タゾバクタム 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
用途
タゾバクタム(略号:TAZ, 英語:tazobactam)とは、細菌のβ-ラクタマーゼ阻害薬のひとつである。これはβ-ラクタマーゼを産生する抗生物質耐性菌に対して効果をもつ。
効能
抗生物質, 細胞壁合成阻害薬, ベータラクタマーゼ阻害薬
説明
Tazobactam often is coadministered with piperacillin because of tazobactam's ability to inhibit β-lactamases.
T azobactam, like other β-lactamase inhibitors, has little or no antibacterial activity. This effect is analogous
to that of clavulanic acid and sulbactam.
化学的特性
White or off-white powder
使用
b-lactamase inhibitor
定義
ChEBI: A member of the class of penicillanic acids that is sulbactam in which one of the exocyclic methyl hydrogens is replaced by a 1,2,3-triazol-1-yl group; used (in the form of its sodium salt) in combination with ceftolozane sulfate for treatment of complicat
d intra-abdominal infections and complicated urinary tract infections.
抗菌性
Tazobactam exhibits little useful antimicrobial activity,
although weak activity against Acinetobacter spp. and Borrelia
burgdorferi has been reported.
作用機序
Tazobactam functions as an irreversible inhibitor by covalently binding to β-lactamases, and prevents the enzyme hydrolysis of ceftolozane, thereby enhancing its activity against resistant ESBL-producing pathogens, along with expanding coverage to include anaerobes (e.g., Bacteroides spp.)
臨床応用
Tazobactam is a penicillanic acid sulfone that is similar instructure to sulbactam. It is a more potent β-lactamaseinhibitor than sulbactam and has a slightly broader spectrumof activity than clavulanic acid. It has very weak antibacterialactivity. Tazobactam is available in fixed-dose, injectablecombinations with piperacillin, a broad-spectrum penicillinconsisting of an 8:1 ratio of piperacillin sodium to tazobactamsodium by weight and marketed under the trade name Zosyn.The pharmacokinetics of the two drugs are very similar. Bothhave short half-lives (t
1/2 ～1 hour), are minimally proteinbound, experience very little metabolism, and are excreted inactive forms in the urine in high concentrations.
Approved indications for the piperacillin–tazobactamcombination include the treatment of appendicitis, postpartumendometritis, and pelvic inflammatory disease caused byβ-lactamase–producing E. coli and Bacteroides spp., skin andskin structure infections caused by β-lactamase–producingS. aureus, and pneumonia caused by β-lactamase–producingstrains of H. influenzae.
タゾバクタム 上流と下流の製品情報
原材料
準備製品