Aztreonam是单环β-内酰胺抗生素,与青霉素结合蛋白3有较高亲和力。
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Aztreonam is a monocyclic beta-lactam antibiotic originally isolated from Chromobacterium violaceum with bactericidal activity.
体外活性
Aztreonam causes significant suppression of human colony forming unit-erythroid (cfu-e), burst forming unit-erythroid (bfu-e) and colony forming unit-granulocyte macrophage (cfu-gm) at both peak and trough serum concentrations in human bone marrow cells. [1] Aztreonam is hydrolyzed at measurable rates by class A beta-lactamases, a TEM-2 type penicillinase and the Proteus vulgaris cephalosporinase with a broad substraterange. Aztreonam is extremely stable as to the typical class C cephalosporinase of Citrobacter freundii, and acts as a competitive and progressive inhibitor for the beta-lactamase. [2] Aztreonam (AZT) combined with clindamycin (CLDM) has synergistic effects on Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, and Haemophilus influenzae, which are sensitive or quasi-sensitive to CLDM, in the presence of CLDM at MIC or sub-MIC. [3] Aztreonam reduces the cfu of some strains by 1 log unit without preserving the integrity of cystic fibrosis airway cell monolayers, while decreasing the biofilms of other clinical isolates by 4 log units and protecting the monolayers from being compromised. [4]
体内活性
Aztreonam (300 mg/kg) results in a significant decrease in the content of hepatic microsomal P450, while no significant change is observed in hepatic cytochrome b5 content and NADPH-cytochrome c (P450) reductase activity. [5]
Cas No.
78110-38-0
分子式
C13H17N5O8S2
分子量
435.43
别名
氨曲南;SQ-26,776
储存和溶解度
Ethanol:<1 mgml
H2O:9 mg/mL (20.7 mM)
DMSO:81 mg/mL (186 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years