Biomaterial Database

Ceftriaxone binding to human serum albumin: competition with bilirubin. 1989

R Brodersen, and A Robertson

Institute of Medical Biochemistry, University of Aarhus, Denmark.

Ceftriaxone, a cephalosporin, is bound reversibly to defatted human serum albumin from adults, with a first stoichiometric binding constant of 60,000 M-1, as found by equilibrium dialysis at pH 7.4, 37 degrees. A second molecule is weakly bound, with a binding constant of 500 M-1. Possible cobinding with bilirubin was studied by the peroxidase method and by equilibrium dialysis with and without added bilirubin. Results indicated competitive binding; formation of an albumin complex containing both bilirubin and ceftriaxone could not be demonstrated. Light absorption spectra of bilirubin-albumin showed little change on addition of ceftriaxone, in agreement with the competitive biding mechanism. Binding to serum albumin from newborn infants is weaker than to the protein from adults, with the first binding constant being about 36,000 M-1. Cobinding of ceftriaxone and bilirubin to albumin from newborn infants is likewise competitive. It is concluded that ceftriaxone is a strong bilirubin displacer with a potential of inducing bilirubin encephalopathy in predisposed newborns.

UI	MeSH Term	Description	Entries
D007231	Infant, Newborn	An infant during the first 28 days after birth.	Neonate,Newborns,Infants, Newborn,Neonates,Newborn,Newborn Infant,Newborn Infants
D007700	Kinetics	The rate dynamics in chemical or physical systems.
D010544	Peroxidases		Ovoperoxidase
D011485	Protein Binding	The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.	Plasma Protein Binding Capacity,Binding, Protein
D002443	Ceftriaxone	A broad-spectrum cephalosporin antibiotic and cefotaxime derivative with a very long half-life and high penetrability to meninges, eyes and inner ears.	Benaxona,Cefatriaxone,Cefaxona,Ceftrex,Ceftriaxon,Ceftriaxon Curamed,Ceftriaxon Hexal,Ceftriaxona Andreu,Ceftriaxona LDP Torlan,Ceftriaxone Irex,Ceftriaxone Sodium,Ceftriaxone Sodium, Anhydrous,Ceftriaxone, Disodium Salt,Ceftriaxone, Disodium Salt, Hemiheptahydrate,Lendacin,Longacef,Longaceph,Ro 13-9904,Ro-13-9904,Ro13-9904,Rocefalin,Rocefin,Rocephin,Rocephine,Tacex,Terbac,Anhydrous Ceftriaxone Sodium,Ro 13 9904,Ro 139904,Ro13 9904,Ro139904
D003956	Dialysis	A process of selective diffusion through a membrane. It is usually used to separate low-molecular-weight solutes which diffuse through the membrane from the colloidal and high-molecular-weight solutes which do not. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)	Dialyses
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D001663	Bilirubin	A bile pigment that is a degradation product of HEME.	Bilirubin IX alpha,Bilirubin, (15E)-Isomer,Bilirubin, (4E)-Isomer,Bilirubin, (4E,15E)-Isomer,Bilirubin, Calcium Salt,Bilirubin, Disodium Salt,Bilirubin, Monosodium Salt,Calcium Bilirubinate,Hematoidin,delta-Bilirubin,Bilirubinate, Calcium,Calcium Salt Bilirubin,Disodium Salt Bilirubin,Monosodium Salt Bilirubin,Salt Bilirubin, Calcium,delta Bilirubin
D012709	Serum Albumin	A major protein in the BLOOD. It is important in maintaining the colloidal osmotic pressure and transporting large organic molecules.	Plasma Albumin,Albumin, Serum
D013057	Spectrum Analysis	The measurement of the amplitude of the components of a complex waveform throughout the frequency range of the waveform. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)	Spectroscopy,Analysis, Spectrum,Spectrometry