Revision Year: 2012 Publisher: Italchimici SpA, Via Pontina 5, Km 29, 00040 Pomezia (Rome)
ATC Class: R01AD05
Budesonide is a gluco-corticosteroid with high local anti-inflammatory activity. Budesonide has a high (90% ) first pass hepatic degradation rate; its metabolites have low gluco-corticosteroid activity. The mechanism of action in the treatment of rhinitis is due to the antiinflammatory effect that derives from the inhibition of the synthesis and release of inflammation mediators and the inhibition of the cytokines mediated inflammation.
In an open trial, 78 children (5-15 years) with perennial rhinitis were treated with intranasal budesonide pressurized metered dose inhaler 200micrgrams twice daily (delivered daily dose 256 micrograms) for 12 months; 43 children stayed in the study for 12 additional months and were switched to aqueous suspension (400 micrograms delivered daily dose) during the last 6 months.
Results show that long-term treatment for 1-2 years with intranasal budesonide 256-400 micrograms daily in children with perennial rhinitis revealed no negative effects on growth or endogenous cortisol production. Local side-effects were mild and patient symptoms decreased. Based on a sample of 78 children, however, the possibility that extremely steroid-sensitive children may react adversely cannot be ruled out.
The systemic bioavailability of budesonide formulated as an aqueous suspension administered nasally is 33%.
The peak plasma concentration of budesonide after nasal administration of 400 microgrammes in aqueous suspension is 1.0 nmo/L within 42 minutes of inhalation. During the hepatic first pass, budesonide is 90% transformed into metabolites with low gluco-corticosteroid activity. Examples are 6-beta-hydroxybudesonide and 16-alfa-hydroxyprednisolone. The corticosteroid activity of these metabolites is less than 1% of that of the parent compound.
Single dose oral administration showed DL50 values greater than 800 mg/kg in mice and 400 mg/kg in rats. Toxicity studies in dogs using repeated dose of 200 mcg per day administered by inhalation up to 12 months showed no toxic effects.
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