Cefonicid was administered intramuscularly 1 h before open-heart surgery to seven patients in doses of 1 g each and to six patients in doses of 2 g each. Cefonicid concentrations were measured in the right atrial biopsy and in serum at onset of surgery, at time of atrial biopsy, 15 min after starting cardiopulmonary bypass, and at completion of cardiopulmonary bypass. Concentrations in the atrial biopsy and in serum at all periods exceeded the minimal inhibitory concentrations for organisms most frequently responsible for postoperative infections.