[Simulation of kinetics of phenazepam and its metabolite 3-hydroxyphenazepam in cat blood]. / Modelirovanie kinetiki fenazepama i ego metabolita 3-oksifenazepama v krovi koshek.

The pharmacokinetics of the tranquilizer phenazepam and its high-active metabolite 3-hydroxyphenazepam in the cat blood was studied in experiments using gas liquid chromatography and mathematic simulation. The experimental findings were computer-processed. An appreciable quantity of 3-hydroxyphenazepam was found in the blood in addition to the unchanged drug at any times after oral administration of phenazepam (2 mg/kg). Joint modelling of the kinetics of phenazepam and 2-hydroxyphenazepam within the same metabolic model allowed calculating the kinetic parameters of both the compounds. The elimination constant of the metabolite in cats was found to be twice as high on the average as compared to that of the unchanged drug.

[Mechanism of the effect of diazepam on acetylcholine concentration in mouse brain]. / Issledovanie mekhanizma vliianiia diazepama na soderzhanie atsetilkholina v golovnom mozge myshei.

Intraperitoneal injection of diazepam (20 mg/kg) caused an increase of free and bound acetylcholine in the mouse brain. Diazepam pretreatment (20 mg/kg) increased galanthamine anticholinesterase activity and its toxicity; as to physostigmine, armine, and paraoxon toxicity--it remained unchanged. It is supposed that diazepam blocks the release of aetylcholine from the cholinergic nerve terminals which should result in a decrease of functional acetylcholine concentrations in the synapse.

[Effect of diazepam on the properties of an erythrocyte-plasma protein complex and the development of shock during the transfusion of heterogenic blood]. / Vliianie diazepama na svoistva kompleksa éritrotsity-belki plazmy i razvitie shoka pri perelivanii geterogennoi krovi.

Preliminary administration of 2 mg/kg of diazepam eliminated the pyrogenic reaction and increased survival of rabbits following intravenous injection of cat blood to them. A study of physico-chemical properties of the blood by measurement of the ionization balance in thermal denaturing demonstrated that injection of heterogenous blood to rabbits and suspension of rabbit erythrocytes in cat plasma in vitro led to a sharp reduction of the rate of proton binding with plasma proteins in the presence of foreign erythrocytes. Preliminary administration of diazepam to rabbits, and diazepam addition to the cat plasma in vitro prevented such changes and promoted retention of normal blood properties. Addition of diazepam in a concentration of about 10--4 M to the heterogenous plasma decreased erythrocyte agglutination considerably.

[Effect of 1,4-benzodiazepine derivatives on the toxic action of oxygen under increased pressure]. / Vliianie proizvodnykh 1,4-benzodiazepina na toksicheskoe deistvie kisloroda pod povyshennym davleniem

The 1,4-benzodiazepine derivatives (diazepam, nitrazepm, lorazepam, clonazepam and two newly synthetized compounds of this series) increase the resistance of albino rats and rabbits to the toxic effect of oxygen under high pressure (7 and 5.5 atm respectively). The compounds under study are apt to avert over a long period the development of metabolic acidosis which appears following the action of high-pressure oxygen on the body.