Displacement of albumin-bound antimicrobial agents by bilirubin.
Article Details
- CitationCopy to clipboard
Bratlid D, Bergan T
Displacement of albumin-bound antimicrobial agents by bilirubin.
Pharmacology. 1976;14(5):464-72. doi: 10.1159/000136629.
- PubMed ID
- 1031216 [ View in PubMed]
- Abstract
The ability of bilirubin to displace antimicrobial agents from their binding sites on albumin was studied in vitro by equilibrium dialysis. Sulfonamides, tetracyclines, penicillins and cephalosporins of different degrees of protein binding were tested. It was found that bilirubin reduced the protein binding of all four classes of antimicrobial agents, although by varying degrees. This effect was most pronounced with the compounds which had the highest degree of protein binding, such as cloxacillin, cephazolin, methacycline and sulfisoxazole, all of which are bound greater than 80% by albumin. On the other hand, the drugs with less than 25% binding, such as ampicillin, cephalexine and tetracycline were not ostensibly displaced by bilirubin. Scatchard plots of the binding of sulfamethoxazole to albumin in the presence of 400 mumol/1 of bilirubin, showed that bilirubin almost completely displaced the sulfonamide molecule from the high affinity site on the albumin molecule. Reduced protein binding of drugs in hyperbilirubinemic infants may have pharmacokinetic significance.
DrugBank Data that Cites this Article
- Drugs
- Drug Carriers
Drug Carrier Kind Organism Pharmacological Action Actions Ampicillin Serum albumin Protein Humans NoOther/unknownDetails Cefazolin Serum albumin Protein Humans UnknownOther/unknownDetails Cephalexin Serum albumin Protein Humans NoBinderDetails Chlortetracycline Serum albumin Protein Humans NoNot Available Details Cloxacillin Serum albumin Protein Humans NoBinderDetails Metacycline Serum albumin Protein Humans NoNot Available Details Sulfamerazine Serum albumin Protein Humans UnknownNot Available Details Sulfamethazine Serum albumin Protein Humans UnknownNot Available Details Sulfamethoxazole Serum albumin Protein Humans NoSubstrateDetails Tetracycline Serum albumin Protein Humans NoNot Available Details