Pharmacokinetics of ceftriaxione, a third-generation cephalosporin, in pediatric patients
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Published on: July 24, 2021
Kyoko Fukumoto1, Shiori Aida, Tomohiro Oishi
1Department Pharmaceutical Sciences, Niigata University of Pharmacy and Applied Life Sciences.
Insights
This study found that once-daily ceftriaxone (CTRX) therapy is effective for pediatric pneumonia. Pediatric pharmacokinetics of CTRX are similar to adults, ensuring therapeutic drug levels.
Area of Science:
- Pharmacology
- Pediatric Infectious Diseases
- Clinical Pharmacy
Background:
- Ceftriaxone (CTRX) is a widely used antibiotic for bacterial infections.
- Understanding CTRX pharmacokinetics in pediatric patients is crucial for optimizing treatment efficacy.
- Previous studies have not fully elucidated CTRX pharmacokinetics and protein binding in children.
Purpose of the Study:
- To clarify the pharmacokinetics of ceftriaxone (CTRX) in pediatric patients.
- To investigate the relationship between CTRX protein binding and serum concentrations in children.
- To evaluate the suitability of once-daily CTRX dosing for pediatric pneumonia.
Main Methods:
- Serum concentrations of CTRX were monitored in 21 pediatric pneumonia patients.
- Blood samples were collected pre- and post-administration for CTRX level determination.
- In vitro and in vivo studies examined the effect of albumin on CTRX protein binding.
Main Results:
- No significant correlation was found between age and CTRX elimination half-life in pediatric patients.
- Pediatric patients showed no significant differences in distribution volume and clearance compared to adults.
- Increased CTRX and albumin concentrations led to higher binding ratios in both in vitro and in vivo settings.
Conclusions:
- Once-daily ceftriaxone (CTRX) administration is pharmacokinetically and bacteriologically effective for pediatric pneumonia.
- Sufficient trough concentrations of CTRX were maintained above the minimum inhibitory concentration for key pathogens.
- Pediatric CTRX pharmacokinetics are comparable to adult profiles, supporting current dosing regimens.
Abstract:
We monitored the serum concentration of ceftriaxone (CTRX) in order to clarify its pharmacokinetics in pediatric patients. Subjects were 21 patients undergoing CTRX therapy (50 mg/kg/d) for pneumonia from January to September 2007. To determine the serum concentration of CTRX and to obtain other laboratory data, blood samples were drawn just before and after drug administration. To clarify the relationship between protein concentration and the protein binding ratio of CTRX in vitro and in vivo, the effect of human albumin on the binding ratio was investigated. Thereafter, the relationship between the protein binding ratio and the concentration of CTRX in pediatric patients was analyzed. There was no significant correlation between age and the elimination half-life of CTRX. Moreover, no significant differences were observed in the distribution volume and the clearance between pediatric patients and adults. The binding ratios increased with increased CTRX and albumin concentrations in both in vitro and in vivo studies. It was suggested that the CTRX concentration just before administration (i.e., C(trough)) was sufficiently maintained above the mean inhibitory concentration against Streptococcus pneumoniae and Haemophilus influenzae. Therefore, CTRX administration once daily to pediatric patients with pneumonia was shown to be bacteriologically and pharmacokinetically superior in terms of efficacy.
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