Vol 12, No 4 (2014)


Kisspeptins in physiology and pathology of sex development - new diagnostic and therapeutic approaches

Nikitina I.L., Bayramov A.A., Khoduleva Y.N., Shabanov P.D.


The article is dedicated to mechanisms of the human reproductive system development mechanisms. The evolution of the opinions on that processes was analysed. The review of modern knowledge of molecular and genetic causes of sex development, new mechanisms of gonadal axis regulation and role of kisspeptins in pubertat start and sexual differentiation of the brain are presented. The new actual directions of scientific research as well as the applications of kisspeptin drugs for new therapeutic approaches, treatment of hormone-dependent diseases and abnormalities of sex developmentare are observed.
Reviews on Clinical Pharmacology and Drug Therapy. 2014;12(4):3-12
pages 3-12 views

Role of reactive oxygen species in cell physiology and pathology and their pharmacological regulation

Novikov V.E., Levchenkova O.S., Pozhilova Y.V.


This review is devoted to analysis of modern scientific investigations about role of reactive oxygen species (ROS) in physiology and pathophysiology of cell. Key issues of ROS generation, their function in signaling pathways, role in the cellular pathology, functioning of antioxidant system are discussed in the paper. The review also summarizes literature data about possibility of pharmacological regulation of the activity of free radical oxidation reactions, which have practical value for effective pharmacotherapy of diseases in pathogenesis of which destructive action of ROS is present.
Reviews on Clinical Pharmacology and Drug Therapy. 2014;12(4):13-21
pages 13-21 views

Redox regulation as a platform for search and design of new type drugs. Search of gastroprotectors among sunstituted coumarins

Parfenov E.A., Trapkov V.A., Shabanov P.D.


Redox homeostasis controls most or all processes of normal and pathological physiology. Important position in the defence mechanisms are redox active metabolites As a robust platform for the development of new effective drugs is not screened, but directed the design and search for low molecular weight metabolites natural redox active compounds. This statement confirms the synthesis and study of new gastroprotektors of complex compounds of copper and zinc with coumarin ligands. On the model of acute ethanol rat gastric ulcer shown that preprocessing all tested complex compounds in equimolar doses of 0.15 mmol/kg leads to a considerable reduction in the size of the damage to the wall of the stomach, compared to control, and sucralfat (for 72,5-87,9 %, sucralfat - 52,3%).
Reviews on Clinical Pharmacology and Drug Therapy. 2014;12(4):22-42
pages 22-42 views

Isolated frog heart performance after stimulation by adrenaline against the background of new metal-complex antihypoxant πQ1983 action

Sosin D.V., Yevseyev A.V., Pravdivtsev V.A., Shabanov P.D.


The dynamic of isolated nonfixed heart bioimpedance changing had been studied in experiments on frogs (Rana temporaria, n = 20) after stimulation by adrenaline and application of the new antihypoxic metal-complex substance πQ1983 just on myocardium. The curve of heart bioimpedance changing (impedancecardiogram) was registered in vitro by the computer reographic apparatus “Reospectr” (Neurosoft, Russia). Simultaneously ECG was registered too. After placing of a heart in condition of the experiment and after placement of all electrodes the stimulation by adrenaline were performed by dropping of 0.1 % adrenaline hydrochloride solution on myocardium (control group). On the hearts of the experimental group were applied the substance πQ1983 solution 15 min before stimulation by adrenaline (experimental group). Was established that substance πQ1983 increases the resistance of frog myocardium to the stimulation by adrenaline in vitro making longer its mechanical and electrical work more than twice. The obtained data confirm presence of soft direct cardiodepressive effect of the substance πQ1983 that supplements the conception of different mechanisms of its antihypoxic impact.
Reviews on Clinical Pharmacology and Drug Therapy. 2014;12(4):43-49
pages 43-49 views

Predictive markers of the efficacy of colon adenocarcinoma treatment by 5-fluoropyrimidines determined by means of immunohistochemistry method

Raskin G.A., Orlova R.V., Protasova A.E., Koshkin S.A., Glushakov R.I.


5-fluorouracil (5-FU) has remained the treatment of choice in the adjuvant and palliative setting of colon cancer (CC).The purpose of this study was to evaluate the expression of the thymidine phosphorylase (TP), thymidylate synthase (TS) and dihydropyrimidine dehydrogenase (DPYD)in CC patients treated with 5-fluorouracil (5-FU) to determine their predictive and prognostic significance. Immunohistochemistry (IHC) analysis of the expression of proteins was performed on tumour tissue of 104 patients with stage IV colon cancer. All patient was treated withfluoropyrimidine/antifolate-based therapy (FOLFOX, De Gramont, FOLFIRI). Usedmultivariate logistic regression analyses we found the level of expression of proteins thymidine phosphorylase (TP), thymidylate synthase (TS) as predictors efficiency 5 - fluoropyrimidine with adenocarcinoma of the colon. The value of expression of TP and TS has a statistically significant effect (p = 0,006 and p = 0.0036) on time to disease progression, respectively.Our data demonstrated the efficacy of the 5-fluoropyrimidine chemotherapy colon adenocarcinoma may be utilized evaluation of expression of TS and TP.
Reviews on Clinical Pharmacology and Drug Therapy. 2014;12(4):50-53
pages 50-53 views

Influence of the new tiazoloindole derivative on the organism resistance to hypoxia in the early and late periods of preconditioning

Levchenkova O.S., Novikov V.E., Marysheva V.V.


The aim of this investigation was to study an ability of tiazoloindole derivative encoded VM-606 to influence the lifespan of mice in experimental acute hypoxia with hypercapnia and hypobaric hypoxia in early and late phase of preconditioning. It was found that the use of VM- 606 in dose of 50 mg/kg leads to significant increase in the duration of animal life in case of subsequent acute hypoxia in early phase of preconditioning, but doesn’t produce effect in the late phase of preconditioning.
Reviews on Clinical Pharmacology and Drug Therapy. 2014;12(4):54-57
pages 54-57 views

Rational pharmacotherapy of hyperkinetic disorders

Glushchenko V.V.


The data concerning hyperkinetic disorder syndrome are shortly reviewed in the paper. Principal attention is focused on the analysis of effects of metabolic activators (atomoxetine), neuroleptics (thioridazine, chlorprotixene) and different antidepressants (fluoxetine, fluvoxamine, sertraline, tianeptine, pipophesine).
Reviews on Clinical Pharmacology and Drug Therapy. 2014;12(4):58-63
pages 58-63 views

Pharmacokinetic peculiarities of intravenous and oral ciprofloxacin administration in preoperative prophylaxis in patients with benign prostatic hyperplasia

Sosin I.V., Rafalskiy V.V., Shabanov P.D.


The study of population pharmacokinetics of ciprofloxacin at various ways of administration helps to found that the once usage of 500 mg ciprofloxacin orally 90-120 min before the surgery as preoperative antibiotic prophylaxis with transurethral resection of the prostate gland creates a significantly higher concentration of the drug in blood, urine and prostate parenchyma compared to intravenously administration of 400 mg ciprofloxacin 30-60 min before operation. Thus, the data obtained explain the higher efficacy of oral administration of ciprofloxacin as preoperative antibiotic prophylaxis in patients undergoing transurethral resection of the prostate.
Reviews on Clinical Pharmacology and Drug Therapy. 2014;12(4):64-66
pages 64-66 views

Effect of cortexin on statokinetic stability in humans

Buynov L.G., Sorokina L.A., Voeykov I.M., Shabanov P.D.


Intranasal administration of peptide bioregulator cortexin (0.25 mg in every half of the nouse, 2 times per day with interval 8 h, 10 days, course dose 10 mg) increased statokinetic stability level in healthy humans. Cortexin prolonged the time of load in modified probe of undiscreted cumulation of Coriolis’ acceleration, the time of stable equilibrium in Bondarevskii’s test. At the same time, head heavity and head aiche were decreased. According to computer stabilography, the tests with open eyes were increased too. In particular, statokinesiographic indicators were elevated by 1.40-1.44 times, the amplitude of the common center of gravity and asymmetry coefficient were declined by 1.22-1.24 times in both the frontal and saggital projections. The positive effect of cortexin was stored over 30 days, after that the indicators were recovered upto normal values. There were no differences in dynamics of other indicators the tested, but there was the general tendency to optimize the functional state of the organism and to improve the statokinetic stability in humans.
Reviews on Clinical Pharmacology and Drug Therapy. 2014;12(4):67-71
pages 67-71 views

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