セフォタキシムナトリウム 化学特性,用途語,生産方法
外観
白色~うすい黄色, 結晶性粉末~粉末
溶解性
水に溶けやすく、エタノール(95)に極めて溶けにくい。
用途
薬理研究用試薬。
用途
第 3 世代セフェム系抗生物質
です。ペニシリン結合タンパク質に結合し、
細胞壁の合成を阻害します。抗菌スぺクトル
は広く、グラム陰性菌に対して強い抗菌作用
を示します。また、緑膿菌に対しても抗菌作
用を示します。
効能
抗生物質, 細胞壁合成阻害薬
商品名
クラフォラン (サノフィ); セフォタックス (日医工サノフィ)
説明
Cefotaxime was synthesized by Hoechst and Roussel-Uclaf in 1977. It was the first derivative of cephalosporin to introduce the methoxyimino and aminothiazole groups at the 7 position of the cephem nucleus. Although it shows unexpectedly low oral absorption, its excellent activity against a wide range of gram-positive and gram-negative organisms, including Serratia, Enterobacter, Citrobacter, and anaerobes, guided research and development of the newer synthetic cephems, the so-called thirdgeneration cephalosporins.
化学的特性
White to pale yellow crystalline powder
使用
Cefotaxime sodium salt acts as a beta-lactamase resistant antibiotic. It is used as an effective antibacterial against gram-negative bacteria, with the notable exception of pseudomonas and penicillin-resistant strains of streptococcus pneumoniae. It is used to treat infections of the bones, joints, skin, respiratory tract and blood stream.
定義
ChEBI: A cephalosporin organic sodium salt having acetoxymethyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side-groups.
一般的な説明
Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards
臨床応用
Cefotaxime (Claforan) was the first third-generationcephalosporin to be introduced. It possesses excellentbroad-spectrum activity against Gram-positive and Gramnegativeaerobic and anaerobic bacteria. It is more activethan moxalactam against Gram-positive organisms. Manyβ-lactamase–producing bacterial strains are sensitive to cefotaxime,including N. gonorrhoeae, Klebsiella spp., H. influenzae,S. aureus, and E. cloacae. Some, but not all,Pseudomonas strains are sensitive. Enterococci and Listeriamonocytogenes are resistant.
The syn-isomer of cefotaxime is significantly more activethan the anti-isomer against β-lactamase–producing bacteria.This potency difference is, in part, because of greaterresistance of the syn-isomer to the action of β-lactamases.The higher affinity of the syn-isomer for PBPs, however,may also be a factor.
Cefotaxime is metabolized in part to the less active desacetylmetabolite. Approximately 20% of the metaboliteand 25% of the parent drug are excreted in the urine. Theparent drug reaches the cerebrospinal fluid in sufficient concentrationto be effective in the treatment of meningitis.Solutions of cefotaxime sodium should be used within 24hours. If stored, they should be refrigerated. Refrigerated solutionsmaintain potency up to 10 days.
セフォタキシムナトリウム 上流と下流の製品情報
原材料
準備製品