Dose-dependent pharmacokinetics of aprindine in healthy volunteers.
The disposition of aprindine following a single oral dose can best be described by a two-compartment open model. The mean plasma half-life (t 1/2 beta) increased from 8.0 +/- 2.1 h (SD) after a 25 mg dose of 9.4 +/- 2.9 h after 50 mg and to 15.8 +/- 2.6 h after 100 mg, with a decrease in total plasma clearance (Cl/F) and volume of distribution at steady state (V dss/F) and during beta-phase (V d beta/F). The area under plasma concentration-time curve (AUC), maximum plasma concentration (C max) and the amount of unchanged aprindine excreted in the urine increased in a non-linear fashion with the increase in dose. The t 1/2 beta after multiple oral doses showed a 3-fold increase over the single dose value. These results indicate that aprindine shows dose-dependent non-linear kinetics.
D000328:Adult; D001073:Aprindine / Q000008:administration & dosage / Q000378:metabolism*; D001798:Blood Proteins / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006207:Half-Life; D006801:Humans; D007192:Indenes / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D011485:Protein Binding
D001798:Blood Proteins; D007192:Indenes; D001073:Aprindine