セフラジン 化学特性,用途語,生産方法
効能
抗生物質, 細胞壁合成阻害薬
説明
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 (ED
50s = 5, 37, 122, and 50 mg/kg, respectively), as well as by penicillin-susceptible or -resistant strains of
S. aureus (ED
50s = 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.
化学的特性
Solid
使用
Cephalosporin antibacterial.
定義
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.
主な応用
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.
抗菌性
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.
臨床応用
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.
セフラジン 上流と下流の製品情報
原材料
準備製品