We studied on the antibacterial activity of gentamicin against various pathogens isolated from clinical materials mainly isolated during 1974 and 1975, comparing with other antibiotics.
Beta hemolytic streptococci, pneumococci and enterococci are less susceptible to gentamicin than staphylococci. Staph. aureus and Staph. epidermidis resistant to various antibiotics are very susceptible to gentamicin, and no resistant strain to this drug was found.
Haemophilus influenzae, H. parainfluenzae and H. parahaemolyticus are very susceptible to gentamicin, and there is no resistant strain to this drug.
Escherichia coli, Klebsiella, Citrobacter, Serratia and five species of Proteus are more susceptible to gentamicin and tobramycin than dibekacin and amikacin. A few resistant or less susceptible strains to gentamicin are found in E. coli, Citrobacter, Serratia, Pr. morganii and Pr. rettgeri. Pr. inconstans is less susceptible to gentamicin than other species of Proteus.
Antibacterial activity of gentamicin against Pseudomonas aeruginosa is very strong, but dibekacin and tobramycin are stronger. Gentamicin-resistant strains of Pseudomonas aeruginosa are now rather few.

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Gentamicin (GM) was studied for on its antibacterial activity, absorption, and excretion, effect on the kidney and clinical effects. The results obtained are as follows:
1. Antibacterial activity: The susceptibility of E. colt, Klebsiella, Proteus mirabilis to GM was almost the same between the periods of 1964-1966 and 1972-1974: No tendency of increase of resistance by year was noted. However, against Pseudomonas aeruginosa, strains showing sensitibity to a concentration of more than 25mcg/ml were isolated in 12.7%, in the latter period (1972-1974), as compared with the former period (1964-1966), which was 0%.
2. Blood levels: The peak level of GM in blood was obtained at 30 minutes after intramuscular injection to a healthy human. The peak level was 7.6mcg/ml with 40mg dose, 8.7mcg/ml with 60mg and 10.6mcg/ml with 80mg, showing a dose-responding curve. The half-life of GM absorption was 1.1 hours with 40 mg dose, 1.3 hours with 60mg and 1.6 hours with 80mg, showing also a doserelated tendency.
3. Urinary levels: The peak level of GM in urine, about 200mcg/ml, was noted in 0-2 hours after intramuscular injection of GM to a healthy human. The urinary recovery was about 44% in 6 hours.
4. Effect on the kidney: The effects of GM on the kidney were studied in rats administering 20mg/kg once a day for 21 days consecutively. The results obtained are a slight increase (20mg/dl) in BUN and a slight decrease (2,600mosm/kg H₂O) in urinary osmotic pressure; and urea lysozyme showed tendency to increase from the third day, the same as with kanamycin. Meanwhile, in the histopathological findings of the kidney tissue, the vacuolar degeneration and flattening of renal tubules were noted. Similar findings were obtained with kanamycin in a similar type of experiment. These results indicate that nephrotoxicity of GM is considered to be approximately the same as that of kanamycin.
5. Clinical results: GM was injected into 22 patients with various infectious diseases (respiratorytract infections 7, liver abscess 1, urinary-tract infections 14). Excellent efficacy was noted in 7 patients, good in 13 and no effect in 2. The effective rate was 90.9%. No serious side effect was noted in this clinical trial.

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Gentamicin (GM) was intramuscularly injected to 29 patients with various infections in the doses of 40-60mg twice a day. The maximum dose was 1, 800 mg. Satisfactory clinical results were obtained in the treatment of not only urinary tract infections but also respiratory tract infections, bile duct infections and others. This clinical results would coincide with the fact that almost all organisms isolated had a high sensitivity to GM.
No significant abnormal finding was observed in this clinical study. This clinical result indicates that GM is a useful drug in the treatment of various infections.

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Gentamicin (GM) was intramuscularly injected to 16 children with various infectious diseases (1 septicemia, 1 purulent meningitis, 4 bronchopneumonia, 1 pyothorax, 3 pyelonephritis, 2 acute cystitis and 4 RITTER'S dermatitis).
The results obtained are as follows:
1. The excellent and good clinical results were noted in all patients except for an indeterminate case with bronchopneumonia because of the concomitant therapy with CEZ. The effective rate was 100.0%. This was possibly because of quite high susceptibility (+++) of all isolates to gentamicin.
2. Doses of GM were adjusted depending on the style of infectious diseases. The satisfactory clinical results were obtained in some cases by increasing its recommended dosage to about 5-8mg per kg per day.
3. No kidney dysfunction, liver dysfunction, the 8th cranial nerve damage, etc. were observed by administering 5 to 8mg per kg per day for at maximum 18 days, in this clinical trial.
4. It has been indicated in this clinical trial that GM is worthy to be used as a first-choice drug in chemotherapy of infectious diseases caused by Staphylococcus, gram-negative bacillus, etc., especially in patients who are hypersensitive to penicillin and cephalosporin derivatives. However, further study would be required for the safety of increase in its dosage and duration of administration.

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1. The MIC of gentamicin and other antibiotics against clinical isolates was determined, and the following sensitivity distribution was obtained.
a) Against 54 strains of Staphylococcus aureus, GM had the lowest MIC, followed by TOB, DKB, BB-K8 in order. The distribution range of 0.1-6.25μg/ml was noted with GM. The peak of MIC was 1.56μg/ml.
b) Against 54 strains of E. colt, the lowest MIC was obtained with GM, and 53 strains (98%) were in the range of 0.4-6.25μg/ml. The peak of MIC was 3.12μg/ml. GM was followed by TOB, CL, DKB in order of superiority.
c) Against 27 strains of Klebsiella pneumoniae, GM and TOB had the lowest MIC, showing the peak of MIC of 0.8μg/ml. No significant difference was noted between GM and TOB. GM and TOB were followed by DKB, CL, BB-K8 in order of superiority.
d) Against 27 strains of Proteus, GM had the lowest MIC, followed by TOB, DKB and BB-K8 in order. But the peak was 6.25μg/ml even in GM. The activity of antibiotics against Klebsiella pneumoniae was generally low.
e) Against 54 strains of Pseudomonas, the peak of MIC of GM was 3.12μg/ml and 49 strains (91%) were in the range of 1.56-12.5μg/ml. Whereas TOB had the peak value of 0.8μg/ml and 49 strains (91%) were in the range of 0.4-3.12μg/ml. TOB was followed by DKB, GM, BB-K8 in order of superiority.
2. Blood levels of GM were 2.7μg/ml at 30 minutes, 1.1μg/ml at 1 hour and 0.6μg/ml at 2 hours after the intramuscular injection of 60mg to a healthy adult human.
3. The peak level of GM was noted in the urine 30 minutes and 1 hour after the intramuscular administration of GM 60mg to a healthy adult. The urinary recovery was 44.1% in 6 hours.
4. The tissue distribution after the intramuscular administration of 20mg/kg GM to rats indicated the remarkably high levels of GM in serum and the kidney. The high levels of GM in the kidney were maintained even after 6 hours. GM was noted in the lung, heart, spleen in order of high concentration. The inconsiderable amount of GM was detected in the brain, but little in the liver.
5. GM was intramuscularly injected to 20 patients with surgical infections. The satisfactory results were obtained in 14 patients (70%). No clinical side effects nor significant abnormal laboratory findings were noted in this clinical study.

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Gentamicin (GM), one of the amino-glucosides, was administered intramuscularly to 27 patients with Pseudomonas and/or other antibiotics resistant infections. The clinical evaluation of the results obtained was classified excellent in 1 case, good 6, fair 8, none 11 and indeterminate 1, the effectiveness accounting for 57.7 percent. Satisfactory results were noted in wound infections, peritonitis and urinary tract infections.
Among untoward side effects, an elevation in GOT and GPT values was observed in 6 cases, an elevation of BUN value in 1, proteinuria in 1 and hematuria in 1. However, it is difficult to conclude that those side effects were attributable to GM itself because blood transfusion or combined therapy with anti-cancer agents was conducted in these cases during the GM therapy.

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Gentamicin (GM) was intramuscularly administered to 24 patients with various infections (including 1 for prophylaxis of a postoperative infection) in the dose of 40mg×2/day for 4-26 days. In children, the maximum daily dose was 3.4mg/kg and the minimum was 1.2mg/kg (mean: 2-3mg/kg).
The results obtained are as follows:
1) Clinical efficacy of GM was excellent in 2, good in 9, fair in 4, null in 4 and indeterminate in 5, out of 24 cases. The effective rate was 57.9% (11/19).
2) In 21 strains isolated in 13 cases out of 24, efficacy of GM was good in 10, fair in 5, null in 3 and indeterminate in 3. The effective rate was 55.6% (10/18).
3) No significant side effect was observed in this clinical study.

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Gentamicin (GM) was intramuscularly administrated to 25 patients with complicated urinary tract infections in doses of 20-120mg a day for 4-16 days. The results obtained are as follows:
1. The clinical results of GM were excellent in 4, good in 3, fair in 1, poor in 3 and indeterminate in 14 patients out of 25 patients. The effective percentage was 63.6%(7/11).
2. The clinical results of GM against 20 isolates were excellent in 4, good in 3, fair in 1, poor in 3 and indeterminate in 9 isolates. The effective percentage was 63.6% (7/11).
3. In laboratory examinations, BUN elevation was noted in 1 patient, GOT elevation in 2 patients and GPT elevation in 1 patient during GM therapy. No other abnormal findings were observed in this clinical study.

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1. Gentamicin was effective in 20 patients out of 25 with urological diseases.
2. Gentamicin was more effective on acute symptoms than on chronicones.
3. No marked side effects were noted.
4. No conclusion was drawn on difference in efficacy of gentamicin by dosage, duration of administration and kinds of organisms in this clinical trial.

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Gentamicin 40mg was intramuscularly administered two times daily to 15 patients with complicated urinary tract infections.
The results are as follows:
1. The clinical efficacy of gentamicin was excellent in 12 cases (80.0%), good in 2 cases (13.3%) and null in 1 case (6.7%). The effective rate was 93.3%.
2. Bacteria disappeared in 16 strains (84.2%), colonized in 3 strains (15.8%) out of 19 isolates.
3. BUN, GOT and GPT values were determined before and after GM administration, and no significant abnormal finding attributable to GM was observed in this clinical study.

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1) Gentamicin (GM) was intramuscularly injected to 1 patient with simple acute cystitis and to 21 patients with complicated chronic urinary tract infections in the doses of 40-160mg per day for 3-12 days (mean: 5.2 days).
2) The clinical effect was excellent in 6, good in 9, poor in 7, which is classified as excellent in 1 with simple acute cystitis, good in 5 and poor in 5 out of 11 with complicated chronic cystitis, and excellent in 4, good in 4 and poor in 2 out of 10 with complicated chronic pyelonephritis.
3) In complicated urinary tract infections, the effective rate was 61.5% (8/13) in GM 80mg/day dosage group and 75.0% (6/8) in GM 120mg/day dosage group.
4) No abnormal change was noted in the kidney, liver and auditory function throughout this clinical study.
5) When GM therapy is conducted in the treatment of complicated urinary tract infections, it is considered that more favorable clinical results could be obtained with dosage of GM 120mg/day or more. However, in this case a caution has to be paid to the kidney and auditory functions.

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Twenty cases with complicated urinary tract infections were treated with gentamicin. Good results were obtained in 7 of 14 cases with chronic pyelonephritis and 2 of 4 cases with chronic cystitis and in 1 of 2 cases with acute prostatitis.
No side effect was observed throughout this treatment. But in laboratory examination, slight elevation of S-GOT and S-GPT was observed in 3 of 20 cases after gentamicin treatment.

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Antibacterial activity of tinidazole (1-2-(ethylsulfonyl)-2-methyl-5-nitroimidazole) against anaerobic bacteria including Peptococcus, Peptostreptococcus, Eubacterium, Propionibacterium, Bacteroides and Fusobacterium was studied by agar dilution method comparing with metronidazole. In addition to this work, bactericidal effect of tinidazole and metronidazole against P. prevotii, B. fragilis ss. fragilis and F. varium was examined by quantitative culture method after incubation in GAM broth containing of 4 MIC, 2 MIC, 1 MIC and 1/2 MIC of both drugs against each of three strains for 1, 3, 6, 12 and 24 hours.
All the strains of Peptococcus and Peptostreptococcus including P. anaerobius, P. saccharolyticus, P. prevotii and Ps. anaerobius and others were susceptible to a concentration of 6.25mcg/ml of this drug.
A concentration of 3.13mcg/ml inhibited all strains of Bacteroides including B. fragilis ss. fragilis (12 strains), ss. vulgatus (5 strains), ss. thetaiotaomicron (4 strains) and ss. distasonis (2 strains). To this concentration all strains of Fusobacterium including F. varium (20 strains), F. mortiferum (2 strains) and other Fusobacterium sp.(5 strains) were susceptible.
On the contrary, Propionibacterium acnes (6 strains) was resistant to 100mcg/ml or more of tinidazole and metronidazole.
The antibacterial activity of tinidazole was stronger against Bacteroides than that of metronidazole, while almost equal against Peptococcus, Peptostreptococcus, Eubacterium and Fusobacterium.
Tinidazole was bactericidal against F. varium in a concentration of 2 MIC and 4 MIC till 24 hours of incubation but did not show such an activity on B. fragilis ss. fragilis in same concentration even after 12 hours of incubation. On the other hand, metronidazole was bactericidal against B. fragilis ss. fragilis while was not against F. varium. Against P. prevotii bactericidal activity of both drugs was similar.
Tinidazole as well as metronidazole is an excellent chemotherapeutic agent against anaerobic bacteria excluding Propionibacterium acnes and Bifidobacterium adolescentis.

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Amoxicillin at a daily dose of 1-1.5g was orally administered to total 30 cases comprising 6 of acute tonsillitis, 6 of chronic tonsillitis, 8 of acute bronchitis, 4 of chronic bronchitis, 4 of bronchiectasis, 1 of suppurative diseases of the lung and 1 of exudative pleurisy. The clinical results and side effects are reported.
1. The effect of amoxicillin was remarkably good in 15 of 30 cases with infections of respiratory apparatus (50%), good in 7(23%), poor in 5(17%) and unknown in 3 (10%); the effectiveness was 73%.
2. In terms of diseases, amoxicillin was effective in 33% of acute tonsillitis, in 50% of chronic tonsillitis and in all of acute bronchitis, chronic bronchitis, bronchiectasia and suppurative disease of the lung. No effect was observed in exudative pleurisy.
3. In terms of strains detected, amoxicillin was effective in 67% of Staphylococcus aureus, in 89% ofHaemophilus and in 50% of Klebsiella. This drug was effective in all cases caused by Escherichia coli, Acinetobacter calcoacetines, β-Streptococcus, Flavobacterium, Streptococcus pneumonia, though these strains were not frequently detected. Pseudomonas aeruginosa had no response to this drug.
4. Two cases of transient hepatic dysfunction, 6 of eruption, 5 of gastro-intestinal disorders, 1 of arthralgia and 1 of pyrexia were observed as side effects (some cases had side effects in overlap).

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Patients with acute otitis media, tonsillitis and upper respiratory tract infections were divided into 2 groups and treated with ampicillin-cloxacillin (Rectocillin) 1g/day or ampicillin (AB-PC) 1g/day, respectively. The therapeutic effect and side effect of these two drugs were studied comparatively by double blind tests.
The effective rate in the Rectocillin group was 85. 1%, and that in the AB-PC group was 86. 7%.
There was no significant difference in the therapeutic effect between two drugs.
Ten cases in the Rectocillin group and 4 cases in the AB-PC group complained of disorders supposedly due to administration of these drugs. Such side effects in the former group were all gastrointestinal disorders, but in the latter, 2 cases of eruption, one case of headache and one case of gastrointestinal disorder.

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[in Japanese]

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