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)

The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of omeprazole are reviewed. Omeprazole, a substituted benzimidazole, has a unique site and mechanism of action because it inhibits the proton pump--i.e., hydrogen, potassium adenosine triphosphatase (H+,K+-ATPase)--and consequently blocks the final common step in the gastric acid secretory pathway. Omeprazole inhibits basal and histamine-, gastrin- and pentagastrin-stimulated gastric hydrochloric acid secretion. It produces a dose-dependent reduction in gastric acidity, gastric acid output, and gastric juice volume and has variable effects on pepsin secretion. Omeprazole has no documented effect on esophageal motility or lower esophageal sphincter pressure. Omeprazole is variably absorbed from the gastrointestinal tract, and food appears to decrease the rate, but not the extent, of drug absorption. The drug is approximately 95% bound to plasma proteins and is metabolized to inactive components that are enterohepatically or renally eliminated. Omeprazole is more effective (in most studies) than H2-receptor antagonists in treating duodenal ulcer, at least as effective in treating benign gastric ulcer, and more effective in treating reflux esophagitis. Omeprazole has been used successfully in patients with Zollinger-Ellison syndrome refractory to treatment with H2-receptor antagonists. Gastrointestinal complaints (nausea and diarrhea) are the most commonly reported adverse effects associated with omeprazole therapy. The most frequently reported laboratory abnormality occurring with omeprazole use is elevation of serum aspartate aminotransferase and alanine aminotransferase concentrations. Omeprazole will serve a valuable role in the management of gastrointestinal tract ulcers and hypersecretory conditions.
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PMID:Therapeutic evaluation of omeprazole. 306 85

Cyclopiazonic acid (CPA) was given daily to groups of guinea pigs at doses of 0.00625, 0.0125, 0.025, 0.05, 0.1, 0.2, 0.4, 0.8, 1.6, and 1.95 mg/day for 30 days. All guinea pigs were sensitized and survivors were skin tested twenty-five days later with Mycobacterium tuberculosis. Mortalities occurred only in the two greatest dose groups. Signs of disease included anorexia, roughened hair coat, diarrhea and incoordination. The major histopathologic changes occurring in these two groups included hepatocellular vacuolar degeneration and necrosis of the gastric mucosa with infiltration of neutrophils in the deep gastric mucosa. CPA did not affect cutaneous hypersensitivity to M. tuberculosis, complement activity, serum glycocholic acid concentrations or weight gains. There were increases in aspartate aminotransferase, alanine aminotransferase, and sorbitol dehydrogenase concentrations in the serum of guinea pigs in the two greater dose groups, but no changes were found in serum concentrations of SAP. There was a slight increase in the serum bilirubin concentrations in the greater dose groups.
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PMID:Effect of cyclopiazonic acid on delayed hypersensitivity to Mycobacterium tuberculosis, complement activity, serum enzymes, and bilirubin in guinea pigs. 309 99

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

Acute toxicity by gardenia yellow color was studied in rats. Oral administration of the colorant at doses of 800 mg/kg up to 5000 mg/kg caused diarrhea and increases in serum alanine aminotransferase and aspartate aminotransferase activities in a dose-dependent manner. After 24 h of oral treatment with 2000 mg/kg of the colorant, liver showed partially hemorrhagic changes and the intestinal tract, especially the duodenum, appeared blue. The toxicity induced by the colorant was stronger by oral administration than by intraperitoneal administration. The content of geniposide, an iridoid compound, was estimated to be 28% of the colorant, and this iridoid accounted for almost all the hepatotoxic activity of the colorant.
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PMID:Hepatotoxicity of gardenia yellow color in rats. 318 76

Twenty three neonates and young infants were treated with imipenem/cilastatin sodium (IPM/CS) and its clinical efficacy and side effects were evaluated. Ages of the patients ranged from 0 to 83 days, and their body weights ranged from 750 to 4,760 g. Doses of IPM/CS ranged from 17.4 to 21.5 mg/kg as IPM every 6 to 12 hours for 3 to 12 days. Sixteen patients with infections including sepsis, meningitis and pneumonia, appeared to have responded to the IPM/CS treatment. Among them, clinical results were excellent in 2, good in 12 and fair in 2 patients. The drug was well tolerated, but 1 patient had diarrhea, 1 had redness of body during infusion, 1 had elevated GOT and GPT, and 2 patients showed only elevated values of GOT only among the 23 patients. The pharmacokinetics of IPM/CS were studied in 7 patients. Their ages ranged from 0 to 9 days, and body weights ranged from 2.5 to 4.0 kg. Serum concentrations of IPM were between 18.0 and 96.9 micrograms/ml and those of CS ranged 31.7 and 144.5 micrograms/ml in 6 patients at the end of intravenous drip infusion 20 mg/20 mg/kg during 30 or 60 minutes. Elimination half-lives of IPM ranged from 1.2 to 2.0 hours, and those of CS ranged from 1.4 to 2.7 hours. Serum concentrations of IPM was 14.7 micrograms/ml and that of CS was 32.4 micrograms/ml in 1 patient at the end of 30 minute-drip infusion 10 mg/10 mg/kg. The elimination half-lives of IPM was 1.5 hours, and that of CS was 2.9 hours.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Clinical and pharmacokinetic evaluation of imipenem/cilastatin sodium in neonates and young infants]. 321 Feb 99

Subjects were in-patients with bacterial urinary tract infections, ranging in age 4 months to 11 years 4 months. As a rule, daily dose was either four 125 mg (in potency) suppositories or four 125 mg (in potency) oral form given at 6-hour intervals over a period of 5 days. The number of children subjected to this study was 105. These children were divided into 2 groups (suppository 54; oral form 51) with matched pretreatment background factors. Therapeutic effectiveness rates were 70.4% for the suppository and 66.7% for the oral form, and no significant difference was observed between the 2 groups. Rates of efficacy by severity, presence or absence of underlying and/or complication diseases, daily dose and causative microorganisms did not differ significantly between the 2 groups. There was no significant difference in time-courses of improvement of clinical signs and symptoms between the 2 groups. Eradication rates for causative microorganisms were 65.9% for the suppository and 62.5% for the oral form. Most frequently isolated causative microorganisms were Escherichia coli and Proteus mirabilis. No significant differences were recognized in the therapeutic effect and usefulness evaluated by physicians in charge. The frequency of side effects did not differ significantly between the suppository group (6 with diarrhea and 1 with anal pain: 12.1%) and the oral form group (5 with diarrhea, 1 with displeasure and 1 with vomiting: 12.7%). Abnormal laboratory findings appeared in 6 cases (2 with eosinophilia, 2 with increased GOT and 2 with increased GPT) in the suppository group and 7 cases (2 with eosinophilia, 2 with thrombocytosis, 2 with increased GOT and 1 with increased GPT) in the oral form group.
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PMID:[Comparative, controlled study on an ampicillin suppository (KS-R 1) with an oral form of ampicillin in urinary tract infections]. 330 42

This work was designed to study effects of HgSO4 on rabbits performance when added in the mash diet for 7 weeks with concentrations of 0, 150, and 300 ppm as Hg (6 animals/group). The Hg application caused mortality associated with diarrhoea, haemorrhage, oedema and liver and stomach necrosis. The contaminated diets caused significantly increased feed intake, drinking water consumption and live body gain. Mercury did not affect organ percentages significantly (P greater than or equal to 0.05). Serum analyses reflected a significant (P less than or equal to 0.05) rise in the glucose content (for the animals fed the 300 ppm Hg-diet) with a slight decrease in Ca level and activity of both transaminases GPT and GOT. The most affected organ by the application of Hg was the liver which reflected a slight increase in its dry matter substance, significant increase (P less than or equal to 0.01) in the ether extract percentage on the 300 ppm Hg-diet and severe reduction (P less than or equal to 0.01) in its vitamin A as well as in the iron content (P less than or equal to 0.05) on the 300 ppm Hg-diet. The highest level of Hg added caused an increase (P less than or equal to 0.01) in bone magnesium.
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PMID:Effect of dietary contamination with mercury on the performance of rabbits. 342 34

Fundamental and clinical studies of a new carbapenem antibiotic, imipenem/cilastatin sodium (MK-0787/MK-0791), were carried out to evaluate the drug in treating infections of the female genital organs. The following results were obtained: In 4 patients undergoing hysterectomy, the penetration of MK-0787 and MK-0791 into female genital organ tissues was studied following a 30-minute intravenous drip infusion of MK-0787/MK-0791 500 mg/500 mg. Plasma levels of MK-0787 and MK-0791 in cubital venous blood following the drip infusion peaked at 0 minute with values of 51.2 micrograms/ml and 61.9 micrograms/ml, respectively, then decreased to 1.9 micrograms/ml and 0.7 microgram/ml, respectively, at 201 minutes. MK-0787 penetrated readily to female genital organ tissues and levels of the drug exceeded 0.5 approximately 1.9 micrograms/g in various organ tissues at 201 minutes following an intravenous drip infusion of 500 mg/500 mg of MK-0787/MK-0791. Clinically, MK-0787/MK-0791 was used for the treatment of obstetrical and gynecological infections at a dosage of 500 mg/500 mg twice daily by intravenous drip infusion. Clinical effects of MK-0787/MK-0791 were analyzed in 22 patients, including 9 patients with intrauterine infections, 7 with intrapelvic infections, 5 with adnexitis, and 1 with an external genital infection. Excellent responses were seen in 5 patients (22.7%), good responses in 15 (68.2%), and poor responses in 2 (9.1%). The efficacy ratio was 90.9%. After the treatment, 15 out of 18 isolates were eradicated for an 83.3% eradication rate. All strains of S. epidermidis (2 strains), Eubacterium lentum (1 strain), Peptococcus sp. (1 strain), beta-Streptococcus (1 strain), Gram-positive rods (2 strains), Enterobacter cloacae (1 strain), Bacteroides bivius (1 strain), Pseudomonas sp. (1 strain), Pseudomonas cepacia (1 strain) and Gram-negative rods (1 strain) were eradicated by the MK-0787/MK-0791 treatment. The safety of the drug was analyzed in 22 patients, effects occurred in 3 (13.6%). Among those 3 patients, diarrhea occurred in 1 patient, rash in another and nausea and vomiting in yet another. One patient had an increased BUN after the MK-0787/MK-0791 treatment. In the other 21 patients, no abnormalities in creatinine, GOT, GPT, or T. Bil. values were observed. It may be concluded that MK-0787/MK-0791 is useful for the treatment of obstetrical and gynecological infections.
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PMID:[Fundamental and clinical studies of imipenem/cilastatin sodium in the field of obstetrics and gynecology]. 346 86

Fundamental and clinical studies were performed by our study group to evaluate the usefulness of the combination (1:1) of imipenem (MK-0787), a carbapenem antibiotic, and cilastatin sodium (MK-0791), an inhibitor of dehydropeptidase-I, in the treatment of patients with obstetric and gynecologic infections. The following results were obtained. Antimicrobial activities of MK-0787 were tested with inocula of 10(6) cells/ml of organisms isolated from patients with obstetric and gynecologic infections. Peak MIC's of MK-0787 were less than or equal to 0.20 micrograms/ml for S. aureus, less than or equal to 0.20 micrograms/ml for S. epidermidis, 1.56 micrograms/ml for E. faecalis, 0.39 micrograms/ml for E. coli, less than or equal to 0.20 micrograms/ml for K. pneumoniae and less than or equal to 0.20 micrograms/ml for B. fragilis. When 0.5 g/0.5 g of MK-0787/MK-0791 was administered by a 30-minute intravenous drip infusion, maximum concentrations of MK-0787 in all female genital tissues were obtained at the end of the infusion, and Cmax ranged from 9.4 micrograms/g to 17.0 micrograms/g. In addition, the maximum concentration of MK-0787 in pelvic dead space exudate was 13.2 micrograms/ml at 88 minutes after the start of the infusion. The penetration of MK-0787/MK-0791 into female genital tissues and dead space exudate was found to be good and sufficient to cover MIC's against organisms isolated from patients with obstetric and gynecologic infections. Clinical efficacy was evaluated in 201 evaluable patients out of a total of 253 patients with obstetric and gynecologic infections. Clinical responses were excellent in 2, good in 181 and poor in 18 patients, and the efficacy rating was 91.0 percent. Efficacy ratings classified by types of infections were 93.2% (82/88) for intrauterine infections, 83.0% (39/47) for intrapelvic infections, 100% (26/26) for adnexitis, 90.0% (18/20) for infections of the external genital organs and 90.0% (18/20) for other infections. Side effects were observed in 6 of the 253 patients; rash in 4, nausea and vomiting in 1 and diarrhea in 1 patient. Abnormal laboratory findings were observed in 10 of the 253 patients; elevation of GOT, GPT, LDH and Al-P in 1, elevation of GOT, GPT and Al-P in 1, elevation of GOT and GPT in 4, elevation of GPT in 1, elevation of BUN in 1, increase of eosinophiles in 1, decrease of segmented neutrophils in 1 patient.
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PMID:[Fundamental and clinical studies of imipenem/cilastatin sodium in the field of obstetrics and gynecology. Study group of imipenem/cilastatin sodium in the field of obstetric and gynecological infections]. 353 68

Ceftazidime (CAZ) was evaluated for its pharmacokinetics and clinical usefulness in neonates and premature infants. The results obtained were summarized below. Following intravenous injection of CAZ 10 or 20 mg/kg to neonates and premature infants, dose response was observed in serum concentrations ranging from 5.1 to 21.9 micrograms/ml at 6 hours after the injection. The serum half-life tended to be longer in premature infants than in neonates; the half-life being longer for an infant with lower day-age. Urinary recovery rates during the first 6 hours after single administrations of 10 mg/kg of CAZ tended to be higher in neonates than in premature infants, and higher rates were observed in older infants. However, no noticeable difference was observed after the administration of CAZ 20 mg/kg. Clinical efficacy was evaluated in 99 neonates and 55 premature infants (156 infections), daily doses ranging from 21.1 to 246.4 mg/kg. Out of 105 cases of common infections, mainly 44 cases with causative organisms identified (including 17 of sepsis, 7 of pneumonia, 4 of purulent meningitis, 11 of urinary tract infections) were examined for the clinical efficacy. The efficacy of CAZ was excellent in 21, good in 18, fair in 1 and poor in 4, with the efficacy rate of 88.6%. In the remaining 61 cases, i.e., 37 with causative organisms unknown and 24 with signs of intrauterine infections, the efficacy rate was 95.1%. Other than these cases, additional 51 cases were given CAZ solely for prophylaxis of infections, and the results were found satisfactory. On the whole, clinical efficacy rate of CAZ was 94.9% in 156 cases. Out of the 44 cases examined for bacteriological responses, 38 were evaluated as 'eradicated', 3 'persisted' and 3 'unknown' with eradication rate of 92.7%. Replacement of organisms (superinfection) was observed in 3 cases. Out of 179 cases in which adverse effects were assessable, adverse effects were observed in a total of 4 cases (2.2%), i.e., 3 cases of diarrhea (1.7%) and 1 case of rash (0.6%), and abnormal laboratory findings were observed in a total of 14 cases (7.8%), i.e., increase in eosinophiles count in 8 (4.5%), elevation of GOT in 3 (1.7%), increase in platelet, elevation of GOT . GPT, and elevation of GOT . GPT . BUN in 1 case each (0.6%). None of them were severe and they were transient. Elevations of bilirubin and cases of positive PIVKA II associated with CAZ were not observed.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[A pharmacokinetic and clinical evaluation of ceftazidime in neonates and premature infants. A study of ceftazidime in the perinatal co-research group]. 354 Mar 39


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