Influence of blood proteins on biomedical analysis. XII. Effects of glycation on gliclazide (oral hypoglycemic drug)-binding with serum albumin in diabetics.
The sera of diabetic patients showed an inverse correlation (r = -0.67, n = 57) between free gliclazide (oral hypoglycemic drug) level and the fructosamine value. The binding capacity of the primary binding site for gliclazide in the albumin molecule was increased from 4.5 x 10(-4) to 8.0 x 10(-4) M-1 by glycation of albumin, but not that of the secondary binding site (1.2 x 10(-4) M-1). This suggests that the glycation of albumin increases its total binding capacity for gliclazide, resulting in a low free gliclazide level. Therefore, a low hypoglycemic activity of the drug is observed when it is administered to diabetic patients with hyperglycemia.
Igaki
A
A
Department of Clinical Pathology, Hyogo College of Medicine, Nishinomiya, Japan.
Kobayashi
K
K
Kimura
M
M
Sakoguchi
T
T
Matsuoka
A
A
D001798:Blood Proteins / Q000032:analysis*; D003920:Diabetes Mellitus / Q000097:blood*; D005907:Gliclazide / Q000097:blood*; D006801:Humans; D007700:Kinetics; D011485:Protein Binding; D012709:Serum Albumin
D001798:Blood Proteins; D012709:Serum Albumin; D005907:Gliclazide