As an experiment in vitro of an antibiotic?aminosidine, we have studied on antibacterial spectrum, sensitivity to clinical isolated bacteria such as Staphylococcus, E. coli, Shigella and P. aeruginosa and influences of pH, serum protein and inoculated bacterial cells on antibacterial activity. On the other hand, we also have worked on designating types of antibacterial activity by means of total cell count method, viable count method and condition of acquired resistance and cross resistance.
Furthermore, we researched in antibacterial activity in vivo to an experimental infectious disease and as the result of the above studies, we could obtain a few findings.

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Pharmacological actions of aminosidine, a new oligosaccharide antibiotic, were investigated. LD₅₀ were the doses of 790(sc), 750(ip) and 22, 3(ic) in mice and 870 (sc) mg/kg in rat respectively. The movement of the excised heart of toad and guinea pig was inhibited (5 X 10^-5 an d 10^-3g/m1) respectively. The movement of excised rabbit intestine was inhibited (10^-4g/m1). The excised rabbit ear vessels were dilated (10^-2g/m1) and the permeability of rabbit skin vessels was stimulated (10 mcg). Temporar fall of blood pressure and acceleration of respiration were observed (20 mg/kg) in the urethaneanesthetised rabbit. Tachycardia took place at the dose of 10 mg/kg. Tremor and vertical nystagmus were observed in the rabbit applied intracisternally. Aminosidine, therefore, has not re markable pharmacological actions at the therapeutic doses.

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The in vitro sensitivity tests of aminosidine, in comparison with kanamycin, were performed to the following bacteria: Shigella (227 strains), Salmonella (232 strains), Proteus (50 strains), Escherichia (50 strains), Vibriop arahaemolyticus( 50 strains) and Vibrio El-Tor (100 strains). This antibiotic was apparently effective to Shigella, S almonella, P roteus and Escherichia, and its minimum inhibitory concentration was each about 6. 25 mcg per ml. Both aminosidine and kanamy cin were non-effective to Vibriop arahaemolyticus, a nd moderately effective to Vibrio El-Tor.

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Acute LD₅₀ of AMD was 21. 62 g/kg (p. o. ) and 1. 20 g/kg (i. m. ) in rats. In chronic administration of over 30 mg/kg of AMD, slight changes in urine and blood occurred irrespective of considerably evident histological changes in kidney and liver. At the end of the first month, neutralization of pH, protein, sugar and occult blood in urine, slight increase in the numbers of erythrocytes, hemogloblin and slight decrease in the activity of alkaline phosphatase appeared. In liver, focal atrophy, fat infiltration of liver cells and round cell infiltration of interstitial tissues occurred. In kidney, atrophy in glomerulus, degeneration of wall cell, dilatation and hyaline cylinders in tubulus appeared. The changes in urine and blood were most evident at the end of first month, became weaker in the third month and disappeared in the sixth month. In the first month, the degenerative changes in liver and kidney was unexpectedly weak, in the third month, became stronger accompanying the equal changes in adrenal, thyroid or thymus, and in the sixth month, these changes still remained in higher doses, but the signs of recovery appeared in lower doses.

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The present experimental study was performed to clarify the ototoxicity of aminosidine (a new oligosaccharide antibiotic) in guinea pigs audiometrically, histopathologically and histochemically. Fiftyseven albino guinea pigs of the Hartley strain (about 250 g at the start of the experiment) were divided into 4 groups. I group: aminosidine was given at dosis of 200 mg/kg/day intramuscularly for 7 and 28 days to 14 guinea pigs. II group: dihydrostreptomycin was injected at dosis of 400 mg/kg/day intramuscularly for 7 and 28 days to 12 animals. III group: kanamycin was administered at dosis of 400 mg/kg/day intramuscularly for 28 days to 26 animals. IV group: control. The results obtai ned were as follows:
1. A m inosidine caused less frequently mild to moderate injury of the inner ear. Preyer's pinna reflex test revealed less frequently mild and moderate impairment of hearing. No remarkable impair138 CHEMOTHERAPY FEB. 1968 ment of equilibrium was found. Histopathologically, slight dilatation of the scala media in the first turn of the cochlea was noticed, but the organ of Corti had intact inner and outer hair cells. Spiral ganglion, cristae ampullares and maculae were almost normal. Histochemically, the inner and outer hair cells of the organ of Corti in the first turn showed slight decrease in the succinic dehydrogenase activity in one animal. These injuries due to aminosidine are thought to be of tentative and reversible damage of the inner ear.
2. Dihydrostreptom ycin produced less frequently severe injuries of the inner ear consisting of extensive missing of the organ of Corti.
3. Kanamycin caused re latively frequently severe injuries of the inner ear consisting of extensive missing of the organ of Corti and atrophy of the peripheral fiber of the auditory nerve.

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The fundamental and clinical studies of a ne w antibiotic aminosidine resulted in the following conclusions.
1. The sensitivities against Staphylococcuasu reus and a variety of gram negative bacilli were generally excellent, but there were almost complete cross resistances between kanamycin and paromOrnycin respectively.
2. The adsorption to red blood corpuscle was in the middle grade. No inactivation by liver homogenate was observed. By the cellophane bag dialysis method the serum protein binding rate was 28% on the average.
3. On mice organ level determination following intramuscular injection, those of kidney, serum, lung, spleen and liver was higher in order. After oral administration, only the level of bowel content was extremely high, and those of other organs were minimal.
4. The effect of aminosidine against experimental subcutaneous infection of Staphylococcuasu aureus and Escherichia coli to the back of mice was similar to kanamycin in both instances.
5. A case of pyelonephritis due to E. coli was successfully treated by intramu scular injection and three cases suffering from acute colitis were cured by oral treatment. The concentration of serum, urine and feces were determined on each case.

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The results of our studies on aminosidine are summarized as follows:
1. The sensitivity of 61 strains of Staph. a ureus, isolated fro m patients, to aminosidine was measured by the plate dilution method. 77% of these strains were less than 3. 2 mcg/ml in MIC. On the other hand, 9 strains were found to have natural resistance to aminosidine. Aminosidine was found to have cross resistance with kanamycin.
2. Blood levels, b ile levels and urinary recoveries were studied after the intravenous administration of 21. 3 mg/kg of aminosidine in dogs. The maximum blood level was 43. 3 mcg/ml, and the maximum bile level was 6. 18 mcg/ml. Biliary recovery was much less than urinary recovery. Values worked out through the study were as follows: t/2= 1. 82 (hours), DV=5. 7 (1), Cr= 14. 4 (ml/min), Cb= 0. 019 (ml/min), Kr= 0. 16 and Kb = 0. 0002 (in normal dogs).
3. Aminosidine was found to be more inactivated in the liver tissue than in other tissues.
4. One, three and five hours after the intramuscular administration of aminosidin e in rats, plasma and renal concentration was measured, but no aminosidine was detected in the liver and the spleen.
5. Eight cases of various infections including urinary and respiratory infections were treated with aminosidine, which was administered intramuscularly for 6∼10 days with daily dose of 0. 35∼-0. 7 g. The effect was excellent in three cases, good in four cases and poor in one case. As to the side effects, hearing disturbance was observed in two cases.

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On aminosidine, fundamental experiment and clinical application were performed.
1. Antimicrobial activities were tested in vitro. The minimal inhibito r y concentrations of aminosidine against Staphylococcuasu reus, K lebsiellap neumoniae, C itrobacter, C roaca, Serratia, Shigella and Salmonella were in the range of 2. 2-8. 8 mcg/ml. The concentrations against Streptococcu s haemolyticus and E. coli were within 8. 8-17. 7 mcg/ml. Proteus and Pseudomonas group were resistant.
2. The peaks of serum level of aminosidine in normal subject s after a single intramuscular injection of 700 mg were between 22 and 49 mcg/ml, and the half-life times were from 0. 42 to 2. 22 h., while in uremic patients the peaks 46-73 mcg/ml and half-life times 16. 68-30. 79 h.
3. Although severe renal tubular damage was observed in rats at dose of 284 mg per kg per day, the damage was minor at the dose of 142 mg per kg per day.
4. Two patients with pneumonia and 1 bronchiectatic received 350 mg of aminosidine twice a day intramuscularly and 4 patients and 10 carriers of bacillary dysentery received oral dosis of 1 g daily. All patients were cured. No side effect, except occasional mild pain at the site of injection, was observed.

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Following results were obtained by our fundamental and clinical studies of aminosidine (AMD). 1. The antibacterial activity of AMD against E. coli was 25∼12. 5 mcg/ml, and in case s against Klebsiella and Proteus mirabilis, the value was 6. 3∼3. 2 mcg/ml. While, as to Staphylococcuasu reu s, some were proved to be resistant to AMD indicating their value more than 100 mcg/ml, but others were found to be sensitive with value 12. 5∼3. 2 mcg/ml. Aminosidine was found not to have strong antibacterial activity against Pseudomonas, E nterococcusS, treptococcuhs emolyticus, and Streptococcusv i ridans. It was observed that AMD had cross resistance with KM, FRM and PRM. 2. Blood concentration and elimination rate in urine were prett y high in cases when AMD was administered intramuscularly. However, in cases of oral administration, the values were low because of the poor absorbability of the drug. 3. AMD was clinically applie d to 4 cases, two of which obtained effective results.

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1. Distribution of Aminosidine (AMD) in Various Organs
In rats and mice, the tissue concentration of AMD following intramuscular injection is highest in the kidney. Next in order of the high level come the serum, lung, spleen as well as muscle and then liver.
2. Serum Concentration of AMD
By muscular injection of AMD 350 mg or 700 mg to healthy adults, the concentration of AMD amounts to the peak of 16. 2 mcg/ml or 33. 3 mcg/m1 1 hour after. In patients with impaired renal function, the serum level of AMD is higher and more prolonged. After oral administration, AMD cannot be detected in the serum.
3. Excretion into Urine
The urinary recove ry rate of AMD is 2 7. 7% for the first 2 hours and 53. 1% for 8 hours.
4. Excretion into Bile
The AMD concentr ation in bile after intravenous injection to dogs is lower than the serum level, but in case of rabbits, that is sometimes higher and sometimes lower than the serum level.
The AMD level in bile collected from the drainage tube of two postoperative patient s is higher than the serum level, but in bile collected from the duodenal drainage tube of 3 patients of cholecystitis, AMD can not be detected.

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From the studies on a new antibiotic, aminosidine (AMD), the following results were obtained.
1. Blood concentration and urinary excretion rate: With 0. 5 g intramuscular injection of AMD, the blood concentration reached to the maximum level of 31. 4 mcg/ml in 1 hour, and the urinary excretion rate was 26. 6 % for 6 fours.
2. Antibacterial activity: Usi ng the dilution method, sensitivity of staphylococci and gram-negative bacilli was observed. Standard strains of Staphylococcuasu reus were inhibited by the concentration of less than 3. 12 mcg/ml. Almost all the strains of pathogenic staphylococci were moderately sensitive. The minimum inhibitory concentrations of AMD against E. coil NIHJ, Klebsiella pneumoniae ST101, P roteus v ulgaris 0X19 and Pseudomonasa eruginosaK U were 12. 5, 25, 25, 25 mcg/ml respectively. Some strains of E. call and Klebsiella isolated from the patients were moderately sensitive, but most of Proteus and Pseudomonas were highly resistant.
3. Clinical effects: AMD was used in the treatment of 4 cases, consisting of acute pyelonephritis, chronic pyelonephritis, acute cholecystitis and sepsis caused by gram negative bacilli. It was effective for 3 diseases except sepsis.
4. Side effects: N o noticeable side effects were observed.

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A study was made on aminosidine with reference to its in-vitro antibacterial activity against various gram-negative bacilli and bacillus tuberculosis.
The results of the above study a s well as the study of the concentration of aminosidine in the serum and the study of the resultant anti-bacillus tuberculosis activity of the serum are discussed and reported,

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Aminosidine was administered to 38 cases with bacillary dysentery, septicemia, cholangitis and pyelonephritis. The results obtained are as follows:
1. The growth of dysentery bacilli on stool culture was remarkably depressed after the administration of aminosidine.
2. R emarkable effect was obtained in the cases of Kiebsiella septicemia.
3. No effect was observed in one case of cholangitis.
4. The clinical and bacteriological effects on the cases of acute pyelonephritis were excellent, but riot in chronic cases.
5. No signifi cant side effects were observed in all the cases.

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First Department of Internal Medicine, Osaka Ci t y University Medical School Fundamental studies were made on aminosidine (AMD), a new antibiotic produced by Streptomyces chrestomicetiuisn, respect of its absorption, elimination and antibacterial activity. The therapeutic effects of AMD on the infectious diseases were also investigated.
Aminosidine was proved to have almost com plete cross resistance with kanamycin (KM). But by St. aureus or by Streptococcust, h e resistance to AMD seemed to be less frequently obtained.
Considerably effective therapeutic results were obtained in the treatment of t he infectious diseases. Almost no side effects were observed.

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1. Sensitivity:
More than 3/4 of test strains of coagulase positive Staphylococcuasn d E. coli were sensitive against aminosidine at the concentration below 6. 3 mcg/ml. The sensitivity against aminosidine was higher than that against SM which was determined at the same time.
2. Blood level:
When injec ted to normal adults intramuscularly, aminosidine showed high blood level. When it was once administered at a dose of 500 mg, its blood level reached the peak (18. 1 mcg/ml) after 2 hours and reduced to 3. 9 mcg/ml after 6 hours.
3. Excretion into urine:
The concentration of aminosidine in urine was very high. Urinary recovery rate was 87. 3 % in the first 12 hours.
4. Renal excretion mechanism:
Renal excretion mech anism was examined with Stop-flow method. As a result, glomerular filtration, absorption at superior renal tubule and secretion at inferior renal tubule were observed.
5. Nephrotoxicity:
After aminosidine was administered to rats and rabbits continuously, renal function and renal tissue findings were examined. Nephrotoxicity of aminosidine is comparatively slight and seems to be more slight than that of CL.
6. Clinical resul ts:
Aminosidine was administered to 7 cases of internal infections. In 5 cases of them, aminosidine was proved to be effective.
7. Side eff ects:
Only in o ne case of the 7 cases given aminosidine, topalgia and slight palsy at the injected place were observed. In other 6 cases, no side effects were observed.

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Aminosidine, a new oligosaccharide antibiotic, was clinically applied to the patients, on whom the influence of the drug was studied from the following points.
Influences of the drug on the function of the liver a nd the kidney; the blood level, . the elimination rate in urine and the bile level of the drug after intramuscular injections; and the sensitivity to E. coli and to St. aureus were studied and discussed in comparison with other antibiotics.
Aminosidine was found not to have very strong sensitivity to any p articular bacteria, but to have very slight side effect. After all, it seems that aminosidine is a useful antibiotics to be administered as a secondary drug.

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Studies were made on aminosidine (AMD) in the field of pediatrics in respect of the following points:
1. The sensitivity of various pathogenic bacteria, isolated from patients of pediatric infect i on, to aminosidine.
2. Blood concentration and urinary excretion rate of AMD in children.
3. Clinical effects of AMD on the acute pediatric infections.
4. The most effective therapeutic dosage and meth od of administration of AMD.

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The in vitro sensitivity of coagulase-positive Staphylococcus, E. coil and dysentery bacillus against aminosidine was found to be about the same with their sensitivity against KM. It was also testified that AMD and PC G have synergistic activity.
Clinically, AMD was tried on 46 case s of pediatric infections. The therapeutic result was remarkable effective in 27 cases, fairly effective in 14 cases and vague in 5 cases.

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The Department of Infectious Disease, Tokyo Municipal Komagome Hospital Eighteen patients in acute stadium and 17 patients in carrier state of bacillary dysentery were treated with aminosidine at the daily dose of 2. 0 g and 1. 0 g orally to adults and children respectively for 5 days. The results in 29 patients were satisfactory, but in 6 patients (17. 1%) the further treatments with kanamycin were required because of persistent discharge or redischarge of causative agents. Twenty nine of isolated strains belonged to Shigella sonnei and only 6 to Shigella flexneri. The M. I. C. of aminosidine against isolated strains tested on the agar plates was 6. 25 to 12. 5 mcg/ml.
In some patients mild diarrhoea was encountered in the courses of the treatment, bu t no other untoward effects were found.

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11 Bacillary dysentery patients, 2 carriers of bacillary dysentery and 2 patients having other forms of acute colitis were admitted Toshima Hospital in September and October of 1966 and were treated with aminosidine.
Adults were given 0. 25 grams of aminosidine every 6 hours for 5 days. Follow-up observation was lasted for from 10 to 15 days after termination of treatment with the drug. Fecal culture was carried out 4 times a week.
a) Effects on bacilli discharge: The drug was found very effective for patients having CP, SM and TC sensitive dysentery bacilli, Vibrio parahaemolyticus and pathogenic Escherichia coil from the beginning, but in the 5 cases which were infected with resistant organismus were found after completion of the treatment.
b) Clinical effects: Remission of fever, normalization of the defecation frequency and return of stool character to normal were almost the same as in cases treated with macrolide antibiotics.
c) No patients showed side effects due to the administration of aminosidine, so an increase in dosage might be tried. It is ou r opinion that evaluation of aminosidine should be concluded after further trial.

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Aminosidine is a new broad-spectrum antibiotic produced by Streptomycecs hrestomyceticiusso lated from soil sample of Massa Marittim (Italy) in Farmitalia Research Laboratory.
In general, aminosidine possessed equally potent bacteriocidal activity Gram negative as well as Gram positive pathogens.
Aminosidine was applied to 21 patients of bacillary dysentery and 15 cases of healthy carriers.
Daily dose of 2. 0 gram in adult was administrated every 6 hours for 5 days. Follow up observation was about 14∼21 days on the average.
a) Clinical effect; Remission of fever was seen in 1. 15 days, normalization of the defection frequency was in 2. 25 days, disappear of bloody feces was in 1. 17 days, recovery of the stool findings was in 4. 89 days on the average.
b) Effect for the duration of bacilli discharge; The bacilli disappeared within 2. 33 d ays after administration of the medicine but reappearance of bacilli was observed 23. 3% in total.
c) The sensitivity test of Shigellato aminosidine was carried out in 54 strains. The minimal inhibitory concentration (MIC) was 3. 13∼4. 56 mcgiml. This concentration was almost the same as another oligosaccharide antibiotics— kanamycin, paromomycin etc.
d) The usefullness of new antibiotic aminosidine in the tr eatment of bacillary dysentery was confirmed.

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The antibacterial activity of aminosidine against Shigella strains isolated from clinical materials was tested and the antibiotic was tried in the treatment of bacillary dysentery. Two groups of dysentery patients were treated: the one was given daily 1. 0 g of the antibiotic orally and the other was 2. 0 g. The results obtained were as follows:
1) The minimal inhibitory concentration of aminosidine againstShigella strains was mostly 3. 12-42. 5 mcg/ml.
2) The antibacterial activity of aminosidine increased at an alkaline pH.
3) When used for the treatment of bacillary dysentery in dose of 2. 0 g daily in 18 cases and 1. 0 g daily in 11 cases for a period of 5 days, fever fell within 1-3 days, diarrhea bound within 1-3 days, stool features restored within 2-7 days and bacterial excretion discontinued within 1-3 days.
4) The bacterial reexcretion cases, however, were observed in only 1 of 18 cases given 2. 0 g daily, as compared within 5 of 11 cases administered 1. 0 g daily.
5) In a severe case due to Shigella flexneri 2b administered 2. 0 g daily for 5 days, no clinical effectiveness was seen and the stool culture became negative on the 5th day.
6) No side effects were observed in all cases.

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Aminosidine was orally administered to the cases of bacillary dysentery. The drug, 30∼50 mg/kg in quantity, showed considerable effect to eliminate the bacteria. It can be said that aminosidine is a drug worthusing inthe present situation when strains ofmultiresistant dysentery bacillus are increasing in number.

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The therapeutic effects of aminosidine to dysentery and enteritis were as follows:
1. Dysentery
One g of aminosidine was daily administered to 2 dysentery patients and 7 carriers of dysentery bacillus and the drug was remarkably effective in all the cases.
2. Enteritis
Amino sidine was used to 17 cases due to Vibrio enteritidis, 4 cases due to Salmonella enteritidis and 3 cases due to others. 2 g of the drug was daily administered for 11 days to cases due to Salmonella enteritidis and for 5 days to the others. The drug was effective in all the cases except the 2 cases. due to Salmonella enteritidis.

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Aminosidine is a new oligo-saccharide antibiotic, which resembles to oral paromomycin in its physical, chemical and antibiotic properties.
In the present study w e used aminosidine sulfate as an injectable sample. 15. 03 m cg/ml of blood concentration and 397. 60 mcg/ml of maximal concentration in the urine were obtained after intramuscular injection of 350 mg in healthy adults. When it was intramuscularly given to dd-mice the peak concentrations of the drug were found high enough in tissues of kidney, lung, spleen, liver and brain in order.
Aminosidine sensitivity of 77% of staphylococci cultured from surgical infections was ranged in 1. 56-12. 5 mcg/ml and of 64. 1% of Escherichia coli in 3. 12∼12. 5 mcg/ml. On the contrary all of Pseudomonas resisted more than 100 mcg/ml. Antibacterial effect of aminosidine was intensified at pH 7. 6∼8. 0 of. media, it was stable at 10⁶∼10⁷ of inoculum size and no influence was observed in coexistence of serum.
In the open clinical test of the drug it was found that the result was excellent in 2 cases of 9, g ood in 4 cases and failed in 3 cases. The drug was intramuscularly given in dose of each 175∼700m g 1∼2 times a day and in duration of 2∼12 days long.
Careful observation did not found any func tional lesions in 8th nerve and kidney.

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From the clinical and basic studies on a new antibiotic, aminosidine (AMD), the following results were obtained.
1) Two hours after intramuscular injection of AMD 500 mg to adult, the level of blood serum was an average of 9. 4 mcg/ml. Besides its level after 12 hours was 0. 4 mcg/ml, and this showed t hat AMD has prolonged action.
2) By the result of the AMD sensitivity test (46 strains of Staphylococcus aureus were examined), 32 strains of 46 showed that the MIC were 0. 1 to 6. 25 mcg/ml.
3) The AMD sensitivity against Phage type 80/81 strains which were so called “Hospital Strains”, was higher than the others, and clinically the AMD will be excellently effective.
4) Cross resistance against KM (Oligosaccharide antibiotic) was recognized but the others were not.
5) li Clinical applications were perfomed to 10 cases. Eight cases were effective, and 2 cases were ttle.
6) Side-effects were not recognized in all cases.
7) The above results suggest that the AMD has an excellent therapeutic effect.

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A new antibiotic, aminosidine, isolated from the culture of Streptomycesc hrestomiceticubse longs an oligosaccharide group of antibiotics. The authors summarize the results of a preliminary study on this new antibiotic as follows:
The peak blood leve l of the antibiotic (16. 0 mcg/ml) was demonstrated 1 hour after an intramuscular administration of aminosidine chloride in a dose of 355 mg (equivalent to 500 mg of aminosidine sulfate), and there was no detectable agent in the blood after 24 hours, a total urinary excretion being accumulated 148. 8 mg (41. 8%) within 24 hours. A remarkable high concentration of the agent was detected in the bile, i. e. 88. 5 mcg/ml 1 hour and 13. 5 mcg/ml 12 hours following a systemic use of the agent in the same dose.
A laboratory investiga tion on antibacterial activity of aminosidine chloride against various bacteria isolated from infected lesions in the field of surgery revealed that i) 28 (87. 5%) of 32 strains of E. coil were inhibited their growth, ii) 11(44%) of 25 strains of Proteus group, and, iii) 28 (93. 3%) of 30 strains of Klebsiella group by aminosidine less than 8. 9 mcg/ml, and, iv) all the 28 strains of Staphylococcus aureus less than 4. 44 mcg/ml, while all the 24 strains of Pseudomonasa eruginosaw ere not inhibited by aminosidine less than 8. 9 mcg/ml.
Seven of 10 patients with v arious infections responded excellently or fairly good to a systemic use of the agent without any significant untoward side effects.

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Studies were made on the in-vitro antibacterial activity, blood level, elimination rate in urine and bile level of aminosidine.
Clinically, aminosidine was found to be effective to some of the cases of surgical infections.

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Aminosidine, a new broad spectrum antibiotic, was studied in the department of gynecology. High concentration of aminosidine was detected in urine and in amniotic fluid, but in lo w concentration in mother's milk after injection.
Clinically, aminosidine w as tried on 14 cases of cystitis and on 17 cases of genital infections. The drug was found to be very effective to cystitis, metroendometritis and salpingitis, but not effective to mastitis.
As to the side effects, toxicodermia was found in 1 case, but it disappeared in a few days.

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Aminosidine, an antibiotic of basic glucoside, was used in the treatment of gynecological infections, especially to the cases of serious urinary infections which tend to occur rather frequently after the operation or under the radio-therapeutic treatment of uterine cancer.
It was proved that aminosidine was considerably effective to all the cases except to the infections due to Pseudomonas.

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In many cases, minimum inhibitory concentration of aminosidine was as high as 0. 78 mcgiml to Staphylococcuasu reus. The distribution of MIC was ranged from 3. 12 to 12. 5 mcg/ml to E. coli an d from 3. 12 to 50 mcg/ml to Klebsiella.
Blood concentration reac hed the peak one hour after intra-muscular injection of 500 mg of aminosidine. The concentration was as high as 16. 6 mcg/ml. Transition into umblical blood and milk was satisfactory. Blood concentration of new born reached the peak after one hour too, and it was as high as 51. 5∼62. 5 mcg/ml.
Aminosidine was cl inically used to 17 cases of intra-pelvic infection and urinary-passage-infection, etc. A result was obtained that aminosidine was effective in 14 cases (82. 3%). Significant side effect was not observed.

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Studies were made on the fundamental and clinical characteristics of aminosidine by applying it to the cases of urinary infections. The MIC value of a minosidne to each strain of the pathogenic bacteria was almost the same with that of kanamycin except to the 2 strains of Providencia. It was also found that aminosidine have cross resistance with kanamycin.

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Clinical investigations of aminosidine with its antibacterial in vitro activities vv-re carried out on 22 cases including 15 cases with pyelonephritis, 2 with renal tuberculosis and 5 after surgeries.
The results were summarized as follows:
1) Patients recieved 500 mg of aminosidine intramuscularly. The highest peak of urine levels was 3, 200 mcg/cc, reached in 1 hour after the administration. The concentration of aminosidine in the blood stream was the highest in 30 minutes and 1 hour. 282 CHEMOTHERAPY FEB. 1968 The level was 12. 8 meg/cc.
2) Antibacterial in vitro activities against Staphylococcus were from 0. 4 to 1. 6 m cg/cc, E. coli, from 2. 5 to 6. 3 mcg/cc, Proteus vulgaris, 3. 2 mcg/cc, Pseudomonas, 100 meg/cc, Klebsiella, 2. 5 mcg/cc.
3) Clinical experience of 22 cases treated with aminosidine was as follows: Good response was found in 8 out of 10 cases with acute pyelonephritis, 4 out of 5 chronic pyelonephritis, 2 out of 5 cases with septic wounds following abdominal operations, 1 out of 2 renal tuberculosis.
4) Bacteriologically, while remarkable response to aminosidine was found in 6 out of 7 cases with Staphylococcus, all 3 cases with Klebsiella, 4 out of 5 cases with E. coli, and I out of 2 cases with Mycobacterium, l ittle response was found in a case with Proteus and Pseudomonas eachrespective ly.

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In our clinic, aminosidine was administered to patients with various urinary tract infections and observations on clinical effects as well as basic experiments were performed.
With 350 mg intramuscular injection, the blood concentration reached to the maximum level in 1 hour. The urinary concentration rate after 350 mg intramuscular injection was 64. 2 % in 8 hours.
Using agar plate dilution, , sensitivity of Staphylococci and E. coil against aminosidine was meas ured. The sensitive levels of concentration were seen in a little high concentration area.
Sixteen patients with various urinary tract infections were treated with ami nosidine, a single dose of 350 mg or 700 mg was administered intramuscularly for 4 to 14 days. In 4 cases of acute urinary tract infections, aminosidine was highly effective in all cases.
In chronic urinary tract infections, consisted of 9 cases chronic cystitis, 1 case of chronic pyelonephritis and 2 cases of chronic urethritis, aminisodine was effective in 8 cases.
No subjective side effect was observed in all cases, but hypofunc tion of kidney was observed in 2 cases.

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Aminosidine was tried on the 44 cases of urinary infections, 90. 9% of which obtained effective results. The in vitro antibacterial activity of aminosidine was almost the same with that of KM. E. coli was found to be most sensitive against this drug when the concentration of the drug was 3. 12 mcg/ml.

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On the clinical application, we used the drug for cystitis, pyelonephritis and other urological infections.
About 73% of simple infections such as cystitis and about 50% of rather complicated infections such as neurogenic bladder and post-operative pyelonephritis obtained effective results.
No significant side effect was observed. About 48 strains were exmined fo r disc sensitivity. Arninosidine and kanamycin were considered to have almost equal sensitivity.
Using biophotometer, growth inhibitory activity of the drug a gainst E. soli was studied.

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Aminosidine (AMD) was studied experimentally and clinically. The following data were obtained.
1) In vitro antibiotic activity: The sensitivity to AMD of 77 strains of coagulase positive Staph. aureus obtained from pyodermas (chiefly deeper) was studied with plate dilution method. MIC was ≤0. 39 against 16, 0. 78 against 27, 1. 56 against 14, 3. 13 against 14, 6. 25 against 1, 12. 5 against 1 and 100 mcgiml <against 4 strains. The 4 strains resistent to 100 mcg/mI of AMD, 3 resisted 100 mcg/ml of KM, SM and FRM, but the other did the same MIC of SM and 25 mcg/m1 of KM and FRM.
2) The serum levels were followed after intramusc ular injection of 350 mg of AMD in 5 persons. The mean values at 15, 30 minutes, 1, 2, 3 and 5 hours were 10. 26, 12. 04, 10. 28, 7. 57, 3. 27 and 1. 24 nice ml. After intramuscular injection of 50 mg of AMD in 3 rabbits the skin and serum concentrations were most dense at 30 minutes and 1 hour.
3) Clinical evaluation: AMD wa s used in 13 cases of skin infection. Of these, 11 cases showed beneficial results. The drug was tried for the prevention of postoperative infection in 10 cases at skin surgery. A good preventive effect was obtained.

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Aminosidine was clinically applied to 30 cases of dermatological infections.
Effective results were obtained in the cases of impetigo, but the results were ineffective in the cases of furuncle or folliculitis and some chronic pyodermas.
It does not seem that aminosidine can be an excellent drug so far as dermatological infections are concerned.

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Following results were obtained by our fundamental and clinical studies of aminosidine (AMD).
1. The in vitro antibacterial activity of aminosidine was similar tothose of erythromycin and kana. mycin when the sensitivity distribution of aminosidine was compared with those of other antibiotics. However, when studies were made more precisely, the sensitivity of each strain against aminosidine was found to be especially close to each of their sensitivity against kanamycin.
2. Aminosidine was clinically applied to 19 cases of various sk in infectious diseases. Of these 19 cases, effective therapeutic results were obtained in 13 of the 15 cases of pyoderma, the 2 cases of disseminated miliary lupus on face, each of the one case of varioliform acne and mycetoma.
No noticeable side effects were observed.

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Bacterial and clinical experiments for ophth almic use of aminosidine (AMD) were performed, and the results summarized as follows.
1) Minimum growth in hibitory concentration of AMD was 0. 07 mcg/ml for K-W bacillus, 0. 18∼0. 35 mcg/ml for M-A bacillus, 3. 55∼35. 5 mcg/ml for Pneumococcus, 0. 35 mcg/ml for C. diphtheriae, 0. 35 m cg/ml for Gonococcus, 35. 5 mcg/ml for Streptococcus, 0. 18∼0. 71 mcg/ml for Staphylococcus and 35. 5∼71 mcgiml for Pyocyaneus.
2) The distribution of the sensitivity for 42 strains of Staph. aureus isolated in 1966 was in the range of ≤0. 07- ≥71 mcg/ml, and majority of them (92. 9) were in <3. 55 mcg/ml.
3) The concentration in the blood by intramuscular injection of a single dose 0. 35 g reached the highest after 1 hour and decreased gradually until 12 hours.
4) After instillation of 1% AMD eye-drops, the con centration was found in the tissue of the outer parts of the rabbit eye. After 15 mg subconjunctival injection, the concentration was obtained not only in the tissue of the outer segment, but also in the inner parts of the eye. After the intramuscular injection of AMD in a dose of 35. 5 mg/kg, the concentration was recognized in the outer and inner parts of the eye.
5) Intram uscular injection of 0. 35 g AMD 1 or 2 times daily revealled excellent effects on 12 cases of hordeolum caused by Staphylococcus, 4 cases of lid abscess, I case of dacryocystitis and corneal ulcer by Pneumococcus, and 2 cases of preventive application against post-removal of foreign body on the cornea.
6) Side effects: Some of patients experienced slight pain on injection, but any other severe side effects were not noticed.

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The results of the clinical application of AMD to the case of oto-rhino-laryngological infections were as follows.
1. AMD in the concentration of 0. 8 mcg/ml was the strongest in its antibacterial activity.
2. Of 30 cases treated with AMD in this department, 20 cases obtained remarka bly effective result, while 5 cases obtained fairly effective and the other 5 cases had no effective result.
3. Side effects were not observed when AMD was administered about 5 g in tot al. And trouble in hearing regarded as the side effect was not observed at all.

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