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[Effect of butyrophenone derivatives on D-serotonin reactive structures].
Farmakol Toksikol
November 1979
Droperidol, haloperidol and azabutyron inhibit the reactions of rabbit aortal stria caused by stimulation of D-type serotonine receptors. Droperidol appears most active in this respect. Its antiserotonine properties are characterised by certain selectivity.
View Article and Find Full Text PDFSpectrofluorometric determination of the noradrenaline content in the non-purified fraction of the rat's brain stem synaptosomes and radioisotope method resulted in finding that carbidine is capable to release noradrenaline from the nerve endings. Azabutyron, droperidol and fluphenazine had no noticeable effect on this process. The release of noradrenaline with carbidine depends upon the presence of Ca2+ ions in the medium.
View Article and Find Full Text PDFIn patients presenting mitral and aortal valvular defects with contemplated valve prosthetics it was shown that after an intravenous administration of azabutyrone in a dose of 4 mg/kg the drug produced a hypotensive effect in the large circulation, reduced insignificantly the cardiac output, venous pressure and the total peripheral resistance, inducing, at the same time, a short-term rise of the heart rate. The drug forced down materially (by more than 50 per cent) the pulmonary artery pressure in patients with pulmonary hypertension. The azabutyrone effects were seen to continue for 30 minutes with its blood plasma concentration of 1.
View Article and Find Full Text PDF[Clinical pharmacokinetics of azabutyron, a new short-term action neuroleptic].
Farmakol Toksikol
August 1978
Pharmacokinetics of azabutyron--a new Soviet-made neuroleptic was studied clinically without anesthesia and also during surgery against the background of deep and surface fluorothan anesthesia in conjunction with artificial nitrous oxide and oxygen ventilation of the lungs (2:1). After intravenous administration of the drug in a dose of 4 mg/kg its maximum concentration (about 8 gamma/ml) was recorded in 5 minutes and the amount eliminated during 2 hours of observation comprised 1--2 per cent of the dose introduced. In practically healthy individuals with no anesthesia the pharmacokinetics of azabutyron lies within the limits of a bicompartment pharmacokinetics model, while surface anesthesia, blood loss changes the pharmacokinetics of the drug to such an extent that is has to be described from the standpoint of the unicompartment model system.
View Article and Find Full Text PDFThin-layer and gas chromatography, spectrophotometry and mass-spectrometry were employed in studying metabolism of the neuroleptic azabutyron in man. It was ascertained that azabutyron is eliminated from the human organism in 24 hours unchanged (10 per cent of the dose administered). The main ways of its metabolism are oxidative N-dealkylation, reduction of the carboxylic group in the molecule, N-oxidation and conjugation of the drug.
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