Biosone

Biosone

beclometasone

Manufacturer:

BioCare

Distributor:

BioCare
Full Prescribing Info
Contents
Beclomethasone dipropionate.
Description
Pressurised Metered-Dose Inhaler canister contains 200 metered doses, each containing 100mcg of Beclometasone dipropionate BP. It does not contain CFC as propellant.
Biosone HFA is a bulk preparation for inhalation, supplied in a pressurised container. On visual examination, the pressurised container has no sign of physical damage or leakage. The product is a clear solution.
Action
ATC Code: R03 BA01.
Pharmacology: Pharmacodynamics: The active ingredient of Biosone 100 HFA Inhaler is Beclometasone Dipropionate (BDP) a topical corticosteroid endowed with potent anti-inflammatory and anti-allergic activity on the airways mucosa. Beclometasone dipropionate, administered by inhalation and in recommended doses, has a glucocorticoid anti-inflammatory action within the lungs but no systemic effect.
Pharmacokinetics: Absorption when administered via inhalation by a MDI: Systemic absorption of unchanged beclometasone dipropionate (BDP) occurs through the lungs. There is negligible oral absorption of the swallowed dose of unchanged BDP. Prior to absorption there is extensive conversion of BDP to its active metabolite B-17-MP. The systemic absorption of B-17-MP arises from both lung deposition (36%) and oral absorption of the swallowed dose (26%). The absolute bioavailability following inhalation is approximately 2% and 62% of the nominal dose for unchanged BDP and B-17-MP, respectively. BDP is absorbed rapidly with peak plasma concentrations observed (tmax) at 0.3 hour. B-17-MP appears more slowly with a tmax of 1 hour. There is an approximately linear increase in systemic exposure with increasing inhaled dose. When administered orally the bioavailability of BDP is negligible but presystemic conversion to B-17-MP results in 41% of the dose being absorbed as B-17-MP.
Distribution: The tissue distribution at steady-state for BDP is moderate (20 L) but more extensive for B-17-MP (424 L). Plasma protein binding is moderately high (87%).
Biotransformation: BDP is cleared very rapidly from the systemic circulation, by metabolism mediated via esterase enzymes that are found in most tissues. The main product of metabolism is the active metabolite (B-17-MP). Minor inactive metabolites, beclometasone-21-monopropionate (B-21-MP) and beclometasone (BOH), are also formed but these contribute little to the systemic exposure.
Elimination: The elimination of BDP and B-17-MP are characterized by high plasma clearance (150 L/hour and 120 L/hour) with corresponding terminal elimination half-lives of 0.5 hour and 2.7 hour. Following oral administration of titrated BDP, approximately 60% of the dose was excreted in the faeces within 96 hours mainly as free and conjugated polar metabolites. Approximately 12% of the dose was excreted as free and conjugated polar metabolites in the urine. The renal clearance of BDP and its metabolites is negligible.
Indications/Uses
Indicated for the prophylactic management of mild, moderate or severe asthma.
Dosage/Direction for Use
Adults: 200mcg twice a day. Alternatively, the total daily dose may be administered as 3 or 4 divided doses. In severe cases, dosage maybe started at 600-800 mcg/day and subsequently reduced when the patient begins to respond. Children: 1 or 2 inhalations (50-100 mcg/day) should be given 2, 3, or 4 times daily accordingly to the response.
Overdosage
Acute: Inhalation of doses in excess of those recommended may lead to temporary suppression of adrenal function. This does not require emergency action. In these patients treatment should be continued at a dose sufficient to control asthma; adrenal function recovers in a few days and can be verified by measuring plasma cortisol.
Chronic: Use of inhaled beclomethasone dipropionate in daily doses in excess of 1,500mcg over prolonged periods may lead to adrenal suppression. Monitoring of adrenal reserve may be indicated. Treatment should be continued at a dose sufficient to control asthma.
Contraindications
Hypersensitivity to Beclometasone inhaler is a contraindication; and special care is necessary in patients with active or quiescent pulmonary tuberculosis.
Warnings
Patients should be properly instructed on the use of the inhaler to ensure that the drug reaches the target areas within the lungs. Patients should also be informed that Biosone 100 mcg/dose HFA Inhalation Aerosol should be used on a regular basis, even when they are asymptomatic. Biosone 100 mcg/dose HFA Inhalation Aerosol does not provide relief of acute asthma symptoms, which require a short-acting inhaled bronchodilator. Patients should have relief medication available.
Severe asthma requires regular medical assessment, including lung-function testing, as there is a risk of severe attacks and even death. Patients should be instructed to seek medical attention if short-acting relief bronchodilator treatment becomes less effective, or more inhalations than usual are required as this may indicate deterioration of asthma control. If this occurs, patients should be assessed and the need for increased anti-inflammatory therapy considered (eg. Higher doses of inhaled corticosteroid or a course of oral corticosteroid).
Severe exacerbations of asthma must be treated in the usual way, ie. By increasing the dose of inhaled beclometasone dipropionate, giving a systemic steroid if necessary, and/or an appropriate antibiotic if there is an infection, together with β-agonist therapy. Treatment with Biosone 100 mcg/dose HFA Inhalation Aerosol should not be stopped abruptly. Systemic effects of inhaled corticosteroids may occur, particularly when prescribed at high doses for prolonged periods. These effects are much less likely to occur than with oral corticosteroids.
Possible systemic effects include adrenal suppression, growth retardation in children and adolescents, decrease in bone mineral density, cataract and glaucoma. It is important 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 reviewed with the aim of reducing the dose of inhaled corticosteroids, if possible, to the lowest dose at which effective control of asthma is maintained.
In addition, consideration should also be given to referring the patient to a paediatric respiratory specialist. Prolonged treatment with high doses of inhaled corticosteroids may result in clinically significant adrenal suppression. Additional systemic corticosteroid cover should be considered during periods of stress or elective surgery. The transfer to Biosone 100 mcg/dose HFA Inhalation Aerosol of patients, who have been treated with systemic steroids for long periods of time or at high doses, needs special care, since recovery from possible adrenocortical suppression may take considerable time.
Reduction of the dose of systemic steroid can be commenced approximately one week after initiating treatment with Biosone 100 mcg/dose HFA Inhalation Aerosol. The size of the reduction should correspond to the maintenance dose of systemic steroid. For patients receiving maintenance doses of 10mg daily or less of prednisolone (or equivalent) reductions in dose of not more than 1 mg are suitable. For higher maintenance doses, larger reductions in dose may be appropriate. These oral dosage reductions should be introduced at not less than weekly intervals. Adrenocortical function should be monitored regularly as the dose of systemic steroid is gradually reduced.
Some patients feel unwell during withdrawal of systemic steroids despite maintenance or even improvement of respiratory function. They should be encouraged to persevere with inhaled beclometasone dipropionate and to continue withdrawal of systemic steroid, unless there are objective signs of adrenal insufficiency. Patients weaned off oral steroids whose adrenocortical function is impaired should carry a steroid warning card indicating that they may need supplementary systemic steroids during periods of stress, eg. Worsening asthma attacks, chest infections, major intercurrent illness, surgery, trauma, etc.
Replacement of systemic steroid treatment with inhaled therapy sometimes unmasks allergies such as allergic rhinitis or eczema previously controlled by the systemic drug. These allergies should be symptomatically treated with antihistamine and / or topical preparations, including topical steroids. As with all inhaled corticosteroids, special care is necessary in patients with active or quiescent pulmonary tuberculosis. Patients should be advised that this product contains small amounts of ethanol (approximately 4.320 mg per actuation) and glycerol. At the normal doses, the amounts of ethanol and glycerol are negligible and do not pose a risk to patients.
Use In Pregnancy & Lactation
The safety of Beclometasone dipropionate for use in human pregnancy has not been established. Reproduction toxicity studies in animals have revealed an increased incidence of foetal damage, the significance of which is considered uncertain in man. Since the possibility of suppression of the adrenal cortex in the newborn baby after long-term treatment must be considered the needs of the mother must be carefully weighed against the risk of the foetus. It is reasonable to assume that the drug is distributed into the breast milk, but at the dosages used for direct inhalation, there is low potential for significant levels in breast milk.
Side Effects
Candidiasis of the mouth and throat (thrush) occurs in some patients, the incidence of which is increased with doses greater than 400mcg Beclometasone dipropionate per day. Patients with high blood levels of Candida precipitins, indicating a previous infection, are most likely to develop this complication. Some patients may find it helpful to rinse their mouth thoroughly with water after using the inhaler. Symptomatic candidiasis can be treated with topical antifungal therapy whilst still continuing with the Beclometasone inhaler. In some patients, inhaled Beclometasone dipropionate may cause hoarseness or throat irritation. It may be helpful to rinse mouth with water immediately after inhalation. As with other inhalation therapy, the potential for paradoxical bronchospasm should be kept in mind. If it occurs, the preparation should be discontinued immediately and alternative therapy instituted.
Drug Interactions
There are no known interactions of inhaled corticosteroids with other drugs. The use of inhaled sympathomimetic drug prior to inhalation of steroid may improve the lung distribution. If used concomitantly with systemic or intranasal steroids the suppressive effect on adrenal function may be potentiated.
Storage
Store below 30°C. Protect from direct sunlight and heat.
Shelf-Life: 2 years.
Patient Counseling Information
HOW TO USE YOUR INHALER CORRECTLY: 1. Remove the cap from the mouthpiece of the actuator.
2. Make sure the mouthpiece is clean inside and outside.
3. Raise the Inhaler to your mouth. Put the mouthpiece between your teeth, but do not bite it. Close your lips around the mouthpiece. Breathe out slowly and gently through the Inhaler until your lungs feel comfortably empty.
4. Tilt your head back slightly. Start to breathe in slowly through your mouth. As you start to breathe in, press down firmly on the top of the can to release your medicine continue to breathe in steadily and deeply.
5. Hold your breath. Remove the inhaler from your mouth. Continue to hold your breath as long as possible, up to 10 seconds. Then breathe out gently. If you are taking a second puff, wait about one minute, then repeat steps 3 to 6.
6. Replace the mouthpiece cap after each use.
In case of emergency situation when you feel you are not relieved despite using your inhaler, you can use inhaler along with spacer (a device that your doctor advise to use with your inhaler). This may save your life on the way to hospital. For more information, consult with your doctor.
A handy tip for Children: Children and others who have weaker hands may have difficulty pressing down on the top of the can with just one hand. They can use both hands to make their Inhaler work.
Cleaning your Inhaler: Keeping the plastic actuator clean is very important to prevent medicine buildup and blockage. The actuator should be washed, shaken to remove excess water and air-dried thoroughly at least once a week. The inhaler may stop spraying if not properly cleaned.
How to clean your Inhaler: 1. Remove the metal canister from the plastic casing of the inhaler and remove the mouthpiece cover.
2. Rinse the actuator thoroughly with warm water.
3. Dry the actuator thoroughly inside and outside.
4. Replace the metal canister and the mouthpiece cover.
5. Do not put the metal canister in water.
Your Inhaler should be cleaned at least once a week.
Shake well the inhaler before each use.
Precaution: 1. Pressurised canister, do not puncture, break or incinerate even when apparently empty.
2. Avoid storage in direct sunlight or heat.
3. Store below 30° C
4. Keep away from eyes
ATC Classification
R03BA01 - beclometasone ; Belongs to the class of other inhalants used in the treatment of obstructive airway diseases, glucocorticoids.
Presentation/Packing
MDI 100 mcg/dose x 200 metered doses.
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