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From 5-cyano-3-chloro-2-pyrazinecarboxamide) (II) hydrolysis in acid medium) yielded 3-chloro-2,5-pyrazinedicarboxamide (III), which in a reaction with sodium hydrogensulfide in dimethyl-formamide) yielded 3-mercapto-2,5-pyrazinedicarboxamide (IV). This compound through condensations with alkyl- and arylhalogenides in triethylamine) yielded 3-alkyl(or aryl) thio-2,5-pyrazinedicarboxamides of type I. The structure of compounds was confirmed by elemental analysis, IR and 1H NMR spectra. A microbiological evaluation was carried out; the antituberculous effect of these compounds is not higher than that of pyrazinamide.

Consupren Spofa was demonstrated in our tests to be a distinguished immunomudulating agent. The preparation did not show any direct lymphotoxicity or myelotoxicity but it markedly influenced maturation of T lymphocytes in the thymus. When testing the functional activity of the immunity system in vivo, the inhibitory effect of Consupren Spofa was manifested only when administering a relatively larger dose of the drug with an antigenic stimulus or shortly after it, i.e., in the period of early activating processes. The use of a suitable time and dosage regimen is therefore decisive to induce an inhibitory effect. On the basis of comparative experiments it can be stated that Consupren Spofa is minimally as much effective as, or in some experiments even more effective than Sandimmun Sandoz.

Biotransformation of the anticholinesterasic agent 9-amino-7-methoxy-1,2,3,4-tetrahydroacridine was studied in the laboratory rat. In the animal urine, the main identified metabolites were 9-amino-7-hydroxy-1,2,3,4-tetrahydroacridine and its conjugate with glucuronic acid, or sulfuric acid, as well as 9-amino-1-hydroxy-7-methoxy-1,2,3,4-tetrahydroacridine and 9-amino-2-hydroxy-7-methoxy-1,2,3,4-tetrahydroacridine. A part of the drug was excreted in an unchanged form.

In a representative group of 10 conventional antihistaminic agents, a comparison of their H1-antagonistic efficacy was carried out in a series of pharmacological tests. A very good correlation of findings obtained under in vivo conditions in guinea-pigs (tests of detoxication of histamine and histamine aerosol) and a test in rats, which examined the influence on local changes induced by histamine in the dermal region, was demonstrated. No statistically significant correlation of in vivo findings and receptor binding studies on membranes of the rat brain (displacement of (3H)-mepyramine) was found. The tests based on displacement of (3H)-mepyramine are usable primarily for the needs of screening research. The predictive value of pharmacological findings obtained under in vivo conditions is substantially higher.

The effects of the novel potential thyrostatic agent 1-p-bromphenyl-5- mercapto-1,2,3,4-tetrazole (Br-FMT) on the serum levels of thyroxine, thyrotropic hormone (TSH), the content of cyclic adenosine monophosphate (cAMP) in the thyroid gland, the body weight and the weight of the thyroid gland in liver transaminases and the white blood picture in Wistar strain rats were investigated. The effect of Br-FMT was compared with the effect of the well-known thyrostatic agent and goitrogen ethylester of 3-methyl-2-thio-4-imidazoline-1- carboxylic acid, carbimazole (Spofa) and with the control group, which received placebo only. The drugs tested were administered to animals in the dose do 7.5 mumol/animal via a gastric tube for the period of one month. Br-FMT and carbimazole decreased the level of serum thyroxine in a statistically significant manner. The serum level of TSH was evidently decreased after Br-FMT; it was not changed after administration of carbimazole in the given dose. The content of cAMP in the thyroid gland was significantly increased only after carbimazole. The weight of the thyroid gland was not significantly changed in any group under study, though after carbimazole the mean value was higher by a quarter as compared with the control group. The body weight and white blood picture were not significantly changed in all groups under study. ALT and AST values were evidently lower after carbimazole and Br-FMT, most probably due to the hypothyroid state of the animals.(ABSTRACT TRUNCATED AT 250 WORDS)

For the determination of mefenoxalon in substance, tablets and biological material (blood plasma), four variants were worked out. The first of them is based on the substitution of the benzene ring with bromine with the use of an excess of bromine, which is determined ionometrically. The second variant is based on direct titration of the hydrolytic product mefenoxalon, 3-(2-methoxyphenoxy)-2-hydroxypropylamine, with the use of the ion-selective electrode of the coated-wire type with a volumetric solution of tetraphenyl-borsodium. The third variant utilizes direct measurements of UV spectra of mefenoxalon in a solution of dichlorethane. The fourth variant consists in its fluorimetric measurement in a solution of dichlorethane, or ethylacetate. A detailed discussion of advantages and disadvantages of all above-mentioned variants of determination is presented.

A hundred years ago, the Pharmaceutical Society in Prague, on the initiative of PhMr. H. Rüdiger, the then pharmacist in Kralupy, and with great participation of PhMr. K. Schürer, the then owner of a firm furnishing pharmacies, participated in the Jubilee Country's Exhibition from May 15 to October 18, 1891 in Prague. Sixteen Czech pharmacists exhibited the products of their laboratories and manufacturing plants, galenical and chemical preparations and the first "specialities of pharmacies", personal and home medicine-cases and various adjusting and auxiliary material (such as bottles and ointment jars), "medicinal wafers" and the pertinent devices for their closing (PhMr. Fr. Sevcík from Prague). K. Schürer exhibited a complete equipment of a modern pharmacy with glass and porcelain drug jars and various pharmaceutical utensils. It was for the first time that pharmaceutical historical material, documentary and literary items were exhibited for the general public. The top exhibit was the Prague baroque pharmacy "The Golden Crown", which was donated to the National Museum in Prague when the exhibition was closed. The exhibition was put under a boycott by some German industrialists and the German pharmacists from Bohemia ostentatiously rejected any participation. The exhibition and its pharmaceutical part thus resulted in a distinguished achievement of Czech effort and work.

An analytical method was worked out to determine Lonazolac in human plasma based on precipitation of human plasma with a precipitating agent and methanol. This deproteinized plasma was analyzed by liquid chromatography with the use of a reverse phase and fluorimetric detection. The described method is sufficiently sensitive (the limit of detection under 0.1 microgram/ml of plasma) and precise (error of the method = 9%). The precision of the method, recovery from the plasma (100 +/- 3%) and stability in frozen plasma (minimally one month) are presented. Application of the method in a comparison of the newly developed Czechoslovak preparation Lonazolac and the foreign preparation Irritren is shown. Results are documented by the course of the levels of both preparations in dependence on time and principal pharmacokinetic parameters derived from the one-compartmental model.