Ceftriaxone. A review of its antibacterial activity, pharmacological properties and therapeutic use

Drugs. 1984 Jun;27(6):469-527. doi: 10.2165/00003495-198427060-00001.


Ceftriaxone is a new 'third generation' semisynthetic cephalosporin with a long half-life which has resulted in a recommended once daily administration schedule. It is administered intravenously or intramuscularly and has a broad spectrum of activity against Gram-positive and Gram-negative aerobic, and some anaerobic, bacteria. The activity of ceftriaxone is generally greater than that of the 'first' and 'second generation' cephalosporins against Gram-negative bacteria, but less than that of the earlier generations of cephalosporins against many Gram-positive bacteria. Although ceftriaxone has some activity against Pseudomonas aeruginosa, on the basis of present evidence it cannot be recommended as sole antibiotic therapy in pseudomonal infections. Ceftriaxone has been effective in treating infections due to other 'difficult' organisms such as multidrug-resistant Enterobacteriaceae. Ceftriaxone was effective in complicated and uncomplicated urinary tract infections, lower respiratory tract infections, skin, soft tissue, bone and joint infections, bacteraemia/septicaemia, and paediatric meningitis due to susceptible organisms. In most of these types of infections once-daily administration appears efficacious. Results were also encouraging in a few patients with ear, nose and throat, intra-abdominal, obstetric and gynaecological infections, and adult meningitis, but conclusions are not yet possible as to the efficacy of the drug in these indications due to limited experience. A single intramuscular dose of ceftriaxone has been compared with standard therapy for gonorrhoea due to non-penicillinase-producing and penicillinase-producing strains of Neisseria gonorrhoeae and shown to be highly effective. In a few small trials the comparative efficacy of ceftriaxone and other antibacterials has been assessed in other types of infections and in perioperative prophylaxis in patients undergoing surgery. Few significant differences in response rates were found between therapeutic groups in these comparative studies, but larger well-designed studies are needed to more clearly assess the comparative efficacy of ceftriaxone and other antimicrobials, especially the aminoglycosides and other 'third generation' cephalosporins, and to confirm the apparent lack of serious side effects with ceftriaxone. If more widespread use confirms the safety and efficacy of ceftriaxone, it will offer an important alternative, particularly for the treatment of serious infections due to multidrug-resistant Gram-negative bacteria and in situations where the long half-life of the drug could result in worthwhile convenience and cost benefits.

Publication types

  • Review

MeSH terms

  • Aging
  • Animals
  • Bacteria / drug effects*
  • Bacteria, Anaerobic / drug effects
  • Cefotaxime / administration & dosage
  • Cefotaxime / adverse effects
  • Cefotaxime / analogs & derivatives*
  • Cefotaxime / metabolism
  • Cefotaxime / pharmacology
  • Cefotaxime / therapeutic use
  • Cefotaxime / toxicity
  • Ceftriaxone
  • Culture Media
  • Drug Resistance, Microbial
  • Drug Synergism
  • Humans
  • Intestinal Absorption
  • Kinetics
  • Postoperative Complications / prevention & control
  • Premedication
  • beta-Lactamases / metabolism


  • Culture Media
  • Ceftriaxone
  • beta-Lactamases
  • Cefotaxime