[Investigation of the anti-motion sickness effect of 3-hydroxypyridine derivatives].

Experiments with rats showed that three out of 12 3-hydroxypyridine derivatives (ethyl-methyl hyd- roxypyrine succinate, SK-132 and IBCP-2 - had an anti-motion sickness effect stronger than of scopolamine, the reference vestiboloprotector. The anti-motion sickness effect of ethyl-methyl hydroxypyrine was also demonstrated in experiments with cats. Apparent anti-motion sickness effect of ethyl-methyl hydroxypyrine (mexydol) was found in 69% of healthy male volunteers which is comparable with the effect of scopolamine (62%). In experiments with immobilized cats (myorelaxation drugs) the microelectrode technique and microontoiphoresis of physiologically active substances revealed that ethylmethyl hydroxypyrine influences the majority of neurons in the medial vestibular nucleus (61%). Suppression of cell spontaneous activities in more than one half of cases can be stopped completely or attenuated significantly by bicucculine, a specific GABA(A)-receptor antagonist. In 42% of neurons ethyl-methyl hydroxypyrine subdues the response to vestibular stimulation which is likely to underlie the anti-motion sickness effect.

[Neuroendocrine factors in pathogenesis of motion sickness and the protective effect of drugs]. / Neiroéndocrinnye faktory v patogenenze bolezni dvizheniia i zashchitnom deistvii lekarstvennykh veshchestv.

The paper presents a generalization of many-year complex investigations performed at various departments of the Institute of Medico-Biological Problems (Moscow) and various laboratories and institutes of the Ministry of Public Health and the Russian Academy of Medical Sciences, devoted to the pathogenesis of motion disease (sea sickness, vestibulo vegetative syndrome, various forms of kinetosis). The main attention is given to interpretation of the mechanisms of therapeutic and prophylactic action of drugs used for the treatment of such disorders. In particular, the role of a hormonal component of the system of regulation of physiological functions is considered as manifested in the models of the vestibulovegetative syndrome and in the pharmacotherapy of the motion disease.

[Pharmacological prophylaxis of vestibulo-autonomous syndrome (motion sickness) in model investigations]. / Farmakologicheskaia profilaktika vestibulovegetativnogo sindroma (bolezni dvizheniia) v model'nykh issledovaniiakh.

The authors summarize results of multiyear investigations at the Institute of Biomedical Problems of induced motion sickness and development of prophylactic medicaments representing various classes of biologically active substances (choline blocking agents, sympathomimetics, antihistamines etc.) prescribed singularly or in an combination based on the knowledge of MS-provoking inter-receptor interactions and therapeutic effects of drugs.

[The pharmacological correction of hemodynamics during the simulation of the early period of adaptation to weightlessness]. / Farmakologicheskaia korrektsiia gemodinamiki pri modelirovanii rannego perioda adaptatsii k nevesomosti.

Investigations of volunteered subjects in whom antiorthostatic hypokinesia was modeled by tilting the cranial end of the body by -15 degrees were to answer whether pharmacological countermeasures of the vestibular/autonomous syndrome (motion sickness, sea sickness) alter the orthostatic tolerance and cardiovascular parameters. As was stated, the drugs allow controlled correction of hemodynamic resistance to the head-down tilt. Ephedrine, phencarol, ephedrine combined with scopolamine and pipolphen, and stugeron normalized cerebral circulation. Medicaments were unable to moderate the sympathoadrenal reaction to the head-down tilt; however, blood concentrations of catecholamines were significantly lower than in the control. The greatest effect was achieved using ephedrine and ephedrine plus pipolphen.

[An experimental validation of pharmacological agents to arrest the vestibulo-autonomic syndrome (motion sickness)]. / Eksperimental'noe obosnovanie farmakologicheskikh sredtsv kupirovaniia vestibulo-vegetativnogo sindroma (bolezn' dvizheniia).

The results of development and experimental evaluation of the efficiency of pharmacological means of cupping the vestibulo-vegetative syndrome in man are presented. A model and procedure of evaluation of pharmacological cupping of the Vestibulo-vegetative syndrome are developed. The intramuscular injection of the mixture containing ephedrine, promethazine hydrochloride and strychnine (25, 50, and 1 mg, respectively) appeared most effective.

[The problems of the experimental and clinical pharmacology of venotropic drugs]. / Voprosy éksperimental'noi i klinicheskoi farmakologii venotropnykh lekarstvennykh sredstv.

The article deals with problems of phenomenology of the selective vasomotor response of veins to the effect of drugs, analyses the peripheral and central hemodynamic effects of venotropic drugs, discusses and systematizes the principles of correct quantitative evaluation of venomotor reactions. Some representatives of the group of venotropic drugs are characterized and the main problems of their clinical use are discussed. The problems of promising trends of research are formulated.

[The role of neurochemical mechanisms in the pathogenesis of kinetoses and the therapeutic-prophylactic action of drugs]. / Rol' neirokhimicheskikh mekhanizmov v patogeneze kinetozov i lechebno-profilakticheskom deistvii lekarstvennykh sredstv.

Experimental and clinical data on the neurochemical and neurohumoral mechanisms underlying the pathogenesis and therapeutic and preventive effects of drugs are generalized. Literature data and the authors' own data concerning drugs used for the prevention and treatment of kinetoses are given. The possible mechanisms of their effect against motion sickness are suggested. New ideas of the means of search for substances possessing vestibuloprotective activity, and the principles of rational pharmacological correction of vestibuloautonomic disorders in motion sickness are discussed.

[Movement disorders in the context of P.K. Anokhin's theory of functional systems]. / Bolezn' dvizheniia s pozitsii teorii funktsional'nykh sistem P.K. Anokhina.

The authors' own findings and the data available in the literature as to movement diseases (MD) in animals and man were reviewed in the context of P. K. Anokhin's theory of functional systems. The functional system of the human body's gravity center is detailed. There is evidence for that disintegration processes underlying MD first occur in the mnestic sphere since due to genetic and/or ontogenetic causes, memory has no preserved no motor programme required to achieve the end net efficiency of performance of this functional system,--to maintain the definite position of the gravity center of the body and its related vegetative status upon stress-induced vestibular exposures. Based on the above concepts of the pathogenesis of MD, its preventive measures have been proposed and tested, which include drug (nootropic agents) and non-drug (a special complex of physical exercises for children aged 2 to 7 years, which will form permanent motor programs in memory in definite periods of their ontogenesis) measures.