Comparative Serum Levels and Urinary Recovery of Cefazolin, Cephaloridine, and Cephalothin in Man

Self Cite

Cefatrizine (SK&F 60771), a new broad-spectrum cephalosporin, was administered in a 0. 5-g dose either orally or intramuscularly to volunteers in a crossover study. After oral administration, the average peak serum levels were 5.6 and 22.1 ,Ag/ml for cefatrizine and cephalexin, respectively. The serum half-life of cefatrizine appeared to be more extended than that of cephalexin. Urinary recovery of cefatrizine (35%) was approximately half that of cephalexin (68%) after oral administration. After intramuscular injection of 0.5 g, the average peak serum level of cefatrizine (12.0 ,ug/ml) was approximately one-fourth that of cefazolin (44.0 ,ug/ml). The serum half-life after intramuscular injection was 86 min for cefatrizine and 118 min for cefazolin. Urinary recovery was 45% of the intramuscularly administered dose, as compared with cefazolin, which was 74%.

supporting

confidence: 80%

Cefatrizine (SK&F 60771), a New Oral Cephalosporin: Serum Levels and Urinary Recovery in Humans After Oral or Intramuscular Administration – Comparative Study with Cephalexin and Cefazolin

Actor¹,

Pitkin²,

Lucyszyn³

et al. 1976

Self Cite

“…However, i.m. injection of P-lactam antibiotics often leads to pain at the injection site (4,10,18,28). Thus, local anesthetics have to be added to the injection solution to increase tolerability (6,11,12,18).…”

mentioning

confidence: 99%

Cefodizime in serum and skin blister fluid after single intravenous and intramuscular doses in healthy volunteers

Körting

Schäfer‐Korting

Maass

et al. 1987

“…Pharmacokinetic studies in normal subjects have shown higher and more prolonged serum levels with cefazolin than with other cephalosporin antibiotics, e.g., cephaloridine and cephalothin (3,11,16,17). While the drugs were under clinical investigation at Smith Kline & French Laboratories, a series of studies were undertaken to obtain additional human pharmacology data on cefazolin and compare it with cephalothin (2).…”

mentioning

confidence: 99%

Pharmacokinetic Interpretation of Blood Levels and Urinary Excretion Data for Cefazolin and Cephalothin After Intravenous and Intramuscular Administration in Humans

Rattie¹,

Ravin²

1975

Blood levels of cefazolin and cephalothin were determined in two separate crossover studies in 20 healthy male adults, each after intravenous and intramuscular administration. Pharmacokinetic parameters were calculated from the intravenous data based upon a two-compartment open model. The rate constants controlling the distribution between the central and peripheral compartments, the overall elimination rate constants, the apparent volumes of distribution, and the fraction of the dose in the central and peripheral compartments were determined. The bioavailability was calculated to be 100% for cefazolin and cephalothin.Cefazolin is a new broad-spectrum cephalosporin antibiotic derived from 7-amino cephalosporanic acid, which has a wide range of activity against gram-positive and gram-negative pathogens. It was synthesized and studied extensively in Japan (6, 11-13, 16) before being developed for clinical use in the United States. Pharmacokinetic studies in normal subjects have shown higher and more prolonged serum levels with cefazolin than with other cephalosporin antibiotics, e.g., cephaloridine and