Application of cephalosporins to obstetrics and gynecology: transfer of cefazolin and cephalothin to uterine tissue.

Antibiotics should be administered so as to maintain effective therapeutic levels in target organs. In routine clinical treatment, however, doses of antibiotics are determined on the basis of their achievable concentrations in blood. To determine the optimum doses of antibiotics against obstetric and gynecologic infections, the authors gave a single intravenous dose of 2 gm of cefazolin or cephalothin to 51 patients before hysterectomy and measured the levels of the antibiotics in uterine tissues and compared them with corresponding serum levels. The maximum tissue levels of cefazolin were generally about 6 to 7 times higher than those of cephalothin: In tthe perimetrium, levels were 154 microgram/gm for cefazolin and 24.1 microgram/gm for cephalothin; in the myometrium, 109.5 microgram/gm for cefazolin, and 15.5 microgram/gm for cephalothin; and in the endometrium, 98.9 microgram/gm for cefazolin and 10.4 microgram/gm for cephalothin. In the tissues, however, cephalothin reached peak levels more rapidly than cefazolin. Comparisons of the tissue levels and MIC of cefazolin and cephalothin revealed that cefazolin was maintained at over 12.5 microgram/gm for at least 150 minutes in the perimetrium, myometrium, and endometrium, whereas cephalothin was maintained at these levels for 40 to 50 minutes only in the perimetrium and myometrium. The ratio of tissue levels to serum levels was 40-70 to 100 for cefazolin and about 30 or less to 100 for cephalothin.