Susceptibilities of clinical isolates of Streptococcus faecalis and S. faecium were determined using Mueller Hinton medium from different sources. Marked differences occurred between CXM, CTX, CZX, CMX, CTRX or CAZ and the other cephems in MICs, which were determined by the agar dilution method with Eiken medium and the other media including Difco medium. With Eiken medium, the majority of S. faecalis strains tested appeared to be susceptible to the abovementioned cephems, all having the oxyimino group at the 7-acyl position, whereas with Difco medium the strains of S. faecalis were resistant to the cephems. A similar tendency was found with CTX, CTRX and CMX in the susceptibility test of S. faecium.
The antibacterial potency of CZX, a typical 7-oxyimin derivative, remained unchanged after 24h incubation in Difco medium with or without S. faecalis.
The relationship between the in vitro and in vivo activities of CTX against intraperitoneal infection in mice after a heavy challenge with bacteria was investigated.CTX was not effective against the same 3 strains for which the MICs differed the most markedly according to the type of media.
The results indicated that the in vitro activity of the oxyimino cephems determined in Difco midium was better correlated with the in vivo activity than that determined in Eiken medium.

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The present study was undertaken to investigate the effects of cephalothin (CET), cephalexin (CEX), and 7-aminocephalosporanic acid (7-ACA) on the contractile response of guinea-pig urinary bladder.
CET, CEX, and 7-ACA in the concentration of 1×10^-5g/ml-1×10^-4g/ml had no effect on the transmural electrical stimulation-induced contractile responses.These agents in the concentration of 1×10^-3g/ml slightly reduced them as 97±3%(n=12), 97±2%(n=10), and 97±3%(n=14) of the controls, respectivdy.These ageats in its concentration, however, had no effect on the contractile responses whether induced by exogenous acetylcholine (1×10^-4g/ml) and KCI (40mM) or spontaneously induced.From these results, it may be concluded that these agents very slightly affect the intramural excitatory nerves of urinary bladder, while they don't affect the muscle in the urinary bladder wall.It is also considered that the effects of these agents on the contractile responses of urinary bladder are extremely weak.

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For the purpose of investigating the effects of non-steroidal anti-inframmatory agents (NSAIA) on the chemotherapy for acute infections, we had some experiments with mice and got the results as follows;
1) The therapeutic activities of an antibiotic (cefmetazole;CMZ) in experimental intraperitoneal infection systems caused by 4 strains of 3 bacteria was enhanced by phenylbutazone (PB) and was suppressed by indomethacin (IDM).Mefenamic acid was found to have weak enhancive effects.
2) The elimination of intraperitoneally challenged E. coli No.704 from peritoneal cavity or circulations by CMZ was quickened or suppressed by the co-administration of PB or IDM respectively.
3) The single-administration of PB or IDM resulted in the quickened growth of challenged E. coli in mice and also resulted in the decrease of LD₅₀ value.
4) Exudation of neutrophils into peritoneal cavity of infected mice and the phagocytosing activity of macrophages or neutrophils were not suppressed by PB or IDM.
5) Luminol-dependent mouse leukocyte chemiluminescence was significantly suppressed in the presence of 10μg/ml of PB or 1μg/ml of IDM.
6) Urinary excretion of CMZ was suppressed by the co-administration of PB to result in the rise of serum concentration of CMZ.
7) Protein-binding ratio of CMZ in mouse serum was decreased under the existence of PB.
When NSAIA was co-administered with CMZ for the therapy of infection, some NSAIA exhibited the activity which resulted in suppression of the effect of CMZ and some exhibited several activities at the same time.These activities resulted in entirely adverse influences each other against the effect of CMZ.Suppressive activity seemed to be caused by the suppression of bacteria-killing activity of leukocytes coming from the suppression of the production of leukocyte active-oxygen.The enhancing effect seemed to originate in the suppression of urinary excretion of CMZ resulting in the rise of serum concentration.

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The transport of cefmenoxime, a cephalosporin antibiotic, into three kinds of exudates (exudate from excoriated skin, exudate from burn wounds, and burn blister fluid) from blood was studied on 37 burn patients after they were given an intravenous bolus of 50mg cefmenoxime per kg body weight.Concentrations of cefmenoxime in serum and in the above exudates or fluid were determined by bioassay.Concentrations of cefmenoxime in serum reached 189±29.7μg/ml (mean±SD) 15min after administration, decreasing to 4.8±1.3μg/ml at 8 hr.Peak concentrations of the antibiotic in exudates from burn wounds and excoriated skin and in blister fluid of burn patients were all found at 1 hr. Calculated by a two-compartment open model, the half-life of the elimination phase (t_1/2(β)) was 1.53hr;volume of distribution (V_dβ), 0. 331/kg;and area under the curve (AUC), 346μg·hr/ml. Cmax (maximum concentration), T_max (time of maximum concentration), and apparent transport ratios (F: k₁v₂/k₂v₃) for exudates from excoriated skin, exudates from burn wounds, and burn blister fluid were 34.9, 19.7, 22.9μg/ml 1.39, 1.47, 2.03h;and 0.47, 0.28, 0.43, respectively.

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1) The concentration of mezlocillin (MZPC) in serum and bile was estimated after drip infusion of 29 of the drug in 8 patients, who have performed cholecystectomy, choledochotomy and T-tube drainage for gallstone diseases or PTC-drainage. Administration of ampicillin (ABPC) 2 g was cornpared by the crossover method.
2) After 2 g drip infusion of MZPC, the mean serum concentration was 142.5±99.0μg/ml at 15 mln, 56.4±20.17mu;g/ml at one hour, 16.9±6.6 μg/ml at 3 hours. The maintenance period of serum conceutration was inclined to be equal in MZPC with in ABPC.
3) After 2 g drip infusion of MZPC, the mean bile concentration reached to 1, 136.4±895.4 μg/ml in 2 hours and it was maintained as high as 1, 008.6±938.3 μg/ml even after 3 hours.On the other hand, after 2 g drip infusion of ABPC, the mean bile concentration was only 20.9±21.7 μg/ml in 3 hours and was low level in the progress.
4) As compared with the highest concentration of MZPC and ABPC in same patient.the mean bile concentration of MZPC (1, 275.7±980.0 μg/ml) was about 50 times higher than that of ABPC (25.5±20.7μg/ml).
5) Minimum inhibitory concentration (MIC) of ABPC in the group of gram-positive cocci was from 0.1 to 3.13μg/ml, MIC of MZPC in that group was from 0.78 to 6.25 μg/ml.But MIC of ABPC in the group of gram-negative bacilli was from 0.78 to over 100 μg/ml, MIC of MZPC in that group was from 1.56 to 100 μg/ml.The value in MZPC was lower than that in ABPC at gram-negative bacilli.
No side effects was seen in all patients.

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The concentration of CMX in various tissues of the urogenital system after a single i.v.injection of 0.5 g or 1.0 g was investigated.The results were as follows.
1) 11 renal tissues of 10 patients were obtained between 60 and 180 minutes after CMX administration. CMX concentration ranged from 11.8 to 227 μg/g (mean value 58.9 μg/g).The tissue/serum concentration ratio (T/S), ranged from 1.8 to 42.9 (mean value 9.5), was higher than other urogenital tissues.
2) The T/S concentration ratio of 6 testes ranged from 0.2 to 1.9 (mean value 1.0).
3) The T/S concentration ratio of 6 epididymides ranged from 0.1 to 0.7 (mean value 0.4). High penetration was observed in case of sever epididymitis.
The high CMX concentrations found in serum and urogenital tissues lead us to expect successful therapy when CMX is used to treat bacterial infections with sensitive pathogens in the urogenital tract.

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The indicators and the criteria of postoperative surgical infections were studied in 132 patients undergoing cholecystectomies for cholecystolithiasis, choledocholithiasis and cholecystopolyp, who received cefotiam as a prophylactic antibiotics;1g intravenous drip, twice daily for 5-7 days after operations.
Four of the 132 patients had postoperative infections: intraabdominal infection in 2, superficial wound infection in 1 and urinary tract infection in 1 patient.
There were significant differences between four patients with infections and 128 patients without infections in maximum body temperature, the fever index, leucocytosis, erythrocyte segmentation rate and CRP.
The results suggest that more than 38.0°C maximum body temperature, more than 8.0 fever index, more than 10, 000 leucocytosis, more than 50mm/hr ESR and more than 3+ CRP are thought to be the signs and criteria as the indicators of infections.

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