Theophylline kinetics in peripheral tissues in vivo in humans |
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Authors: | Markus Müller Bettina vOsten Rainer Schmid Evelyne Piegler Ingeborg Gerngroß |
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Affiliation: | (1) Department of Clinical Pharmacology, Vienna University School of Medicine, Allgemeines Krankenhaus, Währinger Gürtel 18-20, A-1090 Vienna, Austria;(2) Department of Medical and Chemical Laboratory Diagnosis, Vienna University School of Medicine, Allgemeines Krankenhaus, Währinger Gürtel 18-20, A-1090 Vienna, Austria |
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Abstract: | Several biochemical and cellular effects have been described for methylxanthines under in vitro conditions. However, it is unknown, whether threshold concentrations required to exert these effects are attained in target tissues in vivo. We therefore employed the microdialysis technique for measuring theophylline concentrations in peripheral tissues under in vivo conditions.Following in vitro and in vivo calibration, microdialysis probes were inserted into the medial vastus muscle and into the periumbilical subcutaneous adipose layer of healthy volunteers. Following single oral dose administration of 300 mg or i.v. infusion of 240 mg theophylline, in vivo time courses of theophylline concentrations were monitored in tissues and plasma. Major pharmacokinetic parameters (cmax, tmax, AUC) were calculated for plasma and tissue time courses. The mean AUCtissue /AUCplasma-ratio was 0.56 (p.o.) and 0.55 (i.v.) for muscle and 0.55 (p.o.) and 0.72 (i.v.) for subcutaneous adipose tissue.We conclude that microdialysis provides important information on the distribution and the tissue pharmacokinetics of theophylline.Abbreviations FPIA
Fluorescence polarisation immuno assay
- AUC
Area under the curve
- tmax
Time to peak concentration
- cmax
Peak concentration |
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Keywords: | Microdialysis Theophylline Tissue concentration Pharmacokinetics Human |
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