Human pharmacokinetics and distribution in various tissues of ceftriaxone.
Multiple-dose pharmacokinetics of ceftriaxone were investigated in 7 patients with bronchopneumonia using an intramuscular regimen of 1 g given every 24 h for 7 days. Serum, sputum, and urine samples were collected serially following the first dose (day 1) and last dose (day 7). Mean peak serum concentrations of ceftriaxone occurred at 2 h on both days and were 67.8 and 75.1 micrograms/ml, respectively, on day 1 and day 7. Ceftriaxone had a half-life of 6.9 h on day 1 and 7.4 h on day 7. The half-life of ceftriaxone in sputum was 5.9 and 6.6 h, respectively, on days 1 and 7. Approximately 50% of the dose of ceftriaxone was recovered in the urine within 24 h on day 1, 60% on day 7. Tissue distribution of ceftriaxone was determined in 103 patients following intramuscular administration of a single 1-gram dose at different times up to 24 h prior to surgery. High concentrations of ceftriaxone were found in lung, tonsil, middle ear mucosa, and nasal mucosa, and therapeutic levels of ceftriaxone persisted for 24 h after administration.
F
F
Fraschini
P C
PC
Braga
G
G
Scarpazza
F
F
Scaglione
O
O
Pignataro
G
G
Sambataro
C
C
Mariani
G C
GC
Roviaro
F
F
Varoli
G
G
Esposti
D002443:Ceftriaxone / Q000097:blood / Q000378:metabolism* / Q000652:urine; D004334:Drug Administration Schedule; D004432:Ear, Middle / Q000378:metabolism* / Q000601:surgery; D006801:Humans; D007700:Kinetics; D011292:Premedication; D012137:Respiratory System / Q000378:metabolism* / Q000601:surgery; D012141:Respiratory Tract Infections / Q000188:drug therapy / Q000378:metabolism; D013183:Sputum / Q000378:metabolism; D014018:Tissue Distribution
D002443:Ceftriaxone