Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:2.6.1.2 (alanine aminotransferase)
26,722 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Cefodizime (CDZM, THR-221), a new cephem antibiotic, was investigated for its clinical efficacy and pharmacokinetics in children. The results obtained are summarized as follows. 1. Antimicrobial activities Antimicrobial activities of CDZM against clinically isolated organisms were determined. MICs of CDZM against 1 strain each of Streptococcus pneumoniae, Escherichia coli and Klebsiella pneumoniae were 0.05 micrograms/ml to 0.10 micrograms/ml. Especially, MIC against all 6 strains of Haemophilus influenzae was less than or equal to 0.024 micrograms/ml. This MIC value was lower than those of other antibiotics such as cefotaxime, cefotiam, cefazolin, piperacillin. 2. Pharmacokinetics CDZM was given to 1 case at a dose of 20 mg/kg by a 60-minute intravenous drip infusion. The peak value of serum concentration of CDZM was 207.80 micrograms/ml at the end of the infusion. The half-life was 2.15 hours. The mean urinary excretion rate was 68.5% in the first 4 hours, 79.2% in 6 hours and 76.5% in 8 hours after the 30-minute drip infusion. 3. Clinical efficacy CDZM was given to a total of 27 patients, 13 with pneumonia, 1 with bronchitis, 2 with acute pharyngitis, 1 with purulent tonsillitis, 5 with urinary tract infection, 1 each with retrograde cholangitis, acute enteritis, pericementitis, phlegmon and inguinal lymphadenitis. Overall clinical efficacies were excellent in 5 cases, good in 17 and the efficacy rate was 81%. Bacteriological effects were investigated in 13 cases and the eradication rate was 85%. No adverse reactions were observed in any case. As abnormal laboratory findings, elevated GOT, GPT, A1-P, LAP and gamma-GTP, were noted in 1 out of the 28 cases examined.
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PMID:[Clinical and pharmacokinetic evaluation of cefodizime in children]. 279 60

Cefodizime (THR-221, CDZM), a newly developed injectable cephem antibiotic, was injected intravenously to 13 cases of pediatric infections. Patients received the drug at a dose level of approximately 20 mg/kg x 3 times daily. The results obtained are summarized as follows. 1. Clinical efficacy was excellent in 4 patients, good in 6 and poor in 0 for 10 cases (2 phlegmon, 1 periproctal abscess, 5 pneumonia and 2 bronchitis) except 3 Mycoplasma pneumonia. 2. Three strains of pathogens were followed for their changes (Streptococcus pyogenes in 1 phlegmon, Klebsiella pneumoniae in periproctal abscess and Haemophilus influenzae in 1 bronchitis) and they were found to have been eliminated. 3. No adverse reactions occurred. Abnormal changes in laboratory test data found were 2 cases of eosinophilia, 1 cash each of increased GOT and GPT, and thrombocytosis, but none of them was severe.
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PMID:[Clinical experience with cefodizime on pediatric infections]. 279 61

Clinical studies were performed on cefodizime (THR-221, CDZM), a new cephem antibiotic as described below. CDZM was administered to 13 patients in dose levels ranging from 55 to 96 mg/kg/day t.i.d. for 3-7 days (5.5 days on average). These patients included 8 with pneumonia, 2 with tonsillitis, 1 each with bronchitis, phlegmon and urinary tract infection. The overall efficacy rate was 92.3%, i.e., efficacy was excellent in 8, good in 4 and poor in 1. Bacteriological efficacy was 83.3%, i.e., 5 strains of bacteria (Streptococcus pneumoniae 1, Haemophilus influenzae 3, Haemophilus parainfluenzae 1) were eradicated and 1 was unchanged (Enterobacter cloacae, MIC greater than 100 micrograms/ml). Clinical side effect was not observed during the treatment. Laboratory abnormalities were observed in 2 cases, i.e., a slight elevation of GPT and a mild eosinophilia. The above results suggest that CDZM is a useful antibiotic for treating pediatric bacterial infections.
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PMID:[Clinical experience with cefodizime in bacterial infection of children]. 279 62

Therapeutic effects of cefodizime (CDZM, THR-221), a new cephalosporin having a methoxyimino group, were examined in various infectious diseases in children. Clinical efficacy rates were 100% (3/3) in pneumonia, 100% (5/5) in acute bronchitis, 75% (3/4) in upper respiratory infections and 100% (1/1) in each of a croup and a mixed infection with Streptococcus pyogenes and staphylococcal impetigo. Hence, the overall efficacy rate was 92.9% (13/14). Adverse effects were observed in 2 cases, i.e. exanthema provably due to drug allergy in 1 case and a slightly elevated GPT in another. Changes in serum concentrations and urinary excretion of CDZM were examined in a child with no infection. T 1/2 values obtained were 124.5 minutes (bioassay) and 143.4 minutes (high performance liquid chromatography (HPLC]. Eight hour recovery rates in urine were 62.9% (bioassay) and 65.4% (HPLC). CDZM was considered to be a safe and useful drug in treating various infectious diseases in children.
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PMID:[Therapeutic effects of cefodizime in the treatment of various infectious diseases in children]. 279 65

Laboratory and clinical studies on cefodizime (CDZM, THR-221), a newly developed cephem antibiotic, were done. The results obtained are summarized as follows: 1. Absorption and elimination were examined in a total of 5 cases including a case of 10 mg/kg intravenous drip infusion for 30 minutes, 2 cases of 20 mg/kg rapid intravenous injection and 2 cases of 40 mg/kg drip infusion for 30 minutes. Maximum serum levels were attained immediately after drip infusion or rapid injection. Cmax's were 119.2 micrograms/ml for 10 mg/kg, 374.9 micrograms/ml or 255.7 micrograms/ml for 20 mg/kg, and 321.3 micrograms/ml or 431.8 micrograms/ml for 40 mg/kg. These values were determined using an high performance liquid chromatography (HPLC) method. In general, values using the bioassay were higher than those with the HPLC method. T 1/2 (beta)'s were between 1.74 and 1.93 hours using HPLC, and between 1.77 and 2.24 hours using bioassay. Urinary recovery rates were examined in 3 out of 5 cases. Cumulative urinary recovery rates were 57.9-90.6% with HPLC method and 50.4-88.0% with bioassay in a period of 0-8 hours after administration. 2. Clinical efficacy was evaluated in a total of 22 cases including 14 cases of respiratory tract infections, 5 cases of urinary tract infections and 3 cases of cellulitis. Clinical efficacy rate was 95.2%. Bacteriologically, pathogenic organisms were eradicated in 90.0%. As adverse reactions, 1 angular stomatitis, 1 diarrhea and 1 loose stool were noted. Abnormal laboratory test values detected were 1 case of increased GPT and 1 case of increased GOT and GPT.
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PMID:[Laboratory and clinical studies on cefodizime in the pediatric field]. 279 66

Acute toxicity of cefodizime sodium (THR-221) was examined in mice of both sexes, rats of both sexes (including 5-day-old young), and male dogs. The LD50 values of THR-221 (mg/kg) were as follows: (1) mice: intravenous, 7200 for males and 5000 for females; intraperitoneal, 10500 for males and 11000 for females; subcutaneous, 17500 for males and 16500 for females; and oral, 28000 for males and 29000 for females. (2) rats (adult): intravenous, 7000 for males and 8200 for females; intraperitoneal, 9500 for males and 8800 for females; subcutaneous, 17000 for males and 15500 for females; oral, more than 20000 for both sexes; and intramuscular, more than 3200 for both sexes. (3) 5-day-old rats: subcutaneous, 5278 for males and 5314 for females. (4) male dogs: intravenous, more than 5000. Major changes in general conditions observed in mice and rats were decreased spontaneous activity, lying prone, respiratory changes, staggering gait, clonic or clonic-tonic convulsions, and cyanosis, and in the animals dosed orally, diarrhea or salivation was also noted. The changes in 5-day-old rats were respiratory changes, agony, loss of reflex to an external stimulus, and congestion at the injection site, and those in dogs were vomiting, dryness of the nose, and soft or mucous stools. Autopsies on the mice and rats which died revealed hemorrhage on the brain surface. In addition, the following were seen: intraperitoneal retention of fluid and dark red spots on the abdominal wall (i.p.), subcutaneous retention of fluid or jellylike material and hemorrhage at the injection site (s.c.), and retention of fluid and dark red spots on the mucosa in the digestive tract (mice p.o.). In 5-day-old rats which died, the subcutaneous tissue at the injection site showed hemorrhage macroscopically and inflammatory changes microscopically. Hematological and blood chemical tests performed in dogs showed an increase in white blood cells and changes suggesting anemia, increases in GOT, LDH and ALP activities, and slight changes in urea nitrogen and inorganic phosphorus. In one animal given a low dose of 2500 mg/kg, an increase in GPT activity was also seen. However, these changes were all transient. Microscopic findings in dogs were slight inflammatory changes in the subcutaneous tissue around the injection site.
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PMID:[Acute toxicity study of cefodizime sodium]. 317 86

1. The concentrations of alanine, aspartate, glutamate, glutamine and serine plus threonine have been measured by enzymic methods in ;quick-frozen' livers from normal, starved, alloxan-diabetic and phlorrhizin-treated rats. 2. The hepatic concentrations of alanine and serine plus threonine were decreased in rats starved for 48hr. Treatment of these rats with phlorrhizin resulted in a rapid fall (within 2(1/2)hr.) in the concentrations of all the glucogenic amino acids except serine plus threonine, which increased. The pattern for alloxan-diabetic rats was similar to that for phlorrhizin-treated animals, except that here serine plus threonine also decreased in concentration. 3. The effects of anoxia on the hepatic concentrations of the glucogenic amino acids are reported. 4. Inhibition of glutamate-pyruvate transaminase in vivo by l-cycloserine resulted in the accumulation of alanine in situations involving high rates of gluconeogenesis from endogenous amino acids. 5. Measurements of the concentrations of the reactants of the glutamate-pyruvate transaminase and glutamate-oxoglutarate transaminase systems in various metabolic states suggest that they are both at or near equilibrium in rat liver. 6. New enzymic methods are described for the determination of serine plus threonine and alanine.
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PMID:Concentrations of free glucogenic amino acids in livers of rats subjected to various metabolic stresses. 604 91

Effects of varying protein level on hepatic utilization of serine, threonine and glycine were examined by measurements of metabolic fluxes across the liver. Feeding a high protein (HP) diet markedly enhanced hepatic extraction of serine, threonine and glycine, in parallel to alanine. After 20 hours starvation, activity of alanine aminotransferase and serine dehydratase still reflected the induction of these enzymes in fed rats. Thus, in starved rats previously adapted to HP diets, hepatic uptake of serine, threonine and glycine remained very efficient. With a normal diet, gluconeogenesis from alanine may be very active during starvation, in contrast to serine. The present results suggest that serine, and, to a lesser extent glycine, are very efficient glucogenic substrates with HP diets. The serine aminotransferase pathway might be important in rats fed HP diets, particularly for utilization of serine synthesized from glycine in mitochondria. With HP diets, the drop in hepatic alanine, serine and threonine suggest that transport across the plasma membrane might limit their utilization.
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PMID:Control of hepatic utilization of serine, glycine and threonine in fed and starved rats. 640 4

Some experimental and clinical studies were done from the metabolic viewpoint to elucidate the characteristics of myonephropathic-metabolic syndrome. In experimental dogs with their femoral arteries ligated and two third of femoral muscles divided, aldolase and myoglobin showed remarkable increase without significant changes in electrolytes. Slight increase of GPT and GOT was observed. Amino acids showed elevation in urea, taurin, leucin, isoleucin, valine, threonine, 3-methylhistidine, phenylalanine, histidine, lysine, methionine, tyrosine and anserin and decrease in glutamine, alanine, glycine, proline, carnosine, citrullin and arginine. In patients with acute arterial occlusion, potassium, GOT, LDH, CPK, lactate and pyruvate increased moderately and myoglobin showed remarkable increase and aldolase slight increase. Amino acids showed remarkable increase in 3-methylhistidine and beta-amino-isobutyric acid and moderate increase in phenylalanine and arginine. These results revealed that measurement of free amino acid concentration, especially that of methylhistidine as well as myoglobin, pyruvate, lactate and some other enzymes might be of great help to predict the prognosis of patients with acute arterial occlusion of the extremities.
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PMID:[Metabolic study on acute arterial occlusion of the extremities]. 667 89

Serum amino acid (AA) profiles are altered in epilepsy. It is not clear whether this is due to the disease process itself or to other variables such as seizure type, seizure frequency, duration of illness, medication, or altered liver function. We investigated serum AA profiles and liver enzymes in 73 epileptic patients and 90 healthy subjects and evaluated the data by analysis of variance to discriminate between age, sex, seizure type, duration of illness, seizure frequency, antiepileptic drug (AED) and increased serum liver enzyme levels, and their putative interaction with the serum AA profile. There was no correlation between the changes in the AA profile and age, duration of illness, seizure frequency, and seizure type. Seventy-two percent of the AED-treated patients and 33% of the unmedicated patients showed an increase in one or several serum liver enzymes [alanine aminotransferase (ALT), aspartate aminotransferase (AST), and/or gamma-glutamyl transferase (gamma-GT)]; particularly gamma-GT. We observed a significant increase in serum concentrations of glutamine and glycine and decreased levels of taurine, threonine, serine, valine, methionine, isoleucine, leucine, phenylalanine, histidine, tryptophan, and arginine in AED-treated patients but not in unmedicated patients. These results show that the changes in the serum AA profiles of epileptic patients treated with AEDs occur in patients with alteration of serum liver enzymes; whether this implies a causal relation is still uncertain.
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PMID:Serum amino acids, liver status, and antiepileptic drug therapy in epilepsy. 809 92


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