INTRA-OCULAR LEVELS OF CEFAMANDOLE COMPARED WITH CEFAZOLIN AFTER SUB-CONJUNCTIVAL INJECTION IN RABBITS

  • 1 January 1979
    • journal article
    • research article
    • Vol. 18  (3) , 250-255
Abstract
The intraocular pharmacokinetics of cefazolin were compared with those of cefamandole, a recently marketed cephalosporin with enhanced activity against gram-negative bacilli. Following subconjunctival injection of 12.5 mg into infected eyes (Staphylococcus aureus endophthalmitis) of pigmented rabbits, both drugs reached peak concentrations > 100 .mu.g/gm in cornea, sclera and choroid-retina. The half-life was markedly shorter in sclera and choroid-retina than in cornea. Levels in the aqueous humor rose and fell more slowly than those in ocular tissues, reaching a maximum of only 5-10 .mu.g/ml. The pharmacokinetics of the 2 drugs were virtually identical in most intraocular sites. When cefazolin, which was less irritating than cefamandole by the subconjunctival route, was given in a dosage of 100 mg, levels in ocular tissues were increased by 2-4-fold and in aqueous humor by 15-fold, compared to the concentrations produced by the 12.5 mg dosage. Levels in the vitreous humor were exceedingly low with both drugs; mean peak concentrations were 0.24 .mu.g/ml after the 12.5 mg dosage of cefamandole and < 1.6 .mu.g/ml after the 100 mg dose of cefazolin.

This publication has 2 references indexed in Scilit: