Each mL contains: Budesonide 250 mcg.
Budesonide is an anti-inflammatory synthetic corticosteroid. Budesonide is provided as mixture of two epimers (22R and 22S).
Pharmacology: Pharmacokinetics: In a pharmacokinetic study, the estimated daily infant dose was 0.3% of the daily maternal dose for both dose levels, and the average plasma concentration in infants was estimated lobe 1/600.
In adults the systemic bioavailability of budesonide following administration of Budesonide Suspension for Nebulization via a jet nebulizer is approximately 15% of the declared dose and 40-70% of the dose delivered to the patient. A small part of the systematically available dose comes from inhalation suspension that is allowed. The peak plasma concentration following administration of a single dose of 2 mg is achieved 10 -30 minutes after the beginning of inhalation and is approximately 4 nmol/L. In children (4 - 6 years), the systemic bioavailability of budesonide after administration of Budesonide Suspension for Nebulization via jet nebulizer is approximately 6% of the declared dose and 26% of the dose administered to the patient. The peak plasma concentration following administration of a single dose of 1 mg Is approximately 20 minutes after the beginning of inhalation and is approximately 2.4 nmol/L.
Distribution: The volume of distribution in adults is approximately 3 L/kg. Plasma protein binding is approximately 85-90%.
Metabolism: Budesonide undergoes extensive, (90%) first pass biotransformation in the liver via CYP3A4 to metabolites with a low glucocorticosteroid activity. The in-vitro activity of the main metabolites, 6,α-hydroxyprednisolone, and 16-α-hydroxyprednisolone, is less than 1% of that budesonide.
Excretion: The metabolites are excreted in unchanged or conjugated form predominantly via the kidneys.
No unchanged budesonide is found in the urine. Budesonide has a high systemic clearance (approximately 1.2 Liters/min) in healthy adults, and the elimination half-life following intravenous administration is approximately 2-3 hours. Budesonide has a systemic clearance of approximately 0.5 L/min in 4 to 6 year old asthmatic children.
Children have an approximately 50% higher clearance per kg body weight than adults. The half-life of budesonide following inhalation is about 2.3 hours in asthmatic children, which is roughly the same in healthy adults.
Treatment of persistent bronchial asthma in patients where use of pressurized inhaler or dry powder formulation is unsatisfactory or inappropriate.
Route of administration: For inhalation use only.
The dose should be given twice daily.
Administration once daily maybe considered in cases of mild to moderate stable asthma.
Initial dose: The initial dose should be tailored to the severity of the disease and thereafter should be adjusted on an individual basis. The following doses are recommended but the minimum effective dose should always be sought: Children aged 6 months and above: 250 mcg - 1 mg daily. For patients in maintenance therapy with oral steroids a higher initial dosage up to 2 mg daily should be considered.
Adults (including elderly) and children/adolescents over 12 years of age: 500 mcg -2 mg daily. In very severe cases, the dosage may be increased further.
Maintenance dose: The maintenance dose should be adjusted to meal the requirements of the individual patient taking account of the severity of the disease and the clinical response of the patient.
When the desired clinical effect has been obtained, the maintenance dose should be reduced to the minimum required for control of the symptoms.
Children aged 6 months and above: 250 mcg - 1 mg daily.
Adults (Including the elderly) and children/adolescents over 12 years of age: 500 mcg - 2 mg daily. In severe cases the dose may be further increased.
Administration once daily: Administration once daily should be considered for children and adults with mild to moderate stable asthma and with a maintenance dose between 250 mcg and 1 mg budesonide daily. Once daily administration may be initiated both in patients who are not receiving corticosteroid treatment and in well-controlled patients who are already taking inhaled steroids. The dose may be given in the morning or evening. If a worsening of the asthma occurs, the daily dose should be increased by administering the dose twice daily.
Onset of effect: An improvement of the asthma following administration of budesonide may occur within 3 days after initiation of therapy. The maximum effect will only be obtained after 2-4 weeks of treatment.
Patients in maintenance therapy with glucocorticoids: With Budesonide 500 mcg/2 mL Suspension for Nebulization, it is possible to replace or considerably reduce the dose of oral glucocorticosteroids and still maintains or improves the control of asthma.
Stated by reducing the daily dose gradually (by for example 2.5 mg prednisolone or the equivalent each month) to the lowest possible level. It may be possible to completely replace the oral corticosteroid with inhaled corticosteroid.
Transferred patients whose adrenocortical function is impaired may need supplementary systemic corticosteroid during periods of stress e g. surgery, infection or worsening asthma attacks. Patients who have required high dose emergency corticosteroid therapy or prolonged treatment at the highest recommended dose of inhaled corticosteroids, may also be at risk of impaired adrenal function. These patients may exhibit signs and symptoms of adrenal insufficiency when exposed to severe stress. Additional systemic corticosteroid treatment should be considered during periods of stress or elective surgery.
During transfer from oral therapy to inhaled budesonide, symptoms may appear that had previously been suppressed by systemic treatment with glucorticosteroids, for example symptoms of allergic rhinitis, eczema, muscle and joint pain. Specific treatments should be co-administered to treat the conditions. Some patients may feel unwell in non-specific way during the withdrawal of systemic corticosteroids despite maintenance or even improvement in respiratory function. Such patients should be encouraged to continue treatments with inhaled budesonide and withdrawal of oral corticosteroid unless there are clinical signs to indicate contrary, for example signs which might indicate adrenal insufficiency.
As with other inhalation therapies paradoxical bronchospasm may occur, manifested by an immediate increase in wheezing and shortness of breath after dosing. Paradoxical bronchospasm responds to a rapid-acting inhaled bronchodilator and should be treated straight away.
Budesonide should be discontinued immediately, the patient should be assessed and, if necessary, alternative treatments instituted.
When an acute episode of dyspnea occurs despite a well monitored treatment, a rapid-acting inhaled bronchodilator should be used and medical reassessment should be considered. If despite maximum doses of inhaled corticosteroids, asthma symptoms are not adequately controlled, patients may require short-term treatment with systemic corticosteroids. In such cases. It is necessary to maintain the inhaled corticosteroid therapy in association with treatment by the systemic route.
Systemic effects of inhaled corticosteroids may occur, particularly at high doses prescribed for prolonged periods. These effects are much less likely to occur than with oral corticosteroids. Possible systemic effects include Cushing's syndrome, Cushingoid features, adrenal suppression, growth retardation in children and adolescents, decrease in bone mineral density, cataract, glaucoma and more rarely, a range of psychological or behavioral effects including psychomotor hyperactivity, sleep disorders, anxiety, depression or aggression (particularly in children). It is important, therefore, that the dose of inhaled corticosteroid is titrated to the lowest dose at which effective control of asthma is maintained.
It is recommended that the height of children receiving prolonged treatment with inhaled corticosteroids is regularly monitored. If growth is slowed, therapy should be re-evaluated with the aim of reducing the dose of inhaled corticosteroid.
Pregnancy: Results from a large prospective epidemiological study and from world-wide post marketing experience indicate that inhaled budesonide during pregnancy has no adverse effects on the health of the fetus/newborn child.
As with other drugs, the administration of budesonide during pregnancy requires that the benefits for the mother are weighted against the risk for the fetus.
Lactation: Budesonide is excreted in breast milk. However, at therapeutic doses of budesonide, no effects on the suckling child are anticipated. Budesonide can be used during breastfeeding.
Maintenance treatment with inhaled budesonide (200 or 400 mcg twice daily) in asthmatic nursing women results in negligible exposure to budesonide in breast fed infants.
Direction for Use: The spray container should be shaken before use.
To minimize the risk of oropharyngeal candida infection, the patient should rinse their mouth out with water after inhaling.
To prevent irritation of the facial skin, the face should be washed after using the nebulizer with a mask.
The nebulizer should be cleaned after each use.
Wash the nebulizer container and mouthpiece or face-mask in warm water using a mild detergent in accordance with the manufacturer's instructions. Rinse well and dry it by connecting the nebulizer container to the compressor or the air inlet.
Store at temperatures not exceeding 30°C. Protect from light.
R03BA02 - budesonide ; Belongs to the class of other inhalants used in the treatment of obstructive airway diseases, glucocorticoids.
Susp for inhalation (nebulization) 500 mcg/2 mL x 2 mL x 35's.