Цефиксим

Описание

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.

Химические свойства

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.

Определение

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.

Антимикробная активность

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.

Угроза здоровью

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

Фармакокине?тика

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.

Клиническое использование

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.

Побочные эффекты

It is well tolerated, but diarrhea is fairly common and pseudomembranous colitis has been reported. Other side effects common to cephalosporins are occasionally seen.

Меры предосторожности

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.