[Fundamental and clinical studies on imipenem/cilastatin sodium in the field of obstetrics and gynecology].
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. Plasma concentrations of MK-0787 in antecubital vein and uterine artery were 18.2 micrograms/ml and 16.4 micrograms/ml, respectively, and of MK-0791 were 9.5 micrograms/ml and 10.3 micrograms/ml, respectively, at 1.28 hours after the end of a drip infusion of 0.5 g/0.5 g 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 0.7 micrograms/ml and 1.0 micrograms/ml, respectively, and of the latter were 1.5 micrograms/ml and 1.9 micrograms/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. 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. No side effects were observed, but increase of eosinocytes was observed in 1 patient.
Takamura
S
S
Hata
T
T
Kumagaya
J
J
Yamabe
T
T
D000293:Adolescent; D000328:Adult; D000368:Aged; D001424:Bacterial Infections / Q000188:drug therapy*; D015377:Cilastatin; D003521:Cyclopropanes / Q000008:administration & dosage* / Q000378:metabolism / Q000627:therapeutic use; D004150:Dipeptidases / Q000037:antagonists & inhibitors*; D004338:Drug Combinations; D004341:Drug Evaluation; D005260:Female; D005831:Genital Diseases, Female / Q000188:drug therapy*; D005836:Genitalia, Female / Q000378:metabolism; D006801:Humans; D015378:Imipenem; D008875:Middle Aged; D013845:Thienamycins / Q000008:administration & dosage* / Q000378:metabolism / Q000627:therapeutic use
D003521:Cyclopropanes; D004338:Drug Combinations; D013845:Thienamycins; D015377:Cilastatin; D015378:Imipenem; D004150:Dipeptidases