title: Comparative binding of etretinate and acitretin to plasma proteins and erythrocytes.
abstract: The interactions of etretinate and its main metabolite acitretin with human plasma proteins have been investigated in vitro by an erythrocyte partitioning technique that allows a quantitative estimation of the plasma and erythrocyte binding. Etretinate was extensively lipoprotein-bound (75% of plasma etretinate), with a binding constant for its main low density lipoprotein carrier of 40 x 10(6) M-1, accounting for 48% of the total plasma-bound drug. Acitretin was mainly albumin-bound (91% of plasma acitretin), with a binding constant of 0.7 x 10(6) M-1. The total plasma binding of both drugs was > 99% and, in blood, the fractions associated with erythrocytes were 14.5 and 8.1% of the total amount for etretinate and acitretin, respectively.
authors.affiliation: Laboratoire de Pharmacologie, Faculté de Médecine, Université Paris XII, Créteil, France.
authors.forename: S
authors.initials: S
authors.lastname: Urien
authors.forename: P
authors.initials: P
authors.lastname: Claudepierre
authors.forename: J
authors.initials: J
authors.lastname: Meyer
authors.forename: R
authors.initials: R
authors.lastname: Brandt
authors.forename: J P
authors.initials: JP
authors.lastname: Tillement
mesh_terms: D017255:Acitretin / Q000097:blood*; D000328:Adult; D001798:Blood Proteins / Q000378:metabolism*; D003956:Dialysis / Q000379:methods; D004910:Erythrocyte Membrane / Q000378:metabolism; D004912:Erythrocytes / Q000378:metabolism*; D005050:Etretinate / Q000097:blood*; D006801:Humans; D007700:Kinetics; D008074:Lipoproteins / Q000097:blood; D008077:Lipoproteins, LDL / Q000097:blood; D008297:Male; D011485:Protein Binding
chemical_list: D001798:Blood Proteins; D008074:Lipoproteins; D008077:Lipoproteins, LDL; D005050:Etretinate; D017255:Acitretin