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Biomedical subjects

T Trnovec

Publications and source records attributed to T Trnovec.

At least 109 records · Page 6Linked to original sources

Phagocytic activity of reticuloendothelial system of mice in shock-like state following administration of polysaccharide-protein complex isolated from Candida albicans.

Fever and shock are symptoms of acute disseminated candidiasis. Phagocytic activity of the reticuloendothelial system (RES), following a single administration of polysaccharide-protein complex, was studied with respect to the role of the RES in the pathophysiology of circulatory shock. The index of phagocytic activity was determined 15 or 120 minutes following IV administration of polysaccharide-protein complex (50 mg/kg) to mice, from the rates of clearance of carbon particles and of heterologous erythrocytes labeled with 51Cr. The mice were pretreated with hydrocortisone 300 mg/kg, methylprednisolone, 30 mg/kg, or saline 120 minutes before administration of the polysaccharide-protein complex. Depression of the phagocytic activity was observed following administration of polysaccharide-protein complex in both time intervals investigated. This depression could be prevented successfully by administration of both glucocorticoids studied. The fractional distribution of 86Rb was determined in other groups of identically treated mice. An increase of 86Rb uptake was found in the heart, lungs, and adrenals 15 minutes after administration of polysaccharide-protein complex. A decrease of 86Rb uptake was found in the intestines and spleen. These changes were also found in mice pretreated with glucocorticoids. A return to the normal picture of 86Rb fractional distribution was found 120 minutes after polysaccharide-protein administration. It was suggested that changes in phagocytic activity were not a result of altered hemodynamics.

Animals↗

Biliary excretion and enterohepatic circulation of two beta-adrenergic blocking drugs, exaprolol and propranolol, in rats.

Plasma levels and excretion of two beta-adrenoceptor blocking drugs 3H-exaprolol and 3H-propranolol were observed up to 96 h after a single i.v. administration to rats. Terminal half-lives of 26.8 +/- 9.1 h and 51.3 +/- 7.5 h were found for exaprolol and propranolol, respectively. The recovery of 3H radioactivity in feces following i.v. administration of the drugs (34.2 +/- 0.8 per cent and 12.0 +/- 1.3 per cent 3H of exaprolol and propranolol, respectively) is of biliary origin, as 30.7 +/- 3.5 per cent and 13.4 +/- 3.6 per cent 3H of exaprolol and propranolol, respectively, was excreted in the bile after i.v. administration. Enterohepatic circulation of the drugs was studied using the donor-recipient rat method. After intraduodenal administration of donor bile to the recipient rat approximately 50 per cent and 40 per cent of the biliary 3H activity of exaprolol and propranolol, respectively, was re-excreted following absorption. A formula for calculating the amount of the substance together with its metabolites excreted in the bile, urine or feces as a result of enterohepatic circulation has been proposed.

Adrenergic beta-Antagonists↗

The disposition of the local anaesthetic, pentacaine, in rats and mice.

The pharmacokinetics of pentacaine, a new local anaesthetic agent from the group of carbanilates, was investigated in the rat at a dose of 2 mg kg-1 i.v. and per os. A three-compartment open model gave the best fit to the data. The model parameters are: t1/2 99.0 +/- 14.1 min, Vss 7411.1 ml kg-1, Cl 77.9 ml min-1 kg-1; after oral administration t1/2ab 4.9 +/- 1.9 min, bioavailability 59.1 per cent, and extent of absorption 79.3 per cent. Pentacaine is eliminated almost entirely by metabolism. The metabolites are excreted equally in the urine and faeces at a relatively slow rate. The pharmacokinetics of pentacaine was linear in the dose range 0.008-4 mg kg-1. The whole-body autoradiography in mice showed rapid transfer of 3H radioactivity from the vessels to tissues and a markedly heterogeneous disposition pattern in organs.

Administration, Oral↗

The pharmacokinetics of exaprolol and propranolol in rats with interrupted enterohepatic circulation.

The pharmacokinetics of two beta adrenoceptor blocking drugs, exaprolol and propranolol, in rats with interrupted enterohepatic circulation was studied. The tritium-labelled drugs were given intravenously to four groups of rats: control, bile-duct cannulated, bile-duct ligated, and pretreated with neomycin. Plasma levels and excretion were observed up to 96 h after administration. The pharmacokinetic parameters show an enhanced plasma elimination of both drugs at interrupted enterohepatic circulation compared to the control group. Significant changes were observed in the excretion pattern with bile-duct cannulated and bile-duct ligated rats, while the total radioactivity excreted in urine and faeces does not differ between control and neomycin pretreated rats.

Adrenergic beta-Antagonists↗

Tissue distribution of exaprolol in rat.

The disposition of the beta adrenoceptor blocking drug 1-(2-cyclohexylphenoxy)-3-isopropylamino-2-propanol, exaprolol, in organs of the rat has been studied. After i.v. administration of 3H-exaprolol a transient extremely high accumulation of the drug in lungs was observed with a peak of 7.7% of dose/g 30 min post-administration. The disposition pattern in heart, kidneys and liver may be characterized by a tissue to plasma ratio about ten. Lower exaprolol tissue levels were observed after oral administration. The tissue to plasma ratios showed an initial increase followed by constant levels. The distribution of exaprolol in organs of the rat is discussed in the light of the previously determined pharmacokinetic parameters.

Administration, Oral↗

Formation of didesmethylethimizol (4-5-dicarbamoyl-1-ethylimidazole) in man.

The chemical structure of an ethimizol metabolite found earlier in human urine and saliva was established as 4,5-dicarbamoyl-1-ethylimidazole (didesmethylethimizol). The treatment of biological samples comprised a solid-phase extraction, high-performance thin-layer chromatographic separation and high-performance liquid chromatographic purification techniques. The identification of the metabolite was based on the comparison of a mass spectrum of the substance isolated from the biological fluid with the mass spectra of synthetised reference compounds.

Chemical Phenomena↗