Summary
The pharmacokinetics of the glucocorticoid budesonide was studied in 6 children with asthma after i.v. injection of 0.5 mg and oral inhalation of 1 mg as an aerosol. Budesonide is a 1:1 mixture of the epimers 22 S and 22 R, which were assayed separately by HPLC combined with RIA. All pharmacokinetic parameters of the epimers differed except the half-life of about 1.5 h. It was significantly shorter than that reported in adults. Plasma clearance averaged 103 l · h−1 for epimer 22 R and 74 l · h−1 for epimer 22 S; calculated per kg body weight these values were about 50% higher than in adults. The difference was about 40% when calculated per m2 of body surface area. Since budesonide is a high-clearance drug, the data indicate higher liver blood flow · kg−1 body weight and m2 of body surface area in children. The systemic availability of the aerosol was approximately 30% of nominal dose, i.e. the same as in adults. The high clearance and short half-life of budesonide in children are advantageous in reducing the risk of possible systemic side-effects of prophylactic treatment of asthma in childhood.
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References
Andersson P, Brattsand R, Edsbäcker S, Källström L, Ryrfeldt Å (1982a) Biotransformation rate (in vitro) and systemic potency (in vivo) of the topical glucocorticoid budesonide in male and female rats. J Steroid Biochem 17: 703–706
Andersson P, Edsbäcker S, Ryrfeldt Å, von Bahr C (1982b) In vitro biotransformation of glucocorticoids in liver and skin homogenate fraction from man, rat and hairless mouse. J Steroid Biochem 16: 787–795
Dahlberg E, Thalén A, Brattsand R, Gustafsson JÅ, Johansson U, Roempke K, Saartok T (1984) Correlation between chemical structure, receptor binding and biochemical activity of some novel, high active 16 α, 17 α-acetalsubstituted glucocorticoids. Mol Pharmacol 25: 70–78
Du Bois D, Du Bois EF (1916) Clinical calorimetry X. A formula to estimate the approximate surface if height and weight be known. Arch Intern Med 17: 863
Hamilton RA, Garnett WR, Kline BJ (1981) Determination of mean valproic acid serum level by assay of single pooled sample. Clin Pharmacol Ther 29: 408–413
Mihaly GW, Moore RG, Thomas J et al. (1978) The pharmacokinetics and metabolism of the anilide local anaestetics in neonates. Eur J Clin Pharmacol 13: 143–152
Newman SP (1983) Deposition and effects of inhalation aerosols. Rahms Tryckeri, Lund, Sweden
Rane A (1980) Basic principals of drug disposition and action in infants and children. In: Yaffe SJ (ed) Pediatric pharmacology. Grune and Stratton, Philadelphia
Ryrfeldt Å, Andersson P, Edsbäcker S, Tönnesson M, Davies DS, Pauwels R (1982) Pharmacokinetics and metabolism of budesonide, a selective glucocorticoid. Eur J Respir Dis 63 [Suppl 122]: 86–95
Ryrfeldt Å, Edsbäcker S, Pauwels R (1984) Kinetics of the epimeric glucocorticoid budesonide. Clin Pharmacol Ther 35: 525–530
Thalén A, Brattsand R (1979) Synthesis and anti-inflammatory properties of budesonide, a new non-halogenated glucocorticoid with high local activity. Arzneimittelforsch/Drug Res 29: 1687–1690
Aherne GW, Littleton P, Thalén A, Marks V (1982) A sensitive radioimmunoassay for budesonide in plasma. J Steroid Biochem 17: 559–565
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Pedersen, S., Steffensen, G., Ekman, I. et al. Pharmacokinetics of budesonide in children with asthma. Eur J Clin Pharmacol 31, 579–582 (1987). https://doi.org/10.1007/BF00606634
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DOI: https://doi.org/10.1007/BF00606634