セフィキシム 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
説明
Cefixime is the first orally active third-generation cephalosponn with a true broad
spectrum of activity. It is reportedly more effective against Gram-negative bacteria than
conventional oral cephems such as cephalexin and cefaclor.
化学的特性
Cefixime is an oral third generation cephalosporin antibiotic. It was sold under the trade
name Suprax in the United States until 2003. The oral suspension form of “Suprax” was
re-launched. Cefixime is prescribed for bacterial infections of the chest, ears, urinary tract,
and throat (tonsilitis and pharyngitis), and for uncomplicated gonorrhea, upper and lower
respiratory tract infections, acute otitis media, and gonococcal urethritis.
定義
ChEBI: A third-generation cephalosporin antibiotic bearing vinyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-[(carboxymethoxy)imino]acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. It is used in the treatment of gonorrhoea
tonsilitis, pharyngitis, bronchitis, and urinary tract infections.
抗菌性
It is active against N. gonorrhoeae, M. catarrhalis,
H. influenzae and a wide range of enterobacteria, including
most strains of Citrobacter, Enterobacter and Serratia spp.
Its antistaphylococcal activity is poor. It is not active against
Acinetobacter spp., Ps. aeruginosa or B. fragilis. It is resistant to
hydrolysis by common β-lactamases.
健康ハザード
Exposures to cefi xime may cause side effects that include, but are not limited to, stomach
and abdominal pain, diarrhea, vomiting, mild skin rash, headache, fever, urticaria, pruritis, eosinophilia, leucopenia, anaphylaxis, superinfection, hemolytic anemia, dyspepsia,
and fl atulence. Also, cefi xime may cause transient elevation of SGOT, SGPT, alkaline phosphatase, BUN, and creatinine. Reports have indicated that cefi xime is mainly excreted
unchanged in the bile and urine
薬物動態学
Oral absorption: c. 50%
C
max 400 mg oral: 4–5.5 mg/L after 4 h
Plasma half-life: 3-ndash;4 h
Volume of distribution: 0.1 L/kg
Plasma protein binding: 60-ndash;70%
Absorption and distribution
Oral absorption is slow and incomplete, but is unaffected by aluminum magnesium hydroxide. Penetration into cantharides blister fluid was very slow but exceeded the plasma level. CSF concentrations are poor even in the presence of meningeal inflammation, reaching an average of around 0.22 mg/L in children with meningitis.
Metabolism and excretion
It is not metabolized and is excreted unchanged in urine (mainly by glomerular filtration) and in bile, in which concentrations exceeding 100 mg/L have been found. Less than 20% of an oral dose is recovered from the urine over 24 h, falling to less than 5% in patients with severe renal impairment, with a corresponding increase in plasma concentration. It is not removed by peritoneal or hemodialysis.
臨床応用
Cefixime has been used successfully in uncomplicated cystitis,
upper and lower respiratory tract infections and various
other infections. Its failure to provide adequate cover for
staphylococci should be noted.
副作用
It is well tolerated, but diarrhea is fairly common and
pseudomembranous colitis has been reported. Other side
effects common to cephalosporins are occasionally seen.
予防処置
Users of cefi xime should be careful in health conditions such as neonates, pregnancy,
lactation, and renal failure. Users should follow suitable and appropriate health care measures to control superinfection (if it happens during therapy). It is contraindicated
in patients with a known allergy to penicillin or any other ingredients of Taximax.
Taxim-O is contraindicated in patients with a known allergy to the cephalosporin group
of antibiotics.
セフィキシム 上流と下流の製品情報
原材料
準備製品