Budesonide

Generic name
Brand name
Drug Classification
Subclassification
General chemistry

Budesonide
Budecort, Bronex, Asmavent, Budecort, Primavent, Denecort,
Anti-inflammatory, Corticosteroids
Antiasthma, Glucocorticoids, Inhaled corticosteroid
steroids carrying a hydroxyl group at the 21-position of the steroid
backbone

C25H34O6

Gen Mechanism of action

ABSORPTION
Absorption

Onset
Duration of action
Cmax
Tmax
Steady state
Bioavailability
First-pass
Protein Binding
Distribution
Distribution
Vd
Metabolism
Metabolism
Metabolites
Excretion
Excretion
t1/2
Indication

contraindication

1. Decrease formation of cytokines that recruit and activate

eosinophils, and responsible for promoting the production of IgE and
the expression of IgE receptors
2. Inhibit the generation of the vasodilators PGE and PGI2 by inhibiting
induction of Cox-2
3. Inhibit effects of many inflammatory and structural cells that are
activated in asthma; and prevent the recruitment of inflammatory
cells into the airways
Budesonide + Salbutamol:
-Corticosteroid (Budenoside) upregulate and increase the B-adrenergic
responsiveness, decrease microvascular permeability and indirectly reduce
mediator release from eosinophils
-enhance each others beneficial effects in asthma therapy
Inhaled corticosteroid acts locally and may be absorbed from the airway
and alveolar surface and some inhaled steroid deposited in oropharynx is
swallowed and absorbed in the gut
24 hrs
1-2hr
6-13%
budesonide is subject to high first pass metabolism
85-90%
(organs distributed)
3L/kg
Metabolized in the liver by CYTP3A4
16-alpha hydroxyprenisolone, 6-beta hydroxybudenoside
Excreted in urine (60%), feces(40%)
2-3hrs
1. maintenance treatment of asthma, non-infectious rhinitis (including
hay fever and other allergies), and for treatment and prevention of
nasal polyposis.
2. Prophylactic therapy of asthma in adults and children (prevent and
control symptoms of asthma)
Hypersensitivity to the drug or any component

Adverse Effects

Special precautions

Drug formulation

Dosage & Administrations

Localized infections involving nasal mucosa

Local side effects:
Dysphonia, oropharyngeal candidiasis, cough
Systemic side effects:
Adrenal suppression and insufficiency, growth suppression, bruising,
osteoporosis, cataracts, glaucoma, metabolic abnormalities, pneumonia
1. It cannot be used as a primary treatment of status asthmaticus, not
for rapid relief of acute episodes of asthma or bronchospasms
2. Ensure that therapy is periodically reviewed to determine if it needs
to be continued without change or if a dose change
3. Monitor bone mineral density (BMD) in patients at major risk for
decreased bone mineral content since long-term administration of
the drug may cause decrease in BMD.
4. There is a risk of infections thus past or current infections must be
noted.
Available Suspension for nebulizer:
0.25mg/2ml
0.5mg/2ml
1mg/2ml
Available powder for inhalation:
90mcg/actuation
180mcg/actuation
Asthma:
As nebuliser soln: Severe asthma: 1-2 mg bid. Maintenance dose: 0.5-1 mg
bid.
As dry powder inhalation: 200-800 mcg daily in single dose or in 2 divided
doses. Max: 800 mcg bid
As metered-dose aerosol: 400 mcg daily in 2 divided doses, increased up to
1.6 mg daily in severe cases. Maintenance: 200-400 mcg dail
Administer only via jet nebulizer connected to an air compressor with
adequate air flow and equipped with mouthpiece or suitable face mask.
Not for administration by ultrasonic nebulizer.Medication requires no
dilution before administration and is added directly into the nebulizer
reservoir.

Storage

Store upright between 68 and 77F in a dry place. Protect from light. Do
not refrigerate or freeze.