title: Binding of indapamide to serum proteins and erythrocytes.
abstract: The binding of indapamide to isolated serum proteins and erythrocytes was studied in order to understand its blood distribution. In serum, indapamide was mainly bound to alpha 1-acid glycoprotein with a high affinity (K = 73.4/mM), and to albumin and lipoproteins. Indapamide was bound to erythrocytes via a saturable process with a high affinity (K = 385/mM and N = 57 microM for an hematocrit value of 0.48), and erythrocytes were the main binding component in blood (more than 80% of indapamide was associated to erythrocytes in blood). The binding to serum proteins affected indapamide distribution in blood, and alpha 1-acid glycoprotein was shown to be the more effective protein in decreasing the amount of indapamide associated to erythrocytes.
authors.affiliation: Laboratoire de Pharmacologie, Faculté de Médecine, Créteil, France.
authors.forename: S
authors.initials: S
authors.lastname: Urien
authors.forename: P
authors.initials: P
authors.lastname: Riant
authors.forename: A
authors.initials: A
authors.lastname: Renouard
authors.forename: B
authors.initials: B
authors.lastname: Coulomb
authors.forename: I
authors.initials: I
authors.lastname: Rocher
authors.forename: J P
authors.initials: JP
authors.lastname: Tillement
mesh_terms: D001792:Blood Platelets / Q000378:metabolism; D001798:Blood Proteins / Q000378:metabolism*; D004232:Diuretics / Q000493:pharmacokinetics*; D004912:Erythrocytes / Q000378:metabolism*; D006801:Humans; D066298:In Vitro Techniques; D007190:Indapamide / Q000493:pharmacokinetics*; D008074:Lipoproteins / Q000378:metabolism; D009961:Orosomucoid / Q000378:metabolism; D012709:Serum Albumin / Q000378:metabolism
chemical_list: D001798:Blood Proteins; D004232:Diuretics; D008074:Lipoproteins; D009961:Orosomucoid; D012709:Serum Albumin; D007190:Indapamide