[Clinical studies on the effect of imipenem/cilastatin sodium on infections in obstetrics and gynecology. Tissue concentrations and clinical effects].
Tissue transfer and clinical effects of imipenem/cilastatin sodium (MK-0787/MK-0791), a new carbapenem antibiotic, were studied and the following results were obtained. Penetrations of MK-0787 into uterine arterial blood and into pelvic dead space exudate were good. When MK-0787/MK-0791 was administered at a dose of 500 mg/500 mg by a 30-minute intravenous drip infusion, the peak level of MK-0787 in uterine arterial blood was 22.2 micrograms/ml, 30 minutes after the completion of the drip infusion. The peak level of MK-0787 in pelvic dead space exudate was 12.9 micrograms/ml at 2 hours and it dropped to 2.6 micrograms/ml at 6 hours. MK-0791 levels were similar to those of MK-0787. Penetrations of MK-0787 into tissues were also good. When MK-0787/MK-0791 was administered at a dose of 500 mg/500 mg by a 30-minute intravenous drip infusion, the level of MK-0787 was 2.2 +/- 1.1 micrograms/g in the oviduct, 2.7 +/- 2.1 micrograms/g in the ovary, 2.5 +/- 1.2 micrograms/g in the endometrium, 3.0 +/- 1.6 micrograms/g in the myometrium, 3.1 +/- 1.9 micrograms/g in the cervix uteri and 3.8 +/- 2.0 micrograms/g in the portio vaginalis at 1 hour after administration. These levels were reduced to halves, respectively, in approximately 2 hours. Four patients with intrauterine infections and 2 with vaginal stump infections were treated with MK-0787/MK-0791 at a daily dose of 1 g/1 g (500 mg/500 mg X 2). Good clinical and bacteriological responses were observed in 5 patients and causative organisms were eradicated in 2 patients.(ABSTRACT TRUNCATED AT 250 WORDS)
Oomomo
Y
Y
Maruhashi
T
T
Hanaoka
J
J
Minagawa
Y
Y
Yuzawa
H
H
Tokunaga
A
A
Takahashi
T
T
Sasagawa
S
S
Takeuchi
S
S
D000328:Adult; D000368:Aged; D001424:Bacterial Infections / Q000188:drug therapy*; D015377:Cilastatin; D003521:Cyclopropanes / Q000008:administration & dosage* / Q000378:metabolism; D004338:Drug Combinations; D005260:Female; D005831:Genital Diseases, Female / Q000188:drug therapy*; D005836:Genitalia, Female / Q000378:metabolism*; D006801:Humans; D015378:Imipenem; D007262:Infusions, Intravenous; D007700:Kinetics; D008431:Maternal-Fetal Exchange; D008875:Middle Aged; D011247:Pregnancy / Q000378:metabolism*; D013845:Thienamycins / Q000008:administration & dosage* / Q000378:metabolism
D003521:Cyclopropanes; D004338:Drug Combinations; D013845:Thienamycins; D015377:Cilastatin; D015378:Imipenem