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Biomedical subjects

L Safarík

Publications and source records attributed to L Safarík.

32 records · Page 2Linked to original sources

[Changes in pharmacokinetics of trimecaine in patients with liver cirrhosis].

Trimecaine (Mesocain, Léciva) an analogous preparation to lidocaine is used as a local anaesthetic, antiarrhythmic and spasmolytic preparation. The purpose of the investigation was to assess the fate of trimecaine in nine patients with compensated cirrhosis of the liver. The pharmacokinetics were evaluated after intravenous infusion of trimecaine administered at a rate of 150-200 mg.h-1. Plasma concentrations of the drug evaluated by gas chromatography indicate a marked retardation of trimecaine elimination in patients with liver damage. In the group of patients with cirrhosis of the liver the total clearance of the drug was lower (8.7 +/- 5.0 1.h-1), as compared with the group of patients without liver damage (34.7 +/- 19.4 1.h-1). In patients with cirrhosis of the liver also a multiple reduction of distribution volumes was observed. The results indicate a high hepatic extraction of

Humans↗

Peroxidase-mediated reaction of the carcinogenic non-aminoazo dye 1-phenylazo-2-hydroxynaphthalene with transfer ribonucleic acid.

Horseradish peroxidase in the presence of hydrogen peroxide has the ability to mediate the activation of carcinogenic 1-phenylazo-2-hydroxynaphthalene (Sudan I) to DNA- and transfer RNA (tRNA)-bound products in vitro. tRNA is more accessible for modification by the activated carcinogen studied. tRNA modified by activated Sudan I becomes colored and has an absorption maximum of approximately 480 nm. Binding of metabolite(s) to tRNA is inhibited by ascorbate, glutathione, Mg2+ ions and nitrosobenzene. The mechanism of these protections was shown to be different for the different agents. tRNA modified by activated Sudan I exhibits a significantly increased acceptance for L-methionine. Enzymatic hydrolysis of modified tRNA with subsequent separation of nucleosides by HPLC suggests that the covalent modification of tRNA originating from the formation of more than one adduct with the nucleosides in tRNA is the predominant interaction of the activated Sudan I with tRNA.

Animals↗

High-performance liquid chromatography of deacetylmetipranolol in plasma.

A sensitive high-performance liquid chromatographic method with electro-chemical detection is developed for the determination of deacetylmetipranolol (DMP), an active metabolite of beta-sympatholytic drug metipranolol (MP). DMP is extracted from the plasma after basifying with dichloromethane. After evaporation, the residue is reconstituted in the mobile phase, injected onto the reversed-phase ODS column and chromatographed at 50 degrees C. The sensitivity of the method is 2 ng of DMP in 1 ml plasma. Pindolol, another beta-blocking agent is used as internal standard. The method is used for a pharmacokinetic investigation of MP in healthy volunteers and in the patients with liver cirrhosis.

Adrenergic beta-Antagonists↗

Content uniformity test of tablets by nonaqueous titration method.

For the Content uniformity test (CUT) of tablets where the active drug behaves in a nonaqueous medium as a base a very simple method was developed. This method is based on the extraction of the active drug from the tablet into anhydrous acetic acid and direct titration of the solute with HClO4 (0.1 or 0.05 mol/l solution in anhydrous acetic acid). The course of the titration is followed potentiometrically with a glass and calomel electrode coupled and recorded automatically with a suitable registration potentiometer. The method was successfully applied to samples of commercial tablets containing the following drugs: codeine phosphate, embramine, ephedrine, ethylmorphine, pyridoxine, thiamine and tolazoline, all as hydrochlorides. It can be used also for several other drugs.

Alkaloids↗