Dependence of the Renal Excretion of Theophylline on its Plasma Concentrations and Urine Flow Rate in Asthmatic Children

Abstract

Abstract— The dependence of the renal excretion of theophylline on its plasma concentration and urine flow rate has been investigated in asthmatic children of either sex. One group (age 12.25 ± 0.80, mean ± s.d. n = 8) was given aminophylline intravenously (i.v.), while another (age 10.00 ± 3.64 n = 14) was given a sustained release preparation of theophylline orally (single dose and repeated doses). Unchanged drug (11.6% ± 1.75) was excreted in the urine corresponding to a renal clearance of 10.6 ± 1.6 mL h−1 kg−1. Time dependence of the renal clearance of theophylline was found only after i.v. administration. Dependence of the renal clearance on urine flow rate was found both after i.v. administration and at steady state, but not after a single oral dose of theophylline. After oral administration, renal clearance of theophylline was higher at steady state than after a single dose (0.58 ± 0.06 L h−1 kg−1 vs 0.23 ± 0.03 L h−1 kg−1), while urine flow rate was lower (1.1 ± 0.5 mL min−1 vs 1.8 ± 0.9 mL min−1). High correlation of theophylline plasma concentration and theophylline excretion rate was obtained in 10 of 14 patients after administration of a single oral dose of the preparation (r = 0.8567 to 0.9830). There was no dose dependence of the renal clearance of the drug either after a single dose, or at steady state. 1990 Royal Pharmaceutical Society of Great Britain