Some 23 patients suffering from severe gastrointestinal infections were treated with cefoxitin (CFX) at the Bokuto Metropolitan Hospital, surgical ward, from September to November, 1982.Clinical examinations were conducted and the findings bacteriologically evaluated.
The following clinical results were obtained:
1. Of 23 patients, 11 were treated for diffuse peritonitis, 5 for localized peritonitis, and 7 for cholangitis. Following treatment, 5 were judged “excellent”, 12 “good”, 4 “fair”, and 2 “poor”.The clinical efficacy rate was 74%.
2. Antibiotic disc susceptibility testings for ampicillin, cephalexin, gentamicin, and CFX were conducted. Gram-negative rods, such as E.coli, Klebsiella sp., Proteus sp., and especially, anaerobic B.fragilis, indicated susceptibility to CFX. B.fragilis was resistant to the remaining 3 antibiotics.
3. Transient elevations in S-GOT and S-GPT levels were observed in 2 patients.However, this was not thought to be caused by CFX.No other irregularities were found.
4. CFX is considered to be a drug of first choice for the treatment of severe gastrointestinal infections. However, for infections due to mixed Pseudomonas aeruginosa and other bacteria, concomitant treatment with CFX and an aminoglycoside is recommended.

View full abstract

A total of 20 patients involved in gastrointestinal surgery was treated with cefoxitin (CFX).Ten patients were treated for postoperative infections and the other 10 patients were given CFX to prevent postoperative infections.The following results were obtained:
1. In 10 patients treated for postoperative infections, 5 responses were judged “excellent”, 1 “good”, 2 “fair”, 1 “poor” and 1 “unknown”.In 25 strains of bacteria isolated from these patients, 21 were eradicated, 3 were replaced and 1 was unknown.
2. In 10 patients given CFX for prevention of postoperative infections, 9 were judged “excellent” and the remaining 1 “good”.
3. No side effects were observed in any of the patients treated with CFX.

View full abstract

Cefroxadine (CXD) is an orally administered synthesized cephalosporin antibiotic developed by Ciba-Geigy Limited (Switzerland) in 1972.We have studied the clinical effectiveness of this drug in a total of 45 cases of various types of infections in the dentistry and the oral surgery.The studies resulted in showing 18 markedly effective cases, 19 effective cases, 5 slightly effective cases, 1 ineffective case, and 2 unknown cases showing an effective rate of 82.2%.Side effects manifested in 2 cases, of which 1 case was considered to be attributable to CXD, and the occurrence frequency of side effects was as low as 2.2%.In bacteriological test, there were many cases of mixed infections by Gram-positive and Gram-negative bacteria, and these infections were those which are observed in high frequency in dentistry and oral surgery infections.As a result of an overall evaluation of CXD clinical effects, the drug considered to be an antibiotic which is highly useful in dentistry and oral surgery.

View full abstract

We performed a survey of clinical experience of cefotiam (CTM: Pansporin ®) as postmarketing surveillance (PMS), and evaluated the efficacy and safety of CTM in 10,499 cases of data which were collected during the first 2 years after approval. The following results were obtained.
1. The efficacy rate of CTM in the treatment of various infections was 83.2%, which was equal or superior to the clinical results obtained before approval.
2. A total of 472 adverse drug reactions was reported by 10,499 patients (4.50%).
The commonest adverse drug reactions was liver function abnormality (230 cases), followed by dermal symptoms (103 cases), gastrointestinal symptoms (53 cases) and renal function abnormality (20 cases) in the order mentioned.
All of these adverse drug reactions had already been known for cephem antibiotics, and no remarkable adverse drug reactions specific to CTM was found.
The above PMS results indicate the same efficacy of CTM that obtained from premarketing studies.
As regards safety, there was no remarkable unexpected adverse drug reaction and their profile was also the same as that found in premarketing studies. Thus, the utility of CTM was confirmed.

View full abstract

To evaluate the antibacterial potency of cefotiam (CTM) clinical and laboratory studies were carried out and the results were as follows.
1. Clinical evaluation and adverse reaction
CTM was given to total of 23 patients, 10 with bronchopneumonia, 10 with bronchitis and one each with cystitis, enteritis and suspected sepsis.Overall efficacy rate was 78.3% (18/23)(excellent 9, good 9, fair 3, poor 2).Only 1 case showed a side effect of slightly elevated GOT and GPT.
2. Antibacterial activities
MIC of CTM against isolates from sputum was investigated on those patients mentioned above and was compared with MIC of CEZ and CMZ.CTM showed superior antibacterial activity against almost all strains. Especially on Haemophilus and Klebsiella antibacterial activity of CTM was impressive.
3. Organisms in sputum
Four out of 8 causative bacteria disappeared and 1 out of 8 decreased after administration of CTM.
Thus CTM is considered to be the useful drug for the treatment of respiratory infection.

View full abstract

The intent of the study was to investigate the transfer of CMZ to the retroperitoneal space exudate after hysterectomy (11 cases of simple abdominal hysterectomy and 6 cases of radical hysterectomy).
Concentration of CMZ in the lymphnode was also measured in 2 cases. The results were as follows.
1. Concentration in the retroperitoneal space exudate of CMZ after administration (intravenous drip infusion 1 or 2g/hour) reached its peak 2 hours after administration (approximately 1 hour later than its peak in the blood).The peak level in the exudate was 1/3 to 2/3 of the peak level in the blood.After 2 hours, the concentration of CMZ in the exudate decreased gradually.
2. The concentration of CMZ in the retroperitoneal space exudate in cases of simple abdominal hysterectomy was higher than in those of radical hysterectomy.
3. After 1 to 3 days of radical hysterectomy, the transfer of CMZ into the exudate was as good as the transfer of that in the period immediately after operation.
4. CMZ concentration in the lymphnode in the cases of radical hysterectomy reached 9 to 13μg/mg approximately 1 hour after the start of CMZ administration (d.i.2g in 1 hour).
Research results suggest that lymph circulation, in addition to blood stream, plays an important role in the transfer of antibiotics toward the pelvic dead space.

View full abstract

Susceptibilities of 198 strains of 31 bacterial species to cefmetazole (CMZ) were determined by the 2-fold agar dilution method in parallel with the diameter of inhibition zone by the single-disc method, under the experimental condition established by KANZAZWA.
The experiments demonstrated significant correlation between MIC by the dilution method and diameter of inhibition zone in each of conventional assay of the overnight (about 16 hours) incubation, delayed assay (about 24 hours incubation), and rapid assay (about 3 4 or 5-6 hours incubation), thus confirming applicability of the single-disc assay for CMZ.
Analysis of the data obtained by using CMZ disc containing 30μ revealed the primary regression equation to be: D (diameter, mm) =27.9-11.2 log MIC (μg/ml) in conventional assay, D=34.5-13.8 log MIC in delayed assay D=18.1-6.0 log MIC (μg/ml) in 3-4 hours rapid assay and D=22.9-8.5 log MIC (μg/ml) in 5-6 hours rapid assay, respectively.
The range of variations in MICs estimated from the diameter of inhibition zone by the disc test was then calculated in comparison with that in MIC determined by the 2-fold agar dilution assays, as reference for the experimental errors which may be involved in the estimation of MIC of CMZ by the single-disc assay.

View full abstract

Fourteen cases with complicated urinary tract infection were treated with 2g of cefotaxime for 5 days; in total doses of 10g.
Excellent or good results were obtained in 11 cases (78.6%) and no adverse reaction was observed.A curious finding was the development of eosinophilia in some patients.The causative mechanisms and clinical meanings of the phenomenon have not been clarified.

View full abstract

Acute inflammation becomes severe and the risk of perforation of the gallbladder increases every time gall stone colic occurs in patients with cholelithiasis.
In the surgical treatment for these patients, interval operation is said to be preferable to emergency operation in the acute stage.
Furthermore, the flow of bile into gallbladder is blocked by incarceration of stones at the neck of the gallbladder and other causes in the acute stage.
In this case, therefore, how an antibacterial agent in blood moves to the gallbladder wall is important in suppressing infections of the gallbladder wall.
We divided 15 patients with cholelithiasis into cases positive for cholecystogram and negative cases and made a comparative study of piperacillin (PIPC) levels after intravenous drip infusion.
PIPC level in bile in the gallbladder was very low in the cases negative for cholecystogram compared with the positive cases.
However, no definite difference in levels of the gallbladder tissue was observed between positive for cholecystogram and negative cases.
Accordingly, it is concluded that administration of PIPC is not ineffective even in severe cholecystitis in which transference of an antibacterial agent from bile can hardly be expected.

View full abstract

There are few clinical reports about concentration of latamoxef (LMOX) in lung tissues. At present, clinically, we report a concentration of LMOX in serum and lung tissues on 21 patients of chest disease and a study of the administration schedule of LMOX for prophylaxis of postoperative infections on 31 operated patients with chest disease. Our results are the followings:
1. The peak concentration of LMOX in serum is 77.4μg/ml at 1hour after starting drip infusion of LMOX 1g.
2. The concentration of LMOX in lung tissues is from 25% to 50% of serum level.
3. LMOX is more useful to prophylaxis of postoperative infections after thoracotomy than cephalothin, especially in case of administration of LMOX just before operation.
4. No side effects of LMOX are noted in our cases.
5. LMOX has wide antibacterial activity against various clinical isolates and is useful to treatment of postoperative infections.

View full abstract

After the intravenous administration of 1.0g of latamoxef (LMOX), the concentration of LMOX were determined in normal intestinal tissue and serumn of 17 patients underwent surgery for intestinal problems, and the mesults obtained were as follows.
1. At 60-150 minutes after administration, the levels of LMOX were 37.5-26.3μg/ml in serum and 14.8-10.5μg/g in normal intestinal tissues.This values were enough to inhibit the growth of Gram-negative bacteria caused for some postoperative wound infections.
2. For intmavenous administration of 1.0g of LMOX just before operation, no wound infection was observed in 13 patients with large intestinal cancer and 4 patients with benign intestinal disease.

View full abstract

Subsequent to studies of clinical effects of spectinomycin (SPCM) and ampicillin (ABPC) given in combination on acute gonorrhea in female patients, sensitivity of N.gonorrhoeae to each of these antibiotics was determined. Furthermore, cervical discharge of female patients was searched for other organisms.
Combined antimicrobial action of SPCM and ABPC were also examined.
1. Aerobic and anaerobic organisms were obtained from cervical discharge of 20 cases of acute gonorrhea. The predominant aerobe (45%) was S.agalactiae, while the predominant anaerobes (combined 70%) were Peptococcus spp.and Peptostreptococcus spp.The results indicate that mixed infections of N.gonorrhoeae and aerobic and anaerobic Gram-positive cocci should be considered in acute gonorrhea in female.
2. MICs of SPCM for 20 strains of N.gonorrhoeae were determined. SPCM showed MICs of 3.13-12.5μg/ml against 10⁸ and 10⁶ CFU/ml. There were no strains with MICs of 25μg/ml. ABPC had MICs of 0.2μg/ml against 10⁸ CFU /ml and 0.1μg/ml against 10⁶ CFU/ml. Five strains (25%), MICs of which were≥6.25μg/ml against 10⁸ CFU/ml and≥1.56μg/ml against 10⁸ CFU/ml, were all beta-lactamase producing.
3. In vitro combined antimicrobial action of SPCM and ABPC is additive.

View full abstract

Susceptibility of 162 sputum isolates to oral antibiotics was measured by an agar dilution method. The sputum isolates included S.pneumoniae 25 strains, S.aureus 30 strains, H.infhtenzae 37 strains, K.pneumoniae 51 strains and E.coli 19 strains.Minimal inhibitory concentration (MIC) values of cefaclor (CCL), cephalexin (CEX), ampicillin (ABPC) and minocycline (MINO) were measured for each strains.
Eighty percent of S.pneumoniae strains were inhibited at 0.024 to 0.05 μg/ml of ABPC, 0.39 to 0.78μg/ml of CCL, and 1.56 to 3.13μg/ml of CEX and MINO. ABPC, CCL and CEX were considered to be effective clinically when they were used with the usual dosage.However, about 30% of strains were resistant to the usual dosage of orally administrated MINO.
Eighty percent of S.aureus strains were inhibited at 0.20 to 0.39μ of MINO and 3.13 to 6.25μg/ml of the other 3 drugs.MINO is the most effective with the usual dosage.Twenty to 40% of strains showed resistance to CCL, CEX and ABPC.
Eighty percent of H. influenzae strains were inhibited at 0.39μg/ml of ABPC, 0.78 to 1.56 μg/ml of MINO, 3.13μg/ml of CCL and 12.5 to 25μg/ml of CEX.ABPC should be selected as the first choice antibiotic.However, there were 2 ABPC-resistant strains that were highly susceptible to CCL.
Eighty percent of K.pneumoniae strains were inhibited at 0.39 to 0.78μg/ml of CCL, 3.13 to 6.25μg/ml of MINO and CEX, and 12.5 to 25μg/ml of ABPC. CCL seemed to be the only effective oral antibiotic for K.pneumoniae infection.
Eighty percent of E.coli strains were inhibited at 1.56 to 3.13μg/ml of MINO, 12.5 to 25 μg/ml of CCL and CEX, and more than 100μg/ml of ABPC. These concentrations were far above the pulmonary tissue concentration obtained with commonly used dosage.Only 60 to 70% of strains were susceptible to the usual dosage of CCL, CEX and MINO.About 50% of strains were highly resistant to ABPC.
These data indicate that the best selection for the first choice antibiotic in pulmonary infection depends upon the following factors.
1. The in vitro antibacterial activity of each drug against each bacteria
2. The level of pulmonary tissue concentration obtained with each drug when given at the usual dosage
3. The incidence of resistant strains to each drug

View full abstract

Fosfomycin sodium was administered to 36 cases with obstetrical and gynecological infection.
Efficacy was excellent in 6 cases, good in 27 cases and poor in 3 cases and so effective ratio obtained was 91.7% in all.
No side effects were observed in all patients except transient increase of serum transaminase in 2 cases.

View full abstract

Fosfomycin sodium (FOM-Na) was administered to 18 patients with various obstetrical and gynecological infections, at daily dose of 4g.
Out of 18 patients treated with FOM-Na, 16 patients showed excellent or good response to FOM-Na and effective rate was 88.9%.No side effects were observed.
It is recognized that FOM-Na is an excellent drug for the treatment of obstetrical and gynecological infections.

View full abstract

Studies on absorption and excretion of cephapirin (CEPR) are described.CEPR was administered by intravenous drip infusion to 4 healthy volunteers weighing 53kg to 61kg, and the serum levels were measured.
Pharmacokinetic parameters were calculated by one-compartment model and two-compartment model. Each model was comparatively applied to every founds.
Most appropriate administration rate of intravenous drip infusion was discussed due to calculated serum levels, therapeutic AUC and effective time.

View full abstract

1. Cefpiramide (CPM, SM-1652) had broad-spectrum antibacterial activities against most of clinically isolated organisms to which are paid attention as pathogenic organism in the field of pediatrics.
2. Antibacterial activities of CPM against Staphylococcus aureus, Streptococcus pyogenes, Haemophilus influenzae, Bordetella pertussis and Proteus mirabilis were almost the same as those of cefoperazone (CPZ). Antibacterial activities of CPM against Escherichia coli and Klebsiella pneumoniae were somewhat weaker than those of CPZ, but antibacterial activity of CPM against Pseudomonas aeruginosa was rather stronger than that of CPZ and almost the same as that of cefsulodin.
3. Antibacterial activity of CPM has a tendency to decrease in β-lactamase (PCase type) producing S.aureus, E.coli, K.pneumoniae, H. influenzae, etc. It is suggestive that the determination of not only the antibacterial activity of CPM against pathogenic organisms but also the β-lactamase produsing activity of them is important on the occasion of clinical use of CPM.

View full abstract

Thirty-six febrile patients were administered cefpiramide (CPM) of 20-75mg/kg/day for 3-11days, and the clinical and side effects were evaluated.Among children with bacterial infections, including pneumonia, urinary tract infection, sepsis, pharyngitis and bronchitis, the results were excellent in 9, good in 13, and fair in 3 patients.Out of 36 patients, adverse reactions were observed in 9 cases, i.e.vascular pain at one shot intravenous injection in 4, diarrhea in 2, eosinophilia in 2, and diarrhea and eosinophilia in 1 case.
One shot intravenous administration of CPM of 10mg/kg to 4 patients yielded mean serum level of 100μg/ml at 15 minutes and mean serum half-life of 2.5 hours, and administration of 20mg/kg to 3 patients yielded mean serum level of 200μg/ml at 15 minutes and mean serum half-life of 3.5 hours.The half-life in 1 patient with slight liver lesion was 5.36 hours.The rates of urinary recovery within 8-12 hours were 7.2 to 28.0% in 5 patients, 45.1% in a patient with nephrotic syndrome, and 50.9% in a patient with slight liver lesion.

View full abstract

1. Clinical effects of cefpiramide (CPM) on 10 respiratory tract infections were excellent in 9 and poor in 1, and those on 3 urinary tract infections were excellent in 3.
Although CPM is considered to be excreted mainly into bile, it was suggested that the excretion rate of CPM at doses of 10-20mg/kg into urine is good enough.
2. Antibacterial activity of CPM was considered to be almost the same as that of cefmetazole and cefoperazone.
3. As to side effects, weak diarrhea was observed in 2 cases.
This should be considered when CPM is given to children because of its main excretion route to bile duct.

View full abstract

Twenty-one pediatric patients with moderate or severe infections were treated with cefpiramide (CPM). The drug was given intravenously in a dose of 10-52.3mg per kg at 8-42 hourly interval. All 7 patients with urinary tract infection, 4 with bacterial enteritis and 4 out of 7 patients with lower respiratory tract infections responded satisfactory, but 2 patients with either Serratia marcescens septicemia or H. influenzae meningitis not responded to treatment.Over all response rate was 71.4 percent.There was no change in test of liver and renal function.
CPM appears to be effective and well-tolerated antibiotics for the treatment of pediatric patients with various infections.

View full abstract

Cefpiramide (CPM) is a newly developed cephalosporin.Clinical studies on this drug were carried out and the results were as follows;
Forty-three patients (purulent lymphadenitis 2, cellulitis 2, purulent otitis media 1, purulent tonsillitis 3, acute bronchitis 2, pneumonia 22, bronchiectasis 1, urinary tract infection 10) were treated with CPM, in doses of 20-82mg/kg divided 2-4times per day for 3-11 days intravenously.
The overall efficacy rate was 83.7%.
As to adverse reaction, 4 cases, which includes 3 cases of diarrhea and 1 case of exanthema, were observed. Abnormal laboratory data noted were liver dysfunction in 3 cases (6.8%), and eosinophilia in 2 cases (4.5%).

View full abstract

Fundamental and clinical studies of cefpiramide (CPM), a newly developed cephem antibiotic with a broad spectrum, were performed and the following results were obtained.
1. The serum levels of CPM after the intravenous injection or the drip infusion of CPM at dose of 10.0-46.7mg/kg reached the peak of 75.8-274.0μg/ml at 30-60 minutes after infusion and were 3.9-55.1μg/ml at 8hours after the infusion. Half-life of CPM in the blood was between 2.4 and 7.0 hours.
The excretion rates of CPM into urine up to 24 hours after the infusion were 5.7-20.4%.
2. Twenty-five patients with acute respiratory tract infection (RTI, 15 cases), urinary tract infection (UTI, 8 cases), cellulitis (1 case) and salmonellosis (1 case) were treated with CPM. The treatment by intravenous injection or drip infusion of 22-55mg/kg/day (40-50mg/kg/day) for mean 6 days resulted in 100% of good response in 15 cases of RTI and in 88% of good response in 8 cases of UTI.
3. S. aureus, H. influenzae, E.coli, Proteus, Klebsiella and Salmonella group B were isolated from the culture of sputum or urine in the patients, and they were all eradicated by the treatment with CPM.
4. No side effects were observed except eosinophilia in 1 case and the elevation of GOT and GPT in 1 case.

View full abstract

1. Cefpiramide (CPM) was given to 4 patients with respiratory tract infection (H.influenzae 3 cases, P.aeruginosa 1 case), 1 patient with enteritis (enteropathogenic E.coli) and 1 patient with sepsis (E cloacae). Bacteriological eradication was observed in 5 cases (83.3%), and clinical effectiveness was 66.7%.
2. Serum concentration of CPM at a dose of 15mg/kg after intravenous drip-infusion for 30minutes was 105μg/ml at the end of infusion and 67μg/ml at 1 hour.
3. Bacteriological eradication by the administration of CPM was rapidly occurred in 3 strains of H.influenzae including 1 strain of β-lactamase producing ABPC-resistant one, and 1 strain of P.aeruginosa in the sputum.
4. One patient aged 2 years and 5 months with pneumonia was cured by the treatment of CPM as an outpatient.
5. No side effects were observed except 1 case of vascular pain.
6. It was concluded that CPM is a useful drug for the treatment of bacterial infections in children.

View full abstract

Cefpiramide (CPM), a new broad-spectrum cephalosporin antibiotic with good antipseudomonas activities, was evaluated for its safety and efficacy in 20 children with bacterial infections.The diagnoses of the patients included pneumonia (10), acute bronchitis (1), streptococcal pharyngitis (1), purulent cervical lymphadenitis (1), urinary tract infections (2), acute enterocolitis (1), infections in agranulocytosis and acute leukemia (2), and acute purulent meningitis (2).Of the 20 patients, 17 were cured by the CPM therapy.The main etiologic pathogens were H.influenzae, P.aeruginosa, P.fluorescens, S.pneumoniae and E.coli.
The serum half-life of CPM was 2.4 to 4.1 hours after an intravenous bolus injection. As an adverse reaction, diarrhea was encountered in 4 cases, and 1 of them experienced severe watery diarrhea with significant fecal colonization of K.oxytoca.
The data suggest that CPM is an effective antibiotic when used in children with susceptible bacterial infections. Administrations divided in 2 to 3 dosages will be enough to maintain effective serum levels.

View full abstract

1. After the intravenous injection of cefpiramide (CPM) at a dose of 10mg/kg to 2 children, the average blood levels of CPM were 77.7μg/ml at 15 minutes, 64.6μg/ml at 30 minutes, 41.9μg/ml at 1 hour, 31.9μg/ml at 2 hours, 10.7μg/ml at 4 hours and 3.28μg/ml at 12 hours.The half-lives were 3.0 hours and 5.8 hours.
2. When CPM was given to 22 pediatric patients with mainly acute respiratory tract infection at doses of 20-<50mg/kg/day divided into 2 times by intravenous injection (12 cases) and drip-infusion (10 cases) for 2-3 days (10 cases) or 4-6 days (12 cases), the effective rate was 90.9%.
3. No side effects were observed except slight increase of eosinophil in 1 case and slight elevation of GOT in 1 case.
4. It was concluded that CPM is a useful drug for the treatment of infection in pediatric field.

View full abstract

Fundamental and clinical studies on cefpiramide (CPM), a new semisynthetic cephalosporin, weremade and the following results were obtained.
The antibacterial activities of CPM against clinical isolates were almost similar to those of conventional cephems except for Pseudomonas aeruginosa.The antibacterial activity of CPM against P.aeruginosa was excellent and superior than those of the others.
Ten or twenty mg/kg of CPM was given intravenously at one shot to 11 cases.The mean serum levels of CPM reached 231μg/ml at 15 minutes, 119μg/ml at 30 minutes, 88μg/ml at 1 hour, 65μg/ml at 2 hours and 33μg/ml at 6 hours after administration at a single dose of 10mg/kg, respectively with the half-life of 3.42 hours. In case of 20mg/kg, the mean serum levels attained 306μg/ml at 15 minutes, 245μg/ml at 30minutes, 160μg/ml at 1 hour, 118μg/ml at 2 hours and 66 μg/ml at 6 hours respectively after administration with the half-life of 5.20 hours.
CPM was given intravenously to 12 patients with various bacterial infections.
The clinical effects were excellent in 5 cases, good in 6 cases and poor in 1 case and the effective rate was 92%.
No side effect was observed in all cases.

View full abstract

Clinical studies of cefpiramide (CPM), a newly developed cephem antibiotic, were performed in 10 children with respiratory tract infection in 4 cases, acute enteritis in 2 cases and urinary tract infection in 4 cases aged from 2 months to 10 years and 4 months.
CPM was intravenously given to patients at doses of 16-58 mg/kg/day divided into 3 times for 3-22 days, Clinical effects were excellent in 6, good in 3 and fair in 1.
Bacteriologically, 3 strains of pathogenic organisms (Salmonella C₂ group, E.coil and S.faecalis) isolated from the patients were eradicated with the treatment of CPM.
No side effect was observed.

View full abstract

Fundamental and clinical studies on cefpiramide (CPM), a new semisynthetic cephalosporin were performed and the following results were obtained.
1. Antibacterial activity
The antibacterial activity of CPM was investigated in comparison with those of CTT, CPZ, CEZ, LMOX and CFS.Against clinical isolates of S.aureus, CPM was superior to CTT and LMOX, but almost similar to CPZ and inferior to CEZ.Against E.coil, K.pneumoniae, P.mirabilis and S.marcescens, CPM showed the activity almost similar to that of CEZ, but inferior to those of the others.On the contrary, the activity of CPM against P.aeruginosa was satisfactory and was superior to those of CTT, CPZ and LMOX, but slightly inferior to that of CFS.
2. Blood level and urinary recovery
Twenty mg/kg of CPM was given intravenously at one shot to 3 patients.The mean serum levels of CPM were 116.9 μg/ml at 30 minutes, 90.5 μg/ml at 1 hour, 71.1 μg/ml at 2 hours, 55.8 μg/ml at 4 hours, 24.9 μg/ml at 6 hours, 19.3 μg/ml at 9 hours and 12.1 μg/ml at 12 hours after administration, respectively.The mean halflife was very long and the value was 3.85 hours.
The urinary recovery rates in 2 cases were 18.31 and 21.47% respectively up to 12 hours after administration.
3. Clinical results and side effects
CPM was given intravenously to 30 diseases including 11 cases of bronchopneumonia, 3 cases of bronchopneumonia and pleurisy, 2 cases of bronchitis, 4 cases of purulent tonsillitis, 5 cases of pyelonephritis and each one case of pyothorax, parotitis, cellulitis, otitis media and salmonellosis.CPM was effective in 29 out of 30 cases, and the effective rate was 96.7%.
As side effects, 2 cases of fever and 1 case of cough were observed, but no abnormality in clinical laboratory findings was observed.

View full abstract

Fundamental and clinical trials were carried out with cefpiramide (CPM) in pediatric infections. Results were as follows.
1. CPM has a broad spectrum of activity against both Gram-positive and-negative microorganisms, including Pseudomonas.
2. Half-lives of CPM were more prolonged than any others that have ever been reported on cephalosporin derivatives.The mean half-lives in the blood after infection were 4.76 hours and 4.14 hours, when the doses were 10mg/kg and 20mg/kg, respectively.
3. The average recovery rates in the urine between 0 and 8 hours were 17.1% and 24.7%, when the intravenous doses were 10mg/kg and 20mg/kg, respectively.
4. Thirty-two pediatric patients received CPM in doses ranging from 31.9 to 88.2mg/kg divided mainly 2 times a day.They were respiratory tract infection in 23, urinary tract infection in 8, and SSSS in 1.The rate of satisfactory clinical response was 90.6%.
5. Clinical side effect observed were mild diarrhea in 7 cases.Slight elevation of GOT and GPT were observed in 3 cases.All were considered to be minor.

View full abstract

Fundamental and clinical studies of cefpiramide (CPM), a new cephem antibiotic, were carried out in the field of pediatrics.
1. 80% MICs of CPM against S.aureus, S.pyogenes, H.influenzae, E.coli, K.pneumoniae and P.aeruginosa were 1.56, 0.05, 0.39, 6.25, 0.78 and 25μg/ml, respectively.
2. Serum concentration of CPM after intravenous injection at a dose of 20mg/kg to 3 children was 103.7±9.1μg/ml at 15 minutes and 13.4±5.0μg/ml at 8 hours, with half-life of 3.11±0.83 hours.
The excretion rate of CPM into urine was 16.40±7.31% within 8 hours.
3. The transfer of CPM to cerebrospinal fluid was 0.1-0.2μg/ml at 1 hour after intravenous injection at a dose of 20mg/kg to patients with Aseptic meningitis, and 0.4-4.0μg/ml at 1 hour-3 hours 15 minutes after intravenous injection at a dose of 50mg/kg to patients with purulent meningitis.
4. Clinical effects of CPM on 37 patients with various infections were excellent in 28 cases, good in 6 cases, fair in 2 cases and poor in 1 case.The effective rate (excellent and good) was 91.9%.
Bacteriologically, the eradication rate in 23 isolated organisms was 95.5%.
5. No side effects and abnormalities of laboratory findings were noted.
6. It was concluded that CPM has a broad spectrum antibacterial activity both in vitro and in vivo.

View full abstract

The authors have carried out the laboratory and clinical studies of cefpiramide (CPM).The results were as follows;
The sensitivity was estimated by plate dilution method on 27 strains of S.aureus and P.aeruginosa, 26 strains of E.coli, 25 strains of K.pneumoniae and 13 strains of Proteus sp.isolated from patients.The distribution of S.aureus was 0.78-6.25μg/ml and the peak of distribution was 1.56 μg/ml.
The distribution of E.coli was 0.78-50 μg/ml and the peak of distribution was 0.78 and 25 μg/ml. The growth of 24% of K.pneumoniae was not inhibited at concentration of more than 50 μg/ml.
The distribution of Proteus sp.was 6.25-100 μg/ml.
The growth of 77.8% of P.aeruginosa was inhibited at concentration of less than 3.13 μg/ml.
CPM was given by intravenous administration for 5 minutes and drip infusion for 30 minutes at a single dose of 20 mg/kg of CPM to each 2 children respectively. After intravenous administration of CPM, the mean peak serum level was 200.5±37.5 μg/ml at 15 minutes, 44.3±0.9 μg/ml at 6 hours, 19.9±0.3 μg/ml at 12 hours respectively.Half-life time was 4.2 hours.
After drip infusion of CPM, the mean peak serum level was 150.5±14.5 μg/ml at end of infusion, 23.6±3.3μg/ml at 6 hours and 8.2±2.0 μg/ml at 12 hours respectively.Half-life time was 3.8 hours.
The mean urinary excretion rate was 23.15%, 28.2% up to 12 hours after intravenous administration and drip infusion respectively.
CPM was effective in 7 cases out of 7 cases with bacterial infection.
No side effects were observed.

View full abstract

A clinical study was made of cefpiramide (CPM) a new cephem-type antibiotic for injection and the following results were obtained.
1. Blood level of CPM, after 20 mg/kg administration by drip infusion over a period of 1 hour, reached its peak of 86 μg/ml at the end of the infusion and declined to 19.8 μg/ml at 4th hour after infusion with the halflife value of 3.02 hours.Its urinary recovery rate up to 9 hours was 29.2% and the urine concentration from 0 to the 3rd hour was 820 μg/ml and from the 3rd to the 5th hour 650 μg/ml.In another case of the same dose with intravenous administration, the blood level at the end of the first 1 hour reached 56 μg/ml and by the 4th hour it had fallen to 20.6 μg/ml and by the 6th hour to 13.6 μg/ml. The half-life value was estimated as 2.44 hours.
2. CPM was administered in 2 or 3 divided doses at a daily dosage ranging from 41.7 to 62.5 mg/kg by intravenous injection or by 1-hour drip infusion to 6 patients (3 cases of pneumonia, 2 cases of urinary tracti nfections, 1 case of purulent cervical lymphadenitis) and the following clinical results were obtained;“markedly effective” 3 cases, “effective” 2 cases, and “ineffective” 1 case.The overall efficacy rate was 83.3%.
3. No side-effects or abnormal laboratory findings were found in any of the 7 patients including 1 patient who was excluded from the efficacy evaluation because of KAWASAKI'S disease.
4. Based on the above results, administration of a single dose of 20 mg/kg by intravenous injection or drip infusion twice a day is considered adequate for infections of organs showing few restrictions to drug transfer.
Thus this drug will be an extremely practical new cephem type antibiotic.

View full abstract

The effectiveness of antibiotics on biliary tract infections should be evaluated strictly by bacteriological findings rather than clinical results.In this report, the bacteria counts and drug excretion in bile were studied in 4 cases with obstructive jaundice.All patients received cefpiramide (CPM)(1.0g) by the intravenous administration; before and at 1, 2, 4, 8 and 24 hours after injection, bile samples were taken to measure the CPM concentration (by bioassay) and bacteria counts (by plate count and uricult method).
Case 1: After SOUPAULT'S operation.The highest peak of CPM excretion in bile was seen after 2 hours; bacteria counts (plate count) were decreased and/or abolished after 4 hours.
Case 2: On day 25 after PTCD.CPM showed the highest peak after 1 hour, bacteria counts fell between 3-5 hours.
Case 3: 4 months after PTCD. S. faecalis and Streptococcus were gradually diminished but E.cloacae (MIC>100) was almost unchanged.
Case 4: Cholangitis with T-tube.No change was seen in A.anitratum though CPM concentration was 830μg/ml. However by the uricult method, bacteria counts deceased from 10⁷ to 10⁴ on CLED medium, and to 10³ on MACCONKEY medium.
From these results, the bacteria counts in the bile were correlated to the CPM concentrations 2 hours afte r it's peak. It was speculated that the decease of bacteria counts reflected the theoretical antibacterial activity.

View full abstract

The authors treated a total of 23 patients (15 were outpatients, 8 were hospitalized), employing an injectable preparation of cefpiramide (CPM) a new antibiotic of the cephems.Included in this total were 10 cases of acute infectious diseases of skin and soft tissues, 5 cases of acute localized peritonitis, 5 cases of acute urinary tract infection and 3 cases of acute and subacute cholecystitis.To 15 cases of outpatients, CPM in a dose of 500 mg were given by intramuscular injection once a day, and to 8 cases of hospitalized patients weregiven 500mg of CPM by intramuscular injection twice a day.The duration were 3 to 15 days.The clinical efficacy obtained was excellent in 4 cases, good in 17 cases, and fair in 2 cases. In no case was CPM found to be completely ineffective.Clinical adverse effect was not recognized.
Therefore, CPM will be a useful drug when used for chemotherapy of acute or subacute infectious diseases on surgical field following intramuscular administration.

View full abstract