セフトリアキソン 化學(xué)特性,用途語,生産方法
効能
抗生物質(zhì), 細(xì)胞壁合成阻害薬
説明
Ceftriaxone has the same C-7 side-chain moiety as cefotaxime and ceftizoxime, but the C-3 side chain
consists of a metabolically stable and activating thiotriazinedione in place of the normal acetyl group. The
C-3 side chain is sufficiently acidic that at normal pH, it forms an enolic sodium salt; thus, the commercial
product is a disodium salt.
使用
Ceftriaxone is an antibacterial, a third-generation cephalosporin.
定義
ChEBI: A cephalosporin compound having 2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetylamino and [(2-methyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl)sulfanyl]methyl side-groups.
抗菌性
Most β-lactamase-producing enterobacteria are highly susceptible,
as are streptococci (but not enterococci) and fastidious
Gram-negative bacilli, although brucellae are less sensitive
(MIC 0.25–2 mg/L). Treatment failure has been reported in
tularemia. Ps. aeruginosa, mycoplasmas, mycobacteria and L.
monocytogenes are resistant.
獲得抵抗性
Ceftriaxone is hydrolyzed by some chromosomal enzymes, including those of Enterobacter spp. and B. fragilis. Derepression of chromosomal β-lactamase production can cause resistance in some species of Gram-negative bacilli in vitro and has been observed in patients.
臨床応用
Uses of Ceftriaxone are similar to those of cefotaxime, the long half-life offering the advantage of once-daily administration. It is used in the treatment of acute bacterial meningitis and as an alternative to rifampicin (rifampin) in the prophylaxis of meningococcal disease.
副作用
Reactions are those common to other cephalosporins. Mention has been made of thrombocytopenia, thrombocytosis, leukopenia, eosinophilia abdominal pain, phlebitis, rash, fever and increased values in liver function tests. Diarrhea is common and suppression of the aerobic and anaerobic fecal flora has been associated with the appearance of resistant bacteria and yeasts.
Biliary pseudolithiasis due to concretions of insoluble calcium salt has been described in adults but principally in children. The precipitates can be detected in a high proportion of patients by ultrasonography and can occasionally cause pain, but resolve on cessation of treatment. Ceftriaxone is better avoided in patients with pre-existing biliary disease, but the principal hazard appears to be misdiagnosis of gallbladder disease and unnecessary surgery.
セフトリアキソン 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品