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Fundamental and clinical studies of a new carbapenem antibiotic, imipenem/cilastatin sodium (MK-0787/MK-0791), were carried out to evaluate the drug in treating infections of the female genital organs. The following results were obtained: In 4 patients undergoing hysterectomy, the penetration of MK-0787 and MK-0791 into female genital organ tissues was studied following a 30-minute intravenous drip infusion of MK-0787/MK-0791 500 mg/500 mg. Plasma levels of MK-0787 and MK-0791 in cubital venous blood following the drip infusion peaked at 0 minute with values of 51.2 micrograms/ml and 61.9 micrograms/ml, respectively, then decreased to 1.9 micrograms/ml and 0.7 microgram/ml, respectively, at 201 minutes. MK-0787 penetrated readily to female genital organ tissues and levels of the drug exceeded 0.5 approximately 1.9 micrograms/g in various organ tissues at 201 minutes following an intravenous drip infusion of 500 mg/500 mg of MK-0787/MK-0791. Clinically, MK-0787/MK-0791 was used for the treatment of obstetrical and gynecological infections at a dosage of 500 mg/500 mg twice daily by intravenous drip infusion. Clinical effects of MK-0787/MK-0791 were analyzed in 22 patients, including 9 patients with intrauterine infections, 7 with intrapelvic infections, 5 with adnexitis, and 1 with an external genital infection. Excellent responses were seen in 5 patients (22.7%), good responses in 15 (68.2%), and poor responses in 2 (9.1%). The efficacy ratio was 90.9%. After the treatment, 15 out of 18 isolates were eradicated for an 83.3% eradication rate. All strains of S. epidermidis (2 strains), Eubacterium lentum (1 strain), Peptococcus sp. (1 strain), beta-Streptococcus (1 strain), Gram-positive rods (2 strains), Enterobacter cloacae (1 strain), Bacteroides bivius (1 strain), Pseudomonas sp. (1 strain), Pseudomonas cepacia (1 strain) and Gram-negative rods (1 strain) were eradicated by the MK-0787/MK-0791 treatment. The safety of the drug was analyzed in 22 patients, effects occurred in 3 (13.6%). Among those 3 patients, diarrhea occurred in 1 patient, rash in another and nausea and vomiting in yet another. One patient had an increased BUN after the MK-0787/MK-0791 treatment. In the other 21 patients, no abnormalities in creatinine, GOT, GPT, or T. Bil. values were observed. It may be concluded that MK-0787/MK-0791 is useful for the treatment of obstetrical and gynecological infections.
H Naito, and
T Hara, and
T Akagi, and
T Masaoka, and
Y Kudo, and
K Iwasaki, and
M Matsuo, and
T Urabe, and
A Fujiwara
May 1986,
The Japanese journal of antibiotics,
H Naito, and
T Hara, and
T Akagi, and
T Masaoka, and
Y Kudo, and
K Iwasaki, and
M Matsuo, and
T Urabe, and
A Fujiwara
June 1986,
The Japanese journal of antibiotics,
H Naito, and
T Hara, and
T Akagi, and
T Masaoka, and
Y Kudo, and
K Iwasaki, and
M Matsuo, and
T Urabe, and
A Fujiwara
June 1986,
The Japanese journal of antibiotics,
H Naito, and
T Hara, and
T Akagi, and
T Masaoka, and
Y Kudo, and
K Iwasaki, and
M Matsuo, and
T Urabe, and
A Fujiwara
June 1986,
The Japanese journal of antibiotics,
H Naito, and
T Hara, and
T Akagi, and
T Masaoka, and
Y Kudo, and
K Iwasaki, and
M Matsuo, and
T Urabe, and
A Fujiwara
May 1986,
The Japanese journal of antibiotics,
H Naito, and
T Hara, and
T Akagi, and
T Masaoka, and
Y Kudo, and
K Iwasaki, and
M Matsuo, and
T Urabe, and
A Fujiwara
June 1986,
The Japanese journal of antibiotics,
H Naito, and
T Hara, and
T Akagi, and
T Masaoka, and
Y Kudo, and
K Iwasaki, and
M Matsuo, and
T Urabe, and
A Fujiwara
May 1986,
The Japanese journal of antibiotics,
H Naito, and
T Hara, and
T Akagi, and
T Masaoka, and
Y Kudo, and
K Iwasaki, and
M Matsuo, and
T Urabe, and
A Fujiwara
June 1986,
The Japanese journal of antibiotics,
H Naito, and
T Hara, and
T Akagi, and
T Masaoka, and
Y Kudo, and
K Iwasaki, and
M Matsuo, and
T Urabe, and
A Fujiwara
June 1986,
The Japanese journal of antibiotics,
H Naito, and
T Hara, and
T Akagi, and
T Masaoka, and
Y Kudo, and
K Iwasaki, and
M Matsuo, and
T Urabe, and
A Fujiwara
May 1986,
The Japanese journal of antibiotics,
