Human Pharmacokinetics and Distribution in Various Tissues of Ceftriaxone

Fraschini, F.; Braga, P. C.; Scarpazza, G; Scaglione, F; Pignataro, O; Sambataro, Gianluca; Mariani, Chiara; Roviaro, Giancarlo; Varoli, F.; Esposti, G.

doi:10.1159/000238415

Cited by 46 publications

(14 citation statements)

References 9 publications

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“…The results obtained from the study on ceftriaxone and on cefotaxime in blood, pulmonary tissue and bronchial secretion confirmed the data already known from lit erature [11][12][13][14]. Ceftriaxone, a cephalo sporin with a long half-life, can be deter mined in blood, pulmonary tissue and bronchial secretion by means of a micro biological method, 24 h after intramuscu lar administration of 1 g. Peak levels are reached in all the three areas already at the second hour.…”

Section: Discussionsupporting

confidence: 86%

Study on the Relationship between Pharmacokinetics and Antibacterial Activity: Comparison between Ceftriaxone and Cefotaxime within the Respiratory Tract

Fraschini

Scaglione²

1989

Chemotherapy

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The aim of this research was to collect precise data on the antibacterial activity of ceftriaxone and cefotaxime in the respiratory tract. The diffusion into pulmonary tissue and bronchial secretion and the antibacterial activity of the two antibiotics were evaluated in vivo by means of the inhibitory quotient. Ceftriaxone administered at a dosage of 1 g (i.m.) every 24 h resulted in antibacterial levels against the sensitive pathogens over a period of 24 h after each dose. The antibacterial protection afforded by cefotaxime, given at the dosage of 1 g (i.m.) every 12 h, was not as marked and did not extend over the interval between two administrations.

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Section: Discussionsupporting

confidence: 86%

Study on the Relationship between Pharmacokinetics and Antibacterial Activity: Comparison between Ceftriaxone and Cefotaxime within the Respiratory Tract

Fraschini

Scaglione²

1989

Chemotherapy

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“…This dosage schedule, which is unusual for a beta-lactam antibiotic, has been validated by a number of clinical studies since CTX came onto the market (11,31). A pharmacodynamic and bacteriological approach taken together with the specific pharmacokinetics of the compound have formed the theoretical basis of a simplified administration schedule compared with those for other beta-lactams with shorter half-lives (9).…”

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confidence: 99%

Pharmacokinetics and protein binding of ceftriaxone during pregnancy

Bourget

Fernandez

Quinquis

et al. 1993

Antimicrob Agents Chemother

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The purpose of the present work was to study the pharmacokinetics and the protein binding (free fraction of the drug) of ceftriaxone (CTX) during pregnancy. Nine pregnant women (ages, 20 to 34 years) whose gestational ages ranged from 28 4/7 to 40 5/7 weeks were included. The diagnosis of infection was established in all cases; i.e., four women had chorioamnionitis and five women had pyelonephritis. The following triple antibiotic therapy was infused with the aim of achieving cure: CTX, 2 g once every 24 h (constant rate over 60 min); tobramycin, 3 mg/kg of body weight once every 24 h; and ornidazole, 1 g/day. Two series of blood samples were collected, i.e., during the first day of treatment (on day 1), to establish the primary pharmacokinetic profile of CTX, and at the plateau (on day 7), to evaluate a possible accumulation of the drug.This was an open, noncompartmental study, with each patient serving as her own control. Concentrations of total and unbound CTX in serum were measured by a high-performance liquid chromatographic method. Pharmacokinetic analysis was done by a noncompartmental method. Data were compared by a Wilcoxon t test (a P value of .0.05 was considered significant). Data were also compared with those obtained for healthy subjects who received similar treatments. (i) The tolerance to treatment was excellent, and in all cases patients had a complete remission without premature delivery. (ii) No accumulation of CTX was noted during the treatment, and the profiles of the drug determined at days 1 and 7 were not significantly different. (iii) The pharmacokinetic parameters measured in pregnant patients during the third trimester of pregnancy were similar to those measured in healthy subjects. (iv) Residual concentrations of total and unbound CTX measured at 24 h were greater than the MICs for allegedly susceptible organisms, both on day 1 and at steady state. (v) During the final 3 months of pregnancy, the dosage schedule of CTX (2-g infusion per day) required no particular adjustment (i.e., neither a loading dose nor any increase in the maintenance dose).Ceftriaxone (CTX) is the first broad-spectrum cephalosporin prescribed on a single-daily-administration basis (24). This dosage schedule, which is unusual for a beta-lactam antibiotic, has been validated by a number of clinical studies since CTX came onto the market (11, 31). A pharmacodynamic and bacteriological approach taken together with the specific pharmacokinetics of the compound have formed the theoretical basis of a simplified administration schedule compared with those for other beta-lactams with shorter half-lives (9). The dosage recommended by the manufacturer (a single injection of 1 to 2 g every 24 h) is the consequence of an essential peculiarity of CTX: its prolonged terminal half-life (between 6.5 and 8.5 h) (21). The antibacterial spectrum of CTX is similar to that of other broad-spectrum cephalosporins. However, in comparison with other members of the group, it is less active against anaerobic organisms such as Bacteroides fr...

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“…administration of single doses. For ceftriaxone, the simulated peak concentrations in blood (0.5-, 1-, 1.5-, and 3-g doses) were 90 (31), 150 (26), 280 (33), and 400 (33) ,ug/ml; the simulated peak concentrations in bronchial fluid (0.5-and 1-g doses) were 0.9 and 1.5 jig/ml (10); and the simulated peak concentrations in urine (1-, 1.5-, and 3-g doses) were 1,000 (26), 1,500, and 3,000 ,ig/ml. For ampicillin (2-g dose), the simulated peak concentrations were 24 jig/ml in blood (17) 173,1980) and 200 ,ug/ml in urine (3).…”

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Evaluation of ceftriaxone and other antibiotics against Escherichia coli, Pseudomonas aeruginosa, and Streptococcus pneumoniae under in vitro conditions simulating those of serious infections

Satta

Cornaglia

Foddis

et al. 1988

Antimicrob Agents Chemother

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In pursuit of an in vitro system capable of reliably predicting the activities of antibiotics in serious infections and in infections occurring in immunocompromised hosts, we evaluated the abilities of four drugs to achieve virtually complete killing of bacterial cells growing in human body fluids in amounts which are very high and close to those likely to be present in serious infections; drug concentrations varied with time as they vary in human bronchial secretions or blood or urine (dynamic concentrations). The rationale for such a test was (i) to set up in vitro conditions as close as possible to those the antibiotics encounter in serious infections and (ii) to hold the drugs capable of almost completely killing the bacteria used in the assay to be highly active in vitro and likely to be the most efficacious in the treatment of serious infections. Among the antibiotics used, ceftriaxone proved to be highly active under conditions simulating pulmonary infections and septicemias caused by Streptococcus pneumoniae (bacteria grown in bronchoalveolar fluid or blood; antibiotic concentrations varying with time as in human bronchial secretions or blood) and under conditions simulating blood and urinary infections caused by Escherichia coli (bacteria grown in human blood or urine; antibiotic concentrations varying as in the various fluids). Gentamicin (not tested against pneumococci) appeared to be highly active only under conditions simulating urinary infections caused by E. coli; aztreonam (not tested against pneumococci) and ampicillin (tested only against pneumococci) did not appear to be highly active under any of the test conditions. Only the combination of gentamicin plus either ceftriaxone or aztreonam appeared to be highly active under conditions simulating serious septicemias and urinary infections caused by Psudomonas aeruginosa.

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Human Pharmacokinetics and Distribution in Various Tissues of Ceftriaxone

Cited by 46 publications

References 9 publications

Study on the Relationship between Pharmacokinetics and Antibacterial Activity: Comparison between Ceftriaxone and Cefotaxime within the Respiratory Tract

Study on the Relationship between Pharmacokinetics and Antibacterial Activity: Comparison between Ceftriaxone and Cefotaxime within the Respiratory Tract

Pharmacokinetics and protein binding of ceftriaxone during pregnancy

Evaluation of ceftriaxone and other antibiotics against Escherichia coli, Pseudomonas aeruginosa, and Streptococcus pneumoniae under in vitro conditions simulating those of serious infections

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