Ceftriaxone - bilirubin - albumin interactions in the neonate : an in vivo study

The in vivo bilirubin-albumin binding interaction of ceftriaxone (CRO) was investigated in 14 non-jaundiced newborns, aged 33-42 weeks of gestation, during the first few days of life after they had reached stable clinical condition. CRO (50 mg/kg) was infused intravenously over 30 min. The competiti...

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Published in:European journal of pediatrics 1993-06, Vol.152 (6), p.530-534
Main Authors: MARTIN, E, FANCONI, S, KÄLIN, P, ZWINGELSTEIN, C, CREVOISIER, C, RUCH, W, BRODERSEN, R
Format: Article
Language:English
Subjects:
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Bilirubin - metabolism
Binding, Competitive - drug effects
Biological and medical sciences
Ceftriaxone - metabolism
Ceftriaxone - pharmacology
Female
Humans
Infant, Newborn
Infusions, Intravenous
Male
Medical sciences
Pharmacology. Drug treatments
Protein Binding - drug effects
Serum Albumin - drug effects
Serum Albumin - metabolism
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Summary:The in vivo bilirubin-albumin binding interaction of ceftriaxone (CRO) was investigated in 14 non-jaundiced newborns, aged 33-42 weeks of gestation, during the first few days of life after they had reached stable clinical condition. CRO (50 mg/kg) was infused intravenously over 30 min. The competitive binding effect of CRO on the bilirubin-albumin complex was estimated by determining the reserve albumin concentration (RAC) at baseline, at the end of CRO infusion, and at 15 and 60 min thereafter. Immediately after the end of drug administration, RAC decreased from 91.9 (+/- 25.1) mumol/l to 38.6 (+/- 10.1) mumol/l (P = 0.0001). At the same time the plasma bilirubin toxicity index (PBTI) increased from 0.64 (+/- 0.40) before drug infusion to 0.96 (+/- 0.44) thereafter (P = 0.0001). The highest displacement factor (DF) was calculated to be 2.8 (+/- 0.6) at the end of drug infusion. Average total serum bilirubin concentrations decreased from a baseline value of 59.6 (+/- 27.0) mumol/l to 55.2 (+/- 27.1) mumol/l (P = 0.026). Sixty minutes after the end of CRO infusion, RAC was 58.3 (+/- 21.7) mumol/l, PBTI regained baseline, but DF was still 1.9 (+/- 0.2). No adverse events were recorded. Our results demonstrate significant competitive interaction of CRO with bilirubin-albumin binding in vivo. Thus, ceftriaxone should not be given to the neonate at risk of developing bilirubin encephalopathy.
ISSN:0340-6199
1432-1076
DOI:10.1007/BF01955067