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Updated: Jul 27, 2026

The Importance of Correct Protein Concentration for Kinetics and Affinity Determination in Structure-function Analysis
Published on: March 17, 2010
[Protein binding of cephems in the elderly]
M Kuroyama1, S Motohashi, S Murase
1Department of Pharmacy, Kitasato University Hospital.
Insights
Elderly individuals exhibit reduced protein binding of cephalosporins, increasing free drug levels. This may lead to enhanced drug effects and adverse reactions in older patients.
Area of Science:
- Pharmacology
- Geriatrics
- Biochemistry
Context:
- Serum protein binding influences drug efficacy and safety.
- Aging can alter physiological parameters affecting drug disposition.
- Cephalosporins are a class of widely used antibiotics.
Purpose:
- To investigate the impact of aging on the serum protein binding of 12 cephalosporins.
- To compare protein binding in young versus elderly healthy subjects.
- To explore potential reasons for age-related changes in cephalosporin binding.
Summary:
- Serum protein binding of 12 cephalosporins was evaluated in young and elderly healthy adults using equilibrium dialysis.
- Elderly subjects showed significantly lower protein binding for these cephalosporins compared to younger subjects.
- This reduction is potentially due to decreased serum albumin and altered fatty acid profiles in the elderly, leading to higher free drug concentrations.
Impact:
- The decreased protein binding in elderly individuals may result in increased pharmacological effects and a higher incidence of adverse reactions.
- Clinical consideration of age-related changes in protein binding is crucial for optimizing cephalosporin therapy in the elderly.
- Further research into age-specific dosing strategies for cephalosporins is warranted.
Abstract:
The serum protein-binding of 12 representative cephems (CET, CEZ, CZX, CPZ, CZON, CPM, CDZM, CFX, CMZ, CTT, LMOX, FMOX) was assessed, using sera from young healthy subjects (mean age, 28.6 years old) and elderly healthy subjects (mean age, 69.7 years old), applying equilibrium dialysis under the same conditions in vitro. The protein-binding capacity of 12 cephems in elderly subjects was significantly less than that in young subjects, and marked increase in free drug concentration was observed in elderly subjects. This decrease in the protein binding capacity of cephems in elderly subjects was possibly caused by decreased serum albumin and change in non-esterified fatty acid constitution related to aging. As free-drug concentration participates in the appearance of effects and adverse reactions, the possibility of an enhanced pharmacological effects and increased adverse reactions of cephems due to decrease of protein binding in elderly subjects should be considered.
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