セファトリジン 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
Cefatrizine was synthesized by BristolMyers Co. and Smith Klein & French Laboratories in 1974. It shows two to four times higher activity against gram-positive and four to eight times higher activity against gram-negative bacteria than cephalexin. Cefatrizine also shows excellent oral absorption, and its in vivo activity is 30 to 500 times higher than that of cephalexin.
使用
Cefatrizine is a new orally administered cephalosporin with excellent activity against gram-positive cocci, inhibiting all except enterococci at minimal inhibitory concentrations below 1 μg/ml.
定義
ChEBI: A cephalosporin compound having (1H-1,2,3-triazol-4-ylsulfanyl)methyl and [(2R)-2-amino-2-(4-hydroxyphenyl)]acetamido side-groups. An antibacterial drug first prepared in the 1970s, it has more recently been found to be
n inhibitor of eukaryotic elongation factor-2 kinase (eEF2K), which is known to regulate apoptosis, autophagy and ER stress in many types of human cancers.
抗菌性
A semisynthetic cephalosporin formulated for oral use. The
spectrum is similar to that of cefalexin but it is more active
against H. influenzae. Wide strain variations in
susceptibility have been reported.
It is only partially absorbed when given by mouth. A
500 mg oral dose achieves a concentration of c. 6 mg/L after
1–2 h. The normal half-life of 2.5 h is extended to 5.5 h
in end-stage renal failure. Distribution resembles that of
cefalexin. It crosses the placenta readily. Plasma protein
binding is 40–60%.
Urinary recovery in 6 h is 35% of an oral dose, producing
urinary levels of 50–1500 mg/L. It is presumed that the
remainder is metabolized, but no metabolites have been
identified.
Apart from some mild diarrhea, it is well tolerated. It is
available in Japan.
安全性プロファイル
Moderately toxic byintraperitoneal and subcutaneous routes. An experimentalteratogen. Other experimental reproductive effects. Whenheated to decomposition it emits very highly toxic fumesof NOx and SOx.
セファトリジン 上流と下流の製品情報
原材料
準備製品