The clinical usefulness of
injectable biapenem (BIPM) was examined for various
infectious diseases in the fields of internal medicine, urology, surgery, orthopedics, obstetrics and gynecology, otorhinolaryngology, ophthalmology, dermatology,
oral surgery, and plastic surgery. BIPM was administered by
intravenous drip infusion at a dose of 150, 300, or 600 mg twice a day. The concentrations in various body fluid and tissues were also examined. 1. In the total enrollment of 256 cases, the numbers subjected to the analyses for clinical efficacy, bacteriological efficacy, side effects and abnormal laboratory findings were 214, 170, 252 and 251 cases, respectively. 2. The clinical efficacy rate was 85.5% (183/214 cases) as a whole, being 2/2 for
sepsis, 6/8 for
cellulitis and
lymphangitis, 76.2% (16/21) for traumatic, operative
wound and
burn infections, 4/6 for
osteomyelitis and
arthritis, 92.9% (13/14) for
peritonsillar abscess and peritonsillitis, 83.3% (15/18) for chronic lower
respiratory tract infection, 7/7 for
pneumonia, 83.3% (30/36) for complicated
urinary tract infection, 100% (14/14) for
cholecystitis and
cholangitis, 88.2% (15/17) for
peritonitis, 86.5% (32/37) for internal genital
infection, 8/9 for pelvic
peritonitis, 2/4 for
corneal ulcer, orbital
infection and
panophthalmitis, 1/2 for
otitis media, 4/4 for sinustitis, 93.3% (14/15) for
osteitis of jaw and
cellulitis of mouth floor. The efficacy rate in the poor responders to the pretreatment by other
antibiotics was 86.4% (70/81). 3. 300 strains of causative organisms were isolated from 170 cases which contained
polymicrobial infections. The elimination rate of causative organisms was 85.3% (256/300 strains), in terms of bacteriological efficacy. 4. Side effects were noted in 11 of 252 cases (4.4%) with 11 events. The signs and symptoms were the skin symptoms (5 cases), gastro-intestinal symptoms (3 cases),
interstitial pneumonia (2 cases), and feeling bad (1 case), all of which disappeared during treatment or after the discontinuation of treatment. The abnormal laboratory findings were observed in 31 of 251 cases (12.4%) with 50 events, and major ones were an increase in eosinophils, and elevations of AST, ALT, gamma-
GTP and Al-p. 5. The concentrations of BIPM in body fluid and tissues were determined in 46 cases (212 samples) most of which were administered 300 mg of BIPM by
intravenous drip infusion for 60 minutes. The concentrations in the sputum within 6 hours after administration were 0.1-2.5 micrograms/g. The maximum concentrations in body fluid and tissues were 0.2-1.8 micrograms/g or ml in the bile, middle ear mucosa, tonsillar tissue, aqueous humor and bone tissues and were 2.0-5.7 micrograms/g or ml in the gallbladder, maxillary sinus mucous membrane, ethmoidal sinus mucous membrane, oral tissues, skin, woman genitals, synovia, joint tissue, and the eschar. The concentrations in the uterine arterial plasma and retroperitoneal fluid were almost similar to those in the cubitl vein plasma. From the above-mentioned results of clinical efficacy, bacteriological efficacy, and safety,
injectable BIPM was confirmed to be useful in the treatment of moderate, severe and/or refractory
infections in various fields.