The in vitro antimicrobial activity and clinical efficacy of biapenem (BIPM), a new carbapenem, were investigated. The antimicrobial activities of BIPM to 330 strains each of methicillin-resistantStaphylococcus aureus (MRSA), Enterococcus faecalis, Escherichia coli, Citrobacter freundii, Klebsiella pneumoniae, Enterobacter cloacae, Serratia marcescens, Proteus mirabilis, Proteus vulgaris andPseudomonas aeruginosa isolated from the patients with urinary tract infections (UTI) was measured by the agar dilution method. Inoculum size was 10⁶ CFU/ml and the results were compared with those of imipenem (IPM), flomoxef (FMOX), ceftazidime (CAZ) and ofloxacin (OFLX). Antimicrobial activities of BIPM against both gram-positive and gram-negative bacteria were similar to those of IPM, and superior to those of FMOX, CAZ and OFLX.
BIPM was given to 22 patients with 21 of complicated UTIs and one of acute bacterial prostatitis at a dose of 300 or 600mg per day for 5-6 days. The overall clinical efficacy of 20 complicated UTI patients evaluated by doctors was 80%, and that of 18 patients with complicated UTI patients according to the criteria proposed by the Japanese UTI committee was 77.8%. Evaluation of a case acute bacterial prostatitis was excellent by both evaluation method. Twenty seven of 28 strains (96.4%) isolated from patients with UTIs or prostatitis including 10 gram-positive cocci and 2 P. aeruginosa strains. As abnormal laboratory data after administration of BIPM, slight elevation of GOT and GPT in one patient was noted. Adverse reaction was not observed.

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We performed basic and clinical studies on biapenem (BIPM). The antibacterial activity of BIPM against clinical isolates was compared with that of imipenem (IPM), panipenem (PAPM), meropenem (MEPM), ceftazidime (CAZ) and piperacillin (PIPC).
MIC₉₀ was 1.56μg/ml for Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, 100μg/ml for Coagulase-negative Staphylococcus, 25μg/ml for Pseudomonas aeruginosa. BIPM was nearly equal to IPM against S. aureus, E. coli, K. pneumoniae and E. cloacae, and superior to all reference drugs against P. aeruginosa.
BIPM 300mg was administered intravenously by 60minutes drip infusion, and mean plasma levels were 33.1, 9.0, 5.8, 2.4, 0.9μg/ml at 0, 30, 60, 120, 240minutes after d.i.v. Mean biliary levels were 4.1, 5.7, 4.5, 2.0, 0.6μg/ml at 0, 30, 60, 120, 240miniutes after d.i.v.
BIPM was administered intravenously by drip infusion to 14 patients with various infections in the field of surgery. Clinical response were excellent in 7 cases, good in 5 cases, fair in 1 case and unevaluable in 1 case, an efficacy rate of 92.3%. No side effects were noted.

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Basic and clinical studies of biapenem (BIPM), a newly-developed carbapenem antibiotic for parenteral use, were carried out in surgical field, and the following results were obtained.
1) Antibacterial activity: MIC₅₀/MIC₉₀ (μg/ml) against Staphylococcus aureus, Esherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa isolated from surgical lesions were respectively measured to be 25/50, ≤0.20/≤0.20, ≤0.20/0.39, 0.39/0.78.
2) Penetration into bile: After 300mg of BIPM was administered to one of cholelithiasis after operation by intravenous drip infusion, bile and serum levels were measured. The maximum bile and serum levels were 1.4μg/ml and 20.7μg/ml.
3) Clinical results: BIPM was administered to 28 patients with surgical infection. Clinical response was excellent in 9, good in 17, fair in 1 and poor in 1, resulting in a 92.9% efficacy rate. The bacteriological efficacy was respectively evaluated to be eradicated in 19, replaced in 2, partially eradicated in 1, and persisted in 2 cases, showing a 87.5% eradication rate. No adverse reaction was noted. Abnormal laboratory findings were recognized in 6 cases.

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Biapenem (BIPM) is a new 4β methyl carbapenem antibiotic with a broad antibacterial activity against various types of bacteria and is stable to human renal dehydropeptidase-I. Clinical investigations on BIPM in surgical filed were carried out, and the results were as follows;
1) The concentration of BIPM in plasma and bile were determined in 4 PTCD patients receiving 60 min intravenous drip design infusion of 300 and 600mg of BIPM by crosover design. Peak levels were plasma, 19.2±9.1 and 39.8±19.5g/ml after completion of infusion and thore in bile, were 45±16 and 117±6.1g/ml at 1h, respectivery. It was clearly observed a dose response in plasma and bile levels of BIPM between 300 and 600mg administration.
2) BIPM after a single intravenous infusion of 600mg for 60min showed the fast and good penetration to the abdominal wall and intraabdominal organ tissues: the peak concentration in each tissue was 5.6 (stomach), 0.16 (liver), 2.6 (gallbladder), 0.9 (pancreas), 1.1 (spleen), 3.3 (peritnneum), 3.1 (muscle), and 0.9g/g (subcutanous tissue), respectivery.
3) BIPM at a dose of 300mg was administered once to three times daily for 2 to 14 days to 45 patients: 10 with peritonitis, 6 with appendicitis or diverticulitis, 3 with abdominal abscess, 4 with liver abscess, 7 with cholecystitis or cholangitis, 2 with wound infection, 11 with periproctal abscess and 2 with subcutaneous abscess. The clinical efficacy was excellent in 17 patinets, good in 26, fair in 1 and poor in 1, and the efficacy rate was 95.6%. Bacteriological affects of BIPM in 31 patients were 90.3%. Abnormal laboratory data were observed elevated GOT and GPT and increased platelet count each in 1 patient.
Therefore, BIPM in expected to be a useful antibacterial agent surgical infections.

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The pharmacokinetics of biapenem (BIPM) in the biliary system was studied in patients without infection, and in addition, 27 patients were treated with this drug. Serial samples of bile and blood were taken from three patients with bile drainage after the intravenous administration of 0.3 g of BIPM over 30 min. In the plasma, peak levels of BIPM were 12.6-17.5μg/ml at one hour after the start of administration, and the levels decreased to 0.6-1, 1μg/ml by 6h. In the bile, peak levels were 4.5-11.0μg/ml at 1 to 3 h and the levels decreased to 0.4-1.3μg/ml by 5 to 6 h.
Of the 26 surgical infections (25 patients) that were evaluated in 27 patients (the additional patients could not be evaluated), clinical efficacy was excellent in 14, good in five, fair in five, and poor in two, with an efficacy of 73%. For postoperative infection (n=17), efficacy judged to be “excellent” was more common (p=0.028) than for primary infection. The bacteriological response by 26 strains isolated was evaluated. Fifteen strains were eradicated, the number of colony-forming units decreased with four strains, and seven strains persisted, with an eradication rate of 58%. The bacteriological response in the host was evaluated for 16 infections. Bacteria were eradicated in seven infections, decreased in four infections, were replaced in one infection, and persisted in four infections, with an eradication rate of 50%. Three of six strains of Staphylococcus aureus were eradicated. The MIC was 25μg/ml or more for 10 of the 27 strains, examined. Fifteen (62%) of 24 strains, for which the MIC was calculated were eradicated, 10 of the 13 strains for which the MIC was less than 12.5μg/ml were eradicated, and 5 of the 11 strains for which the MIC was 12.5μg/ml or more were eradicated. The safety of this drug could be evaluated in all 27 infections, and abnormal changes in laboratory data were found in five patients. One change involved renal function, and according to the attending physicians, the drug might be the cause.
BIPM seemed to be fairy effective for surgical infections, including those involving the biliary system.

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Basic and clinical studies of biapenem (BIPM), a new carbapenem antibiotic, were performed in the field of gastroenterological surgery and the results were as follows:
1. Antibiotic activity: BIPM exhibited excellent antibiotic activity against clinically isolated MSSA, Staphylococcus aureus against which the MICs of methicillin were less than 6.25μg/ml, while the MICs of the drug were high against clinically isolated MRSA. S. aureus against which the MICs of methicillin were not less than 12.5μg/ml. The drug also showed excellent activity against Enterococcus sp. by its MIC₉₀ of 6.25μg/ml and against gram-negative bacilli including Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Proteus mirabilis, Enterobacter cloacae, Enterobacter aerogenes, Citrobacter freundii, Acinetobacter calcoaceticus by its MIC₉₀ being less than 3.13μg/ml. The antibiotic demonstrated good activity against Serratia marcescens, Pseudomonas aeruginosa and Pseudomonas cepacia except for a part the strains, against which its MICs were high.
2. Pharmacokinetics: Intravenous drip infusion of BIPM (300mg) were administered to patients undergoing cholecystectomy (2), colectomy (1), total gastrectomy (1) and distal pancreatectomy (1), and the distributions of the drug in the plasma, ascites, peritoneum, pancreas, gallbladder wall and urine were measured. The distribution in the ascites was almost same as that in the plasma. The concentration in the peritoneum was 1.3μg/ml at 1hr after completion of the infusion.
3. Clinical effects: BIPM was administered to 25 patients with postoperative wound infection (7), perforative peritonitis (5), intraabdominal abscess (5), subphrenic abscess (2), intraabdominal abscess concurring with wound infection (1), retroperitoneal abscess (1), local peritonitis (1), cholangitis (1), cholecystitis (1) and catheter sepsis (1) as infection in the field of gastroenterological surgery. The results were excellent in 3 cases, good in 18 cases and fair in 4 cases. Eruption was observed in one case as side effect, and abnormal laboratory finding was noted in another case.
From the above results, BIPM was considered to be a useful antibiotic against surgical infections.

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The clinical effects of biapenem (BIPM) on infectious diseases in obstetrics and gynecology and the transferability of BIPM in female genital tissues were assessed. Concentrations of BIPM in the blood and female genital organs after 300mg single intravenous drip infusion of this drug were measured. Blood concentrations in the uterine artery at 90-120 minutes after the treatment were respectively found to be 3.2-6.2μg/ml. Tissue concentrations in the uterus and adnexa ranged from 0.5-2.2μg/ml.
BIPM was administered to 5 patients with intrauterine infections, 4 with adnexitis, 8 with pelvic infections and 2 with bartholin's abscess. The overall clinical efficacy was excellent in 3 patients, good in 11 and poor in 2. The overall efficacy rate was 87.5%(14/16).
As an adverse reaction, eruption was observed in only one patient, and there were no abnormal clinical laboratory data.

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Biapenem (BIPM), a newly developed carbapenem antibiotic, was evaluated for its tissue penetration into female genital organs and its clinical usefulness, with the following results.
The intravenously administered BIPM, a single drip infusion (60 minutes) of 300mg, showed the fast and good penetration to the tissues (endometrium, myometrium, cervical canal, raginal portion of the cervix, uterine tube and ovaries): the peak concentration in the cubital vein and uterine artery were 4.46 and 4.42μg/rnl, respectively. Maximum concentrations in genital tissues were 1.23 3.52μg/g.
BIPM was administered to 5 patients, 1 with infected abortion, 2 with endometritis and 2 with salpingitis at doses of 150-300mg twice a day for 4 to 8 days. The clinical response was good in all cases. 2 and 1 of the 5 patients in whom the bacteriological effects weree valuated showed bacterial elimination, partially elimination, respectively. In other 2 patients, one patient was superinfection and the other patient was unknown bacteriologically. There were no specific side effects or abnormal values of clinical laboratory tests.

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The pharmacokinetic and clinical studies of biapenem (BIPM), a new 4-methylc arbapenem antibiotic possessing a stability for human renal dehydropeputidase-I were carried out.
1. The concentration of BIPM was examined in serum, internal genital organs and retroperitoneal fluid after intravenous administration of 0.3 g dose. The peak serum concentrations in the cubital vein and uterine artery were 15.8 and 15.0 ugfrnl, respectively, while the genital tissue concentration was 5.3 μg/g. The peak level of retroperitoneal fluid was 8.2 μg/ml.
2. BIPM was administered to 11 patients. Clinical response was good in 9 cases andunknown in 2 cases. Principal causative organisms were Eikenella corrodens, Clostridium sp. and Fusobacterium sp. and the bacteriological response was evaluated as eradicated in 2 strain and as replaced 1 strain. In one patient, the side effects of lip numbness and vomiting and the elevation of GOT, GPT, γ-GTP value in laboratory findings were observed.

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Fundamental and clinical studies on biapenem (BIPM), a newly developed parenteral carbapenem antibiotic, were performed and the results were summarized as follow.
1. The concentrations of BIPM in plasma and female genital organs after a single d. i. administration of 300 mg for 60 minutes were examined. The drug transferred into tissues of female genital organs and remained a level of 0.6μg/g even at 176 min.
2. BIPM was given to 6 patients with gynecological infections. Clinical results were excellent in 1, good in 4, and poor in 1.
3. No side effects or abnornal laboratory findings were observed.

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Basic and clinical studies on biapenem (BIPM), a newly-developed parenteral carbapenem antibiotic, were performed, and the following results were obtained.
1. The concentration of BIPM in serum and internal genital organs after intravenous drip infusion of 300mg were examined.
The peripheral serum level was 10.6μg/ml at 15 minutes, decreasing to 2.11μg/ml (mean) at about 2.5 hours.
Although there were some variation among sex organs, the concentration in the tissues was 2.05-4.42±g/g at 15 minutes and 0.18-0.40μg/g at about 3hours after administration.
2. The concentration of BIPM in serum and retroperitoneal fluid after intravenous drip infusion of 300mg were examined. The concentration in retroperitoneal fluid were 8.67 ± 1.69μg/ml at 15 minutes, decreasing to 0.46 ± 0.21μg/ml at 6.5hours after administration.
3. In a clinical trial, BIPM was administered to 10 patients with obstetric and gynecological infections (6 cases of parametritis, 1 of puerperal intrauterine infection, 1 of salpingitis, 1 of pyometra and 1 of infectious lymphocystitis).
The results were as follows: 7 cases were judged as good and 3 poor. The efficacy rate was 70%, Bacteriologically, 16 organisms were isolated from 9 patients. The iradication rate was 87.5%(14/16).
No side effects and abnormal laboratory findings were observed in any of the cases.
Hence it appears that BIPM will be a very useful antibiotic in obstetric and gynecologic infections.

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We studied biapenem (BIPM), a new carbapenem antibiotic, for its clinical efficacy and transfer into serum and tissues, and obtained the following results.
1) After 30 min intravenous administration of 0.3g of BIPM, the serum concentration in the uterine artery was almost equal to that in the elbow vein and peak level was around 24-26μg/ml in 18 minutes. Favorable results were also obtained for concentrations in both adnexal and uterine tissues studied.
2) The clinical response in 19 patients with gynecological infections was excellent in 4, good in 15, the efficacy rate being 100%.
3) No side effects or abnormal laboratory findings were observed.
This drug showed excellent efficacy and high safety in the treatment of gynecological infections.

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The pharmacokinetic and Clinical studies of biapenem (BIPM), a new 4-methyl carbapenem antibiotic possessing a stability for human renal dehydropeptidase-I were carried out.
1. The concentrations of BIPM in serum, internal genital organs and retroperitoneal fluid after intravenous drip infusion of 300mg dose were examined. The peripheral serum level was 13.6μg/ml at 0 min, decreased to 0.4μg/ml at 6 hr after administration. The genital tissue's concentrations were 2.2-3.9μg/g at 75 min, and detected 0.2μg/g in all tissues without Endmetrium until 250 min after administration. The concentrations in retroperitoneal fluid were 7.8μg/ml at 30 min (peak level), decreased to 0.7μg/ml at 6 hr after administration.
2. In a clinical trial, BIPM was administered to 6 patients. Clinical response was excellent in 3 cases and good in 3 cases. Principal causative organisms were Staphylococcus. aureus, Staphylococcus. epidermidis and the bacteriological response was evaluated as eradicated in 2 strain. No side effects or abnormal laboratory findings due to BIPM were observed.

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Biapenem (BIPM) is a new 4 α-methyl carbapenem antibiotic with an exceptionally broad spectrum of an antibacterial activity in vitro and is stable to human renal dehydropeptidase-I (DHP-I).
Pharmacokinetic and clinical studies of BIPM, a newly carbapenem compound were performed.
The intravenously administered BIPM, a single drip infusion (60min) of 300mg, showed the fast and good penetration to the tissues (cervix uteri, portio vaginalis, myometrium, endometrium, oviduct and ovary): the peak concentration in the elbow vein and uterine artery were 6.9 and 6.3 μg/ml, respectively. Maximum concentrations in genital tissues were 1.6-4.5μg/g.
BIPM was administered to 5 patients, 2 with puerperal intrauterine infection, 1 with uterine adnexitis and 2 with pelvicperitonitis at a dose of 300mg, 2 or 3 times for 6 to 10 days.
As a result, the clinical effects of BIPM were good in all cases. Two strains Escherichia coli and Klebsiella pneumoniae, were eradicated after treatment. Neither side effects nor abnormal laboratory test values were observed. Ultimately, BIPM were very useful for gynecologic infections.

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The utility of biapenem (BIPM), a new carbapenem antimicrobial agent, was examined in the field of orthopedics. The following results were obtained.
1. Clinical evaluation
A total of 44 patients with orthopedics infections were treated with BIPM. The clinical efficacy against osteomyelitis was excellent in 5 cases, good in 18 and poor in 7, with an efficacy rate of 76.7%, and that against pyogenic arthritis was excellent in 2, good in 3 and poor in 5, with an efficacy rate of 50.0%. Bacteriologically, the causative organisms were eradicated in 8 out of 13 cases (61.5%). As to side effects, headache was observed in 1 case. Abnormal laboratory findings, which were mostly elevation of GOT and GPT, were observed in 5 cases.
2. Bone and joint tissue levels of BIPM
Penetration of the BIPM into bone and joint tissue was found to be good, with a bone tissue/serum rate of 2.5-9.3%. The levels in synovia were 1.3-10.2 μg/ml, and those in capsula articularis were 1.7-4.1μg/g.

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The minimum inhibitory concentrations (MICs)(10⁶CFU/ml) of biapenem (BIPM), imipenem (IPM) and flomoxef (FMOX) were determined against 113 strains of Staphylococcus aureus isolated from skin infections. BIPM and IPM showed a peak of MIC distribution at≤0.06 μg/ml and FMOX at 1μg/ml.
Plasma and skin levels of BIPM after drip infusion (300mg, 30min) were determined in pa-tients (n=5). Skin concentration/Plasma concentration ratio was 0.25 ± 0.04.
BIPM was used clinically in 19 cases at a dose of 150-600mg twice daily.
Results were excellent in 9 patients and good in 10. No severe adverse reactions were observed.

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Basic and clinical studies on biapenem (BIPM), a new carbapenem, in otorhinolaryngological infections were performed with the following results.
I. Plasma and tissue (middle ear mucosa, maxillary sinus mucosa and nasal polyp) concentration of BIPM were determined. The concentration of BIPM were 1.00-2.66μg/g in maxillary sinus mucosa (60-80min), 1.57μ/g in middle ear mucosa (60min) and 2.45μ/g in nasal polyp (60min) after 300mg i.v.
2. Clinical study results
BIPM (300-1200mg per day) was given to 26 patients, 3 cases of chronic otitis media, 4 cases of choronic otitis media acute exacerbation, 1 case of acute sinusitis, 3 cases of chronic sinusitis, 2 cases of chronic sinusitis acute exacerbation, 5 cases of acute tonsillitis, 1 case of peritonsillitis, 4 cases of peritonsillar abscess and others with acute nasopharyngitis, acute infections atheroma, acute gingival abscess, for 2-14days. Clinical response was excellent in 16, good in 6, fair in 1 and poor in I of the 24 patients available for evaluation. The effecacy rate was 91.7%, All of clinical isolates were eradicated. No side effects were observed. One patient developed temporary eosinophilia which was possibly related to the drug.
From above results, we consider BIPM to be one of the most useful antibiotics for otorhinolaryngological infections.

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1. Pharmacokinetic and clinical studies were caned out with biapenem (BIPM) in otorhinolaryngological infections. The results were as follows.
2. The concentration in mucous membrane of auris media was 0.44-0.99μg/g, in mucous membrane of maxillary sinus was 0.2-2.0μg/g, in tonsil was 0.4-1.4μg/g.
3. The drug was administered to 67 patients. Overall clinical efficacy was high, 82.8%. In two cases, side effects were observed, and in other two cases, abnormal findings in labolatory were observed.

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Pharmacokinetic, clinical and bacteriological studies were carried out with biapenem (BIPM) on infectious diseases of the otolaryngological field.
The results were as follows:
The levels of BIPM in the maxillary sinus mucosa and in serum were 0.68μg/g, 1.68μg/g and 4.14μg/ml, 3.98μg/ml, respectively, at 55, 105min following the intravenous drip infusion of the drug at a dose of 300mg.
In the clinical study, 18 patients with otolaryngological infection were given BIPM at a dose of 300mg, 2 times a day by intravenous drip infusion. The overall efficacy rate was 70.6% in 17 cases, excellent in 6, good in 6, fair in 4 and poor in 1 cases. The bacteriological eradication rate was 88.9% in 16 of 18 strains isolated from the subjects. Adverse effects were observed in 3 cases. One was eruption and another was a slight elevation in GOT and GPT in one case, and a slight elevation in platelet.
From the above results, BIPM was considered to be a useful antibiotic in the treatment of otolaryngologicalinfectious diseases.

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We performed basic and clinical studies of biapenem (BIPM), a new parenteral carbapenem antibiotic, in ophthalmology.
BIPM showed a broad antibacterial spectrum against gram-positive, gram-negative and anaerobic bacteria.
The MIC₈₀s against clinical isolates of Staphylococcus aureus (20 strains) and Pseudomonas aeruginosa (20 strains) were 0.19μg/ml and 1.56μg/ml, respectively.
Penetration of BIPM into aqueous humor of the anterior chamber reached a peak of 12.2μg/ml at 30 min after intravenous administration of 50mg/kg to mature white rabbits, and thereafter the level decreased to 0.1μg/ml at 6 hours after administration.
The rate of aqueous humor to blood concentration was 15.1%. Ocular tissue concentrations were 7.7-26.3μg/ml in extraocular tissues and 0.5-2.2μg/g or ml in intraocular tissues at 30min after administration.
Penetration of BIPM into human aqueous humor of the anterior chamber reached 0.24-2.60μg/ml at 35-190min after intravenous drip infusion of 300mg to human volunteers. The penetration into human tear reached a peak of 2.25μg/ml at 15min after initiation of BIPM (300mg) drip infusion for 30min, and the level decreased to 0.31μg/ml 4 hours after administration. The rate of tear to blood concentration was 14.2%.
We treated 21 patients (dacryocystitis 1, lid abscess 1, corneral ulcer 10, endophthalmitis 5 and orbital infection 4) with BIPM drip infusion at a dose of 150, 300, 450 or 600 mg one to three times a day. Three unevaluable cases were deducted, hence 18 cases were evaluated for analysis of the clinical effect. Clinical responses were excellent in 4, good in 11 and fair in 3, therefore the efficacy rate was 83.3%.
The following organisms were isolated from the patients: gram - positive bacteria from 8, gramnegative bacteria from 2 and anaerobic bacteria from 4. The eradication rate was 92.3%.
No side effects were observed in any of the 21 patients. In laboratory data, decrease of white blood cell and increase of BUN were observed in one patient.

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We performed laboratory and clinical studies on biapenem (BIPM), a new carbapenem antibiotic in oral surgery.
In rabbits, the ratio of maximum concentration (Cmax) of BIPM in tissues to Cmax in plasma was 13.1% in tongue, 19.0% in gingiva, 3.3% in parotid gland, 1.9% in submandibular gland and 5.6% in mandibular bone after 10mg/kg d.i.v. over 60min.
In patients surgically treated in oral cavity, the ratio of Cmax of BIPM in tissues to Cmax in plasma was 1.6-12.6% in gingiva, 7.9% in parotid gland, 8.1% in submandibular gland, 9.0% in mandibular bone and 35.7% in wound exudate after 300mg d.i.v. over 30min or 60min.
BIPM was administered to 39 patients with oral surgery infection and the clinical efficacy was studied.
The patients consisted of 16 with osteitis of jaw, 23 of cellulitis of mouth floor. 150 300mg of BIPM was dissolved in 100ml of saline, and administered to the patients via i.v. drip infusion twice daily for 3-12days.
Clinical efficacy was excellent in 7, good in 29 and poor in 3. The efficacy rate was 92.3%. For the bacteriological effect, “eradicated” cases were 18, “replaced” and “unknown” cases were 1 respectively. The eradication rate was 90.0%.
Rash was observed in 1. Slight elevation of transaminase was observed in 5, and slight hepatic dysfunction and eosinophilia was observed in 1.

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We investigated the in vitro antibacterial activity of biapenem (BIPM), imipenem (IPM), penicillin G (PCG) and ampicillin (ABPC) with the presence of human serum albumin.
As the test organism, Staphylococcus aureus ATCC 25923, Eschrichia coil ATCC 25922, three clinical isolates of Streptococcus anginosus and three clinical isolates of Streptococcus sanguis were used.
The MICs and MBCs of several agents against these strains were measured in Mueller-Hinton broth with or without 5g/dl of human serum albumin by the broth dilution method.
The presence of human serum albumin in the medium influenced the antibacterial activity of PCG, whereas not those of biapenem, IPM and ABPC.

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The in vitro activity of biapenem (BIPM), a newly developed carbapenem antibiotic by Lederle (Japan) Ltd., was studied by determining minimum inhibitory concentration (MIC) using the agar twofold dilution method. The range of MIC of BIPM against Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae and Pseudomonas aeruginosa isolated from blood of patients between 1989 and 1990 admitted to Keio University Hospital were 0.02 to 1.56μg/ml, 0.1 to 1.56μg/ml, 0.1 to 0.39μg/ml and 0.78 to 12μg/ml, respectively. BIPM was more active than not only imipenem but also panipenem against all of these organisms.

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We studied biapenem (BIPM), a new carbapenem antibiotic, in terms of postoperative penetration into peritoneal exudate.
We measured daily concentration of BIPM in peritoneal exudate after radical gastrectomy for gastric cancer or gastric leiomyosarcoma for 3 days. BIPM was administered by intravenous drip infusion at a dose of 0.3g twice a day. The average concentrations in peritoneal exudate in 3 patients were 0.68, 0.33 and 0.11μg/ml on days 1, 2 and 3, respectively.
No side effects and no abnormal laboratory findings were observed.

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We studied the efficacy, usefulness, and safety of biapenem (BIPM), a new injectable carbapenem antibiotic for the treatment of respiratory infections.
One patient with pneumoniae was given 300mg of BIPM by i.v. drip infusion over 60 minutes. The BIPM concentration in blood was 9.08μg/ml immediately after the drip infusion, and 1.90μg/ml after 3 hours. The maximum concentration in sputum was 0.72μg/ml which was observed at 30 minutes after the infusion, and the transfer of BIPM into the sputum was 12.6%, these findings suggesting a rapid transfer into the sputum.
BIPM in a dose of 150mg or 300mg was administered two or three times per day to a total of 18 patients including 10 with pneumonia, one with lung abscess, and one with acute exacerbation of chronic bronchitis. The remaining six patients were unevaluable or had diseases other than subjected. The patients were treated for 2 to 16 days, and the total amount of BIPM administered ranged from 1.8 to 9.0g.
Clinical response was excellent in five patients, good in five, fair in one and poor in one. The efficacy rate was 83.3%.
No side effects were observed. Abnormal laboratory findings attributable to this drug were elevations of GOT, GPT and γ-GPT in two patients and elevations of Alp and LAP in one patient.
From the results, we can conclude that BIPM is effective and useful for the treatment of respiratory infections.

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We evaluated the clinical efficacy and safety of biapenem (BIPM), a new carbapenem, at a dose of 300mg twice daily for 5-20 days in 16 patients with respiratory tract infections, including 13 cases of bacterial pneumonia, one of chronic bronchitis, one of mycoplasma pneumonia and one of interstitial pneumonia. The clinical efficacy in the 14 evaluable cases was excellent in 4 patients, good in 9, poor in one. The efficacy rate was 92.9%.
A side effect was observed in one patient, who showed abdominal pain and diarrhea. Elevation of eosinophils was found in one case.

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A clinical study on biapenem (BIPM), a new carbapenemn antibiotic for injection, in the treatment of respiratory infections were performed.
Eight patients with acute pneumonia and one patient with bronchiectasis were treated with BIPM with their own consent. BIPM was given intravenously in a daily dose of 300-600mg by drip infusion for 14-15days, with the total administrated dose ranging from 8.4 to 18grams.
Clinical efficacy was rated as excellent in 2, good in 7. With regard to the bacteriological effects, all of the eight strains isolated from 5 patients were eliminated by the administration of BIPM. As side effects, mild diarrhea occured in one patient on the 6th day after the treatment, however, the patient could easily tolerated to continuation of the treatment. Increase of platelet count were observed in one patient but it was transient.

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We studied the clinical efficacy and safety of biapenem (BIPM), a new carbapenem antibiotic, in pulmonary suppuration and infectious endocarditis. The clinical response was excellent in these cases. The causative organisms, Prevotella intermedia, Bactroides sp. and Peptostreptococcus sp. were isolated in pulumonary suppuration and were eradicated.
No side effect were observed, but the laboratory findings revealed GOT, GPT, ALP and LAP in pulmonary suppuration.

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Clinical investigation was performed on biapenem (BIPM), a new carbapenem. BIPM was adminstered to 2 lung cancer patients with respiratory tract infections (lung abscess and pneumonia), at a daily dose of 600mg.
The clinical response was excellent in 1 and good in 1. Neither clinical side effects nor abnormal laboratory findings were observed during or after administration of BIPM.

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A clinical evaluation of biapenem (BIPM), a new carbapenem antibiotic, was performed 13 patients (5 with pneumonia, 4 with lower respiratory tract infection, 3 with empyema and 1 with lung abscess).
The clinical responses in 13 cases were excellent in 1, good in 7 and poor in 3, an efficacy rate of 72.7%.
Side effects were noted in 3 cases (eruption, anorexia, vomiting), Abnormal laboratory finding was observed in 1 case (eosinophilia).

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Carbapenem antibiotic, biapenem (BIPM) was administered to 10 patients with respiratory infections (pneumonia in 4 cases, lung abscess in 2 cases, pyothorax in 2 cases, acute bronchitis in a case, chornic bronchitis in a case) by intravenous drip infusion for 3.5-16 days at a dose of 0.6 or 1.2g per day.
Clinical efficacy was excellent in 1, good in 6, fair in 1, poor in 2 cases, an overall clinical efficacy rate was 70%.
No serious adverse reaction was observed, though 4 patients showed abnormal laboratory findings during the treatment: eosinophilia in a case, neutropenia, lymphocytosis, elevation of GOT and GPT in a case, elevation of urinary protein in a case, and leukopenia in a case.
So, this new drug was thought as usefull for the treatment of respiratory bacterial insfections.

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The clinical response to biapenem (BIPM) was evaluated in 20 cases of respiratory tract infections.
(1) The overall efficacy rate was 95.0%.(excellent in 7, good in 12 and fair in 1)
(2) The bacteriological eradication rate was 88.2%.
(3) Side effects, eruption and fever were observed in each one case, respectively. Laboratory tests revealed eosinophilia and elevation of LDH in 1, eosinophilia in 1 and elevation of GOT and GPT in 1.
Based on the above results, we consider BIPM to be a useful drug for respiratory tract infections.

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We evaluated the clinical effect of biapenem (BIPM) in 7 cases of respiratory tract infection and 1 case of subcutanesus abscess.
The drug was given intravenous drip infusion at 150mg or 300mg twice a day. Clinical response was good in 6, fair in 1, poor in 1 case. There were no side effects and abnormal laboratory findings to the treatment with BIPM.
From these results, BIPM was thought to be useful for the treatment of mild to severe respiratory infections.

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A new antibiotic, biapenem (BIPM), was administered for 4.5-14 days at daily doses of 600mg to 8 patients, including 4 cases of pneumonia, 2 cases of acute exacerbation of chronic bronchitis, lease of bronchial asthma with infection and 1 case of mycoplasmal pneumonia.
The clinical effects were good in 5 cases, poor in 2 cases and not evaluable in 1 case. Side effects were not observed in any of these patients.

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We have studied the clinical efficacy and safety of biapenem (BIPM), a newly developed carbapenem antibiotic.
BIPM was administered to 11 patients with respiratory infections and one patient with urinary tract infections by intravenous drip infusion. The clinical efficacy was evaluated to be excellent in 2, good in 9, fair in 1, showing 91.7% of efficacy rate.
Isolated organisms were Pseudomonas aeruginosa (4), Klebsiella pneumoniae (2), Haemophilus parainfluenzae (1), Enterococcus faecalis (1), Alcaligenes xylosoxydans (1), Serratia marcescens (1).
Of the ten strains, K. pneumoniae, S. marcescens and two cases of P. aeruginosa were eradicated, and the other cases of P. aeruginosa, E. faecalis and A. xylosoxydans persisted. H. parainfluenzae was replaced.
Side effects were not observed. In one patient, elevation of an amylase value in laboratory findings was observed.

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The clinical efficacy and safety of biapenem (BIPM) were evaluated in 9 patients with respiratory tract infections.
The clinical efficacy was evaluated to be good in 8 patients, poor in 1, showing an 88.9% efficacy rate. Bacteriological efficacy was determined to be eradicated in 3 strains, decreased in 1. Diarrhea occurred in one patient as a side effect. Abnormal laboratory findings (elevation of transaminase, LDH) were observed in 2 patients, however these changes posed no clinical problems.

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Biapenem (BIPM), a new carbapenem antibiotic, was administered in ten patients with respiratory ract infection at the dose 600 mg or 1200 mg daily; bacterial pneumonia in 8, mycoplasma pneumonia in 2.
Clinical efficacy were excellent in 3, good in 1, fair in 1, poor in I and unevaluable in 4.
No side effects were observed. A slight and transient elevation of serum OPT level was observed in one patient.
These results suggested that BIPM might be effective and safe in respiratory tract infections.

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We evaluated the clinical efficacy and safety of biapenem (BIPM), a new carbapenem antibiotic. BIPM was administrated to 11 respiratory tract infections. The patients received the drug, intravenously, for 6 to 15 days in dose of 0.3-0.6g/day. Clinical effects were excellent in 1, good in 8, poor in 1, unknown in 1. No side effects were noticed. But as abnormal laboratory findings, microhematuria was observed in one case.

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We evaluated the clinical effecacy and safety of biapenem (BIPM), a new injectable carbapenem antibiotic. BIPM was used to 9 patients. Clinical response was excellent in 2, good in 6, fair in 1patients.
Adverse reactions were not observed. Abnormal laboratory values were noted in 1 patient (GPT) but was not clinically significant.

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Biapenem (BIPM) is a new carbapenem with broad and potent antimicrobial activity against gram-positive and negative organisms as well as imipenem/cilastatin, BIPM was given parenterally to 1 with acute tonsillitis, 6 with pneumonia, 2 with purulent pleurisy, and 1 with abscess of buttock and septic shock. 9 of these patients responded well to the therapy. No.adverse reaction was observed in the all patients. As to abnormal laboratory findings, slightly elevated S-GPT was observed in one case.

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We evaluated the clinical efficacy and safety of biapenem (BIPM) in 18 patients with respiratory tract infection. BIPM was administered to 7 patients with pneumonia, 2 with bronchopneumonia, 1 with lung abscess, 4 with exacerbation (bronchiectasis), 2 with exacerbation (diffuse panbronchiolitis) and 2 with secondary infection. The daily dose was 0.6-1.2g and duration was 4-14 days. The following results were obtained.
1) The clinical efficacy of BIPM was excellent in 5, good in 11, fair in 1, poor in 1.
2) Of 7 strains (6 species) isolated from 7 cases before treatment, 5 strains were eradicated after treatment, but S. aureus persisted, and Haemophilus sp. was unknown.
3) No side effect were observed during treatment in 19 patients. As abnormal laboratory findings, elevation of GOT·EGPT and eosinophilia were observed in each two cases.
The above results suggest that BIPM is a valuable and safe agent for treating, respiratory tract infection.

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Biapenem (BIPM), a new carbapenem antibiotic, was administered to 20 patients with respiratory tract infections (RTI). A clinical evaluation of BIPM was carried out in 17 patients, 16 with pneumonia and 1 with chronic bronchitis.
The clinical efficacy rate was 76.5%. Six organisms were isolated out of 6 patients. The eradication rate was 100%.
No side effects were observed. Abnormal laboratory findings were observed in 2 episodes.

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We investigated the efficacy and safety of biapenem (BIPM) in 19 patients with respiratory infections: 12 with pneumonia, 2 with lung abscess, 2 with acute bronchitis, 3 with lower respiratory tract infection. Excluding 4 patients whose response was not assessable, clinical response was exellent in 2, good in 11, poor in 2, giving an efficacy rate of 86.7%. Bacteriological assesement produced the following results: one strain each of S. aureus, S. pneumoniae and two strains of A. calcoaceticus were eradicated. As for adverse reaction, diarrhea in 1 case was observed.
With regard to abnormal laboratory findings, eosinocytosis and increased LDH and increased GOT-GPT·Al-p·γ-GTP and decreased WBC were noted in one case each.

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Biapenem (BIPM) was administered by intravenous drip infusion at 300mg b. i. d. to nine patients with respiratory tract infections for 7 to 10 days. The clinical responses were good in seven and poor in one of the two cases of bronchopneumonia and poor in one case of bronchitis. Of ten strains (4 species) isolated from seven patient before treatment, eight were eradicated after treatment, but two strains of P. aeruginosa persisted.
As abnormal laboratory findings, elevation of LDH and decrease of platelet and s-K eosinophilia were observed in one patient each.
The above results suggest that BIPM is a valuable and safe agent for treating respiratory tract infection.

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Biapenem (BIPM) was administered to five patients, two with septicemia, one with infected bronchiectasis, one with pulmonary tuberculosis and one with infected cystic kidney, at a dose of 300mg twice daily for 3 to 20.5 days through intravenous drip infusion.
Clinical response was excellent in one (septicemia), good in two (septicemia and infected bronchiectasis). Pulmonary tuberculosis and infected cystic kidney with slight symptoms and signs of inflammation were excluded from the clinical evaluation.
Two strains of Escherichia coli, which were identified as causative organism in each case with septicemia, were eradicated after biapenem treatment.
Slight and transient elevation of GOT, GPT and LDH in one case, and that of GOT, GPT, ALP, γ-GTP and LAP in one case were noted. No subjective or objective adverse reaction was observed in all cases.

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The clinical efficacy and safety of biapenem (BIPM), a new injectable carbapenem antibiotic, were studied in 13 patients with moderate or severe infectious diseases (7 patients with pneumonia, one patient with sepsis, acute tonsillitis, chronic bronchitis, bronchiectasis, and acute pyelonephritis respectively). The drug was given by dripping intravenous injection of two times daily of 150, 300, and 600 mg for an average of 12.6 days.
The clinical response in 13 patients was excellent in 3, good in 9, and poor in 1. The overall efficacy rate was 92.3%(12/13). bacteriologicaly, 6 strains were isolated from 6 patients; 5 strains were eradicated and 1 persisted. Persisted strain was H. influenzae.
No adverse symptoms were detected. A mild elevation of serum GPT was 1 patient, GOT and GPT in 1, and BUN in 1.

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We studied the clinical efficacy and safety of biapenem (BIPM) in 5 patients with respiratory infection (pneumonia 3, and exacerbated bronchiectasis 2), who were treated with BIPM at 300mg twice a day for 7-11days.
Overall clinical effect was excellent in 2, good in 2, and poor in 1. No clinical side effect was observed. A slight increase in peripheral eosinophil in one case was the only abnormal laboratory finding.

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Clinical evaluation of biapenem (BIPM), a new carbapenem antibiotic, was carried out in 16 patients with pneumonia. BIPM was administered 0.3g twice daily in 16 patients by intravenous drip infusion. Clinical efficacy was excellent in 9 cases, good in 4 cases, fair in 1 case, poor in 1 case and unevaluable in 1 case, and the overall clinical efficacy rate was 86.7%. No side effect was observed, but as for abnormal laboratory findings, white blood cell in 1 case decreased transiently.

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Biapenem (BIPM) was administered to bacterial pneumonia in 9 cases, acute bronchitis in 2 cases, epiglottic abscess in 1 case, pyelonephritis in 1 case and hepatic abscess in 1 case. The drugs were given intravenously for 5-15 days at a dose of 150-600mg, twice per day.
Clinical efficacy was excellent in 5 cases, good in 6 cases, fair in 1 case and excluded in 2 cases. Causative organisms were Haemophilus influenzae (1 case), Escherichia coli (1 case), Streptococcus pneumoniae (1 case), and all them were eradicated. No adverse reaction was observed. The elevated γ-GTP was seen in a patient as to abnormal laboratory finding.

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Biapenem (BIPM), new carbapenem antibiotic, was administered to 5 patients with bacterial pneumonia. The clinical efficacy was excellent in 1 case, good in 3 cases and unknown in 1 case. Causative organisms were detected in 2 strains of 2 species (Pseudomonas aeruginosa, Streptococcus pneumoniae), were eradicated.
No adverse reaction was observed, though two patients showed abnormal laboratory findings during the treatment: elevation of OPT, γ-GTP, LAP in I case, elevation of GOT, OPT, Al-P, γ-GTP in 1 case.
These results suggest that BIPM is useful in the treatment of bacterial pneumonia.

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