Jun 9, 2006 - Abstract Objective: To describe in detail the intravenous, single oral and multiple oral dose enantioselective pharma- cokinetics of tramadol in ...
Eur J Clin Pharmacol (2006) 62: 513–521 DOI 10.1007/s00228-006-0135-x
PH ARMA COK INETICS AND DISPOSITION
Rasmus Steen Pedersen . Per Damkier . Kim Brøsen
Enantioselective pharmacokinetics of tramadol in CYP2D6 extensive and poor metabolizers
Received: 27 January 2006 / Accepted: 23 March 2006 / Published online: 9 June 2006 # Springer-Verlag 2006
Abstract Objective: To describe in detail the intravenous, single oral and multiple oral dose enantioselective pharmacokinetics of tramadol in CYP2D6 extensive metabolizers (EMs) and poor metabolizers (PMs). Methods: Eight EMs and eight PMs conducted three phases as an open-label cross-over trial with different formulations; 150 mg single oral tramadol hydrochloride, 50 mg single oral tramadol hydrochloride every 8 h for 48 h (steady state), 100 mg intravenous tramadol hydrochloride. Urine and plasma concentrations of (+/−)-tramadol and (+/−)-M1 were determined for 48 h after administration. Results: In all three phases, there were significant differences between EMs and PMs in AUC and t1/2 of (+)-tramadol (P≤0.0015), (−)-tramadol (P≤0.0062), (+)-M1 (P≤0.0198) and (−)-M1 (P≤0.0370), and significant differences in Cmax of (+)-M1 (P
