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Vol 18, No 3 (2020)

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Properties and biological potential of single wall carbon nanohorns (SWCNH)

Piotrovskiy L.B., Kudryavtseva T.A., Litasova E.V.


Nanohorns (or nanocons) are formed when pentagons are accumulated at the top of the formed nanocarbon structure. hey are a cone formed by one layer of graphene with a diameter of 2–4 nm and a length of 40–50 nm. The review considers the structure of these structures and their properties. The possibilities of using these structures in biology are described in detail.

Reviews on Clinical Pharmacology and Drug Therapy. 2020;18(3):185-195
pages 185-195 views

Relief of microecological imbalances and barrier dysfunction of the intestinal mucosa in a therapeutic strategy for life-threatening conditions

Chepur S.V., Pluzhnikov N.N., Chubar’ O.V., Cygan V.N., Bakulina L.S., Sidorov S.P., Bazhenov M.V., Mosin A.V., Vinogradov M.V., Semakin R.V.


Arguments are given about the expediency of early enteral treatment in life-threatening conditions to improve the functions of the intestinal barrier structures, prevent the transformation of the symbiotic microbiome phenotype and translocation of its representatives with the formation or aggravation of a systemic inflammatory response. The expediency of including proteins and beta-glucans and phosphates in the composition of nutritional mixtures was determined. For the purpose of pharmacological support, the possibility of including iron skevingers, valproates as histone acetylase inhibitors, antioxidants, statins and infusion solutions enriched with hydrogen was considered. The implementation of the paradigm of early enteral nutrition will improve the prognosis of patients in intensive care units.

Reviews on Clinical Pharmacology and Drug Therapy. 2020;18(3):197-212
pages 197-212 views

Pathophysiological mechanisms of neurological disorders in experimental animals exposed to vibration

Vorobieva V.V., Levchenkova O.S., Shabanov P.D.


The review presents an analysis of literature on the study of nervous system changes in experimental animals exposed to vibration. The hypoxic type of cellular metabolism against the background of vibration is the result of vascular mechanoreceptors stimulation and spasm of blood vessels as well as intravascular pressure phase fluctuations and impaired blood and lymph outflow. Hemodynamic disorders and microangiopathy in the central nervous system can reach the level of cerebral vascular impairment and capillary-trophic insufficiency of the brain. Changes in calcium homeostasis at the cellular and tissue levels is a key mechanism of neuronal destruction occurring alongside with impaired blood supply to the nervous tissue in patients with vibrational disease. Long-term exposure to vibration results in reduced tissue respiration in the brain structures of experimental animals, that is most pronounced in the cortex and leads to a pathological change of spontaneous electrical activity of brain structures. Acute vibration stress stimulated the synthesis and excretion of serotonin not only in the hippocampus and hypothalamus but also in the cerebellum, which explains the disturbances of the oculomotor reactions observed in vibration exposure in the control system of the vertical vestibular ocular reflex. A decrease in the total number of neurons as well as an increase in the number of astroglia cells against the background of paravascular tissue edema were revealed against the background of changes in neurotransmitters levels. An increase in the concentration of the biomarker of structural and functional damage to brain tissue specific protein S-100B accompanies the development of professional sensorineural hearing loss and dysfunction of cerebral level vegetative regulation.

Reviews on Clinical Pharmacology and Drug Therapy. 2020;18(3):213-224
pages 213-224 views

Original articles

Antifungal activity of new derivatives of 4-(het)aryl-2,4-dioxobutanoic acids

Novikova V.V., Pulina N.A., Sobin F.V., Lipatnikov K.V.


Among more than 600 types of micromycetes of clinical importance, fungi of the Candida spp. are the most common pathogen, causing different forms of candidiasis (superficial candidiasis, visceral candidiasis). The aim of this work was to determine the antifungal activity of new derivatives of 4-(het)aryl-2,4-dioxobutanoic acids, in relation to typical strains of Candida yeast and to identify the most active compounds. The study of the antifungal activity of the compounds was carried out by the micromethod of double serial dilutions in a liquid medium. The antifungal activity of 6 compounds in relation to 4 typical strains of Candida spp. was studied; the high antimycotic activity of 4 compounds against the Candida albicans strain was established. A leader compound with high antifungal activity for all the studied strains was revealed. The prospects of studying the modified compounds of this series are shown.

Reviews on Clinical Pharmacology and Drug Therapy. 2020;18(3):225-228
pages 225-228 views

Wound healing effect benzosulfonate 1-ethyl-3-methyl-4,5-bis(n-methylcarbamoyl) imidazolium

Khnychenko L.K., Selina E.N., Rodionova O.M., Piotrovskiy L.B., Shabanov P.D.


Materials and methods. In experiments on 180 male rats weighing 180–200 g, the wound-healing effect of derivatives of imidazole (IEM-1181) was evaluated as a 10% ointment on models of aseptic full-layer linear and planar skin wounds.

Results. It was found that the compound IEM-1181 in the form of 10% ointment has a pronounced on skin wound healing effect, manifested in the qualitative features of the regenerative healing process. With local application of the ointment containing the tested compound, the strength of the tissue formed on the site of a full-layer linear skin wound was increased when its edges were stretched, and the healing time of full-layer planar wounds was reduced. The morphological picture of the tissue formed at the site of the wound defect corresponded to complete healing by primary tension with complete epithelization of the surface and squamous cell differentiation of the epithelial regenerate without signs of inflammation and scar formation.

Conclusion. The results of the study on experimental models of full-layer linear and planar skin wounds indicate that the wound healing effect of the tested ointment is due to the anti-inflammatory activity of the IEM-1181 compound

Reviews on Clinical Pharmacology and Drug Therapy. 2020;18(3):229-235
pages 229-235 views

Clinical pharmacology

Drugs for gene therapy: features of usage in geriatrics and pediatrics

Gurevich K.G., Sorokina Y.A., Urakov A.L., Gavrilova D.M., Lovtsova L.V., Zanozina O.V.


Advances in modern medicine and biotechnology allow specialists to adjust the patient’s proteome and metabolome. Gene engineering allows us to create drugs that affect the cause of the disease at the level of gene expression. Thus, not the links of pathogenesis or the symptom of the disease are subjected to correction, but the trigger itself, a defective gene that provokes a cascade of pathological processes. According to the definition of the State Pharmacopoeia, gene therapeutic drugs are drugs whose pharmaceutical substance is a recombinant nucleic acid or includes a recombinant nucleic acid that allows for the regulation, repair, replacement, addition or removal of a genetic sequence. The article reflects all available, developed and used in real clinical practice gene therapy drugs of russian and foreign production. The mechanisms of action, features of the use of these drugs in pediatric and geriatric practice, as well as existing problems and limitations of their use, including deontological issues, are noted.

Reviews on Clinical Pharmacology and Drug Therapy. 2020;18(3):237-244
pages 237-244 views

Structural changes in the Russian pharmaceutical market of anti-tb drugs

Usacheva N.E., Novikov V.E., Myakisheva T.V., Pavluchenkova N.A., Trun E.V.


In Russia, the epidemic situation for tuberculosis has stabilized with a tendency to improvement, according to the dynamics of the main indicators for the disease. However, the problem of tuberculosis infection is still far from being resolved, which is largely due to the development of drug resistance of the infectious agent to the main anti-TB drugs.

The purpose of the study is to form macro-structures of the Russian market of anti-TB drugs for 2008 and 2018 and analyze the dynamics of their structural changes.

Materials and methods. The State registers of medicines of the Russian Federation for 2008 and 2018 were analyzed. Into account were taken following characteristics of the range: the number of registered anti-TB drugs, dosage forms, dosages, manufacturers, and the number of combined anti-TB drugs. The necessary data was obtained using the content analysis method. The results of the study allowed us to build macro-structures of the Russian market of anti-TB drugs and compare the indicators in the dynamics over 10 years.

Results. Over the past 10 years, about 500 anti-TB drugs have been registered and re-registered in the Russian Federation. The range of the selected segment was supplemented by the 3rd new series, which according to 2018 included 166 (30.0%) drugs, taking into account all dosage forms and dosages. The group of anti-TB drugs of the 2nd series in 2018 was the leader in the selected segment (52.2%) and there was a tendency for its growth. In the structure of the assortment of medicinal forms of anti-TB drugs, tablet drugs prevailed (43.5%). The production vector has shifted towards domestic manufacturers. The share of new drugs put into circulation in 2008-2018 was 37%. The nomenclature of the Russian anti-TB market corresponds to international recommendations and contains the main groups of drugs.

Conclusion. Analysis of the segment of anti-TB drugs in the domestic pharmaceutical market showed that the phthisiological service has a sufficient range of drugs for the treatment of tuberculosis infection, including those with drug resistance of the pathogen. This allows to personalize therapy based on the stage and severity of the disease, the functional characteristics of the patient’s body, and the sensitivity of the pathogen to chemotherapy.

Reviews on Clinical Pharmacology and Drug Therapy. 2020;18(3):245-254
pages 245-254 views

Efficacy assessment of modern regimens of preventive antituberculosis therapy in patients basically treated with TNF-α inhibitors

Barnaulov A.O., Rasmagina I.A., Kondakova M.N., Khabirov V.V., Lelekova E.B.


Background. Biological agents, especially anti-tumor necrosis factor blocking agents, frequently are used to treat autoimmune inflammatory rheumatic diseases. Due to their negative impact on immune system and high risk of reactivation of latent tuberculosis infection all the patients must be well examined before initiation of an anti-tumor necrosis factor therapy (ATNFT).

Purposes and tasks. An estimation of efficiency of preventive anti-tuberculosis therapy (PATT) with patients undergoing ATNFT.

Methods and materials. In the research took part 128 patients, suffering from different inflammatory rheumatic diseases, whom was planned anti-tumor necrosis factor therapy. In 62 cases were found the indications for prescription PATT for 4 weeks before initiation of biological therapy and from 8 to 20 weeks after.

Results. An active tuberculosis has been developed in 8 cases, the process was similar to tuberculosis and human immunodeficiency virus. The factors of risk were the prescription adalimumab and infliximab, impaired glucose tolerance, diabetes type 2 and drunkenness abuse.

Conclusion. The existing preventive anti-tuberculosis therapy is not able to preclude the development of tuberculosis in all cases and needs to be optimized.

Reviews on Clinical Pharmacology and Drug Therapy. 2020;18(3):255-258
pages 255-258 views

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