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[Cefixime, the first oral third-generation cephalosporin]

G Roche1

  • 1Pharmuka SF, Paris.

Presse Medicale (Paris, France : 1983)
|October 11, 1989
PubMed

Insights

Cefixime, an orally active cephalosporin, offers the potent antibacterial activity of third-generation parenteral antibiotics. It is a safe and effective treatment for various infections, including respiratory and urinary tract infections.

Area of Science:

  • Microbiology
  • Pharmacology
  • Infectious Diseases

Background:

  • Parenteral third-generation cephalosporins revolutionized hospital antibiotic use in the early 1980s due to their low minimum inhibitory concentrations (MICs) against Enterobacteriaceae and enhanced beta-lactamase stability.
  • Development of orally active antibiotics with similar efficacy to parenteral third-generation cephalosporins was a significant research goal.

Purpose of the Study:

  • To introduce cefixime as an orally active cephalosporin with third-generation parenteral-like antibacterial activity.
  • To describe the structural features and absorption mechanisms of cefixime.
  • To outline the clinical efficacy and safety of cefixime for various infections in adults.

Main Methods:

  • Cefixime was developed through molecular modification to achieve oral activity.
  • The role of the vinyl group at the 3-position for intestinal absorption via carrier-mediated transport was identified.
  • The contribution of the aminothiazole ring and R-oxyimino group at the 7-position to antibacterial activity was established.

Main Results:

  • Cefixime demonstrates antibacterial activity comparable to parenteral third-generation cephalosporins.
  • Clinical studies in thousands of adults confirm cefixime's safety and efficacy.
  • Effective treatment of lower respiratory tract, ear-nose-throat, and urinary tract infections was observed.

Conclusions:

  • Cefixime is a safe and effective oral antimicrobial agent.
  • Key indications include bronchial and pulmonary infections, acute otitis/sinusitis, and urinary tract infections (excluding prostatitis).
  • The standard dosage for cefixime is 200 mg twice daily (b.i.d).

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