Budesonide

Bronchial asthma

Pharmacodynamic properties: Budesonide is a glucocorticosteroid with

powerful local anti-inflammatory effects The exact MOA of glucocorticosteroids in the

treatment of asthma is not fully understood Budesonide has anti-inflammatory

effects,which manifested themselves as reduced bronchial obstruction during both the early and the late phase of an allergic reaction.

In hyper-reactive patients budesonide reduce the histamine and metacholine reactivity in the airways

Asthma, like inhaled corticosteriods can delay growth. However, studies in children and adolescents who are treated with budesonide for a long period (up to 13 years) show that the patients reach the expected adult height

Inhalation therapy with budesonide is effective in preventing effort-induced asthma.

Pharmacokinetic propertiesAbsorption:

Rapidly absorbed. Peak plasma concentrations are reached within

30 minutes of inhalation. The average deposition of budesonide in the

lungs after inhalation via pressurised spray has been show to be 10-15 % of the given dose. But, via turbuhaler has been shown to be 25-35 % of the given dose. For using MDI, the systemic bioavailability is approx. 26%. But using turbuhaler is approx. 38%.

Distribution and metabolism Binding to plasma protien The volume of distribution is approx. 3litres/kg.

Elimination Budesonide eliminated through metabolism,

which catalysed primary by the enzyme CYP3A4. the metabolites are excreted in the urine in unchanged or conjugated form. Only negligible amounts of unchanged budesonide are recovered in the urine.

Budesonide has a high systemic clearance (1.2litres/min)

The half life in the plasma after intraveneous administration is on average 4 hours.

The dosage of pulmicort is individual and the maintenance dose should be the lowest possible

At the beginning of inhaled corticosteroid therapy, for therapy during periods of severe asthma, or when scaling down or withdrawing oral corticosteroids the dosage should be:

Pulmicort MDI Pulmicort turbuhaler

Patient aged 6 month-7 years:*200-400mcg per day*divided into 2-4 administration

Patient aged 5-7 years:*100-400mcg per day*divided 2-4 inhalations*the fully dose may be given in one administration

Children aged 7years and older:*200-800mcg per day *divided into 2-4 administrations.

Children aged 7years and older:*100-800mcg per day *divided into 2-4 inhalations*with daily doses up to 400mcg the full doses may be given in one administration

Adults:*400-1600mcg per day divided into 2-4 administrations

Adults:*normal dose range is 200-800mcg per day, divided into 2-4 inhalations*severe cases daily doses up to 1600mcg

The maintenance dose should be the lowest possible

After a single dose an effect may be expected after a few hours.

The full therapeutic effect is only achieved after several weeks of treatment.

Clinical trials indicate that a larger amount of budesonide is deposited in the lung when administrated with Pulmicort turbuhaler.if a patients with stable phase is tranferred from using Pulmicort MDI to Pulmicort turbuhaler, a reduction in dose may therefore be appropriate.

Patients dependent on oral steroids:When transfer from oral steroids, the

patient’s conditions must relatively stableFrom 10 days a high dose of Pulmicort is

given in conjunction with the previously used dose of oral steroids. After that, the oral dose should be reduced gradually. The oral steroids can often be withdrawn completely.

Hyper-sensitivity to budesonide Any of the other ingredients in the

product

The patients should be instructed to rinse the mouth with water after each dose of administration to avoid the risk of Candida infections

Concomitant treatment with ketoconazole, itraconazole or other potent CYP3A4 inhibitors should be avoided

Particular care is needed in patients transferring from oral steroids, since they may remain at risk of impaired adrenal function for a considerable time

During the transfer from oral steroid therapy, the patients may experience the return of previous symptoms such as muscle pain and joint pain. A temporary increase of the oral steroid dose.

When systemic steroid treatment is replaced by Pulmicort, ellergies, e.g. rhinitis and eczema, are sometimes revealed

Patients must be warned to contact physician if the effect of the treatment is diminished in general

CommonAir ways: Candida infections in the oral

cavity and throat, mild throat irritation, cough, hoarseness

RareGeneral: Angio-oedemaCNS: nervousness, restlessness, depression,

behavioural disturbancesSkin: Urticaria, rash, dermatitis, skin

bruisingAirways: Bronchospasm

Ketoconazole Itraconazole

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