Effectiveness of vitex agnus castus extract in the treatment of primary dysmenorrhea

Актуальність. Первинна дисменорея (ПД) — один з найпоширеніших видів гінекологічної патології, що спостерігається у 31–52 % молодих жінок, серед яких у 10 % інтенсивність процесу призводить до інвалідності. Патогенез ПД враховує вплив представника ейкозаноїдів тромбоксану А2 з вираженою судинозвужувальною дією. У статті надані результати клініко-гормонального обстеження жінок з ПД та розроблена на цій основі методика лікування. Мета: розробити й оцінити ефективність лікування ПД з урахуванням багатокомпонентного патогенезу захворювання. Матеріали та методи. Під спостереженням перебувало 60 жінок, випадковим чином розподілених на дві групи: 30 жінок із ПД (основна група) та 30 здорових жінок (контрольна група). Діагноз ПД встановлювався на підставі скарг пацієнток на болючі менструації та супутні симптоми, за винятком органічної гінекологічної патології та захворювань внутрішніх органів, на консультаціях у гінеколога й ендокринолога. Лікування хворих на ПД проводили комбінованим препаратом, до складу якого входять стандартизований екстракт Vitex agnus castus L., індол-3-карбінол, 3,3-диіндоліл-метан, екстракт пасифлори, екстракт каліфорнійської ешольції. Результати. В результаті лікування у хворих на ПД значно зменшилася інтенсивність болю, а у 60 % біль зник повністю, у всіх зник страх очікування наступної менструації, значно зменшилися прояви вегетативно-судинної системи (з 17 до 3 % пацієнток), вегетативні (від 10 до 0 % хворих), метаболічні й ендокринні (від 13 до 0 % хворих) розлади та розлади емоційно-психічної сфери (від 23 до 7 % хворих). Через 1 місяць після лікування поліпшення якості життя відзначали 70 % (21/30) пацієнток з ПД, а підвищення працездатності — 60 % (18/30), через 2 місяці — 93 % (28/30) і 83 % (25/30) відповідно. В жодної пацієнтки під час лікування не було виявлено побічних ефектів. Висновки. З огля­ду на безпеку та високу терапевтичну ефективність препарат на основі екстракту Vitex agnus castus можна рекомендувати для лікування молодих хворих із ПД тривалістю не менше трьох місяців.

Abstract.  Background. Primary dysmenorrhea (PD) is one of the most common types of gynecological pathology and is observed in 31–52 % of young women, in 10 % of them the pain is so intense that leads to disability. In the pathogenesis of PD consider a representative of eicosanoids — thromboxane A2 with a pronounced vasoconstrictor effect. The article presents the results of clinical and hormonal examination of women with PD and developed on this basis a method of treatment. The purpose was to develop and evaluate the effectiveness of treatment of PD, taking into account the multicomponent pathogenesis of the disease. Materials and methods. There were 60 women observation, randomly divided into two groups: 30 women with PD (main group) and 30 healthy women (control group). PD was diagnosed on the basis of patients’ complaints of painful menstruation and related symptoms, excluding organic gynecological pathology and diseases of the internal organs in consultation with a physician and endocrinologist. Treatment of patients with PD was performed with a combined drug, which includes a standardized extract of Vitex agnus castus L., indole-3-carbinol, 3,3-diindolyl-methane, passionflower extract, California escholzia extract. Results. As a result of treatment in patients with PD significantly reduced the intensity of pain, and 60 % completely disappeared pain, all disappeared fear of waiting for the next menstruation, significantly reduced the manifestations of autonomic vascular (from 17 % of patients to 3 %), autonomic (from 10 % of patients to 0 %), metabolic and endocrine (from 13 % of patients to 0 %) disorders and disorders of the emotional and mental sphere (from 23 % of patients to 7 %), no patient had a combination of symptoms.
Conclusions. Given the safety, high therapeutic efficacy, the drug based on Vitex agnus castus extract can be recommended for the treatment of young patients with PD lasting at least 3 months.
Keywords:  menstrual pain; hormonal balance; primary dysmenorrhea

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1,4-Naphthoquinone Motif in the Synthesis of New Thiopyrano[2,3-d]thiazoles as Potential Biologically Active Compounds

A series of 11-substituted 3,5,10,11-tetrahydro-2H-benzo[6,7]thiochromeno[2,3-d][1,3]thiazole-2,5,10-triones were obtained via hetero-Diels-Alder reaction of 5-alkyl/arylallylidene/-4-thioxo-2-thiazolidinones and 1,4-naphthoquinones. The structures of newly synthesized compounds were established by spectral data and a single-crystal X-ray diffraction analysis. According to U.S. NCI protocols, compounds 3.5 and 3.6 were screened for their anticancer activity; 11-Phenethyl-3,11-dihydro-2H-benzo[6,7]thiochromeno[2,3-d]thiazole-2,5,10-trione (3.6) showed pronounced cytotoxic effect on leukemia (Jurkat, THP-1), epidermoid (KB3-1, KBC-1), and colon (HCT116wt, HCT116 p53-/-) cell lines. The cytotoxic action of 3.6 on p53-deficient colon carcinoma cells was two times weaker than on HCT116wt, and it may be an interesting feature of the mechanism action.
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C60 fullerene attenuates muscle force reduction in a rat during fatigue development

C60 fullerene (C60) as a nanocarbon particle, compatible with biological structures, capable of penetrating through cell membranes and effectively scavenging free radicals, is widely used in biomedicine. A protective effect of C60 on the biomechanics of fast (m. gastrocnemius) and slow (m. soleus) muscle contraction in rats and the pro- and antioxidant balance of muscle tissue during the development of muscle fatigue was studied compared to the same effect of the known antioxidant N-acetylcysteine (NAC). C60 and NAC were administered intraperitoneally at doses of 1 and 150 mg kg−1, respectively, daily for 5 days and 1 h before the start of the experiment. The following quantitative markers of muscle fatigue were used: the force of muscle contraction, the level of accumulation of secondary products of lipid peroxidation (TBARS) and the oxygen metabolite H2O2, the activity of first-line antioxidant defense enzymes (superoxide dismutase (SOD) and catalase (CAT)), and the condition of the glutathione system (reduced glutathione (GSH) content and the activity of the glutathione peroxidase (GPx) enzyme). The analysis of the muscle contraction force dynamics in rats against the background of induced muscle fatigue showed, that the effect of C60, 1 h after drug administration, was (15–17)% more effective on fast muscles than on slow muscles. A further slight increase in the effect of C60 was revealed after 2 h of drug injection, (7–9)% in the case of m. gastrocnemius and (5–6)% in the case of m. soleus. An increase in the effect of using C60 occurred within 4 days (the difference between 4 and 5 days did not exceed (3–5)%) and exceeded the effect of NAC by (32–34)%. The analysis of biochemical parameters in rat muscle tissues showed that long-term application of C60 contributed to their decrease by (10–30)% and (5–20)% in fast and slow muscles, respectively, on the 5th day of the experiment. At the same time, the protective effect of C60 was higher compared to NAC by (28–44)%. The obtained results indicate the prospect of using C60 as a potential protective nano agent to improve the efficiency of skeletal muscle function by modifying the reactive oxygen species-dependent mechanisms that play an important role in the processes of muscle fatigue development.
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The use of opioid analgesics in palliative care in Ukraine: changes in legislation and availability

Abstract
Introduction: The main task of palliative care is to improve the quality of life of a patient, and the therapy of chronic pain with opioids is a significant problem for palliative care patients in Ukraine. Therefore, this study aimed to assess the opioid availability for palliative care patients in Ukraine.
Methods: Analysis of the list and consumption of opioids according to the scientific publications and legal documents.
Results: It was found that in Ukraine as of June 2021, 12 international non-proprietary names of opioids were registered, most of which are represented by several dosage forms, which makes it possible for patients to receive adequate pain relief through non–invasive therapy with oral forms. It was shown that two thirds (63.2%) of trade names of opioids registered in Ukraine were of domestic origin. Based on a comparative analysis of the range of opioids, available in current regulatory documents, it was established that in the State Register of Medicines of Ukraine and the Unified clinical protocol there is an almost identical list of opioids (12 drugs). However, in the State Drug Formulary and the National List of Essential Medicines, this list is much smaller (8 and 5 drugs, respectively). Since 2013 changes in the regulatory documents on the medical use of opioids in Ukraine have occurred, and oral morphine was registered for the first time, allowing access to adequate pain relief. Analysis of the morphine consumption level by dosage forms has shown that before 2013, the pharmacies sold only morphine in injections, and since 2013, the consumption of oral morphine increased.
Conclusions. Changes in regulatory documents partially simplified the complicated process of obtaining opioids by patients. However, more than 80% of patients still do not receive adequate pain therapy due to the hesitancy of doctors to prescribe opioids and an extremely insufficient number of pharmacies (1.8%) that sell opioids for the population.

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Research on the use of motivational tools in the practical activity of pharmaceutical specialists

The aim. Research on the peculiarities of the use of modern motivational tools by domestic employers in the pharmaceutical industry (including training and involvement of pharmaceutical specialists in social projects).

Materials and methods. An anonymous online survey in the Google Form was conducted from April 3, 2021 to November 1, 2021 on the social network "Facebook" (including in four pharmaceutical groups of this network). Methods: analysis, synthesis, and generalization.

Results of the research. The main motivating factors of respondents and the main motivational tools used by employers in the pharmaceutical industry have been identified. The state of training and education during professional activities and the evaluation of their effectiveness by respondents have been studied. Professional and motivational-psychological trainings are in the lead in the ranking of educational projects (75.2 % of respondents). The methods of evaluation of pharmaceutical specialists used by employers in the pharmaceutical industry have been generalized. The attitude of respondents to the participation of employers in the pharmaceutical industry in social and charitable projects has been studied. Most respondents (67.5 %) positively perceives the participation of employers in social and charitable projects, for some of them this is a motivational advantage when choosing a place of work.

Conclusions. An online survey of 508 pharmaceutical professionals, conducted in a Google Form has allowed us to establish the features of current motivational approaches used today in pharmaceutical organizations and the attitude of respondents to them. It has been found that such motivational tools as trainings (innovative form of education) (55.1 %), as well as material forms of incentives (73.2 %) are widely used. At the same time, the main topics of the trainings are regarding the professional aspects of activity. An important factor in the life of a pharmaceutical organization is its social and charitable work, which forms a positive attitude towards it on the part of pharmaceutical professionals, and sometimes serves as a motivational advantage in choosing a place of work

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