Possible relation between the changes in the penicillin pharmacokinetics and coagulograms under the effect of trypsin in rats and man was analysed. It was found that parenteral administration of the enzyme was accompanied by a simultaneous increase in the penicillin blood level, oliguria, a decrease in the antibiotic amount excreted with urine and drop of the fibrinogen level in plasma. The latter is consequent on intravascular coagulation which results in temporary impairment of the excretion function of the kidneys defining the changes in the penicillin pharmacokinetics under the effect of trypsin.