Vol 14, No 3 (2016)

The review is devoted to the questions of improvement of the efficacy of myocardial infarction treatment by means of pharmacological drugs possessing pre- or postconditioning effect. The proofs of clinical efficacy of reperfusional therapy of the myocardial infarction are observed using examples of adenosine, activators of KATP channels (diazoxide and nicorandil), opiates (fentanyl, morphine) and some other drugs. The data are analyzed from the point of modern view of molecular mechanisms of hypoxia, the findings of objective laboratory and instrumental control in therapy of myocardial infarction in differend known clinical trials. It is concluded that pharmacological preconditioning is perspective approach in therapy of the acute myocardial infarction both in animal models and in humans.

The authors analyze the data of modern national literature about the importance of spiral computed tomography (SCT) and its role in solving diagnostic and therapeutic problems in respiratory tuberculosis. The most frequently discussed aspects at the present stage include questions of activity of tuberculosis process, thedifferential diagnosis of rounded formations, disseminated lesions of the lung tissue. The application of the currently proposed contrasting techniques of SCT improves the quality of diagnosis from the syndrome to the nosological level. The results presented show that the inclusion of SCT of the chest in standards of the examination of a patient with suspected tuberculosis will improve the quality of care for the discussed patients.

 

The GABA molecule was shown to the methods of quantum mechanic characteristics and molecular geometry has three conformational states: linear (GABA-1 conformer), cyclic (GABA-2 comformer) and bucket-like (GABA-3 conformer). The play different functions in the brain neurons: cyclic and bucket-like conformers play role of endogenous transmitters, and linear conformer participates in neuronal metabolism. The theoretical conformational analysis shows there are two types of GABA receptors in the CNS neurons: GABA-2 receptors, agonists of which are cyclic conformer of GABA, glycine and β-alanine and antagonists are bemegride, pentilentetrazol and strychnine; and GABA-3 receptors, agonists of which is bucket-like conformer of GABA and antagonists are picrotoxin and bicuculline. Anticonvulsive and other behavioral effects of derivatives of barbituric acid, benzazepine, benzodiazepine, gidantoine, succinimide and oxasolidindione are realized probably via GABA-2 receptors to switch on them the following functional centers of their structure are nessesary: α, γ and [δ-ε] for barbitirates; β, [δ-ε] and γ for carbamazepine; β and [δ-ε] for benzodiazepine derivatives, gabapentine and vigabatrine; α, β, γ and [δ-ε] for gidantoine and oxasolidindione derivatives; α, β, γ for succinimide derivatives. The power of any behavioral effect of anticonvulsants and inhibitory amino acids depends on power, location and numbers of hydrogen bounds developed between active centers of pharmacophore of anticonvulsant or inhibitory amino acids and active centers of functional skeleton of GABA-2 receptor complex, these properties determine absense of nootropic activity in anticonvulsive drugs and presense of them in inhibitory amino acids. It is concluded there are perspectives of synthesis of conpounds, pharmacophore of which should be like as cyclic conformer of GABA, glycine and β-alanine on their quantum mechanic characteristics and molecular geometry

In an experimental model of respiratory failure induced by a single intraperitoneal injection of 1 LD50 of paraquat (24 mg/kg) the changes of physical activity tolerance, respiratory function parameters were studied and histomorphologic validation of experimental results was confirmed. In a model of respiratory failure the assessment of analgesic activity and toxicity of fentanyl, dexmedetomidine and their combination was made and compared with intact animals. The integral tolerance rates (therapeutic action width) were also estimated. It was shown that on the background of pulmonary pathology for each of the drugs 13-28% decrease of average lethal doses was observed. At the same time when administered in combination an average effective dose of the drugs wasn’t changed in contrast with single-drug analgesia.