Antibacterial activities were determined and pharmacokinetics and a clinical studies were performed on biapenem (L-627), a novel parenteral carbapenem antibiotic, in infections in children. The ...following results were obtained: 1. MICs of L-627 against clinical isolates were as follows: Among Gram-positive bacteria, MICs were 0.78 microgram/ml to > 100 micrograms/ml against 3 strains of methicillin-resistant Staphylococcus aureus (MRSA), and 0.10 microgram/ml to 0.39 microgram/ml against 8 strains of methicillin-sensitive S. aureus (MSSA), MICs against 5 of them were similar to those of imipenem (IPM), and MICs against 3 of them were slightly higher than those of IPM. MICs were < or = 0.025 microgram/ml to 0.39 microgram/ml against 7 strains of Streptococcus pneumoniae, and were similar to those of IPM, and lower than those of ceftazidime (CAZ) and piperacillin (PIPC). Among Gram-negative bacteria, MICs were 0.78 microgram/ml and 3.13 micrograms/ml against 2 strains of Haemophilus influenzae, and were similar to those of IPM. 2. Maximum plasma concentrations determined by the bioassay method after intravenous infusion of L-627 over 30 minutes at doses of 6.0 and 12.0 mg/kg, respectively, in 2 different pairs of 2 children each (total 4 cases) were observed upon completion of the treatment. Maximum concentrations at a dose of 6.0 mg/kg were 28.8 micrograms/ml and 24.6 micrograms/ml, and at a dose of 12.0 mg/kg were 65.4 micrograms/ml and 39.6 micrograms/ml, exhibiting a dose response. Plasma half lives in the beta phase were 0.97 and 1.20 hours at 6.0 mg/kg, and 0.72 and 0.94 hour at 12.0 mg/kg. Plasma concentrations determined by the HPLC method were lower than those determined by the bioassay. 3. Urinary excretion rates in the first 5.5 hours after the 6.0 mg/kg dose were 81.4 and 75.3%, and after the 12.0 mg/kg dose were 91.0 and 73.8%, and these values were higher than those obtained using HPLC. 4. Concentrations of L-627 in cerebrospinal fluid were determined in 2 cases of purulent meningitis. In one case, 30.3 mg/kg of L-627 was infused intravenously over 30 minutes and concentrations on days 1, 3, 7 and 14 observed at 60, 60, 45 and 45 minutes after respective dosages were 7.60, 1.30, 1.42 and 0.38 microgram/ml. Cerebrospinal fluid-plasma concentration ratio was determined on days 7 and 14 to be 5.5 and 1.2% respectively.(ABSTRACT TRUNCATED AT 400 WORDS)
An investigation was done on the permeation of drug through the model membrane consisting of Millipore filter saturated with an oil, indicating that the method employed here might be satisfied for ...obtaining the permeation curve with an excellent reproducibility. The theoretical treatment of the data obtained by this method proved that the permeation of drug through the present system depended on the diffusion mechanism. The ionized molecules of salicylic acid and aminopyrine did not permeate through the membrane. The temperature dependence of the permeation was well expressed by Stokes-Einstein's equation concerning diffusion constant. The experiment using different oils showed that the permeability constant increased with the increase in distribution constant in oil and decreased with the increase in viscosity of oil. Actually, the apparent permeability constant increased proportionally with the increase in distribution constant in oil, and decreased with the increase in the viscosity of the oils used.
Pharmacokinetic, bacteriological and clinical studies on SY5555, a new oral penem, were carried out, and the following results were obtained. 1. MICs were determined for 6 drugs, SY5555, clavulanic ...acid/amoxicillin (CVA/AMPC), cefaclor (CCL), cefotiam (CTM), cefpodoxime (CPDX), cefdinir (CFDN) against 20 strains of bacteria isolated from patients who were subsequently treated with SY5555. MICs of SY5555 for Gram-positive cocci ranged from 0.05 to 0.10 microgram/ml against 10 strains of Staphylococcus aureus. The MIC was < or = 0.025 microgram/ml against one strain of Streptococcus pyogenes, and MICs were from < or = 0.025 to 0.39 microgram/ml against Streptococcus pneumoniae. These MIC values were equivalent or superior to those of the other 5 drugs. MICs of SY5555 for Gram-negative bacilli were 0.39 and 6.25 micrograms/ml against Haemophilus influenzae, and these values were equivalent to those of the other drugs, except CPDX. The MIC of SY5555 was 0.39 microgram/ml against 2 strains of Escherichia coli, and this value was equivalent or superior to those of CVA/AMPC and CCL, similar or inferior to those of CPDX and CFDN, and inferior to that of CTM. The MICs of several drugs were determined for 10 strains of Bordetella pertussis and 30 strains of Campylobacter jejuni isolated from patients before this clinical study. The MICs of SY5555 against the 10 strains of B. pertussis were compared with those of 7 drugs, CCL, CTM, CPDX, ampicillin (ABPC), piperacillin (PIPC), imipenem (IPM) and erythromycin (EM). The MIC of SY5555 was 0.78 microgram/ml against all of the strains. This value was superior to those of CCL, CTM and CPDX, similar or inferior to that of IPM and inferior to those of PIPC and EM. The MICs of SY5555 against the 30 strains of C. jejuni were compared with those of 7 drugs. CCL, CTM, CPDX, CFDN, ABPC, IPM and EM, and the MIC of SY5555 was < or = 0.025 microgram/ml or 0.05 microgram/ml and these values were equivalent or superior to those of the 7 reference drugs. 2. SY5555 dry syrup was administered orally at 30 min. after meals, to a total of 5 patients, at doses of 5.0 and 10.0 mg/kg to 2 patients each and at a dose of 15.0 mg/kg to one patient and the plasma concentrations were determined. Peak concentrations were detected 1 to 3 hours after administration in all patients and the peak concentrations were 0.93 and 1.21 micrograms/ml at the 5.0 mg/kg dose, 2.85 and 5.49 micrograms/ml at the 10.0 mg/kg dose and 5.79 micrograms/ml at the 15.0 mg/kg dose.(ABSTRACT TRUNCATED AT 400 WORDS)
A CLINICAL STUDY ON NOISE DEAFNESS ZUSHO, HIROYUKI; TAKEUCH, MINAKO; NAKAJIMA, JIN ...
Nippon Jibi Inkoka Gakkai Kaiho
85, Številka:
5
Journal Article
Recenzirano
Odprti dostop
The relationship between the pneumatization of the temporal bone and progress of noiseinduced deafness was studied in 328 patients with noise-induced deafness. The results obtained were as follows: ...1) The size of pneumatization as measured by the rectangular method on the X-ray films averaged 19.6cm2. 2) The difference in hearing between right and left ear was examined in each frequency and in average hearing threshold level. There was a similar tendency through frequencies tested. 3) The difference in the size of pneumatization between right and left ear was compared with that in the hearing loss, and it revealed that the difference in the development of pneumatization between the right and left was clearly conspicuous. 4) The correlation between the area of the development of pneumatization and the average hearing threshold was examined statistically in all ears. No correlation was observed between the two. 5) The development of the pneumatization was divided into three groups, i. e., large, medium and small. The average hearing threshold level measured by the hexagonal method in these groups and the significant difference between the groups were found. As a result, a significant difference was noted between the large group and small group or between the medium group and small group. 6) The results obtained under5) were examined as to each frequency. All frequencies showed results almost similar to those with the average hearing threshold level measured by the hexagonal method. But results at 4kHz were not particularly different from those at other frequencies. The results above suggested that the development of pneumatization of the temporal bone would exert somewhat inhibitory action on the advance of noiseinduced deafness.
Both ALDECIN Nasal and Polaramine were markedly effective when used in perennial allergic rhinitis. ALDECIN Nasal was superior to polaramine in the success rate and utility rate. Moreover, fewer side ...effects were observed with ALDECIN Nasal. Patients with severe symptoms, such as rhinorrhoea and nasal obstruction, who did not respond to antihistamine and found difficulty in life due to the side effect, drowse should be given ALDECIN Nasal in preference to polaramine. ALDECIN Nasal showed superior sustained effects to polaramine.
Intranasal beclomethasone dipropionate was given to 245 patients with perennial nasal allergy for a week in 17 institutions. The optimum dose, clinical effects and safety of the drug were studied. 1. ...One puff into each nostril four times a day (400μg) was more effective than one puff twice a day (200μg) in adults. In children, the efficacy of one puff twice a day (200μg) was comparable to that of one puff four times a day in adults. Overall improvement rate was 81.2% with four doses a day (400μg) and 58.6% with two doses a day (200μg) in adults. Children showed overall improvement in 76.2% with two doses a day (200μg). 2. The efficacy was confirmed by doctor's evaluation, questionnaire filled out by patients, patients daily records, and clinical data of rhinoscopy, examination of nasal eosinophils and nasal provocation test. 3. Almost no side effects except local irritation (9.7%) were observed and they were slight, if any. Plasma cortisol levels did not change before and after treatment. Thus, high usefulness was obtained; i. e, 77.0% with four doses a day and in 51.7% with two doses a day for adults and in 76.2% with two doses a day for children.
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