Cefradine

Описание

Cefradine is an orally bioavailable β-lactam cephalosporin antibiotic. It is active against S. pyogenes, E. coli, K. pneumoniae, and E. cloacae (MICs = 0.04, 9.4, 9.4, and 6.3 μg/ml, respectively). Cefradine is also active against clinical isolates of S. aureus (MICs = 0.8-6 μg/ml) and S. pyogenes (MICs = 0.1-0.4 μg/ml), as well as H. influenzae, E. coli, and K. pneumoniae (MICs = 6.2-12.5 μg/ml). It increases survival in mouse models of systemic lethal infection by S. pyogenes, E. coli, K. pneumoniae, or E. cloacae (ED₅₀s = 5, 37, 122, and 50 mg/kg, respectively), as well as by penicillin-susceptible or -resistant strains of S. aureus (ED₅₀s = 18 and 91 mg/kg, respectively). Formulations containing cefradine have previously been used in the treatment of respiratory and urinary tract infections, skin infections, and otitis media.

Химические свойства

Solid

Использование

Cephalosporin antibacterial.

Определение

ChEBI: A cephalosporin with a methyl substituent at position 3, and a (2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetamido substituent at position 7, of the cephem skeleton.

прикладной

Cephradine was synthesized by the Squibb Institute of Medical Research in 1971. It shows almost the same antibacterial activity and pharmacokinetic properties as cephalexin. Cephradine has been used for therapy of urinary and respiratory tract infections caused by Staphylococcus, Streptococcus, Escherichia coli, Klebsiella, and Proteus mirabilis.

Антимикробная активность

Cephradine. A semisynthetic cephalosporin available in both oral and injectable forms. The antibacterial spectrum and susceptibility to β-lactamases are almost identical to those of cefalexin .
It is almost completely absorbed when given by mouth. A 500 mg oral dose achieves a concentration of about 18–20 mg/L after 1 h. The peak is delayed and reduced by food, but the half-life is not altered. Intramuscular administration of 1 g results a plasma concentration of 10–12 mg/L within 2 h. The plasma half-life is around 1 h and protein binding low.
Concentrations of up to 40% of those simultaneously found in the serum have been demonstrated in lung tissue. Penetration into the CSF is poor. Levels in sputum were about 20% of those simultaneously present in the plasma following a 1 g oral dose and similar levels have been found in bone. Breast milk concentrations approaching 1 mg/L have been found after 500 mg orally every 6 h and similar concentrations have been found in amniotic fluid. Cord blood concentration is said to be similar to that in the maternal blood.
It is excreted unchanged in the urine mostly in the first 6 h, achieving concentrations exceeding 1 g/L. Probenecid markedly increases the plasma concentration and delays the peak.
There is some biliary excretion. The parenteral forms may give rise to local pain or thrombophlebitis. Other side effects common to cephalosporins have been described. In some patients Candida vaginitis has been troublesome.
Clinical use is similar to that of cefalexin, but it has been largely superseded by later cephalosporins.

Клиническое использование

Cephradine (Anspor, Velosef) is the only cephalosporinderivative available in both oral and parenteral dosageforms. It closely resembles cephalexin chemically (it maybe regarded as a partially hydrogenated derivative ofcephalexin) and has very similar antibacterial and pharmacokineticproperties.
It occurs as a crystalline hydrate that is readily soluble inwater. Cephradine is stable to acid and absorbed almostcompletely after oral administration. It is minimally proteinbound and excreted almost exclusively through the kidneys.It is recommended for the treatment of uncomplicated urinarytract and upper respiratory tract infections caused bysusceptible organisms. Cephradine is available in both oraland parenteral dosage forms.