title: Binding of colchicine and thiocolchicoside to human serum proteins and blood cells.
abstract: The binding of 3H-colchicine and its derivative 3H-thiocolchicoside to human serum, purified human proteins and blood cells was studied by equilibrium dialysis and centrifugation. Binding of colchicine and thiocolchicoside to human serum was 38.9 C +/- 4.7 and 12.8 C +/- 5.3%, respectively, essentially to albumin. Protein binding was not dependent on the concentration of either drug between 10(-10) and 10(-5)M. The binding of colchicine and thiocolchicoside to isolated erythrocytes (55 C +/- 5.6 and 16.5 C +/- 2.1%, respectively) decreased markedly in the presence of human serum proteins, i.e. in whole blood (38.7 C +/- 3.1 and 3.4 C +/- 0.8%). Binding of colchicine and thiocolchicoside to other blood cells was very low C < 3%). These binding properties in the blood compartment do not predispose colchicine and thiocolchicoside to be pharmacokinetically sensitive to binding displacement by drug interactions.
authors.affiliation: INSERM U26, Hôpital F. Widal, Paris, France.
authors.forename: A
authors.initials: A
authors.lastname: Sabouraud
authors.forename: O
authors.initials: O
authors.lastname: Chappey
authors.forename: T
authors.initials: T
authors.lastname: Dupin
authors.forename: J M
authors.initials: JM
authors.lastname: Scherrmann
mesh_terms: D001792:Blood Platelets / Q000378:metabolism; D001798:Blood Proteins / Q000378:metabolism*; D002498:Centrifugation; D003078:Colchicine / Q000031:analogs & derivatives* / Q000378:metabolism*; D003956:Dialysis; D004347:Drug Interactions; D004912:Erythrocytes / Q000378:metabolism*; D006098:Granulocytes / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D007963:Leukocytes, Mononuclear / Q000378:metabolism; D011485:Protein Binding / Q000187:drug effects; D012709:Serum Albumin / Q000378:metabolism
chemical_list: D001798:Blood Proteins; D012709:Serum Albumin; D003078:Colchicine; C004280:thiocolchicoside