아조트리오남

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Danger

• 유해·위험 문구

  H334：흡입 시 알레르기성 반응, 천식 또는 호흡 곤란 등을 일으킬 수 있음

  H400：수생생물에 매우 유독함

• 예방조치문구

  P261：분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.

  P273：환경으로 배출하지 마시오.

  P285：환기가 잘 되지 않는 곳에서는 호흡기 보호구를 착용하시오

  P304+P341：들이마신 경우,호흡이 어려운 경우 환자를 신선한 공기가 있는 곳으로 옮기고 호흡하기 편한 자세로 안정을 취하게 함

  P342+P311：호흡기 증상이 나타나면 의료기관(의사)의 진찰을 받으시오.

  P391：누출물을 모으시오.

  P501：...에 내용물 / 용기를 폐기 하시오.

아조트리오남 화학적 특성, 용도, 생산

• 개요

  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.

• 화학적 성질

  White Crystalline Powder

• 역사

  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.

• 용도

  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.

• Antimicrobial activity

  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.

• Pharmacokinetics

  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.

• Clinical Use

  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

• 부작용

  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.

• Safety Profile

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

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