Vol 2, No 4 (2020)

From the editor

From the editorial Board

Perelygin V.V., Zvyagin Y.Y.

Abstract

Any major epidemic outbreak causes negative consequences both for individuals and for society as a whole, covering almost all aspects of life at the macro and individual levels.
We, the members of the editorial Board and editorial staff, want to Express our serious concern about the development of the situation related to the outbreak of the SARS-CoV-2 virus this year.

Pharmacy Formulas. 2020;2(4):1-1
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Pharmaceutical Sciences

Multi-vector analysis of the market for drugs used to treat hepatitis C

Narkevich I.A., Nemyatykh O.D., Siukaeva D.D., Tsitlionok E.A., Lisacenco V.O., Grinyuk A.S.

Abstract

The article presents a study on the structural assessment of the range of drugs for the treatment of hepatitis C. Methods of content analysis, data aggregation, grouping, comparative and marketing analysis have been used. The information base of the study was the State Register of Medicines and National Register of Medicines of April 24, 2020, as well as instructions for the medical use of drugs. It was revealed that 52 trade names of medicinal products (23 INN) and 17 substances had been registered in the Russian Federation. The analysis carried out by pharmaceutical producing countries has shown that the leading positions in the supply structure are occupied by Russian manufacturers (73.08%). Structuring by dosage forms enables to isolate tablets, covering 32.69%, as well as solutions and capsules, which are 23.08%, respectively. The largest share in the structure of the assortment of substances is occupied by interferon alpha-2b (20.93%). The results of the analysis has shown that the manufacturer carries out all stages of production for the majority of drugs. The index of renewal of the researched drug market over the past 5 years is 16.27%.

Pharmacy Formulas. 2020;2(4):8-17
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Generalized data of criteria of risk factors for the use of the drug torasemide from the materials of its preclinical studies

Anisimova N.A., Selizarova N.O., Plisko G.A., Semivelichenko E.D., Napalkova S.M.

Abstract

Thе article reviewed, analyzed and summarized the results of experimental (preclinical) pharmacological studies of the drug Torsemide. Torsemide is the first of the new generation of loop diuretics, which fundamentally differs from the first generation of loop diuretics in the spectrum of pharmacological effects.

The present review considers safety aspects, pharmacokinetics, pharmacodynamics of Torsemide found in various studies in preclinical research. Information on the effectiveness of Torsemide- based preparations in the treatment of chronic heart failure and arterial hypertension is given in the relevant sections of the article.

The search for information sources for the review was carried out using domestic and international databases elibrary and PubMed, applying contextual queries, including international non-proprietary names, terms of preclinical studies of pharmacokinetics, pharmacodynamics, and animal species used.

The summarized data presented in the study, in our opinion, may be used by researchers who are engaged in preclinical and clinical studies, as well as the issues of studying the efficacy and safety of generic drugs used in the treatment of patients with arterial hypertension and other cardiovascular pathology.

Pharmacy Formulas. 2020;2(4):18-26
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Biomedical Sciences

Identification of actoprotective compounds among Krebs cycle acid/aminoethanol derivatives

Bolotova V.T., Shustov E.B., Okovityi S.V.

Abstract

This study was carried out taking into account the fact that the search for and introduction into medical practice of drugs for the pharmacological correction of fatigue and restoration of physical performance in asthenic phenomena after illness, physical exertion in military personnel, athletes and the elderly continues to remain relevant.
In the course of the study, we aimed to study the effect of dimethylamino and diethylaminoethanol derivatives with
tricarboxylic acid cycle intermediates (aminoethanol derivatives with Krebs cycle acids) on the physical performance of white outbred male mice.
The study was carried out on 490 outbred male mice with body weight 22-24 grams. The limit swimming test with a load was chosen as a screening model to study the effect of new compounds on physical performance.
To select the most effective of the synthesized compounds, a screening of the pharmacological activity of the effect of the new compounds, fumar ester of diethylamino and dimethylaminoethanol with Krebs cycle intermediates, on the physical performance of male mice was performed.
Statistical processing of the data obtained to establish differences between groups was performed using the F-test of ANOVA.
Studies have shown that in their effect on physical performance, these compounds were superior to the reference drug - deanol aceglumate at an optimal dose of 50 mg / kg.
In the process of developing new actoprotective agents, we consider it appropriate to use the ability of the Krebs cycle acids to enhance the antihypoxic, actoprotective and nootropic activity of the base cationic groups in salts.

Pharmacy Formulas. 2020;2(4):28-35
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The benefits or harms of systemic corticosteroids for community-acquired pneumonia in adults: аn overview of reviews

Efimov N.V., Sayfullin R.F., Shunkov V.B.

Abstract

Background: The problem of reducing mortality in patients with community-acquired pneumonia remains extremely important despite the progress in the development of antibiotics. There is a certain consensus on the etiological treatment of typical and atypical variants of the disease, however, the efficacy of corticosteroids as a means of pathogenetic therapy for many years has remained a subject of discussion, in spite of the large number of studies conducted and several dozen reviews of them.

The aim of our study is to summarize more than one systematic review of randomized controlled trials to assess the evidence for the effect of adjuvant systemic CS in adults with CAP on mortality, symptom dynamics, risk of complications, and harmful side effects.

Methods: From July to September 2020, we searched for systematic reviews in the PubMed, Embase, CENTRAL databases in accordance with the recommendations of the Cochrane Guidelines for Systematic Reviews 6 version up to 2020. The methodological level of the selected reviews was assessed using the АMSTAR-2 form.

Results: 12 systematic reviews were selected that were performed in different countries from 2012 to 2018, covering 24 clinical trials with 2,791 participants. Comparison and generalization of review data confirms that additional prescription of CS led to a decrease in mortality in severe CAP, and with any severity of CAP - to a decrease in the risk of treatment failure in the first 5–7 days from its onset, acceleration of the onset of signs of clinical improvement, and a decrease in the risk of development respiratory failure and transfer to artificial lung ventilation, reducing the length of hospital stay and treatment in the intensive care unit. Short courses of steroid therapy did not increase the risk of harmful plug events, with the exception of hyperglycemia, which was easily controlled.

Our analysis has also shown that there is a feasibility of bridging the gap between existing regulations and the evidence base for current systematic reviews of RCTs on the use of CS in CAP.

Pharmacy Formulas. 2020;2(4):36-51
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Modern aspects of myocardial infarction treatment in older patients

Kozlov K.L., Bogomolov A.N., Lukianov N.G., Senkina E.I., Pukhalskaya A.E.

Abstract

In this study, the authors attempted to systematize current information based on recommendations, large studies and meta-analyzes of the treatment of myocardial infarction in the elderly. Cardiovascular heart disease represents the leading cause of death in people aged 65 years and over. Acute myocardial infarction is one of the most socially important diseases with a high rate of mortality and disability. In elderly and old patients atypical forms of myocardial infarction are common. High rate of comorbidities, functional and socioeconomic status, side effects associated with drug administration create difficulty in the diagnosis and selection of treatment in the elderly. These patients need a prolonged monitoring with using an additional examinations and dynamic observation. Compared to younger subjects, elderly patients with acute myocardial infarction are less likely to receive evidence-based treatment, including myocardial revascularization therapy. Endovascular revascularization is currently the main standard for the treatment of acute myocardial infarction, but the advantage of the use of interventional cardiology techniques in elderly patients has been insufficiently studied. Older patients are generally underrepresented in cardiovascular trials. Modern scientific literature, illuminating issues of application of pharmacological and endovascular treatment of acute myocardial infarction in elderly and old age patients, contains fragmented and, in some cases, contradictory data, which forces researchers to continue studying new and promising methods of diagnosis and treatment of myocardial infarction in the elderly.

Pharmacy Formulas. 2020;2(4):52-59
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Development of the design of the preclinical trials of radiopharmaceuticals for the radionuclide diagnostics and therapy based on the AMBA peptide

Stanzhevsky A.A., Mosunov A.A., Chipiga L.A., Vodovatov A.V., Naurzbaeva L., Kushnarenko S.M., Lavreshov D.D., Petrova A.E.

Abstract

The present study is related to one of the promising areas of nuclear medicine: the use of peptides – bombesin analogues, labeled with 68Ga – for diagnosis and 177Lu – for therapy of prostate cancer. In the Russian Federation, preclinical trials of similar radiopharmaceutical drugs are in the study design stage. The aim of the current study was to develop the design of the preclinical study for the radiopharmaceutical drugs to assess the biodistribution of a peptide, an analogue of bombesin, intended for the diagnosis and treatment of prostate cancer.
The study was based on the meta-analysis of the available publications in peer-reviewed journals. The analysis was performed using the full-text archive of biomedical and life sciences journals PubMed Central for the following keywords: “radionuclide therapy”, “nuclear medicine”, “AMBA”, “68Ga” и “177Lu”. The study included the comparative analysis of the animal and patient samples, methods of data collection and results of the accumulation of radiopharmaceuticals in nodules and radiosensitive organs and tissues.
The results of the study allowed proposing the minimal requirements for the animal samples (at least 30 animals for each radiopharmaceutical), data collection (direct radiometry and PET) and time points (not less than 5 measurements in 120-240 minutes for the radiopharmaceuticals labeled with 68Ga and 5 measurements in 336 hours for the radiopharmaceuticals labeled with 177Lu) for the assessment of the biodistribution of the radiopharmaceuticals.

Pharmacy Formulas. 2020;2(4):60-71
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Search for the optimal mass profile of neuropeptides for the implementation of antihypoxic and activating actions

Shustov E.B., Ivkin D.Y., Ivkina A.S., Kim A.E., Lublin S.L., Nesterov M.S.

Abstract

In this study, the dependence of the pharmacological effects of neurotropic peptides of natural and synthetic origin on their structure was studied in laboratory rats. First, the study of the relative molecular profiles of peptide complexes was carried out using HPLC (gel-penetrating chromatography) with an internal standard. Then peptide complexes were administered to animals rectal and verified their biological activity on two independent models – antihypoxic activity (method of altitude the lift timing of the animal's life at a critical height) and the model of assessment of physical performance (time of forced swim test of animals with a load of 10% of the body weight to failure). The obtained data on biological activity (increase) were compared with the features of the structure of peptides. To assess the effect of drug doses on their activity, a single-factor analysis of variance was performed.

It has been shown that antihypoxic activity and performance stimulation are more or less inherent in all the studied peptide preparations, and are dose-dependent and related to the features of the molecular mass distribution of peptide components. It was also found that the specific antihypoxic activity of peptide preparations from brain tissues is associated with components having a mass range from 5 to 10 kDa. The optimal proportions of the peptide components for the implementation of biological activity by mass ranges were determined.

In addition, the chromatographic characteristics (molecular weight distribution over mass ranges) of natural neuropeptide complexes can be used to predict the severity of their biological effects.

Pharmacy Formulas. 2020;2(4):72-81
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Antipsychotics: from first to third generation

Petrova N.N., Sofronov A.G.

Abstract

The review is devoted to comparative analysis of antipsychotics of three generations. When writing the review, a systematic search in the databases PubMed, Medline, Elsevier was carried out, a simple filter for keywords was used. Pharmacological and clinical issues of antipsychotic therapy were considered, the mechanisms of action of antipsychotics of different generations were revealed. Current trends in the development of approaches to the therapy of schizophrenia and the concept of “atypicality” of antipsychotics were discussed. A comparative analysis of indications for use, tolerance (safety of use) and efficacy of various antipsychotic drugs with an emphasis on the effect on negative (primary, persistent) symptoms has been conducted. The hypothesis underlying new approaches to the therapy of schizophrenia, based on the effect on dopamine autoreceptors, consisting of a high density of D2 and low density of D3 receptors, has been presented. It has been shown that antipsychotics of the third generation open up new possibilities in the therapy of psychosis within the framework of a personalized approach in psychiatry with the achievement of functional recovery of patients. The characteristics of the drugs – representatives of the third generation of antipsychotics – aripiprazole and cariprazine were given. The uniqueness of cariprazine as the only drug that inhibits D3 receptors in vitro, as well as in vivo in patients with schizophrenia was emphasized. The data of evidence-based studies of the effectiveness of cariprazine in the treatment of negative, including predominant negative symptoms were presented.

Pharmacy Formulas. 2020;2(4):82-89
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The aspects that describe the pre-clinical studies of aceclofenac, as an instrument of registration of a generic drug

Anisimova N.A., Selizarova N.O., Plisko G.A., Semivelichenko E.D., Napalkova S.M.

Abstract

The paper presents the aspects of the toxicity, specific activity, pharmacokinetics and pharmacodynamics of aceclofenac, given in various sources describing its preclinical studies.

The search for information sources for the study was carried out using domestic and international databases: elibrary and PubMed using contextual queries, including terms of the international nonproprietary name, preclinical studies of pharmacokinetics, pharmacodynamics, and animal species.

Aceclofenac is one of the most prescribed drugs for acute and chronic pain. It refers to non-steroidal anti-inflammatory drugs, considered as drugs of first choice in the treatment of inflammation and pain.

On the pharmaceutical market of the Russian Federation, aceclofenac is presented in the form of tablets, powder for suspension preparation, cream for external use, which allows it to be prescribed for various diseases. It has shown itself to be highly effective in the symptomatic treatment of diseases of the musculoskeletal system, for the relief of acute and chronic pain.

A review of preclinical studies materials cited in various literature sources and including aspects of studying the toxicity, specific activity, pharmacokinetics and pharmacodynamics of aceclofenac, in our opinion, will allow using the data obtained in our study as one of the tools for further registration of generics.

Pharmacy Formulas. 2020;2(4):90-97
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Approaches to assessing the sexual behavior of male rats in the study of the effects of compounds that have a stimulating effect on sexual function

Subbotina S.N., Kryazhevskikh A.A., Kryazhevskikh A.A., Yudin M.A., Eletskaya E.I.

Abstract

The paper presents a comparative analysis of information content of methods for assessing the copulatory behavior of male rats with the introduction of compounds that have a stimulating effect on the sexual activity of animals. The social significance of the problem of sexual dysfunctions determines the relevance of the development of various experimental models of sexual behavior that allow assessing the effectiveness and safety of new drug. The probability of detecting the activating effect of pharmacological agents on sexual activity directly depends on the correct choice of the experimental model. The drugs of the central mechanism of action – galantamine hydrobromide (1 mg/kg) and loxidan (1,7 mg/kg), were used as pharmacological agents; drugs of peripheral action were yohimbine hydrochloride (2,6 mg/kg) and vardenafil hydrochloride (1,7 mg/kg). It has been shown that the determination of the stimulating effects of compounds of the central mechanism of action is possible using methods with different testing duration (from 15 to 180 min). Thus, the introduction of galantamine enhances the sexual activity of males in terms of the «copulation rate», «the number of perfect ejaculations» and «the duration of the post-ejaculatory refractory period», loxidan – in terms of the «total number of intromissions» and «relative rest time» in tests of limited duration. In the test showing the completed sexual cycle of males, the stimulating effects of galantamine are shown in terms of «the number of completed copulatory series» and «the number of completed ejaculations». To assess the activating effects of compounds of the peripheral mechanism of action, the expediency of using experimental models with a test duration of 30 minutes or more was shown. The most informative test is the test of paired interaction between a male and a female until the male reaches the state of «sexual exhaustion». A method with high information content is presented, which provides a high probability of detecting the activating effect of compounds on the sexual function of male rats.

Determination of the stimulating effects of compounds of the central mechanism of action is possible using methods with different test duration

Pharmacy Formulas. 2020;2(4):98-103
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Biological sciences

Ensuring energy efficiency at pharmaceutical enterprises in the paradigm of reducing the technogenic load on the environment

Perelygin V.V., Sklyarova N.A., Miroshnichenko Y.V., Ivanov S.V., Sakharov V.A., Drachkova I.M., Zharikov M.V.

Abstract

In this paper, the approaches to optimizing the environmental management system at pharmaceutical manufacturing enterprises and the environmental policy of pharmaceutical corporations in general were proposed. In the course of the study, it has turned out that the indicators of the negative impact on the environment as a result of the economic activities of industrial pharmaceutical enterprises do not take into account all the specific features of technological processes. At modern pharmaceutical enterprises, direct environmental risks are minimized at working areas and, in fact, their assessment is replaced by the calculation of barrier and isolation measures, which is in the competence of calculating sanitary and epidemiological risks only for employees of enterprises. In the course of pre-design, design work and the creation of pharmaceutical manufacturing enterprises, owing to the requirements and mandatory application of GxP, in fact, the negative impact on the environment at the enterprise itself within the boundaries of its sanitary zone is reduced to zero. However, a number of questions remain to be resolved, including how and to what extent a pharmaceutical business entity, in the course of its activities, causes a negative impact on the environment outside its location.

With this article, we begin series of publications of the results of our research in the direction of multilateral analysis of environmental risks in pharmaceutical organizations of different profiles and groups of pharmaceutical companies, united into separate corporate companies.

Compared to those approaches to assessing environmental risks as a result of the activities of pharmaceutical manufacturing enterprises, which are mainly focused on meeting the GxP requirements and relate to the quality of manufactured pharmaceutical products, we propose to take into account information with an emphasis, inter alia, on the energy saving policy of the Russian pharmaceutical industry.

The main goal of an integrated approach to the development of environmental policy and environmental management system in the pharmaceutical industry is for the management of manufacturing enterprises to comprehensively monitor and assess all environmental risks and energy conservation, in particular, taking into account the provision of energy efficiency to reduce the negative impact on the environment.

Pharmacy Formulas. 2020;2(4):104-117
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Prevention and treatment of cancer using so-called medicinal mushrooms raw materials: Criticism, facts, and perspectives

Zmitrovich I.V., Vlasenko V.A., Perelygin V.V., Figurin I.S.

Abstract

The purpose of the present review is the analysis of modern knowledge on use of “medicinal mushrooms” metabolites in cancer treatment, including in vitro experiments and clinical studies, with a preliminary assessment of the prospects for the development at least of some tactics of immunotherapy for malignant neoplasms. The data on the efficacy of adjuvant therapy of tumors in combination with mushroom extracts in relation to tumor regression as well as improving overall survival rates are presented. It is postulated that the improvement of long-term results of treatment can be most successfully reached with the use of “medicinal mushrooms” raw materials. This is due to the fact that an important task after adjuvant therapy (i.e. enhancing the immune surveillance of tumor derivatives) can be successfully solved using polysaccharides of fungal origin. In their final links and targets, such a practice coincides with clinically proven cytokine therapy. The involvement of Russian clinicians in practice of assessment of long-term results of treatment with fungal dectin-stimulation seems to us to be important task of clinical oncology.

Pharmacy Formulas. 2020;2(4):118-127
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Information and Prevention

“Young pharmacy-the potential of the future” 2020: result of conference

Zagorulko E.Y., Rozhkov G.A., Povydysh M.N.

Abstract

The X all-Russian scientific сonference of students and postgraduates «Young pharmacy-the potential of the future» in 2020 was held in two stages: breakout sessions at the University departments, where reports were selected for the combined sections of the second stage. Based on the results of the second stage, the top 10 reports were
selected for participation in the plenary session on November 6, 2020.

Pharmacy Formulas. 2020;2(4):128-130
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Investigation of the antibacterial effectiveness of drinking water preparation using the “TYENT Water Ionizer”

Paramonov S.G.

Abstract

Every year, the requirements for the quality of drinking water undergo significant changes, which is reflected in the updated versions of the relevant sanitary rules and regulations [SanPiN 2.1.4.1074-01 Drinking water. Hygienic requirements for the water quality of centralized drinking water supply systems. Quality control. Hygienic requirements for ensuring the safety of hot water systems. September 26, 2001 N 24 (as amended on April 2, 2018)]. Nevertheless, domestic indicators and standards are far from foreign modern hygienic requirements for drinking water.

Pharmacy Formulas. 2020;2(4):132-134
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Heritage

Adel Fedorovna Hammermann (1888–1978)

Narkevich I.A., Luganin V.G., Bespalova N.V., Zvyagin Y.Y., Perelygin V.V.

Abstract

Thanks to Nina Vladimirovna Bespalova for the active support of the present essay. She cherishes the memory of her grandmother Adele Fedorovna Hammermann all her life, a scientist who opened the way for women to the scientific community of Russian pharmacists. A.F. Hammermann became one of the leading specialists in pharmacognosy, the founder of the school for the study of Tibetan traditional medicine in Russia.

For almost half a century, Adel Fedorovna's life was inextricably linked with the present Saint Petersburg State Chemical and Pharmaceutical University. Here she first studied, and then taught and headed the Department of Pharmacognosy.

A.F. Hammermann has become one of those dedicated scientists that the Russian pharmaceutical school is proud of, and generations of university students have learned from her unique scientific heritage.

In the essay, based on materials from the home archive and the memoirs of teachers who at different times worked at the Department of Pharmacognosy of the University, we managed to describe the main milestones in the life path and scientific achievements of Adele Fedorovna Hammermann.

In the future, the authors of the essay hope to collect additional materials about this amazing woman and publish them in a separate edition.

Pharmacy Formulas. 2020;2(4):140-147
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