Ceftriaxone: a beta-lactamase-stable, broad-spectrum cephalosporin with an extended half-life

Abstract

Ceftriaxone is an aminothiazolyl-oxyimino cephalosporin. It possesses the typical in vitro activity of a third-generation cephalosporin with excellent activity against many gram-negative aerobic bacilli: Escherichia coli; species of Proteus, Klebsiella, Morganella, Providencia and Citrobacter; and Enterobacter agglomerans. Ceftriaxone also has outstanding bactericidal action against pneumococci, group B streptococci, meningococci, gonococci and Hemophilus influenzae. In healthy volunteers, it has an exceptionally long serum half-life of 5.8-8.7 (mean 6.5) hours. It distributes well throughout all body spaces, including cerebrospinal fluid in the presence of inflammation. Dosage modification is necessary only when there is combined hepatic and renal dysfunction. Adverse reactions characteristic of cephalosporins have been observed with the administration of ceftriaxone. No unique toxicities have been identified, and hypoprothrombinemic bleeding is not part of the adverse reaction profile. Ceftriaxone has been used to treat serious bacterial infections in neonates, infants, children and adults. Bacteriologic and clinical success rates have consistently exceeded 90%. The drug has also been used as single-dose chemoprophylaxis in coronary artery bypass, biliary tract, vaginal hysterectomy and prostatic surgery. Efficacy and safety were similar to multiple-dose cefazolin. Ceftriaxone warrants special consideration because its extended half-life allows for less frequent dosing than other antimicrobials. Significant cost savings can be realized with proper use of this antibiotic.