par Gepts, Elisabeth;Sonck, Walter;Camu, Frédéric 
;Vercruysse, Antoine
Référence European journal of anaesthesiology, 4, 1, page (35-43)
Publication Publié, 1987
;Vercruysse, AntoineRéférence European journal of anaesthesiology, 4, 1, page (35-43)
Publication Publié, 1987
Article révisé par les pairs
| Résumé : | The pharmacokinetics of meptazinol (3 mg kg-1 i.v.), a centrally acting opioid agonist-antagonist, were studied in six male and six female patients during anaesthesia with 1-3 vol.% enflurane and an infusion of 10-30 μg kg-1 min-1 etomidate. Arterial blood samples were taken up to 300 min postinjection. The plasma meptazinol concentrations, determined by HPLC, best fitted to a three-compartment open mamillary model with central elimination using a non-linear extended least-squares regression analysis. Derived pharmacokinetic parameters indicated a rapid distribution (T( 1/2 ) π=1.24±0.83 min, T( 1/2 ) α=7.55±3.97 min), a short elimination half-life (T( 1/2 ) β=86.9±15.6 min), a volume of the central compartment twice as large in females (V(c)=0.557±0.237 1 kg-1) as in males (V(c)=0.274±0.144 1 kg-1), a small distribution volume at steady state (V(ss)=2.52±0.66 1 kg-1) and a high total plasma clearance (Cl(p)=1547±385 ml min-1). The elimination rate microconstant in females (k10=0.0577±0.0337 min-1) was significantly lower than in males (k10=0.1093±0.0437 min-1 with a lower drug fraction in the central compartment in the post-distributive phase (F(c)= males: 0.08±0.02, females 0.19±0.11). As V(ss) and Cl(p) were similar in both groups, sex-related differences were only observed in the dynamics of distribution of the drug. From a pharmacokinetic point of view we suspect that meptazinol shows very little cumulation on repeated i.v. administration as necessary during anaesthesia. |
