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Biomedical subjects

R Fujii

Publications and source records attributed to R Fujii.

At least 19 recordsLinked to original sources
PubMed1992

Potentiation of the vincristine effect on P388 mouse leukemia cells by a newly synthesized dihydropyridine analogue, PAK-200.

A newly synthesized dihydropyridine analogue, 2-[benzyl(phenyl)amino]ethyl 1,4-dihydro-2,6-dimethyl-5-(5,5-dimethyl-2-oxo-1,3,2-dioxaphosphorina n-2-yl)-1- (2-morpholinoethyl)-4-(3-nitrophenyl)-3-pyridinecarboxylate (PAK-200), at 1 microM completely reversed the resistance to vincristine in vincristine-resistant P388 mouse leukemia cells (P388/VCR), in vitro. PAK-200 at 2 microM inhibited the efflux of [3H]vincristine from P388/VCR and increased the accumulation of [3H]vincristine in P388/VCR to a level similar to that in P388 cells. P-Glycoprotein in membrane vesicles from P388/VCR cells was photolabeled with [3H]azidopine. The labeling was completely inhibited by 10 microM PAK-200. The calcium antagonistic activity of PAK-200 was about 1000 times lower than that of another dihydropyridine analogue, nicardipine. Experiments with P388 and P388/VCR-bearing mice showed that PAK-200 enhanced the effect of vincristine on both leukemia cells in vivo. These results suggest that PAK-200 interacts with P-glycoprotein and reverses drug resistance in P388 mouse leukemia cells in vitro, and that PAK-200 has an ability to potentiate the effect of vincristine on P388 mouse leukemia cells in vivo.

Animals↗
PubMed1992

Plasma cells in the spleen of the Aleutian skate, Bathyraja aleutica.

Splenic white pulp of the Aleutian skate (Bathyraja aleutica), an elasmobranch, was investigated using light and transmission electron microscopy. The major cellular constituent was plasma cells, of the typical Marshalko type, characterized by well developed rough-endoplasmic reticulum and a Golgi complex. The morphology of the rough-endoplasmic reticulum was variable, being lamellar in some cells and spherical in others. Plasma cells with distended cisternae of rough-endoplasmic reticulum and cells with Russel bodies were often observed. Only a small number of lymphocytes were encountered. These findings indicate that the splenic white pulp is the major site for immunoglobulin production in this fish, thus confirming our previous immunocytochemical observation. Globules presumably containing immunoglobulin were found consistently associated with the Golgi complex. The secretion mechanism of immunoglobulin by plasma cells is discussed in connection with the globules.

Animals↗
PubMed1992

Membrane trapping of carbon-11-labeled 1,2-diacylglycerols as a basic concept for assessing phosphatidylinositol turnover in neurotransmission process.

The uptake mechanism of 1,2-[11C]diacylglycerols (DAG) was studied and its use as a probe for the measurement of phosphatidylinositol (PI) turnover was verified. A method of synthesis for producing rac-1,2-[11C]DAG using [11C]ethylketene was developed to label the 1- or 3-hydroxyl group of 2-monoacylglycerol. After intravenous injection, these tracers were metabolized rapidly in the rat brain cortex to phosphatidic acids, phosphatidylinositols and phosphatidylinositol phosphates. The brain cortex anesthetized by barbiturate, which represents inhibited state of synaptic transmission, did not produce differences in uptake values between sn-1,2-[11C]DAG and rac-1,2-[11C]DAG. However, in the liver, lung, and pancreas under the same conditions, the uptake values of rac-1,2-[11C]DAG were higher than those of sn-1,2-[11C] DAG, in which the labeling position was on the 2-hydroxyl group in the sn type. These findings suggest that the lipase activity in the brain should be disregarded because lipase predominantly hydrolyzes the 1- or 3-position of rac-1,2-[11C] DAG, which should be the main factor producing the differences in uptake values in other organs. Cholinergic stimulation prompted accumulation of 1,2-[11C]DAG in the conscious rat brain. In conclusion, sn-1,2-[11C]DAG, administered even in the racemic mixture, could serve as a tracer that becomes mixed with receptor-linked PI turnover and could accumulate in the brain based on the membrane trapping mechanism.

Animals↗
PubMed1992

Triacetin as food additive in gummy candy and other foodstuffs on the market.

The qualitative and quantitative analytical methods were proposed for the simple and rapid determination of triacetin (TAc) in commercial gummy candies and other foodstuffs by gas chromatography (GC), thin layer chromatography (TLC) and infrared spectroscopy (IR). Each extract from the samples was obtained by pretreatment of the foodstuffs as follows: (A) Gummy candy was dissolved in warm water and the solution was extracted with chloroform. The organic (chloroform) layer was separated. (B) Samples (such as ice cream) containing substantial water were mixed with anhydrous Na2SO4 and stirred to sandy appearance and dried. The residue was homogenized with ether, followed by centrifuging, and the organic (ether) layer was separated. (C) Dried samples (such as chocolate and cookie) were smashed, homogenized with ether, and followed by centrifuging, and the organic (ether) layer was separated. (D) Candy was dissolved in warm water and the solution was extracted with ether. The organic (ether) layer was separated. Each organic layer from (A)-(D) was washed with 10% NaHCO3 and evaporated. The residue containing TAc was dissolved in dichloromethane. The extract obtained was subjected to column chromatography on silica gel. The fractions containing TAc were employed in GC with 25% PEG-20M column, TLC, and IR analyses. Recovery of TAc from gummy candy was 99.1 +/- 3.0% and those from other foodstuffs ranged from was 82.1 to 99.4% by GC. Detection limit by this method was 10 ppm. TAc was found to contain at a level as high as 550 ppm in one domestic gummy candy. On the other hand, one imported gummy candy contained no more than 20 ppm of TAc gummy candy.

Beverages↗
PubMed1992

[Overall clinical evaluation of cefprozil against infections in pediatric fields. Pediatric Study Group for Cefprozil].

Cefprozil (CFPZ, BMY-28100) granule preparation was studied for pharmacokinetic, bacteriological and clinical aspects in the pediatric infections. The results obtained are summarized as follows: 1. Serum concentrations and urinary excretion. The pharmacokinetics of CFPZ in pediatrics was investigated by single oral administration of fine granules at doses of 4.0, 7.5 and 15.0 mg/kg. Peak blood levels of CFPZ were 3.06, 4.62 and 9.65 micrograms/ml, respectively, at 1.00-1.30 hours after each dose and AUCs were 7.44, 12.50 and 27.01 micrograms.hr/ml, respectively. These data showed that Cmax and AUC depended on dose levels. T 1/2 (beta) at these dose levels were 1.03, 0.94 and 1.01 hours, respectively. There were no differences related to dose. Urinary recovery rates in the first 6 hours after administration were 51.5-57.1%. The pharmacokinetics of CFPZ before or after meals were also investigated at a dose of 7.5 mg/kg. Peak blood levels were 4.88 micrograms/ml at 1.17 hours after administration in the fasting state, and 4.30 micrograms/ml at 1.54 hours after administration in the non-fasting state. Delay of Tmax and slight decrease of Cmax were observed in the non-fasting state, but T 1/2 and AUC were 0.91 hour and 12.96 micrograms.hr/ml, respectively, in the non-fasting state, and were similar to those in the fasting state, 0.93 hour and 12.82 micrograms.hr/ml, respectively. Urinary recovery rates in the first 6 hours after administration were 63.8% in the fasting state and 50.7% in the non-fasting state. 2. Clinical results. Clinical efficacies of CFPZ granules in various infectious diseases were studied in 804 cases. Twenty nine cases, mostly viral or mycoplasmal infections, were excluded from the statistical analysis. The clinical efficacy rate in 527 cases with causative bacteria isolated was 97.2%; and in 248 cases from whom no significant isolate had been obtained was 96.0%. The clinical efficacy rate in 475 cases with monobacterial infections (proven by culture of isolates) was 97.3%, and that in 52 case with polybacterial infections was 96.2%. Haemophilus influenzae was isolated mostly from acute respiratory infections. In 88 cases from whom H. influenzae was isolated, clinical efficacy rate was 95.5%. In cases from whom H. influenzae was found concomitant by with Staphylococcus aureus, Streptococcus pyogenes or Streptococcus pneumoniae, the clinical efficacy rates were also high. The bacteriological eradication rate in cases with 582 strains was 83.3%; the eradication rate for Gram-positive organisms was 95.8%; and for Gram-negative organisms, it was 64.2%.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1992

[Pharmacokinetic and clinical studies with meropenem in the pediatric field. Pediatric Study Group of Meropenem].

Pharmacokinetic and clinical evaluations in pediatrics were made on meropenem (SM-7338, MEPM), a new parenteral dehydropeptidase-1 stable carbapenem used without any inhibitors, at 33 medical institutions. The results are summarized as follows. 1. Pharmacokinetic studies. MEPM at a dose of 10, 20, or 40 mg/kg was administered to 53 children by 30-minute drip infusion. Peak plasma concentrations (Cmax's) and plasma half-lives (T1/2's) of these doses were 28.5, 47.2 and 130.0 micrograms/ml, and 0.80, 0.93 and 0.94 hours, respectively. A clear dose response was observed in Cmax's and T1/2 values were quite similar to those observed in adults. In the first 6 hours after administration, 54.4 to 68.1% of the administered drug was recovered in urine. The cerebrospinal fluid (CSF) levels of MEPM in patients with purulent meningitis were 0.13 microgram/ml at a dose of 6 mg/kg, and 0.64 to 4.22 micrograms/ml at a dose of 29 to 44 mg/kg within day 4 of onset. The penetration rate of MEPM showed an intermediate value among those for other cephalosporin antibiotics. 2. Clinical study. Clinical efficacies of MEPM were evaluated in 389 cases. The most common doses used were 10 to 20 mg/kg/once, 2 to 3 times a day. The maximum dose was 173 mg/kg/day q.i.d. MEPM gave "excellent" or "good" responses in 242 (97.6%) out of 248 cases in which causative organisms were documented and in 134 (95.0%) out of 141 cases in which causative organisms were not identified. Clinical efficacy rates were 100% in 11 patients with purulent meningitis, 85.7% in 7 with septicemia, 98.8% in 173 with pneumonia, and 100% in 65 with UTI. Bacteriologically, 260 strains (96.7%) out of 269 strains were eradicated by MEPM treatment. Eradication rates were 89.2% for Staphylococcus aureus (37 strains) and 100% for Streptococcus pneumoniae (35 strains). The overall eradication rate for Gram-positive bacteria was 94.6%. Among Gram-negative bacteria, 98.3% out of 172 strains were eradicated. The eradication rate of Haemophilus influenzae (73 strains) was 98.6% and Pseudomonas aeruginosa (11 strains) was 90.9%, and all of Branhamella catarrhalis (15 strains), Escherichia coli (42 strains), and Klebsiella pneumoniae (6 strains) were eradicated. Out of 84 cases for which previous antibiotic therapies of 3 days or longer were not successful, MEPM gave "excellent" or "good" responses in 77 cases (91.7%) and excellent bacteriological responses (95.7%).(ABSTRACT TRUNCATED AT 400 WORDS)

Bacterial Infections↗
PubMed1992

[Pharmacokinetic, bacteriological, and clinical studies on panipenem/betamipron in children].

Pharmacokinetic, bacteriological and clinical studies were performed on panipenem/betamipron (PAPM/BP) in children. The results are summarized as follow: 1. Twelve patients with various bacterial infectious diseases were treated with PAPM/BP. Each dose was 20 mg/20 mg/kg, administered 3 times daily, in 30-minute intravenous drip infusion. Treatments were continued for 5-22 days. Clinical efficacies of PAPM/BP in 12 patients with bacterial infections (1 with suspected sepsis, 5 with pneumonia, 1 with acute maxillary sinusitis, 2 with acute otitis media, 1 with cervical abscess and 2 with urinary tract infection complexed type) were evaluated as excellent in 7, good in 4 and fair in 1, with an efficacy rate of 91.7%. Seventeen causative organisms found in 10 patients (Haemophilus influenzae in 4, Branhamella catarrhalis in 3, Streptococcus pneumoniae in 2, Pseudomonas aeruginosa in 2, Staphylococcus aureus in 1, alpha-Streptococcus in 1, Corynebacterium sp. in 1, Peptostreptococcus micros in 1 and Klebsiella pneumoniae in 2) were eradicated except 2 strains (S. aureus and P. aeruginosa) from 1 patient (patient No. 2). No adverse reactions were observed in any of the 12 patients. 2. MICs of PAPM were examined against 22 clinical isolates (H. influenzae 5, B. catarrhalis 3, alpha-Streptococcus 3, S. pneumoniae 2, Corynebacterium sp. 2, S. aureus 1, P. aeruginosa 1, P. micros 1, Enterobacter cloacae 1, Escherichia coli 1, Group D Streptococcus 1 and Staphylococcus epidermidis 1) from children with bacterial infections. PAPM showed a good antibacterial activity comparable to the activity of cefoperazone (CPZ) against S. pneumoniae strains relatively tolerant to penicillins. However, the activity of PAPM against H. influenzae was somewhat weaker than that of CPZ. 3. Pharmacokinetic studies.(ABSTRACT TRUNCATED AT 250 WORDS)

Bacterial Infections↗
PubMed1992

[Clinical evaluation of panipenem/betamipron in children].

Panipenem/betamipron (PAPM/BP), a new injectable carbapenem antibiotic, was evaluated for its safety and efficacy in children. Ninety three percentage (14 in 15 cases) of various infections were cured with PAPM/BP therapy. Transient skin rash occurred in 1 case, probably due to the histamine-like effect of PAPM/BP. The plasma half life of panipenem was 0.85 +/- 0.07 hours. PAPM/BP was evaluated to be a less-epileptogenic carbapenem antibiotic.

Bacterial Infections↗
PubMed1992

[Clinical evaluation of a new carbapenem, meropenem, in infants and children].

A new carbapenem antibiotic, meropenem (MEPM), was evaluated for its safety and efficacy in 33 infants and children. MEPM was effective in all the 32 evaluable cases including 4 cases of bacterial meningitis and 5 cases of Pseudomonas aeruginosa infections. The mean half life of plasma concentrations of MEPM was 0.84 +/- 0.09 hours after 30 minutes intravenous drip infusion. Mild diarrhea (2 cases), transient elevation of transaminases (8 cases), and transient eosinophilia (2 cases) were associated with the MEPM therapy, but none of them was problematic. These data suggest that MEPM is safe in infants and children and could be one of the therapeutic agents for severe infections or infections in compromised hosts.

Adolescent↗
PubMed1992

[Overall clinical evaluation of panipenem/betamipron against infections in pediatric field].

To conduct a basic-clinical study on newly developed panipenem/betamipron (CS-533/CS-443, PAPM/BP) against various infections in pediatrics, a study group was organized and a joint research by 17 institutions and their related hospitals was undertaken. The obtained results are as follows. 1. Blood concentrations and urinary excretion Pharmacokinetics of PAPM/BP in children was studied using 30 minutes intravenous drip infusion of 10 mg/10 mg/kg, 20 mg/20 mg/kg and 30 mg/30 mg/kg, respectively. Maximum blood levels of PAPM/BP were observed at the completion of drip infusion and were 26.72 +/- 8.78 micrograms/ml/18.33 +/- 8.54 micrograms/ml (mean +/- S.D.) with administration of 10 mg/10 mg, 64.80 +/- 18.50 micrograms/ml/38.74 +/- 16.41 micrograms/ml with administration of 20 mg/20 mg and 91.70 +/- 29.42 micrograms/ml/50.08 +/- 22.41 micrograms/ml with administration of 30 mg/30 mg. Dose dependency was noted with these doses. The half-life was about 1 hour for PAPM and about 0.5 hour for BP. As for urinary excretion, PAPM was excreted about 30% and BP about 70% in the first 6 hours after the start of drip infusion. 2. Clinical results Twenty-five cases of exclusion and drop-out were deducted from a total of 391 cases and 8 cases having 2 diseases concurrently were added to the remaining 366 cases, hence 374 cases were evaluated in the study as the subjects of analysis of clinical effects. As for clinical effects in cases where pathogenic bacteria were detected, 215 out of 221 cases were rated as effective or above, hence the efficacy rate of 97.3% was obtained. In cases where pathogenic bacteria were not detected, 145 out of 153 cases were rated as effective or above, thus the efficacy rate was 94.8% which is similar to that in the cases where pathogenic bacteria were detected. The daily dose levels most commonly employed were 30 to 60 mg/kg (as PAPM) administered in 3 divided doses a day, and this regimen method accounted for 52.7% of the total cases, and the efficacy rate with this regimen was 97.0%. As for the bacteriological effect 87 (96.7%) out of 90 strains of Gram-positive bacteria (GPB) disappeared and 136 (91.3%) out of 149 strains of Gram-negative bacteria (GNB) disappeared upon the treatment. The overall bacterial eradication rate for the pathogenic bacteria was 93.4%.(ABSTRACT TRUNCATED AT 400 WORDS)

Bacteria↗
PubMed1991

Clinical trials of cefpodoxime proxetil suspension in paediatrics.

The pharmacokinetics, bacteriological and clinical efficacy, and safety of the suspension formulation of cefpodoxime proxetil, an oral cephalosporin antibacterial, were evaluated in paediatric patients with various infections. With single doses of 3 and 6 mg/kg (cefpodoxime equivalent) a dose response was evident in the serum concentration values. Absorption, as evidenced by serum concentrations and areas under the concentration-time curve, was enhanced when the suspension was administered before a meal. The overall clinical efficacy (defined as an excellent or good response) in evaluable patients (those from whom a pathogen was isolated) was 94.7% (451 of 476). Bacteriological eradication rates were as follows: Gram-positive bacteria 91.3%; Gram-negative bacteria 88.6%, and 90.0% overall. Side effects occurred in 17 (2.29%) patients, and transient and reversible abnormal laboratory values were found in a few patients.

Adolescent↗
PubMed1991

[Clinical evaluation of cefdinir 10% granules in children].

Cefdinir (CFDN, FK482) was evaluated in children with infections. CFDN was given at a daily dose of 6.4-19.8 mg/kg in 2 or 3 divided portions. CFDN was effective in 94% of 32 cases with respiratory tract, middle ear, urinary tract or skin structure infections. Side effects were loose stool and diarrhea (12.5%). In a pharmacokinetic study, 6.0 mg/kg of CFDN was given to each of the subjects before meal. Cmax was 0.81 +/- 0.38 microgram/ml, T 1/2 was 2.31 +/- 0.77 hours. Antibacterial activity against Staphylococcus aureus was the most excellent of oral cephem antibiotics tested. The data suggest that CFDN 10% granular preparation is safe and effective when used in children with infections caused by susceptible bacteria.

Administration, Oral↗
PubMed1991

[Pharmacokinetic and clinical studies of cefdinir in the pediatric field. Pediatric Study Group of Cefdinir].

We studied pharmacokinetics and clinical effects of 5% and 10% fine granules of cefdinir (FK 482, CFDN), a new oral cephalosporin, in the pediatric field and the following results were obtained. 1. Pharmacokinetics (blood concentration and urinary excretion) Pharmacokinetics of CFDN in 163 children was investigated. Cmax and T 1/2 were 0.92 +/- 0.45 micrograms/ml and 1.95 +/- 1.06 hours, respectively, in the fasting state, and were 0.63 +/- 0.29 micrograms/ml and 2.26 +/- 0.65 hours, respectively, in the non-fasting state, at a dose level of 3 mg (potency)/kg. At a dose level of 6 mg (potency)/kg, Cmax and T 1/2 were 1.29 +/- 0.49 micrograms/ml and 2.11 +/- 1.85 hours, respectively, in the fasting state and were 1.28 +/- 0.48 micrograms/ml and 2.01 +/- 0.84 hours, respectively, in the non-fasting state. Data of Cmax and AUC showed that blood concentration of the drug depended on dose levels. Urinary recovery rates in the first 8 hours were 20.5 +/- 8.8% in the fasting state and 14.8 +/- 5.9% in the non-fasting at a dose level of 3 mg (potency)/kg and 16.5 +/- 6.7% and 17.8 +/- 2.4%, respectively, at 6 mg (potency)/kg. 2. Clinical effects Clinical effects of CFDN on various infections were studied in 612 children who were treated with 5% fine granules of CFDN (5% granule group) and in 208 with 10% fine granules of CFDN (10% granule group). CFDN granules were administered mainly at daily doses of 9.0-18.0 mg (potency)/kg in 3 divided portions. Clinical efficacy rates in 428 children of the 5% granule group and in 159 of the 10% granule group from whom causative bacteria were isolated, were 94.9% and 96.2%, respectively. The clinical efficacy rates for patients who were responsive to previous antibiotic therapy were 91.2% in the 5% granule group and 100% in the 10% granule group. Bacteriological eradication rate was 82.1% for 491 strains in the 5% granule group, and was 84.0% for 175 strains in the 10% granule group. The incidences of side effects were 3.9% (24/608) in the 5% fine granule group and 5.8% (12/206) in the 10% granule group. All of the side effects were slight gastrointestinal disorders, and no serious side effects were found. As for clinical laboratory test results, slight elevations of eosinophile, platelet or transaminase were observed. Based on the above results, it is considered that the appropriate dose levels of CFDN for pediatric infections ranged from 9.0 to 18.0 mg (potency)/kg a day, divided into 3 portions.

Administration, Oral↗
PubMed1991

No-carrier-added carbon-11-labeled sn-1,2- and sn-1,3-diacylglycerols by [11C]propyl ketene method.

This article describes the preparation of sn-1,2-[11C]diacylglycerols and sn-1,3-[11C]diacylglycerols by a no-carrier-added reaction based on a labeling method using [1-11C]propyl ketene, which is one of the most potent acylating agents. [1-11C]Propyl ketene was produced by pyrolytic decomposition of [1-11C]butyric acid and was trapped in pyridine containing L-alpha-palmitoyl-lysophosphatidylcholine, producing L-alpha-palmitoyl-2-[1-11C]butyryl-sn-glycero-3-phosphorylcholine. We adopted an enzymatic reaction to remove the phosphorylcholine, in which L-alpha-palmitoyl-2-[1-11C]butyryl-sn-glycero-3-phosphorylcholine was incubated with phospholipase C, hydrolyzing to produce 1-palmitoyl-sn-2-[1-11C]butyrylglycerol. Total synthesis time was about 50 minutes and the specific activity was estimated at 93 GBq/mumol (2.5 Ci/mumol) at end of synthesis. Radiochemical yield was 3.8% based on the trapped 11CO2. sn-1,3-[11C]Diacylglycerol was also synthesized by [1-11C]propyl ketene reaction with 1-palmitoyl-sn-glycerol in a single procedure. The regional brain tissue radioactivities obtained in sn-1,2-[11C]diacylglycerol were higher than those of sn-1,3-[11C]diacylglycerol, and the regional values varied widely. In autoradiography of brain slices from conscious rats, sn-1,2-[11C]diacylglycerol incorporation sites were discretely localized, especially in the amygdala, cerebral cortex, and hippocampus, suggesting that intensive neuronal processing occurred in these areas on the basis of phosphatidylinositol turnover.

Acylation↗
PubMed1991

[Bacteriological, pharmacokinetic and clinical evaluations of cefpirome sulfate in the pediatric field. Pediatric Study Group of Cefpirome].

A research group was organized with the purpose of making basic and clinical studies on cefpirome sulfate (HR810, CPR), a newly developed cephalosporin antibiotic, in the pediatric field. Through meetings a joint research was done involving 19 key institutions and their related facilities throughout Japan. The obtained results are summarized as follows. 1. Antibacterial Activities Minimum inhibitory concentrations (MICs) were determined against 71 Gram-positive and 110 Gram-negative bacteria in the present clinical trials. CPR showed antibacterial activities 2-16 times higher than those of ceftazidime (CAZ) against Staphylococcus aureus and other Gram-positive bacteria including MRSA. Against Gram-negative bacteria, CPR showed a somewhat broad range of distribution in MIC against Branhamella catarrhalis, while the antibiotic inhibited the growth of all the strains of Escherichia coli and Haemophilus influenzae at concentrations no more than 0.10 and 0.20 micrograms/ml, respectively. 2. Blood Concentrations and Urinary Excretion Rates The pharmacokinetics in pediatric patients was investigated with a dose of 20 mg/kg in most cases via one shot intravenous injection or 30- and 60-minute intravenous drip infusion. Mean blood concentrations of CPR at 15 minutes after one shot intravenous injection of 10, 20, and 40 mg/kg were 51.2, 70.5, and 123.5 micrograms/ml, with half-lives of 1.21, 1.39, and 1.53 hours, respectively. Urinary excretion rates in 6 hours were 63.6, 66.0 and 71.6%, respectively for the 3 dose levels. After 30- and 60-minute intravenous drip infusions at the same dose, the pharmacokinetic parameters observed were similar to those obtained with one shot injections. 3. Concentration in the Cerebrospinal Fluid CPR penetrated well into the cerebrospinal fluid in patients with purulent meningitis and levels of 1.85-24.2 micrograms/ml 45-60 minutes were achieved after intravenous injection at a dose of 40-80 mg/kg, the penetration rate of CPR was at an intermediate degree compared with other cephalosporin antibiotics. 4. Clinical Results Clinical efficacies of CPR on infectious diseases were analyzed in 454 plus 3 cases which were complicated with other infectious diseases, hence totaling 457 cases out of 499 cases originally chosen for clinical evaluation. The remaining 45 cases were excluded from the clinical evaluation. As for the clinical efficacy, CPR was found to be effective (good or excellent) in 430 (94.1%) of the 457 cases. CPR was found to be effective in 243 (95.3%) of 255 cases for which causative bacteria were identified. The efficacy rate was 92.6% (187 of 202) in those cases in which causative bacteria were not identified.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1991

[Clinical evaluation of cefpirome in children].

A new injectable cephem antibiotic, cefpirome (CPR), was evaluated clinically in children. CPR was effective in all the 17 evaluable cases with acute bacterial infections including 1 case of purulent meningitis due to Haemophilus influenzae type b. Diarrhea and elevation of serum GOT and GPT were associated with CPR therapy in 2 young infants, although they were mild and transient. The plasma T 1/2 beta of CPR was 1.17 +/- 0.22 hours after bolus injection and mostly excreted in 6 to 8 hours into urine of children with normal renal functions. The data indicate that CPR is safe and effective, when used in children with susceptible bacterial infections.

Bacterial Infections↗