アズトレオナム

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H334：吸入するとアレルギー、喘息または、呼吸困難 を起こすおそれ

  H400：水生生物に強い毒性

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P273：環境への放出を避けること。

  P285：換気が十分でない場合には、呼吸用保護具を着用する こと。

  P304+P341：吸入した場合：呼吸が困難な場合には、空気の新鮮な場 所に移し、呼吸しやすい姿勢で休息させること。

  P342+P311：呼吸に関する症状が出た場合：医師に連絡すること。

  P391：漏出物を回収すること。

  P501：内容物/容器を．．．に廃棄すること。

アズトレオナム 価格

アズトレオナム 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

• 商品名

  アザクタム (エーザイ)

• 説明

  Aztreonam is the first member of the monobactam class of antibiotics to be introduced into the world market. It possesses high β-lactamase stability and moderately good activity against gram negative aerobes such as E. coli, S. marcescens, -9 Proteus Providencia, Salmonella, g. influenzae, E. gonorrhea, and &. pneumonia. While somewhat less potent against Pseudomonas aeruginosa, it is nonetheless one of the better β-lactams against this species. It has poor activity against gram positive organisms.

• 化学的特性

  White Crystalline Powder

• 来歴

  Aztreonam was synthesized by the Squibb Institute for Medical Research in 1981 starting with l-threonine. The synthesis was based on findings about bacterial β-lactam compounds of a monocyclic nature . The β-lactam compounds, called monobactams, were isolated from Chromobacterium violaceum, Agrobacterium radiobacter, etc. Such monocyclic βlactams of bacterial origin had previously been found independently in 1981 by Takeda Chemicals Industries in the culture broths of Pseudomonas acidophila and P. mesoacidophila and named sulfazecin and isosulfazecin, respectively. Aztreonam was selected from among hundreds of derivatives as a candidate for clinical trials because of its unique antibacterial spectrum and strong activity. This antibiotic shows excellent activity against a variety of gram-negative aerobic bacteria but no activity against gram-positive bacteria or anaerobes. Its efficacy and safety are now being clinically evaluated.

• 使用

  Aztreonam is a synthetic β-lactam antibiotic of the monobactam class. It is effective against Gram-negative bacteria but inactive against Gram-positive bacteria. Its mechanism of action involves the inhibition of mucopeptide synthesis in the bacterial cell wall, thereby blocking peptidoglycan crosslinking. Aztreonam is resistant to hydrolysis by some β-lactamases, but is inactivated by extended-spectrum β-lactamases.

• 抗菌性

  Concentrations (mg/L) inhibiting 50% of other organisms are: Aeromonas spp., 0.1;Acinetobacter spp., 16; Mor. catarrhalis, 0.1; Burkholderia cepacia, 2; and Yersinia spp., 0.1. Synergy has been shown with gentamicin, tobramycin and amikacin against 52–89% of strains of Ps. aeruginosa and gentamicin-resistant Gram-negative bacteria.

• 薬物動態学

  C_max 1 g intravenous: 90 mg/L end infusion
  1 g intramuscular: 46 mg/L after 1 h
  Plasma half-life: 1.7 h
  Volume of distribution: 0.18 L/kg
  Plasma protein binding: 56%
  Absorption and distribution
  Oral bioavailability is less than 1%. Peak concentrations above the median MIC for most Gram-negative pathogens are achieved in most tissues and body fluids after 1 g intramuscular or intravenous doses.
  Metabolism and excretion
  It is not extensively metabolized, the most prominent product, resulting from opening the β-lactam ring, being scarcely detectable in the serum and accounting for about 6% of the dose in the urine and 3% in the feces.
  It is predominantly eliminated in the urine, where 58–72% appears within 8 h. Less than 12% is eliminated unchanged in the feces, suggesting low biliary excretion.

• 臨床応用

  Urinary tract infections, including pyelonephritis and cystitis
  Lower respiratory tract infections, including pneumonia and bronchitis
  caused by Gram-negative bacilli
  Septicemia
  Skin and skin structure infections, including postoperative wounds, ulcers
  and burns
  Intra-abdominal infections, including peritonitis
  Gynecological infections, including endometritis and pelvic cellulitis

• 副作用

  Local reactions occasionally occur at the injection site. Systemic reactions include diarrhea, nausea and/or vomiting and rash (1–1.3%). Neutropenia was seen in 11.3% of the pediatric patients younger than 2 years. Pseudomembranous colitis has been reported.
  There are no reactions in patients with immunoglobulin E (IgE) antibodies to benzylpenicillin or penicillin moieties. It is rarely cross-reactive with other β-lactam antibiotics and is weakly immunogenic.

• 安全性プロファイル

  Moderately toxic by severalroutes. An experimental teratogen. Other experimentalreproductive effects. When heated to decomposition itemits toxic fumes of NOx and SOx.

アズトレオナム 上流と下流の製品情報

アズトレオナム 生産企業

Global(535)Suppliers

アズトレオナム スペクトルデータ(¹HNMR)

78110-38-0, アズトレオナム キーワード