Each 1 metered dose (capsule) contains Budesonide 200 mcg.
Pharmacology: Pharmacodynamics: Budesonide, a synthetic corticosteroid, has potent glucocorticoid and weak mineralocorticoid activity. In studies, the activity of budesonide measured as its affinity for glucocorticosteroid receptors is approximately 15 times higher than affinity of prednisolone.
The exact mechanism of action relevant to therapeutic effects is not clearly known, but is believed to work by reduction number of mediator cells in the nasal mucosa (including basophils, eosinophils, T-helper cells, mast cells and neutrophils), decrease in nasal reactivity to allergens, and inhibition of the release of proteolytic enzymes and inflammatory mediators.
Pharmacokinetics: Absorption: After inhalation of budesonide, absorption is rapid and peak plasma concentrations are reached within 30 minutes. From the studies, approximately 25-35% of the budesonide given dose is deposited in the lungs after inhalation. The systemic bioavailability of budesonide has been estimated to 38%.
Distribution: Budesonide is approximately 85-90% bound to plasma protein. The volume of distribution is approximately 3 liters/kg.
Metabolism: Budesonide undergoes extensive (about 90%) first-pass metabolism by cytochrome P-450 (CYP) isoenzyme 3A4 in the liver. The 2 main metabolites, 6 β-hydroxybudesonide and 6 α-hydroxyprednisolone, are low glucocorticoid activity. They have less than 1% of affinity for glucocorticoid receptors than budesonide (parent compound).
Elimination: After administration by the inhalation route, budesonide has half-life 2-3 hours. Its metabolites are excreted by urine (approximately 60%) and feces.
At relevant dosages, the pharmacokinetics of budesonide are dose proportional.
In children and in patients with impaired renal function, the pharmacokinetics of budesonide are unknown but expose to budesonide may be higher in patients with liver disease.
Bronchial asthma: Children 6 to 11 years: 100 to >400 micrograms daily in 2 to 4 divided doses.
The full daily dose may be given in one administration.
Adult: 200 to >800 micrograms daily in 2 to 4 divided doses.
The daily doses may be increased up to 1600 micrograms in more severe cases.
Patients taking up to 400 micrograms/day may take the full dose in one administration.
After asthma stability has been achieved, titrate to the lowest effective dose to reduce the possibility of adverse effects.
Conversion from oral systemic corticosteroid to orally inhaled corticosteroid: The patients' asthma condition should be in reasonably stable on oral corticosteroids before initiating oral inhalation therapy. A gradual dose reduction of oral corticosteroids should begin 7-10 days after starting high dose of inhaled therapy concurrently with the previously used dose of oral corticosteroid such as reducing prednisolone dose by 2.5 mg per month (or equivalent of other corticosteroids).
Mode of Administration: PULVISONIDE 200 capsules should only be used with the inhaler and inhaled through your mouth (oral inhalation).
Do not intake or swallow PULVISONIDE 200 capsules.
PULVISONIDE 200 capsules should always be stored in blister and only removed immediately before use. The capsules should not be stored in the inhaler.
After receiving orally inhaled budesonide, patients should rinse their mouth with water to remove residual drug in the oropharyngeal area and to reduce the development of fungal overgrowth and infection.
Instruction for using PULVISONIDE 200: Remove the protection cap from the inhaler.
Hold the base of the inhaler firmly.
Open the inhaler by turning the mouthpiece in the direction of the arrows.
Take a capsule and place it in the capsule chamber of the inhaler.
Check whether the capsule is completely inside the capsule chamber. If not, put the capsule in correctly.
Close the inhaler by turning the mouthpiece back to the closed position.
Hold the inhaler upright (with the mouthpiece upwards). Hold the push buttons between thumb and index finger. Use both fingers at the same time to press these buttons once. (Figure 6) The capsule is now evenly punctured.
Deeply breathe out (not through the inhaler). After that, hold the inhaler horizontally.
Tilt the head back slightly. Insert the mouthpiece of the inhaler completely into the mouth, behind the teeth and on the tongue. Close the lips tight round the mouthpiece.
Breathe in rapidly but steadily, as deeply and forcefully as the patient can. The inhaler makes a rattling noise if it is operating properly. This is because the capsule spins in the chamber as the powder disperses.
Remove the inhaler from the mouth. Hold the breath for about 5-10 seconds so that the lungs can take up the medication. Breathe out gently.
Open the inhaler and check whether the capsule is empty, if not repeat the previous four steps.
Open the inhaler and remove the empty capsule. Put the protection cap back on the inhaler.
Instruction for cleaning PULVISONIDE 200: Clean the inhaler of PULVISONIDE 200 once a week.
Open the inhaler by turning the mouthpiece as far as possible in the direction of the arrows.
Rinse the mouthpiece with running water.
Before using the inhaler again, it should be completely dry.
The potential for acute toxic effect following overdose is low. Chronic use in excessive doses may result in symptoms of glucocorticosteroid effects such as hypercorticoidism and adrenal suppression.
PULVISONIDE 200 is contraindicated in person with a history of hypersensitivity reaction to budesonide, or any of its components.
PULVISONIDE 200 is contraindicated as primary treatment of status asthmaticus.
PULVISONIDE 200 is contraindicated as primary treatment of acute episode of asthma.
PULVISONIDE 200 must not be used to relieve acute bronchospasm.
Budesonide should be used with caution in patients with thyroid disease, cardiovascular disease, diabetics, glaucoma, cataracts and myasthenia gravis.
Budesonide should be used with caution in patients with hepatic impairment because hepatic impairment may affect elimination of budesonide.
Budesonide should be used with caution in patients at risk for osteoporosis, seizures and GI diseases (diverticulitis, peptic ulcer, ulcerative colitis).
Budesonide should be used with caution in patients with acute myocardial infarction because corticosteroids have been associated with myocardial rupture.
Bronchospasm may occur following oral inhalation of budesonide. If bronchospasm occurs, stop budesonide and treat immediately with a short-acting inhaled bronchodilator.
Particular care is needed in patients who are switched from oral systemic corticosteroid to orally inhaled corticosteroid because the symptoms of steroid withdrawal caused by adrenal insufficiency may occur. Moreover, patients may experience the return of previous symptoms such as muscle and joint pain, allergies which were previously controlled by systemic steroid.
The growth of children and adolescents who are on long term treatment with corticosteroids should be monitored. The benefits of the corticosteroid therapy must be weighed against the possible risks of growth suppression.
Effects on ability to drive and use machine: PULVISONIDE 200 has no or negligible influence on the ability to drive and use machines.
Pregnancy: Category B according to US pregnancy category; Either animal-reproduction studies have not demonstrated a fetal risk but there are no controlled studies in pregnant women, or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the first trimester and there is no evidence of a risk in later trimesters.
In some animal reproduction studies, adverse events have been observed with corticosteroids. Hypoadrenalism may occur in infants born to women receiving corticosteroids during pregnancy. Based on available data, an overall increased risk of congenital malformations or a decrease in fetal growth has not been associated with maternal use of inhaled corticosteroids during pregnancy.
In addition, studies of pregnant women specifically using inhaled budesonide have not demonstrated an increased risk of congenital abnormalities.
Labor and delivery: The effects of budesonide on labor and delivery in pregnant woman are unknown.
Lactation: Although budesonide is secreted in breast milk, but at therapeutic dose of budesonide no effects on the suckling children are anticipated. PULVISONIDE 200 can be used during breast feeding.
Data with budesonide delivered via powder for oral inhalation demonstrates that approximately 0.3% to 1% of the dose inhaled by the mother was found in breast milk. The maximum concentration appeared within 45 minutes of dosing. Plasma budesonide levels obtained from infants 90 minutes after breast-feeding (140 minutes after maternal dose) were below the limit of quantification.
Very common effects (≥1:10): Respiratory, thoracic and mediastinal disorders:
Rhinitis, Upper respiratory tract infections.
Common effects (≥ 1:100 to < 1:10): Dermatologic Disorders:
Eczema, Pruritus, Rash.
Abdominal pain, Anorexia, Diarrhea, Gastroenteritis, Nausea, Vomiting, Oral candidiasis.
Respiratory, thoracic and mediastinal disorders:
Coughing, Dysphonia, Nasal congestion, Pharyngitis, chest pain.
Ear infection, Earache.
Infection, Influenza-like syndrome.
Rare effects (< 1:1,000): Nervous system disorders:
Nervousness, Restlessness, Depression, Behavioral disturbances.
Angioedema, Anaphylactic reaction, Urticaria, Rash, Dermatitis, Skin bruising.
Respiratory, thoracic and mediastinal disorders:
Budesonide should not be used together with the inhibitors of CYP3A4 isoenzyme such as ketoconazole, itraconazole because concomitant use may result in increased plasma budesonide concentration. If the combination cannot be avoided, the time interval between the administration of budesonide and inhibitors of CYP3A4 isoenzyme should be as long as possible.
Budesonide should not be used together with the inducers of CYP3A4 isoenzyme because concomitant use may result in decreased plasma budesonide concentration.
Avoid concomitant use of budesonide with aldesleukin or loxapine.
Do not store above 30°C.
Replace the mouthpiece cap firmly.
R03BA02 - budesonide ; Belongs to the class of other inhalants used in the treatment of obstructive airway diseases, glucocorticoids.
Inhalation powd cap 200 mcg (white powd filled in brown, clear-colorless cap no. 3) x 20 x 5's.