Interaction of beta-lactam antibiotics on bilirubin-albumin complex: comparison by three methods, total bilirubin, unbound bilirubin and erythrocyte-bound bilirubin.
The effects of 'third-generation' cephalosporins and penicillin analogues on the concentrations of total unconjugated bilirubin, unbound bilirubin and erythrocyte-bound bilirubin were determined in blood samples. This study was performed, in vitro, at two bilirubin/albumin molar ratios and at various concentrations of antibiotics. The most effective displacers, considering the three methods, were antibiotics tightly bound to albumin: ceftriaxone and cefotetan. Cefoperazone, which is bound to albumin as tightly as these two antibiotics, caused no significant increase in unbound bilirubin but should be considered as a displacer drug on the basis of the variations of erythrocyte-bound bilirubin and total bilirubin. We suggest that drug interaction on bilirubin-albumin binding be investigated by several methods.
Gulian
J M
JM
Laboratoire de Chimie Biologique, Faculté de Médecine, Marseille, France.
Dalmasso
C
C
Gonard
V
V
D000900:Anti-Bacterial Agents / Q000097:blood / Q000378:metabolism* / Q000494:pharmacology; D001663:Bilirubin / Q000097:blood / Q000378:metabolism*; D004347:Drug Interactions; D004912:Erythrocytes / Q000032:analysis / Q000378:metabolism*; D006801:Humans; D011485:Protein Binding / Q000187:drug effects; D012709:Serum Albumin / Q000032:analysis / Q000378:metabolism*; D047090:beta-Lactams
D000900:Anti-Bacterial Agents; D012709:Serum Albumin; D047090:beta-Lactams; D001663:Bilirubin