Ceftriaxone pharmacokinetics in patients with various degrees of renal impairment

Abstract

The effects of renal impairment on the pharmacokinetics of ceftriaxone in humans were examined after intravenous infusion of a 1-g dose over 15 min to 30 renally impaired patients. The study included 12 dialysis patients and 18 patients with severe, moderate, or mild renal impairment. Plasma and, where appropriate, urine and dialysate samples were collected at predetermined times and analyzed for ceftriaxone by highpressure liquid chromatography. The elimination half-life (group mean ranged from 11.7 to 17.3 h) and plasma clearance (group mean ranged from 529 to 705 ml/h) did not correlate linearly with creatinine clearance. The renal clearance and fraction of dose excreted unchanged in urine were related'linearly, however weakly, with creatinine clearance. Ceftriaxone was not, removed from plasma to a significant extent during hemodialysis. The half-life was prolonged twofold, the plasma clearance was lowered less than 50%, and the volume of distribution was relatively unchanged in renally impaired patients compared with young or elderly healthy subjects with normal renal function at an equivalent dose. Since these changes are moderate, adjustment in the dosage regimen of ceftriaxone for patients with impaired renal ftinction should not be necessary when ceftriaxone

Ceftriaxone Is an Efficient Component of Antimicrobial Regimens in the Prevention and Initial Management of Infections in End-Stage Renal Disease

“…In ESRD patients the T ½ of the drug has been reported to be much longer but variable, ranging from 11.7 to 17.3 h [19,23,24]. It has been shown that ceftriaxone is not removed to any significant extent from plasma by hemodialysis [19,20]. Thus, in these patients ceftriaxone is a truly once-a-day antibiotic.…”

“…Its major route of elimination is via the kidney (41-60%), wherein it is disposed by glomerular filtration without any significant renal tubular secretion [15,16,22]; the remainder is excreted in the bile [15,16]. In ESRD patients the T ½ of the drug has been reported to be much longer but variable, ranging from 11.7 to 17.3 h [19,23,24]. It has been shown that ceftriaxone is not removed to any significant extent from plasma by hemodialysis [19,20].…”

Are Antibiotic Drugs Well Prescribed in Case of Renal Insufficiency? A Retrospective Study

“…The pharmacokinetics of cloxacillin, [11] oxacillin, [12] pefloxacin, [13] ceftriaxone, [14] and fusidic acid [15] should not be influenced by RI. In renal impairment (including patients with end-stage renal failure), these drugs are reported to be safe and effective.…”

Single-Dose Pharmacokinetics of Ceftriaxone in Patients with End-Stage Renal Disease and Hemodialysis

“…Ceftriaxone is a third-generation ce phalosporin (2-amino-thiazolylmethoxyimino cephalosporin) that, because of its prolonged elimination half-life, can be ad ministered safely in a once-a-day dosage schedule [2,6,7], This characteristic is an advantage over similar cephalosporins such as cefotaxime, cefoperazone and latamoxef. They all have an excellent antib acterial activity against many pathogens previously considered resistant to the firstand second-generation cephalosporins [9], The pharmacokinetic parameters of cefo taxime, cefoperazone and latamoxef do not differ substantially from those of the older cephalosporins and their elimina tion half-lives ranging from 1.2 to 2.4 h in man are shorter than the 8 h value ob served for ceftriaxone [2,6,16].…”