Vol 7, No 2 (2019)



Kataev S.S., Dvorskaya O.N., Gofenberg M.A.


Background. At the beginning of 2019, the use of a new representative of synthetic cannabimimetics of the methylbutanoate indazole carboxamides group, MDMB(N)-073F, was recorded in a number of regions in the Russian Federation. Characteristic features of the pharmacological effect, the clinical picture of MDMB(N)-073F poisoning have not been studied, the psychoactive effects produced by MDMB(N)-073F remain unexplored. In this regard, the study of the new cannabimimetic metabolism is an important aspect in establishing the fact of taking MDMB(N)-073F during expert studies of biological objects.The aim of the research is identifying metabolites of synthetic MDMB(N)-73F cannabimimetics in real urine samples using solid-phase extraction (SPE) and gas chromatography (GC) with mass spectrometric detection (GC-MS).Materials and methods. 10 urine samples were collected from March 15 to March 29, 2019. 8 urine samples were taken from the medical examination offices of the city of Yekaterinburg and the Sverdlovsk region from the persons examined for intoxication; 2 urine samples were obtained from the patients of the Sverdlovsk regional center of acute poisoning upon enrolment to the toxic-intensive care unit with a preliminary diagnosis of “acute poisoning by synthetic cannabimimetics”. In the research, SampliQ EVIDEX-200 mg - 3 ml (Agilent, USA) cartridges were used for the sample preparation; β-glucuronidase Type HP-2, From Helix Pomatia, 100000 U/ml (Sigma-ALDRICH CHEMI, Germany) was used for enzymatic hydrolysis. Gas chromatography - mass spectrometry with the use of Agilent 7820 gas chromatograph with Agilent 5975 mass selective detector (Agilent, USA) was used as an instrumental method of the analysis.Results. The metabolites that make it possible to establish the fact of taking MDMB(N)-073F cannabimimetics via urine screening procedure to detect the presence of narcotic and medicinal substances with the use of solid-phase extraction and gas chromatography methods with mass spectrometry, have been described. The major metabolites MDMB(N)-073F in the urine of smoking mixtures consumers have been identified. The metabolism of MDMB(N)-073F has been found to be mainly due to hydrolysis of the ester group, hydroxylation, oxidative defluorination and N-dealkylation. Most of the resulting metabolites are excreted in the urine in the conjugated form.Conclusion. Gas chromatographic and mass spectrometric characteristics of some derivatives of the main metabolites of the new synthetic MDMB(N)-073F cannabimimetic have been obtained. This data can be used in the practice of forensic chemical and chemical toxicological analysis.
Pharmacy & Pharmacology. 2019;7(2):70-83
pages 70-83 views


Avdeeva N.V.


Parkinson’s disease is the second most common (after Alzheimer’s) neurodegenerative disease. All over the world, there is a search for new drugs aimed at the treatment of Parkinson’s disease. Till up to the present, there is no “ideal” medicine that can completely cure this disease and has minimal adverse side effects. Belgorod research institute of pharmacology of living systems is studying Rapitalam, a new drug for the treatment of tremulous Parkinson’s disease. This is an agonist of the mGluR4 group of metabotropic receptors.The aim of the article is to study Rapitalam influence on the oxotremorine-induced tremor in rats.Methods. The study comprised 60 rats (6 groups of 10 males), which were administered intragastrically with the studied substances for 10 days. All the animal groups except Control group 1, were administered with Rapitalam and the reference drug Levodopa. 30 minutes after Rapitalam and Levodopa, they were administered abdominally with the solution of Oxotremorine at the dose of 1.5 mg/kg. The animals of Control group 1, instead of Oxotremorine, were similarly administered with a solvent of 0.9% sodium chloride in the equivalent volume.Results. In comparison with the reference group, Rapitalam at the dose of 3 mg/kg significantly reduced the severity of tremor 50 min. after its administration. The same effect took place 30 min after the administration of Oxotremorine at the dose of 10 mg/kg. At the dose of 3 and 10 mg/kg, Rapitalam also decreased the number of rats in the group (in %) with the signs of tremor 60 min. and 50 min. after the administration of Oxotremorine, respectively.Conclusion. The study revealed that Rapitalam has a pronounced anti-tremor effect. Its administration at the studied doses reduced the symptoms of Oxotremorine-induced tremor in rats.
Pharmacy & Pharmacology. 2019;7(2):84-89
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Efremova M.P.


The aim of the study is to determine a lipid spectrum of blood plasma and liver in rats in with simulated dyslipidemia against the background of the administration of the fatty oil extract from the seeds of Nigella damascena L.Materials and methods. Laboratory animals - Wistar male rats - were used in the work. To study the hypolipidemic activity, such models as acute Tween, subchronic vitamin-D2 models and a model of chronic heart failure were used. The identifiable parameters were the concentration of cholesterol and triglycerides in the blood serum and liver, as well as the concentration of atherogenic and non-atherogenic lipoproteins in the blood serum, and the atherogenic coefficient.Results. As a result of the study, it was found out that a course administration of the fatty oil extract from the seeds of Nigella damascena L. against the background of simulated chronic heart failure (CHF) by the right ventricular type, normalizes the lipid spectrum of the experimental animals’ blood serum, causing an increase in the concentration of high-density (non-atherogenic) lipoproteins, and reduces the concentration of low-density (atherogenic) lipoproteins. A single administration of the fatty oil extract from the seeds of Nigella damascena L. promotes the correction of lipid metabolism disorders under the conditions of acute Tween lipidopathy, while the direction of the object being studied reduces the concentration of cholesterol and triglycerides in the liver and blood serum under the conditions of subchronic dyslipidemia. At the same time, the effect of the use of the fatty oil extract from the seeds of Nigella damascena L. was not inferior to “Omaсor”, the reference drug.Conclusion. The possibility of using a fatty oil extract from the seeds of Nigella damascena L. for preventive and therapeutic aims in cardiovascular diseases has been established.
Pharmacy & Pharmacology. 2019;7(2):90-96
pages 90-96 views


Timchenko T.V., Pogorelyi V.E., Voronkov A.V., Makarova L.M., Scherbakova L.I., Kompantsev V.A., Medvetskyi A.I., Platonova A.Y.


The aim of the work was a comparative experimental study of the effect of oral administration of Pentoxifylline microparticles based on PLGA, and “standard” Pentoxifylline, on the ADP-induced platelet aggregation process in rats.Materials and methods. Pentoxifylline substance (100 mg/kg) was used as a reference drug, and PLGA-based Pentoxifylline microparticles with an average dynamic radius of 175.4 nт were used as the object in study. In the experiment, male Wistar rats (m = 300-330 g), the same age group (9 months) were used. They were divided into 3 groups, each of 6 animals. The antiplatelet activity was assessed by determining the degree and rate of platelet aggregation in 1, 3, 5, 8 and 24 hours after a single oral administration of the reference drug and the object under study. Adenosine diphosphate (ADP) at the concentration of 5 μM was used as an aggregation inducer. The aggregation process was recorded using a two-channel laser platelet aggregation analyzer ALAT-2, wavelength of 0.785 μm. by determining the average conventional size of the aggregates.Results. The experiment has proved the following: PLGA-based Pentoxifylline microparticles are more effective at reducing the possibility of platelets to aggregate within 24 hours of the investigation (more than 40%) conventional to the control group value. Besides, it should be noted that according to the effectiveness of the pharmacological action during AD-induced platelet aggregation, the microparticles are commensurate with the standard sample - Pentoxifylline. The action of the microparticle object under study lasts for 24 hours, while the effect of the reference drug is over after 3 hours and then the indicators of the reference group do not differ from those of the control onel.Conclusion. When administered per os, PLGA-based Pentoxifylline microparticles prolong the pharmacological effect significantly - up to 24 hours.
Pharmacy & Pharmacology. 2019;7(2):97-104
pages 97-104 views


Ryzhova O.A., Moroz T.L.


The aim. Due to the social importance of anticancer drugs, the aim of the study is to conduct a comparative analysis of the range of domestic and foreign anticancer medications included in the Lists of Vital and Essential Drugs in 2013 and 2018 in the aspect of import substitution.Materials and methods. The study was conducted by comparing the data on the registered anticancer preparations included in the list of Vital and Essential Drugs in the State Register of Medicines in 2013 and 2018. Statistical processing of the data was carried out on the basis of Fisher Z-test method.Results. All in all, there were 286 trade names of anticancer drugs registered in the Russian Federation in 2013. 94 of them, i.e. 33%, were Russian-made. In 2013, there were 19 pharmaceutical substances of domestic production in the analyzed group, which accounted for 27% of 71 INNs (International nonproprietary name). As for 71 INNs, in 2018 there were 393 registered trade names of anticancer drugs. 162 drugs, i.e. 41%, were Russian-made. From 2013 to 2018, a statistically significant positive trend of the increase in the number of domestic anticancer drugs by 8% was revealed.Conclusion. In order to increase the volume of import substitution in the production of anticancer drugs, it is necessary to provide state support to Russian manufacturers, who register domestic analogues for the first time. A particular attention should be paid to the production of domestic pharmaceutical substances, without which it is impossible to ensure the drug safety of the country.
Pharmacy & Pharmacology. 2019;7(2):105-111
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Kozminykh V.O., Kozminykh E.N.


In connection with the 100th anniversary of Professor Oleg Kozmich Kozminykh, the brief biographical data are presented herein. O.K. Kozminykh made a great contribution to the development of pharmaceutical education and science in the Urals being the leader of Perm Pharmaceutical Institute for more than 20 years. Based on documents and personal memories, the biographical essay is provided and general data of life as well as scientific, pedagogical and public activities of O.K. Kozminykh are summarized here.
Pharmacy & Pharmacology. 2019;7(2):112-116
pages 112-116 views

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