[Pharmacokinetics and pharmacodynamics of proxyphylline in asthmatic children].
In 15 asthmatic children and 3 healthy adult volunteers the pharmacokinetics and pharmacodynamics of proxyphylline under oral treatment, and the pharmacokinetics after intravenous administration were determined. The concentration-time-courses after intravenous application could best be fitted to an open 2-compartment model whereas the pharmacokinetics after oral treatment followed an open 1-compartment model. Under oral administration great inter- and intraindividual variances of the serum levels occurred. These differences which showed no age-dependency were suggested to be due to variations of the absorption velocity and the elimination half-lifes. In order to evaluate the curative efficacy of proxyphylline on lung function parameters all children had to undergo a whole body-plethysmography. No significant antiobstructive effects on the relevant baseline ventilation parameters could be observed. The protective efficacy of proxyphylline was determined in asthmatic children who developed an exercise induced asthma after a 7 minutes run. Only in 3 of 11 children a significant reduction of the enhanced airway resistance occurred. No correlation between serum levels and the protective effects was found. The present results show that there is no positive association between pharmacokinetics and pharmacodynamics of proxyphylline in asthmatic children. A safe antiobstructive therapy appears to be impossible within the dose range recommended so far.
D000284:Administration, Oral; D000293:Adolescent; D000628:Aminophylline / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000097:blood / Q000627:therapeutic use; D001249:Asthma / Q000097:blood / Q000188:drug therapy*; D001985:Bronchial Provocation Tests; D002648:Child; D003692:Delayed-Action Preparations; D004305:Dose-Response Relationship, Drug; D005260:Female; D006207:Half-Life; D006801:Humans; D007275:Injections, Intravenous; D007700:Kinetics; D008176:Lung Volume Measurements; D008297:Male; D008657:Metabolic Clearance Rate; D013806:Theophylline / Q000031:analogs & derivatives
D003692:Delayed-Action Preparations; C003237:proxyphylline; D000628:Aminophylline; D013806:Theophylline
Pharmakokinetik und Pharmakodynamik von Proxyphyllin bei asthmatischen Kindern.