Pharmacokinetics of ceftriaxone in humansстатья из журнала
Аннотация: Pharmacokinetics of the investigational cephalosporin ceftriaxone were studied after 30-min intravenous infusions of three ascending single doses of 0.5, 1, and 2 g crossed over in 12 normal subjects. Serially collected plasma and urine samples were analyzed for ceftriaxone by high-performance liquid chromatography. Plasma concentration-time profiles were characterized by a linear two-compartment open model with the following respective mean (+/- standard deviation) parameters at 0.5-, 1-, and 2-g dose levels: elimination half-life, 6.5 +/- 0.7, 6.2 +/- 0.8, and 5.9 +/- 0.7 h; apparent volume of distribution, 8.5 +/- 1.1, 9.0 +/- 1.1, and 10.1 +/- 1.0 liters; and plasma clearance, 929 +/- 150, 1,007 +/- 130, and 1,190 +/- 150 ml/h. The respective renal excretion parameters were as follows: renal clearance, 373 +/- 60, 399 +/- 50, and 533 +/- 128 ml/h; and percentage of dose excreted unchanged in the 48-h urine samples, 41 +/- 8, 39 +/- 5, and 43 +/- 10. The 6-h elimination half-life of ceftriaxone was 2- to 10-fold longer than those reported for marketed and other known investigational cephalosporins. The small dose-related increases in the apparent volume of distribution and clearance parameters can be explainhe 48-h urine samples, 41 +/- 8, 39 +/- 5, and 43 +/- 10. The 6-h elimination half-life of ceftriaxone was 2- to 10-fold longer than those reported for marketed and other known investigational cephalosporins. The small dose-related increases in the apparent volume of distribution and clearance parameters can be explainhe 48-h urine samples, 41 +/- 8, 39 +/- 5, and 43 +/- 10. The 6-h elimination half-life of ceftriaxone was 2- to 10-fold longer than those reported for marketed and other known investigational cephalosporins. The small dose-related increases in the apparent volume of distribution and clearance parameters can be explained by the concentration-dependent plasma protein binding of ceftriaxone in humans. The impact of the small dose-dependent changes in the pharmacokinetics of ceftriaxone is anticipated to be of negligible clinical significance.
Год издания: 1981
Авторы: Indravadan H. Patel, S Chen, Mia Parsonnet, Martin R. Hackman, Marvin A. Brooks, J Konikoff, S. A. Kaplan
Издательство: American Society for Microbiology
Источник: Antimicrobial Agents and Chemotherapy
Ключевые слова: Antibiotics Pharmacokinetics and Efficacy, Drug-Induced Adverse Reactions, Pharmacological Effects and Toxicity Studies
Другие ссылки: Antimicrobial Agents and Chemotherapy (HTML)
Europe PMC (PubMed Central) (PDF)
Europe PMC (PubMed Central) (HTML)
PubMed Central (HTML)
Europe PMC (PubMed Central) (PDF)
Europe PMC (PubMed Central) (HTML)
PubMed Central (HTML)
Открытый доступ: green
Том: 20
Выпуск: 5
Страницы: 634–641