Pharmacological Properties of Sulfonamide Derivatives, New Inhibitors of Carbonic Anhydrase.

Selective blocking of individual isoforms of carbonic anhydrase (CA) is now one of the main directions in the development of its inhibitors. The new 1,2,4-oxadiazole-containing sulfonamides B12 and B13 predominantly block CA II and CA IX. The study of acute toxicity of B12 and B13 showed their safety. Substance B13 caused a relatively short-term, but rapid (within 30 min) decrease in the intraocular pressure in rabbits, which indicates the promise of its use for the emergency decrease in the intraocular pressure in medical practice. Analysis of the effects of sulfonamides on the functions of CNS showed that compound B12 probably exhibit tranquilizing activity; B13 is promising for the creation of drugs that have an antidepressant effect and at the same time increase the mental and physical performance.

[Clinical and laboratory assessment of indicators of oxidative status in the cerebrospinal fluid of patients with ischemic stroke].

The objective of the present study was to estimate parameters of oxidative status in the cerebrospinal fluid in the course of ischemic stroke and in the prediction of recovery of neurological functions. Concentration of superoxide dismutase (SOD) as a marker of antioxidant adaptation, the secondary lipid peroxidation products reacting with thiobarbituric acid (PRTBA), cyclic guanosine monophosphate (cGMP) as an indirect product of NO generation, and N-acetylneuraminic acid (NANA) as a marker of destruction of neuronal membranes were studied. One hundred and fifty patients with hemispheric ischemic stroke admitted to a hospital during the first 12 h after stroke were examined. It has been shown that the development of cerebral infarction is accompanied by increased concentrations of oxidative stress markers. Progressive ischemic stroke was characterized by the significantly prolonged increase in PRTBA, cGMP, NANA to the third day from the first symptoms of disease while regressive course was accompanied by the lack of higher production of TBKRP, cGMP, NANA to the third day of disease. The decrease in concentrations of factors of brain damage (PRTBA, cGMP, NANA) in the cerebrospinal fluid, along with the increasing role of processes of antioxidant adaptation, expressed in the growth of SOD concentrations, can be considered as a criterion for the prediction of recovery of disturbed neurologic function to the 21th day of disease.

Lipid composition in rats with nonischemic chronic heart failure.

The initial stages of nonischemic chronic heart failure in rats (model of oleothorax) were accompanied by the development of dyslipidemia. This state was characterized by an increase in total cholesterol concentration (due to the fraction of low-density lipoproteins) and atherogenicity index. The concentrations of plasma total cholesterol and low-density lipoproteins were shown to decrease in animals with severe course of nonischemic chronic heart failure. These changes were accompanied by a decrease in the atherogenicity index. Intragastric administration of cholesterol had little effect on the lipid composition of blood plasma in rats, irrespective of the severity of heart failure.

[Neurohumoral mechanisms of the rat heart adaptation to overload].

The present study confirms involvement of the sympathicoadrenal system in adaptation of heart to overload. Besides, at formation of chronic heart failure (CHF) there have been revealed a rise of the histamine and serotonin levels in blood plasma and myocardium as well as glucocorticoid hyperactivation.

[Influence of ecdysteron-80 on the hormonal-mediator balance and lipid metabolism in rats with chronic cardiac failure].

Administration of ecdysteron-80 made of Serratula coronata L. to rats with experimental chronic cardiac failure partially corrects hormonal and mediator imbalance typical for this pathology. By some parameters this correction is full. By improving lipid metabolism, ecdysteron-80 reduces blood plasma atherogenicity.

Effect of beta-adrenoblockers on heart rate variability in awake and narcotized rats.

In narcotized rats, beta-adrenoceptor blockers changed all parameters of heart rate variability indicating up-regulation of parasympathetic activity and down-regulation of the sympathetic one. In immobilized awake rats, the temporal and geometrical parameters varied similarly, while spectral analysis indicated possible activation of other neurohumoral mechanisms against the background of beta-blocker treatment.

Survival of rats with experimental chronic heart failure depending on pharmacodynamic and pharmacokinetic parameters of angiotensin-converting enzyme inhibitors and beta-adrenoceptor blockers.

Lipophilic inhibitors of angiotensin-converting enzyme increased 6-month survival and/or lifetime of rats with experimental chronic heart failure. These drugs had no effect on the mortality rate of animals with acute decompensation of the disease. beta-Adrenoceptor blockers without intrinsic sympathomimetic activity not only prolonged 6-month survival and lifetime, but also decreased the mortality rate of rats with decompensation of chronic heart failure.

[A dynamic model of total chronic heart failure in rats].

A dynamic model ofbiventricular chronic heart failure (CHF) induced by fractional introduction of silicon oil into the pleural cavity in rats is proposed. Silicon oil led to enlargement of the heart, myocardial hypertrophy of both ventricles, considerable pulmonary and hepatic congestion due to circulatory failure, decreased stroke volume and cardiac output, increased peripheral vascular resistance, changes in the activity of sympathoadrenal system of the heart and blood. The severity of the induced CHF varied with the dose and number of silicon oil administrations.

[Free radicals in cerebral ischemia]. / Svobodnye radikaly pri ishemii golovnogo mozga.

The review considers an involvement of active oxygen forms, nitric oxide (NO) and its active forms in accumulation of low molecular weight cytotoxic compounds that lead directly to cell death. A dual role of free radicals in cerebral ischemia, free radical function as secondary messengers are analysed.

[Radionuclide accumulation in fruit bodies of macromycetes]. / Akkumuliatsiia radionuklidov v plodovykh telakh makromitsetov.

Coefficients of 137Cs accumulation and 90Sr were determined in macromycetes of different trophic groups (137Cs in 43 species and 90Sr in 19 species) in the conditions of droughty year (1992). Their variability in forest formations was determined in the period from 1992 to 1998. In the year with increased atmospheric humidity (1998), two-fold rise of 137Cs accumulation in fruit bodies was registered on average. The pollution of Boletus edulis correlates with photosynthetically active part of Betula pendula and Pinus silvestris closer than with soil pollution. This shows the possibility to indicate the pollution of short-living fruit bodies of fungi by the pollution of plants-symbiotrophs.

[A comprehensive clinico-neurophysiological study of the efficacy of the pharmaceutical preparation glycine in acute ischemic stroke]. / Kompleksnoe kliniko-neirofiziologicheskoe izuchenie éffektivnosti farmatsevticheskogo preparata glitsina v ostrom periode ishemicheskogo insul'ta.

In intensive care unit 226 patients underwent step-by-step clinical and neurophysiological investigation of glycin chemotherapy efficiency in the acute period of ischaemic stroke. Investigation included double-blind placebo controlled method, monitoring (by means of EEG, toposelective mapping of EEG, SSEP, transcutaneous cortical electric stimulation, ENMG) of changes of brain functional state after the first drug dose and course of treatment, analysis of dose-dependent action of the drug, posticchemic follow-up. It was found out, that usage of the drug glycin (daily dose 1-2 grams) in the combined intensive treatment of stroke provided for significant acceleration of regress of disorders of consciousness and other general and focal signs (in comparison with severity-matched control group), and more complete and stable restoration of function to the end of acute period of the disease.

[Acute postoperative pancreatitis]. / Ostryi posleoperatsionnyi pankreatit.

The authors analysed 373 patients with acute pancreatitis which developed after operations on the organs of the pancreatoduodenal zone. Acute postoperative pancreatitis developed in 17.15% of cases after operations on the biliary tract, in 26.8% after resection of the stomach for ulcer, and in 51.47% of cases after resection of the stomach for carcinoma. A comparative evaluation of various methods for the prevention and treatment of acute postoperative pancreatitis (APP) is given, with appraisal of the traditional therapy (154 patients) without the use of protease inhibitors, and various methods of administration of protease inhibitors (135 patients) and cytostatics (84 patients). The mortality rate in progressive forms of APP was 25.2%, mortality being highest (30.4%) in treatment by the traditional methods including protease inhibitors and lowest in inclusion of cytostatics in the complex of therapeutic measures (7.1%).

[Injuries to the pancreas]. / Povrezhdeniia podzheludochnoi zhelezy.

The authors analysed 105 patients with traumatic damage of the pancreas in its closed (92) and open (13) injury. Isolated damages were encountered in 25, multiple in 67, and combined in 13 patients. Contusion of the gland was found in 73, injury to the parenchyma in 21, and parenchymal-duct injuries in 11 patients. The features of the clinical manifestations are discussed according to the time, type, and severity of the trauma and the efficacy of various methods of examination in early diagnosis is evaluated. The therapeutic tactics is discussed according to the type and severity of the damage, and the results of nonoperative (7) and various surgical treatment (98) are shown. The complications and the causes of fatal outcomes are analysed. Traumatic pancreatitis was the most frequent complication, its destructive forms were encountered in 24.5% of cases; pancreonecrosis occurred in 2.7% of patients with mild trauma of the gland. The mortality rate of progressive forms of pancreonecrosis was 12.24%.