dose of the oral steroid is gradually reduced, until the minimum required amount is reached. A slow transition from oral steroid treatment to AIRCORT nebuliser suspension is recommended. In many cases it is possible to completely replace the oral steroid with AIRCORT suspension to be nebulised.
Splitting the dose and mixing
AIRCORT suspension to be nebulised can be mixed with 0.9% physiological solution and with nebulisation solutions of terbutaline, salbutamol, fenoterol, acetylcysteine, sodium chromoglycate or ipratropium bromide.
The mixture should be used within 30 minutes.
The contents of the single-dose container can be divided to allow for dosage adjustment.
A line is clearly visible on the single-dose containers of AIRCORT suspension to be nebulized. When the single-dose container is held upside down, the line indicates a volume equal to 1 ml. If only 1 ml is to be used, empty the contents of the single-dose container until the liquid surface reaches the indicated line.
Before using the remaining liquid, shake the contents carefully with a twisting motion
DOSAGE TABLE
* The product must be mixed with 0.9% physiological solution to reach the volume of 2 ml.
Subglottic laryngitis: In infants and children with subglottic laryngitis the usual dose is 2 mg of AIRCORT suspension for nebulisation which can be given as a single administration or with two 1 mg administrations 30 minutes apart. repeated every 12 hours for up to 36 hours or until clinical improvement.
Note:
Nebulization time and the amount of drug delivered by a nebulizer depend on the flow rate of the compressor and the fill volume.
In vitro the quantity of budesonide delivered by the nebulizer varies between 30-70% of the nominal dose, depending on the type of nebulizer and compressor used and not all nebulizers and compressors are suitable for the use of AIRCORT suspension to be nebulized.
To obtain the maximum budesonide delivery, a compressor is required that guarantees a flow of 5 to 8 l / min and a filling volume of 2-4 ml. Studies performed in vivo have shown that the dose of nebulised budesonide administered to patients varies between 11 and 22% of the nominal dose.
For children, we recommend the use of a perfectly tight and well-fitting face mask, capable of optimizing the administered dose of budesonide.
Due to the small delivered amount of budesonide, ultrasonic nebulizers should not be used to administer AIRCORT suspension to be nebulised.
Instructions for Use
Gently shake the single-dose container with a twisting motion.
Hold the single-dose container upright and open by rotating the flap until the container opens.
Put the open end of the single-dose container well into the nebulizer tank and press slowly.
Note: Rinse the mouth with water after each administration in order to reduce the appearance of oropharyngeal thrush.
If a face mask is used, it must be ensured that the mask adheres well during spraying. After using the face mask, wash your face with water to prevent irritation.
Cleaning: The nebulizer chamber must be cleaned after each administration. Wash the nebulizer chamber and mouthpiece or face mask in warm tap water using a mild detergent or follow the manufacturer's instructions. Rinse well and dry the chamber by rejoining the compressor and inhaler.
Overdose What to do if you have taken an overdose of Aircort
Acute overdose with AIRCORT suspension for nebulisation, even in high doses, should not cause clinical problems. In case of accidental intake of a dose of AIRCORT, notify your doctor immediately or go to the nearest hospital.
IF YOU HAVE ANY DOUBT ABOUT USING THE AIRCORT SUSPENSION TO NEBULIZE, CONTACT YOUR DOCTOR OR PHARMACIST.
Side Effects What are the side effects of Aircort
Like all medicines, AIRCORT can cause side effects, although not everybody gets them.
Clinical trials, literature and marketing experience suggest that the following adverse reactions may occur. The following definitions refer to the incidence of undesirable effects.
Frequencies are defined as: very common (> 1/10), common (> 1/100 to 1,000 to 1 / 10,000 to
* Refer to Description of selected adverse reactions; facial skin irritation, listed below
** Please refer to the "Pediatric Population" section below.
Rarely, for unknown mechanisms, drugs administered by inhalation can cause bronchospasm.
With inhaled administration of glucocorticosteroids, signs and symptoms of systemic glucocorticosteroid effects may rarely occur including adrenal hypofunctionality and decreased rate of growth which are likely to depend on dose, exposure time, concomitant and previous steroid treatment and by individual sensitivity.
Description of selected adverse reactions
Some cases of facial skin irritation have been observed following the use of the face mask for nebulization. To prevent irritation the skin of the face should be washed after use of the face mask.
Patients recently diagnosed with chronic obstructive pulmonary disease (COPD) who start treatment with inhaled corticosteroids are at increased risk of developing pneumonia.However, a weighted evaluation of 8 pooled clinical trials conducted in 4643 patients with COPD and treated with budesonide and 3643 patients randomized to treatments without inhaled corticosteroids found no increased risk of developing pneumonia. The results of the first 7 of these 8 clinical studies were published in a meta-analysis.
Pediatric population
Given the risk of growth retardation in the pediatric patient population, growth should be monitored as described in the "Precautions for use" section.
The compliance with the instructions contained in the package leaflet reduces the risk of undesirable effects.
Reporting of side effects
If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. Side effects can also be reported directly via the national reporting system at: https://www.aifa.gov.it/content/segnalazioni-reazioni-avverse. By reporting side effects you can help provide more information on the safety of this medicine.
Expiry and Retention
See the expiration date printed on the package. This date means for the product in intact packaging, properly stored.
Warning: do not use the medicine after the expiry date indicated.
Rules for conservation
Store at a temperature not exceeding 25 ° C in the original packaging to protect the product from light.
After opening the aluminum bag, the single-dose containers are valid for 3 months. After this time, the residual product must be eliminated.
After opening the foil pouch, unused single-dose containers must be stored in the pouch protected from light.
The opened single-dose container must be used within 12 hours. After this time, the residual product must be eliminated.
Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. This will help protect the environment.
KEEP THE MEDICINAL PRODUCT OUT OF THE SIGHT AND REACH OF CHILDREN.
AIRCORT 0.25 mg / ml suspension to be nebulised
1 single-dose container contains:
active ingredient: budesonide 0.5 mg
Excipients: Disodium edetate; sodium chloride; polysorbate 80; anhydrous citric acid; sodium citrate; water for injections.
AIRCORT 0.5 mg / ml suspension to be nebulised
1 single-dose container contains:
active ingredient: budesonide 1 mg
Excipients: Disodium edetate; sodium chloride; polysorbate 80; anhydrous citric acid; sodium citrate; water for injections.
Pharmaceutical form and content
Suspension to be sprayed.
Each package contains 20 single-dose containers divided into 5-unit strips contained in an aluminum bag.
Source Package Leaflet: AIFA (Italian Medicines Agency). Content published in January 2016. The information present may not be up-to-date.
To have access to the most up-to-date version, it is advisable to access the AIFA (Italian Medicines Agency) website. Disclaimer and useful information.
01.0 NAME OF THE MEDICINAL PRODUCT
AIRCORT suspension to be sprayed
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
AIRCORT 0.5 mg / 2 ml suspension for nebulisation
1 single-dose container contains:
active principle: budesonide 0.5 mg
AIRCORT 1 mg / 2 ml suspension for nebulisation
1 single-dose container contains:
active principle: budesonide 1 mg
03.0 PHARMACEUTICAL FORM
Suspension to be sprayed
04.0 CLINICAL INFORMATION
04.1 Therapeutic indications
AIRCORT suspension to be nebulized is indicated in the treatment of bronchial asthma.
AIRCORT suspension for nebulisation is also indicated in the treatment of acute laryngotracheobronchitis (croup).
04.2 Posology and method of administration
Bronchial asthma:
Initial dose
The dosage of AIRCORT suspension to be nebulised is individual.
The starting dose should be:
Children over 3 months and up to 12 years of age:
0.25-0.5 mg twice a day. In some cases the dose may be further increased up to 1 mg twice a day.
Adults and the elderly:
0.5-1 mg twice a day. If necessary, the dose can be further increased.
In cases where a greater therapeutic effect is required, it is possible to administer higher doses of AIRCORT suspension to be nebulized; in fact the risks of systemic effects are low, if compared with those detectable following a treatment in combination with oral glucocorticosteroids.
Maintenance dose:
The maintenance dose is individual.
Once the desired clinical results are achieved, the maintenance dose should be gradually reduced until the minimum amount necessary to control symptoms is achieved.
Onset of effect:
Improvement in asthma control and following administration of AIRCORT inhaled nebuliser suspension may occur within three days of starting treatment, although maximum benefit is obtained after 2 - 4 weeks.
Patients treated with oral steroids:
AIRCORT suspension to be nebulized, can allow the replacement or significant reduction of the dosage of oral steroids, maintaining or improving the control of asthma.
Initially, AIRCORT Nebuliser Suspension should be administered in conjunction with the patient's usual maintenance dose of the oral steroid.
After about a week, the dose of the oral steroid is gradually reduced until the minimum required amount is reached. A slow transition from oral steroid treatment to AIRCORT nebuliser suspension is recommended. In many cases it is possible to completely replace the oral steroid with AIRCORT suspension to be nebulised.
Splitting the dose and mixing
AIRCORT suspension to be nebulised can be mixed with 0.9% physiological solution and with nebulisation solutions of terbutaline, salbutamol, fenoterol, acetylcysteine, sodium chromoglycate or ipratropium bromide.
The mixture should be used within 30 minutes.
The contents of the single-dose container can be divided to allow for dosage adjustment.
A line is clearly visible on the single-dose containers of AIRCORT suspension to be nebulized. When the single-dose container is held upside down, the line indicates a volume equal to 1 ml. If only 1 ml is to be used, empty the contents of the single-dose container until the liquid surface reaches the indicated line.
Before using the remaining liquid, shake the contents carefully with a twisting motion.
Dosage table
* The product must be mixed with 0.9% physiological solution to reach the volume of 2 ml.
Laryngotracheobronchitis:
In infants and children the usual dose is 2 mg of AIRCORT suspension to be nebulised which can be given as a single administration or with two doses of 1 mg 30 minutes apart.
Note:
Nebulization time and the amount of drug delivered by a nebulizer depend on the flow rate of the compressor and the fill volume.
In vitro the quantity of budesonide delivered by the nebulizer varies between 30-70% of the nominal dose, depending on the type of nebulizer and compressor used and not all nebulizers and compressors are suitable for the use of AIRCORT suspension to be nebulized.
To obtain the maximum budesonide delivery, a compressor is required that guarantees a flow of 5 to 8 l / min and a filling volume of 2-4 ml.
Studies performed in vivo have shown that the dose of nebulised budesonide administered to patients varies between 11 and 22% of the nominal dose.
For children, we recommend the use of a perfectly tight and well-fitting face mask, capable of optimizing the administered dose of budesonide.
Due to the small delivered amount of budesonide, ultrasonic nebulizers should not be used to administer AIRCORT suspension to be nebulised.
04.3 Contraindications
Hypersensitivity to the active substance or to any of the excipients.
Generally contraindicated in pregnancy and lactation (see 4.6).
04.4 Special warnings and appropriate precautions for use
AIRCORT Nebuliser Suspension is not intended for the rapid improvement of acute episodes of asthma, for which a short-acting bronchodilator is required.
The physician must carefully evaluate the cases of patients who do not benefit from the use of short-acting bronchodilators or who increase the number of inhalations compared to the usual one. In these cases, the physician should evaluate the need for increased therapy with anti-inflammatory drugs, for example by increasing the dose of inhaled budesonide or by starting a course of oral glucocorticosteroid therapy.
Particular attention should be paid to transferring patients from oral steroid therapy as the risk of adrenal compromise may remain for a long period of time. Patients who have required emergency therapy with high doses of corticosteoids or prolonged treatment with high doses of inhaled corticosteroids may also be at risk. Patient drapes may show signs and symptoms of adrenal insufficiency when exposed to severe stress. In times of stress or in the case of elective surgery, additional coverage with systemic corticosteroids should be considered.
During the suppression phase of systemic glucocorticosteroid therapy some patients may experience general malaise such as muscle and joint pain. General glucocorticosteroid insufficiency should be suspected in the rare cases of onset of symptoms such as fatigue, headache, nausea and vomiting.
Some patients may experience symptoms of systemic glucocorticosteroid suppression such as joint and / or muscle pain, fatigue and depression despite the maintenance or even improvement of lung function during the period of withdrawal of oral steroid treatment. Such patients should be encouraged to continue therapy with AIRCORT Nebuliser Suspension but should be monitored for objective signs of adrenal insufficiency. If there is evidence of adrenal insufficiency, the dose of systemic corticosteroid should be temporarily increased and the transfer to AIRCORT Nebuliser Suspension may be continued later, more slowly. During times of stress or during a severe asthma attack, patients who are replacing systemic steroid treatment with inhaled therapy may need additional systemic corticosteroid treatment.
Replacing systemic steroid treatment with inhaled therapy can sometimes manifest allergies, such as rhinitis and eczema, previously controlled by systemic steroid treatment. These allergic manifestations should be symptomatically controlled with antihistamine drugs and / or topical preparations.
Impaired hepatic function may affect the elimination of glucocorticosteroids, this may be clinically relevant in patients with severely impaired hepatic function.
In vivo studies have shown that oral administration of ketoconazole and itraconazole (known inhibitors of CYP3A4 activity in the liver and intestinal mucosa - see also Interactions) may increase systemic exposure to budesonide. This is of limited clinical importance in the case of short-term treatment (1 - 2 weeks) but must be taken into account in long-term treatment.
Special considerations are needed in the case of patients with pulmonary tuberculosis.
AIRCORT should be used with caution in patients with fungal and viral infections (such as measles and chickenpox) and in those with glaucoma and cataracts.
The local and systemic effects of long-term treatment in humans with AIRCORT Nebuliser Suspension are not fully known. Once control of asthma is achieved, the dose to be used in maintenance treatment should be the least effective. AIRCORT should be used with caution in children. Physicians should carefully monitor the growth of children and adolescents taking corticosteroids by any route of administration and evaluate the benefits of corticosteroid therapy and asthma control against the possibility of growth suppression.
04.5 Interactions with other medicinal products and other forms of interaction
No interactions of budesonide have been observed with any other drug used in the treatment of asthma.
The metabolism of budesonide is mainly mediated by CYP3A4, the cytochrome p450 isoenzyme. Inhibitors of this enzyme, such as ketoconazole and itraconazole, may therefore increase systemic exposure to budesonide (see Precautions for use).
At recommended doses cimetidine has a slight effect on the pharmacokinetics of orally administered budesonide not clinically relevant.
Tell your doctor or pharmacist if you have recently taken any other medicines, even those without a prescription.
04.6 Pregnancy and lactation
There are no adequate and well-controlled studies on the use of the drug in pregnancy or lactation. Therefore, the medicine should only be used in case of need, under the direct supervision of the doctor, after carefully evaluating the expected benefit to the mother in relation to the possible risk to the fetus or infant. Ask your doctor or pharmacist for advice before taking any medicine.
04.7 Effects on ability to drive and use machines
AIRCORT Nebuliser suspension does not restrict the ability to drive and use machines.
04.8 Undesirable effects
Clinical trials, literature and marketing experience suggest that the following adverse reactions may occur:
Rarely, for unknown mechanisms, drugs administered by inhalation can cause bronchospasm.
With inhaled administration of glucocorticosteroids, signs and symptoms of systemic glucocorticosteroid effects may rarely occur including adrenal hypofunctionality and decreased rate of growth which are likely to depend on dose, exposure time, concomitant and previous steroid treatment and by individual sensitivity.
Some cases of facial skin irritation have been observed following the use of the face mask for nebulization. To prevent irritation the skin of the face should be washed after use of the face mask.
04.9 Overdose
Acute overdose with AIRCORT suspension for nebulisation, even in high doses, should not cause clinical problems.
05.0 PHARMACOLOGICAL PROPERTIES
05.1 Pharmacodynamic properties
Pharmacotherapeutic group: other anti-asthma, inhalers, glucocorticoids.
ATC code: R03BA
Local anti-inflammatory activity
The exact mechanism of action of glucocorticoids in the treatment of asthma is not fully understood. The anti-inflammatory activity directed against T cells, eosinophils and mast cells, as well as the inhibition of the release of inflammatory mediators and the inhibition of the cytokine mediated immune response are probably important. The intrinsic potency of budesonide, measured as affinity in comparisons of glucocorticoid receptors, is approximately 15 times higher than that of predmisolone.
A clinical study conducted in asthmatic patients, in which the administration of inhaled budesonide was compared with that by mouth at similar plasma concentrations, demonstrated "evidence of significant efficacy with inhaled administration, but not with administration orally, compared to placebo. Therefore, the therapeutic effect of conventional so-called budesonide, administered by inhalation, can be largely attributed to local action in the respiratory tract.
In provocative studies conducted in animals and patients, budesonide has been shown to have an anti-anaphylactic and anti-inflammatory effect, represented by the reduction of the degree of bronchial obstruction in the immediate and late allergic response.
Respiratory Tract Reactivity:
In hyper-reactive patients, budesonide has been shown to reduce the reactivity of the airways to histamine and methacholine.
05.2 Pharmacokinetic properties
Absorption
In adults, the systemic bioavailability of budesonide, after administration of the suspension to be nebulized via a jet nebulizer, is approximately 155 of the nominal dose and 40-70% of the dose delivered to patients. A minor fraction of the drug's systemic availability comes from ingested drug. After administration of a single dose of 2 mg, the maximum plasma concentration, which is reached approximately 10-30 minutes after the start of nebulization, is approximately 4 nmol / l.
Distribution
Budesonide has a volume of distribution of approximately 3 l / kg. Plasma protein binding is, on average, 85-90%.
Biotransformation
First pass hepatic budesonide is rapidly metabolised in a high percentage (> 90%) to metabolites characterized by poor glucocorticosteroid activity. The main metabolites are 6-β-hydroxybudesonide and 16-alpha-hydroxyprednisolone, the glucocorticosteroid activity is less than 1%, compared to that of budesonide. The metabolism of budesonide is mainly mediated by the isoenzyme CYP3A4, belonging to the cytochrome p450.
Elimination
The metabolites of budesonide are excreted as such or in conjugated form, mainly by the kidney. Unchanged budesonide is not found in the urine. In healthy adults, budesonide has a high systemic clearance (approximately 1.2 l / min) and, after IV administration, the terminal half-life is, on average, 2/3 hours.
Linearity
At clinically relevant dosages, the kinetic parameters of budesonide are dose dependent.
Children
After administration of the nebuliser suspension, in asthmatic children aged 4-6 years, the systemic bioavailability of budesonide is approximately 6% of the nominal dose and 26% of the dose delivered to patients. In children, the systemic bioavailability is approximately half that found in healthy adults. In 4-6 year old asthmatic children, after the administration of a 1 mg dose, the maximum plasma concentration which is reached about 20 minutes after the start of nebulization, is equal to about 2.4 nmol / l.
In 4-8 year old asthmatic children, the systemic clearance of budesonide is approximately 0.5 l / min. With reference to body weight, expressed in kg, children have a clearance3 that is approximately 50% higher than that found in adults. In asthmatic children, the terminal half-life of budesonide after inhalation is approximately 2.3 hours. This value is similar to that observed in healthy adults.
In children aged 4-6 years, the exposure (Cmax and AUC) of budesonide following administration of a single 1mg dose by nebulisation is comparable to that observed in healthy adults treated with the same dose using the same nebulisation system. .
05.3 Preclinical safety data
The results of acute, subacute and chronic toxicity studies show that the systemic effects of budesonide are either less severe, or similar to those observed after administration of other glucocorticosteroids, for example, decreased weight gain, lymphoid and adrenal tissue atrophy .
Budesonide, evaluated with 6 different tests, did not demonstrate any mutagenic or clastogenic effects.
The increase in the incidence of cerebral gliomas, found in a carcinogenicity study conducted in male rats, was not confirmed in 2 subsequent studies, in which the incidence of gliomas observed in the groups treated with active drugs (budesonide, prednisolone, triancinolone acetate ) was similar to that observed in the control groups.
Carcinogenicity studies conducted in male rats allowed to observe liver changes (primary hepatocellular neoplasms) which were confirmed in another study by treating the animals with budesonide and reference glucocorticosteroids. These manifestations are probably related to receptor effects of glucocorticosteroids and represent an effect typical of the therapeutic class.
The available clinical experience shows that there is no evidence that budesonide, or other glucocorticosteroids, cause brain gliomas or primary hepatocellular neoplasms in humans.
06.0 PHARMACEUTICAL INFORMATION
06.1 Excipients
Disodium edetate, sodium chloride, polysorbate 80, anhydrous citric acid, sodium citrate, water for injections.
06.2 Incompatibility
There are no known incompatibilities.
For compatible products, see section 4.2.
06.3 Period of validity
3 years.
06.4 Special precautions for storage
Store at a temperature not exceeding 25 ° C in the original packaging to protect the product from light.
After opening the aluminum bag, the single-dose containers are valid for 3 months. After this time, the residual product must be eliminated.
After opening the foil pouch, unused single-dose containers must be stored in the pouch protected from light.
The opened single-dose container must be used within 12 hours. After this time, the residual product must be eliminated.
06.5 Nature of the immediate packaging and contents of the package
Single-dose container in low density polyethylene containing 2 ml of suspension.
Each package contains 20 single-dose containers divided into 5-unit strips contained in an aluminum bag.
06.6 Instructions for use and handling
Gently shake the single-dose container with a twisting motion.
Hold the single-dose container upright and open by rotating the flap until the container opens.
Put the open end of the single-dose container well into the nebulizer tank and press slowly.
Note:
Rinse mouth with water after each administration.
If a face mask is used, it must be ensured that the mask adheres well during spraying. After using the face mask, wash your face with water to prevent irritation.
Cleaning:
The nebulizer chamber must be cleaned after each administration. Wash the nebulizer chamber and mouthpiece or face mask in warm tap water using a mild detergent or follow the manufacturer's instructions. Rinse well and dry the chamber by rejoining the compressor and inhaler.
07.0 MARKETING AUTHORIZATION HOLDER
Italchimici SpA, Via Pontina 5, Km 29, 00040 Pomezia (Rome)
08.0 MARKETING AUTHORIZATION NUMBER
AIRCORT 0.5 mg / 2 ml suspension for nebulisation - 20 single-dose containers AIC: 033736063
AIRCORT 1 mg / 2 ml suspension for nebulisation - 20 single-dose containers AIC: 033736075
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION
10.0 DATE OF REVISION OF THE TEXT
December 2007
