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Acta Physiologica Hungarica
Authors:
F. Burdan
,
Barbara Madej
,
Elzbieta Radzikowska
,
J Dudka
,
Agnieszka Korobowicz
,
M Pasternak
, and
R Maciejewski

Cathepsins are lysosomal enzymes that are used as sensitive markers in various toxicological investigations. The purpose of this study was to evaluate and compare the influence of cimetidine and famotidine on the cerebral cortex, particularly on the activity of cortical cathepsin B, D and L in the frontal lobe of rat brain. The drugs were administered intraperitoneally, twice a day, for six weeks to male Wistar rats in two doses. The initial dose was 2.85 mg/kg for cimetidine and 0.285 mg/kg for famotidine. The second dose was 10 times higher. Control animals were injected with 0.9% NaCl. Half of the animals from each of the drug-treated and control groups were sacrificed on the 42nd day of the experiment. The remaining animals were raised for another 6 weeks without any xenobiotics, and sacrificed on the 84th day. The frontal lobe of the right cerebral hemisphere was taken for biochemical investigation. The activities of free and bound fractions of cathepsin B, D and L were evaluated spectrophotometrically in cortical homogenates. The activity of bound fraction of cathepsin D and L decreased significantly in animals exposed to the higher dose of cimetidine and sacrificed on the 42nd day. Also significant elevation of the free fraction of cathepsin L was noted in the same group of rats. Cathepsin activities were normalized during the next six weeks. No behavioural changes were noted among the observed animals. Unlike cimetidine, famotidine did not change profiles of the cerebral cathepsins.

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Acta Veterinaria Hungarica
Authors:
Ž. Grabarević
,
P. Džaja
,
J. Perić
,
V. Šerman
,
Z. Biđin
,
H. Mazija
,
N. Mas
,
Ž. Mikulec
,
K. Čuljak
,
Z. Šimec
, and
B. Njari

The work describes the effects of cimetidine on stress-induced gizzard erosions (Experiment A) and the influence of the long-term application (42 days) of the same drug on weight gain and feed consumption during broiler fattening (Experiment B). For Experiment A, 60 male, three-day-old chicks were divided into two groups: C (n = 30) - control chicks treated with 0.5 ml saline; CIM (n = 30) - chicks treated with cimetidine in a dose of 5 mg/kg body weight (b. w.) in-tragastrically. All chicks were stressed using a modified water-immersion stress method according to which the chicks, after 24 h of feed deprivation, were immersed in tap water (17 °C) for a few seconds. Under chloroform anaesthesia ten chicks from each group were killed 1, 2 and 3 h after the stressing. The morphometric analysis of gizzard erosion (GE) and histopathological examinations of gizzards were performed for each chick. In Experiment B, 32 one-day-old broilers of both sexes were used. The control group was untreated (n = 16) while the CIM group (n = 16) was fed the same diet supplemented with 10 mg of cimetidine per kilogram of feed throughout the fattening period (42 days). The results of Experiment A showed decreased mean length of the GE in the cimetidine-treated birds as compared with the GE lesions of the controls. In Experiment B, the treated chicks had reduced liveweight (1835.1 g), carcass weight (1474.6 g) and increased feed consumption (2115 g of feed per kilogram of weight gain) compared to the controls in which the same parameters were 1898.5 g, 1574.2 g and 1797 g, respectively. The results show that while stress-induced GE of chicks can be medicated pharmacologically, long-term application of the same substance impairs the results of fattening.

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Abstract  

The thermodynamic energy relationship between two crystal modifications of cimetidine was investigated and compared with differences in their processing properties with respect to transformation from one modification to the other.The crystal energies of the two modifications A and D were found to be almost identical and therefore the polymorphs are regarded as virtually isoenergetic crystals. This statement is based on DSC measurements of the melting points and of the enthalpies of fusion for the two crystal forms, which enable the calculation of the Gibbs free energy functions. Furthermore, the statement is supported by measurements of the enthalpies of solution in two different solvents. Both DSC and solution experiments reveal a slightly higher stability of the D modification with respect to the A form. In addition, tribomechanical treatment also indicates modification D to be the more stable one, as well as the higher density of the D form. No transformation during DSC at low heating rate was found which could be used in a stability consideration.As the explicit crystal structures of the two modifications are resolved, it was possible to calculate crystal energies theoretically as well. The theoretical results showed a remarkable difference in the crystal energies at zero degree Kelvin. Furthermore, they were just contradicting experimental findings by stating A being more stable than D. Possible reasons for this discrepancy and the feasibility of today's calculation methods with respect to prediction of stability properties are discussed.

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Acta Physiologica Hungarica
Authors:
J Dudka
,
F Burda
,
Barbara Madej
,
Justyna Szumilo
,
Edyta Tokarska
,
Agnieszka Korobowicz
,
R Klepacz
,
Monika ChyüyÅska
, and
Elżbieta Korobowicz

Metabolic acidosis complicates methanol, ethylene glycol and other alcohol intoxications. It is caused firstly by acid metabolites and secondly by the lactate elevation. The aim of the study was to evaluate the effect of alcohol dehydrogenase (ADH; EC 1.1.1.1) inhibitors and substrates: 4-methylpyrazole (4-MP), cimetidine, EDTA, ethanol and methanol on lactate dehydrogenase (LDH; EC 1.1.1.27) activity. The activity of LDH was determined spectrophotometrically in in vitro human heart homogenates with the mentioned compounds at 0.01, 0.1, 1.0 mM concentrations of 4-MP, cimetidine, EDTA, and 12.5, 25.0, 50.0 mM of ethanol and methanol. The LDH activity was significantly inhibited by 0.1 mM (p<0.05) and 1.0 mM (p<0.01) 4-MP and 1.00 mM EDTA (p<0.05). Higher LDH activity vs. control was observed in the samples incubated with all studied ethanol and methanol concentrations but these differences were not statistically significant. Thus, 4-MP was found to be the most effective inhibitor of LDH of all compounds tested. Therefore, such effect of 4-MP seems to be an additional advantage in methanol and ethylene glycol intoxications.

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Journal of Thermal Analysis and Calorimetry
Authors:
Nadábia de Souza
,
F. de Souza
,
I. Basílio
,
Ana Medeiros
,
E. Oliveira
,
Ana Santos
,
R. Macwdo
, and
R. Macędo
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]. In this study, FT-IR and/or thermal analysis using DSC was employed to study any interactions between grewia polysaccharide gum and the active pharmaceutical ingredients, cimetidine and ibuprofen. FT-IR spectroscopy provides a useful tool for the

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Gastric ulcer, a major gastrointestinal disorder is currently being treated by drugs which may come with side effects in a long run. Dietary intake of foods may alleviate or prevent gastric ulcer. This study was carried out by pretreating Sprague-Dawley rats with methanolic extracts of soya beans, soya beans fermented with Schizophyllum commune (a common medicinal-edible mushroom), cimetidine (positive control) and 10% Tween 20 (negative control) to evaluate protective effects against ethanol-induced injury in the gastric mucosa. Rats of negative control group showed haemorrhaging in gastric mucosa and were markedly alleviated in rats pretreated with soya bean extracts and cimetidine. When ulceration area was analysed, unfermented and fermented soya bean extracts and cimetidine were significantly better in the protection of the gastric mucosa against ethanol-induced injury compared to the negative control. However, no significant difference was found between pretreatment of both soya bean extracts and cimetidine. In terms of acidity of gastric mucosa content, rats pretreated with fermented soya beans were significantly acidic; whereas the mucus weight was significantly higher in gastric mucosa of rats pretreated with unfermented soya beans. Histological examination of gastric mucosa walls found that rats of the negative control group showed lesions in the mucosa area, oedema and leukocytes infiltration in the submucosa area, and that these were distinctly decreased in gastric mucosa tissue samples of rats pretreated with soya bean extracts and cimetidine; whereby fermented soya beans had a comparable effect with cimetidine. The study shows that S. commune fermented soya beans offer protection against ethanol-induced gastric ulcers in rats.

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Abstract

A simple, sensitive, and rapid RP-HPLC method for analysis of enalapril in the presence of H2-receptor antagonists has been developed and validated. Enalapril maleate was separated from H2-receptor antagonists by use of a 250 mm × 4.6 mm, 5-µm particle, C18 column with 86:14 (υ/υ) methanol-water, pH adjusted to 3.5, as mobile phase, at a flow rate of 1.5 mL min−1. UV detection was performed at 227 nm. The retention times of enalapril maleate, ranitidine, cimetidine, and famotidine were 3, 5, 7, and 7.5 min, respectively. The detection limit for enalapril was 10 ng mL−1 and the calibration plot was linear in the range 2.5–50 µg mL−1. In-vitro interaction of enalapril with the commonly administered H2-receptor antagonists cimetidine, ranitidine, and famotidine in simulated gastric juice at different pH and 37°C was also studied by use of this method. These studies clearly indicated that most of these H2-receptor antagonists bind to enalapril causing drastic changes in the availability of the drug. The HPLC method is accurate, selective, sensitive, and reproducible.

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Petersen-hernia, egy ritka sérvtípus megjelenése osztályunkon

Petersen hernia, a rare type of hernia in our department

Magyar Sebészet
Authors:
Keresztély Merkel
,
Tímea Vass
,
György Herczeg
,
Péter Ágh
, and
Miklós Máté

of peptic ulcer in the United States. Trends before and after the introduction of cimetidine. Lancet 1981; 1: 1305–1307. 5 Morgan H, Chastanet R

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