Pharmacokinetics and Pharmacodynamics

Journal Information
ISSN / EISSN : 2587-7836 / 2686-8830
Published by: Publishing House OKI (10.37489)
Total articles ≅ 34
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I. B. Tsorin, A. O. Efimova, Е. С. Пекельдина, M. B. Vititnova,
Pharmacokinetics and Pharmacodynamics; https://doi.org/10.37489/2587-7836-2020-4-9-13

Abstract:
The purpose of the study. In experiments on a hind limb ischemia model in rats, the effect of the TrkA-receptor agonist of the NGF 4th loop dimeric dipeptide mimetic compound GK-2 has been studied on microcirculation in ischemic skeletal muscle. Methods. the Hind limb ischemia was caused in white male mongrel rats by the femoral artery resection. The compound GK-2 was administered intravenously (1 mg/kg/day during 14 days). Microcirculation parameters were recorded using a computer laser analyzer "LAKK-OP2". Registration was carried out simultaneously in the intact and operated limb before the operation, 1 and 14 days after it. Results. In the conditions of the hind limb ischemia model, it was shown that the compound GK-2 almost completely restored the perfusion index and its variation coefficient in the ischemic muscle to the intact contralateral limb level by the 14th day after surgery. Conclusion. It can be assumed that the anti-ischemic effect of the compound GK-2 is associated with the restoration of microcirculation as a result of increased neoangiogenesis.
I. A. Miroshkina, A. V. Sorokina, A. V. Volkova, , I. V. Alekseev, K. S. Kachalov, A. D. Zakharov, S. V. Alekseeva
Pharmacokinetics and Pharmacodynamics pp 48-54; https://doi.org/10.37489/2587-7836-2020-4-47-53

Abstract:
Assessment of acute toxicity is a necessary stage of preclinical research of the substance GIZh-298. The aim of present research is study of acute toxicity GIZh-298. Methods. GIZh-298 was administered once intraperitoneally to mice at doses 200-330 mg/kg. Equivalent volume of 1 % starch solution was administered to animals of the control groups. Periods of intoxication and death of animals with a detailed description of the observed clinical picture were registered. Euthanasia and pathoanatomical dissection were performed 14 days after drug administration. Results. The median lethal doses were identified: LD50 = 299,6 (279,7 – 320,8) mg/kg in female mice, LD50 = 302,3 (281,5 – 324,6) mg/kg in male mice at intraperitoneal introduction. The morphological view of the internal organs, detected during pathoanatomical dissection of all surviving experimental animals, did not differ from that observed in control animals. Conclusion. It was determined that GIZh-298 at intraperitoneal introduction concerns to low-toxic substances. According to classification Sidorov K.K. GIZh-298 may be related to 4th toxicity class.
S. V. Alekseeva, A. V. Sorokina, A. V. Volkova, , I. A. Miroshkina, K. S. Kachalov, I. V. Alekseev, A. D. Zaharov
Pharmacokinetics and Pharmacodynamics pp 41-47; https://doi.org/10.37489/2587-7836-2020-4-41-46

Abstract:
Acute toxicity testing is a commonly accepted procedure for preclinical testing of the safety of potential drugs. The compound GIZh-290, which is a derivative of 4-phenylpyrrolidone– 2,6 - dimethylanilide (2-oxo-4-phenylpyrrolidine-1-yl) acetic acid and has a nootropic and anticonvulsant effect, was studied. The results obtained after a single oral and intraperitoneal administration to mice allow us to attribute GIZH-290 to the 4th class of toxicity – "lowtoxic substances". The study revealed the neurotoxic effects of GIZH-290, which may be due to the main pharmacological activity of the compound used in sublethal doses.
, S. A. Litvinova, I. G. Kovalev
Pharmacokinetics and Pharmacodynamics; https://doi.org/10.37489/2587-7836-2020-4-14-18

Abstract:
The effect of levetiracetam (a derivative of 4-phenylpyrrolidone) and its original analog, the compound GIZH-290, on primary generalized epileptic activity (EpA) in rat brain structures (sensorimotor cortex, dorsal hippocampus-CA3 field and lateral hypothalamus field) on EEG models of bemegridinduced seizures was studied. It was found that EpA, after the introduction of bemegrid, appears in 1–2 minutes in the form of prolonged generalized high-amplitude discharges and is registered within 3 hours. GIZH-290 (5 mg/kg, intraperitoneal, 15 minutes after bemegrid) causes a significant (p < 0.05) decrease in the number of epileptic discharges in the cortex and at the level of the trend in the hippocampus, which is accompanied by a decrease in the amplitude of the Epi-discharges. Levetiracetam at a dose of 200 mg / kg does not significantly change the severity of paroxysmal activity (the number of convulsive discharges and their duration) caused by bemegrid.
G. B. Kolyvanov, A. A. Litvin, R. V. Shevchenko, S. Yu. Raskin, P. O. Bochkov,
Pharmacokinetics and Pharmacodynamics; https://doi.org/10.37489/2587-7836-2020-4-3-8

Abstract:
The review discusses relationships between pharmacokinetic parameters and effects of psychotropic drugs, both in preclinical studies and clinical practice. The identification of such correlations can serve as a basis for understanding the complex system of relationships between pharmacokinetic and pharmacodynamic mechanisms in the manifestation of the action of this group of drugs and allows us to use the data of pharmacokinetic studies to optimize therapeutic approaches in medical practice.
, , , A. N. Galustyan, I. V. Gogoleva, T. R. Grishina, A. N. Gromov, , , V. M. Kodentsova, et al.
Pharmacokinetics and Pharmacodynamics; https://doi.org/10.37489/2587-7836-2020-4-19-40

Abstract:
The search for original publications on fundamental and clinical medicine that would produce results of the highest scientific quality represents an urgent need for every medical researcher. Such publications are essential, in particular, for the development of reliable treatment standards. The Englishlanguage resources PUBMED and EMBASE are essential to help in solving this problem. However, there is an obvious problem in assessing the quality of the studies found. The paper formulates a method for analyzing the texts of biomedical publications, which is based on an algorithmic assessment of the emotional modality of medical texts (so-called sentiment analysis). The use of the topological theory of data analysis made it possible to develop a set of high-precision algorithms for identifying 16 types of sentiments (manipulative turns of speech, research without positive results, propaganda, falsification of results, negative personal attitude, aggressiveness of the text, negative emotional background, etc.). On the basis of the developed algorithms, a point scale for assessing the sentiment quality of research was obtained, which we called the "β-score": the higher the β-score, the less the evaluated text contains manipulative language constructions. As a result, the ANTIFAKE system (http://antifake-news.ru) was developed to analyze the sentiment-quality of Englishlanguage scientific texts. An analysis of ~ 20 million abstracts from PUBMED showed that publications with low sentiment quality (β-score <0, that is, that the prevalence of manipulative constructions over meaningful ones) is only 19 %. In the overwhelming majority of thematic headings (27,090 out of 27,840 headings of the MESH system PUBMED), a positive dynamics of sentiment quality of the texts of publications is shown by years). At the same time, as a result of the study, 249 headings were identified with sharply negative dynamics of sentiment quality and with a pronounced increase in manipulative sentiments characteristic of the "yellow" English-language press. These headings include tens of thousands of publications in peer-reviewed journals, which are aimed at (1) legalizing ethically unacceptable practices (euthanasia, perversions, so-called "population control", etc.), (2) discrediting psychiatry as a science, (3) media the war against micronutrients and (4) discrediting evidence-based medicine under the guise of developing the so-called "international standards of evidence-based medicine". In general, the developed system of artificial intelligence allows researchers to filter out pseudoscientific publications, the text of which is overloaded with emotional manipulation and which are published under the guise of "evidence-based standards".
, R. V. Zhurikov, K. V. Korzhova,
Pharmacokinetics and Pharmacodynamics; https://doi.org/10.37489/2587-7836-2020-3-48-51

Abstract:
The research of immunotoxicity of extended-release form of Afobazol was conducted on male CBA, C57BL/6 and F1 hybrids (CBA×C57BL/6) mice. Afobazol was administered per os for 14 days in doses of 12 mg/kg and 120 mg/kg. Control group received a placebo. Weight of thymus, spleen and popliteal lymph nodes was not affected by the extended-release form of Afobazol in doses of 12 mg/kg and 120 mg/kg in F1 hybrids (CBA×C57BL/6) mice compared to the control group (p> 0.05). Cellularity of thymus was significantly increased by the extended-release form of Afobazol in dose of 12 mg/kg (p< 0.01 vs control group). Administration of the extended-release form of Afobazol in doses of 12 mg/kg and 120 mg/kg decreased spontaneous chemiluminescence activity of peripheral blood lymphocytes in 2.0 and 2.2 times, in dose of 120 mg/kg level integral chemiluminescence response S was decreased in 2.4 times (p< 0.05 vs control group). Phagocytic activity of peritoneal macrophages and antibody production in F1 hybrids (CBA×C57BL/6) mice were not affected by administration of the extended-release form of Afobazol in doses of 12 mg/kg and 120 mg/kg (p > 0.05 vs control group). 14 days of the extended-release form of Afobazol in doses of 12 mg/kg and 120 mg/kg did not cause any significant change to intensity of delayed-type hypersensitivity reactions (p> 0.05 vs control group). The results of the study allow us to conclude that administration of the extended-release form Afobazol in the range of studied doses does not induce immunotoxicity.
О. . А Лиманова, , L. E. Fedotova
Pharmacokinetics and Pharmacodynamics; https://doi.org/10.37489/2587-7836-2020-3-30-39

Abstract:
Combined oral contraception and treatment of new coronavirus infection (COVID-19): issues of drug interaction This article examines the interaction of combined oral contraceptives with drugs recommended in the treatment of new coronavirus infection (COVID-19) at the pharmacodynamic and pharmacokinetic levels, with an assessment of the effectiveness and safety of therapy for the female body.
S. S. Boyko, K. N. Koljasnikova,
Pharmacokinetics and Pharmacodynamics; https://doi.org/10.37489/2587-7836-2020-3-25-29

Abstract:
In the article presented the results of research of the influence pharmacokinetics, bioavailability for CNS cyclo-L-prolylglycine to the manifestation of its main pharmacological effects in experimental animals.
I. B. Tsorin
Pharmacokinetics and Pharmacodynamics; https://doi.org/10.37489/2587-7836-2020-3-3-24

Abstract:
The article discusses descriptive statistics of data measured in ordinal and quantitative scales, and criteria for determining the statistical significance of differences between samples when it is impossible to analyze using parametric methods. Special attention is paid to the problem of multiple comparisons of this type of data. For each method, examples of processing data obtained in pharmacological studies are given.
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