[A study on the penetration of imipenem/cilastatin sodium into the female genital tissues].
A new carbapenem antibiotic, imipenem/cilastatin sodium (MK-0787/MK-0791), was administered by intravenous drip infusion at a dose level of 500 mg/500 mg to 30 patients who underwent total abdominal hysterectomy for uterine myomas with or without benign ovarian tumors. The uterine arteries were clamped bilaterally at 0.25, 0.5, 1, 2, 3, 4, 6 and 8 hours after administration, and plasma samples and uterine tissues were taken for measurements of MK-0787 by bioassay and MK-0791 by HPLC. The measured values were analyzed using a two-compartment open model. Maximum concentrations of MK-0787 at 0.5 hour after the start of intravenous drip infusion were 98.5 micrograms/ml in the antecubital vein, 100.1 micrograms/ml in the uterine artery, 26.5 micrograms/g in the oviduct, 21.2 micrograms/g in the ovary, 19.1 micrograms/g in the endometrium, 19.0 micrograms/g in the myometrium, 22.1 micrograms/g in the cervix uteri and 16.4 micrograms/g in the portio vaginalis. These results suggest that the penetration of MK-0787/MK-0791 into female genital tissues is good, and sufficient concentrations are obtained enough to inhibit organisms which are frequently isolated from patients with pelvic inflammatory disease.
Hongo
M
M
Shimizu
R
R
Sakae
K
K
Kohchi
T
T
Tada
K
K
Tani
M
M
D000290:Adnexa Uteri / Q000378:metabolism; D000328:Adult; D015377:Cilastatin; D003521:Cyclopropanes / Q000008:administration & dosage* / Q000097:blood; D004338:Drug Combinations; D005260:Female; D005836:Genitalia, Female / Q000378:metabolism*; D006801:Humans; D015378:Imipenem; D007262:Infusions, Intravenous; D007700:Kinetics; D008875:Middle Aged; D013845:Thienamycins / Q000008:administration & dosage* / Q000097:blood; D014599:Uterus / Q000378:metabolism
D003521:Cyclopropanes; D004338:Drug Combinations; D013845:Thienamycins; D015377:Cilastatin; D015378:Imipenem