Dose-dependency of Theophylline Clearance and Protein Binding

Overview

Journal Thorax

Date 1981 May 1

PMID 7314008

Citations 8

Authors

J A Fleetham

C E Bird

K Nakatsu

R D Wigle

P W Munt

Affiliations

Soon will be listed here.

Abstract

Dose-dependency in theophylline pharmacokinetics and protein binding characteristics was examined in 10 healthy male volunteers. Theophylline disposition was determined after an intravenous infusion of both 1 mg/kg and 6 mg/kg aminophylline in a randomised crossover study. There was considerable intrasubject variability in theophylline clearance but no significant dose-dependency. Theophylline protein binding was assessed by equilibrium dialysis at varying theophylline concentrations. The percentage of free non-protein bound theophylline was significantly increased at high theophylline concentrations. This increase in free theophylline would lead to a non-linear increase in the risk of toxicity with increasing drug concentration.

Citing Articles

Dose dependent pharmacokinetics of theophylline: Michaelis-Menten parameters for its major metabolic pathways.

Dadashzadeh S, Tajerzaden H Eur J Drug Metab Pharmacokinet. 2001; 26(1-2):77-83.

PMID: 11554438 DOI: 10.1007/BF03190380.

Prediction of optimum oral theophylline dose in patients with obstructive airways disease.

Taylor D, Kinney C, McDevitt D Br J Clin Pharmacol. 1983; 15(6):689-94.

PMID: 6871068 PMC: 1427920. DOI: 10.1111/j.1365-2125.1983.tb01551.x.

Determinants of the plasma protein binding of theophylline in health.

Buss D, LEOPOLD D, Smith A, Routledge P Br J Clin Pharmacol. 1983; 15(4):399-405.

PMID: 6849774 PMC: 1427801. DOI: 10.1111/j.1365-2125.1983.tb01521.x.

Free and total plasma theophylline concentrations in chronic airflow obstruction.

Ebden P, LEOPOLD D, Smith A, Buss D, Routledge P Thorax. 1984; 39(5):352-5.

PMID: 6740537 PMC: 459801. DOI: 10.1136/thx.39.5.352.

Protein binding of theophylline.

Buss D, Ebden P, Baker S, Routledge P Br J Clin Pharmacol. 1985; 19(4):529-31.

PMID: 3994902 PMC: 1463821. DOI: 10.1111/j.1365-2125.1985.tb02684.x.

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