Abstract
The following results were obtained during pharmacokinetic, bacteriological and clinical evaluation of the usefulness of the combination (1: 1) of imipenem (MK-0787) and cilastatin sodium (MK-0791), an inhibitor of dehydropeptidase-I, in the treatment of patients with obstetric and gynecologic infections.
1. Plasma concentrations of MK-0787 in antecubital vein and uterine artery were 18.2μg/ml and 16.4μg/ml, respectively, and of MK-0791 were 9.5μg/ml and 10.3μg/ml, respectively, at 1.28 hours after the end of a drip infusion of 0.5g/0.5g of MK-0787/MK-0791.
Plasma concentrations of both MK-0787 and MK-0791 decreased slowly, and concentrations of the former in antecubital vein and uterine artery were 0.7μg/ml and 1.0μg/ml, respectively, and of the latter were 1.5μg/ml and 1.9μg/ml, respectively at 2.83 hours after the end of a drip infusion.
Concentrations of the 2 agents in female genital tissues decreased with increasing time in a manner similar to concentrations in the plasma.
2. Clinical responses in 10 patients were excellent in 2 and good in 8, and the efficacy rate was 100 percent.
Organisms were isolated from all 10 patients before the treatment, but were eradicated in 9 patients by the treatment.
3. No side effects were observed, but increase of eosinocytes was observed in 1 patient.