scholarly journals Current and Emerging Classes of Pharmacological Agents for the Management of Hypertension

2021 ◽  
Author(s):  
Utkarsh Ojha ◽  
Sanjay Ruddaraju ◽  
Navukkarasu Sabapathy ◽  
Varun Ravindran ◽  
Pitchaya Worapongsatitaya ◽  
...  
Keyword(s):  
Pharmacological Agents

Haemostatic Platelet Plug Formation in the Isolated Rabbit Mesenteric Preparation - An Analysis of Red Blood Cell Participation

1980 ◽  
Vol 44 (01) ◽  
pp. 006-008 ◽  
Author(s):  
D Bergqvist ◽  
K-E Arfors
Keyword(s):  
Whole Blood ◽  
Platelet Rich Plasma ◽  
Adenosine Diphosphate ◽  
In Vitro Test ◽  
Pharmacological Agents ◽  
Vitro Test ◽  
Releasing Effect ◽  
Plug Formation

SummaryIn a model using an isolated rabbit mesenteric preparation microvessels were transected and the time until haemostatic plugs formed was registered. Perfusion of platelet rich plasma gave no haemostasis whereas whole blood did. Addition of chlorpromazine or adenosine to the whole blood significantly prolonged the time for haemostasis, and addition of ADP to the platelet rich plasma significantly shortened it. It is concluded that red cells are necessary for a normal haemostasis in this model, probably by a combination of a haemodynamic and ADP releasing effect.The fundamental role of platelets in haemostatic plug formation is unquestionable but there are still problems concerning the stimulus for this process to start. Three platelet aggregating substances have been discussed – thrombin, adenosine diphosphate (ADP) and collagen. Evidence speaking in favour of thrombin is, however, very minimal, and the discussion has to be focused on collagen and ADP. In an in vitro system using polyethylene tubings we have shown that "haemostasis" can be obtained without the presence of collagen but against these results can be argued that it is only another in vitro test for platelet aggregation (1).To be able to induce haemostasis in this model, however, the presence of red blood cells is necessary. To further study this problem we have developed a model where haemostatic plug formation can be studied in the isolated rabbit mesentery and we have briefly reported on this (2).Thus, it is possible to perfuse the vessels with whole blood as well as with platelet rich plasma (PRP) and different pharmacological agents of importance.

Correction of the Hematological Homeostasis Parameters during Physical Loads by Using Energy Orientation Pharmacological Agents

2019 ◽  
Vol 4 (6) ◽  
pp. 377-383
Author(s):  
M. V. Kuzmenko ◽  
◽  
L. M. Gunina ◽  
O. V. Nosach ◽  
R. V. Golovashchenko ◽  
...  
Keyword(s):  
Pharmacological Agents

Physiological and Hereditary Hyperbilirubinemia in Athletes: Role in Reducing Efficiency and Correction Methodology

2020 ◽  
Vol 5 (5) ◽  
pp. 386-393
Author(s):  
L. M. Gunina ◽  
◽  
Kazys Mylashyus ◽  
Voitenko V. L. ◽  
◽  
...  
Keyword(s):  
Physical Activity ◽  
Functional State ◽  
Oxygen Demand ◽  
Diagnostic Algorithm ◽  
Drug Prevention ◽  
The Body ◽  
Erythrocyte Membranes ◽  
Pharmacological Agents ◽  
Bilirubin Metabolism ◽  
The Individual

Under high-intensity loads, the athlete's bodies take place a number of biochemical reactions and physiological processes that can lead to hyperbilirubinemia. The factors that can initiate the onset of this phenomenon include the syndrome of micro-damage muscle, violation of the integrity of erythrocyte membranes, decreased blood pH, malnutrition and increase oxygen demand of the body. Degree of expression of manifestations of physiological bilirubinemia depends on the level of adaptation of the athlete to the physical activities offered. Hyperbilirubinemia in athletes can be one of the components of the deterioration of the functional state, forming the symptoms of endogenous intoxication. The relevance of this problem in sport lies in the relatively low detection rate of hyperbilirubinemia due to the lack of regular screening studies. However, in drawing up a plan of nutritional- metabolic support for training and competitive activity and recovery measures, must not only the individual reaction of the athlete body to physical activity, but also the severity of shifts in the indicators of bilirubin metabolism and their ratio. The article describes the reasons for the increase in bilirubin levels, which can be caused by both the effect of physical activity and by the presence of pathological processes in athletes. The factors influencing the blood serum’s bilirubin content are also highlighted, which include the state of erythrocyte cell membranes and the rate of hemoglobin destruction, the functional state of the liver, the specifics of physical loads and the use of ergogenic pharmacological agents by athletes. Particular accent has been placed on the illumination of hereditary hyperbilirubinemias, which may have been detected at the stage of selection of athletes. The most common phenomenon is Gilbert's syndrome, which occurs in 2-5% of cases in the general population, is characterized in the clinic by a benign flow and is manifested by episodes of jaundice and an increase in total bilirubin content to moderate values due to indirect. The frequency of detection of hyperbilirubinemias in the population of athletes is 4.68%, among which Gilbert's disease accounts for almost half (48.7%). Conclusion. The work highlighted the pathogenesis and diagnostic algorithm of Gilbert's disease, and also emphasized that its drug prevention and correction in athletes to maintain functional and physical fitness should be carried out taking into account anti-doping rules, which requires upon diagnosis timely receipt of a therapeutic exclusion

Design, Synthesis and Pharmacological Evaluation of New Thiazole Derivatives as Anthelmintic Agents

2020 ◽  
Vol 13 (5) ◽  
pp. 5075-5081
Author(s):  
Sirisha Kalam ◽  
Sai Krishn G ◽  
Kumara Swamy D ◽  
Sai Santhoshi K ◽  
Durga Prasad K
Keyword(s):  
Anthelmintic Activity ◽  
Docking Studies ◽  
Molecular Property ◽  
Thiazole Derivatives ◽  
Pharmacological Agents ◽  
Design Synthesis ◽  
Standard Drug ◽  
Lipinski’S Rule ◽  
Mass Spectral ◽  
Tubulin Protein

Pharmacological agents that kills parasites are essential drugs in some tropical countries. In this study, a series of 2-amino substituted 4-phenyl thiazole derivatives (4a-e) have been synthesized by the conventional method. The thiazole derivatives were synthesized by three steps. The obtained five derivatives were purified by recrystallization using methanol as a solvent or column chromatography. They were characterized by melting point, TLC, FTIR, 1H NMR and MASS spectral data. Compounds 4a-e were evaluated in silico by using different software’s (Lipinski’s Rule of 5, OSIRIS molecular property explorer, Molsoft molecular property explorer, and PASS & docking studies). These compounds were then evaluated for their possible anthelmintic activity against Indian adult earth worms (Pherituma postuma). All the compounds displayed significant anthelmintic activity. Compound 4c and 4e were more potent compounds when compared with the standard drug (mebendazole). Molecular docking studies guided and proved the biological activity against beta tubulin protein (1OJ0). In conclusions, these new molecules have promising potential as anthelmintic for treatment of parasites.   

New Insights on KCa3.1 Channel Modulation

2020 ◽  
Vol 26 (18) ◽  
pp. 2096-2101
Author(s):  
Giuseppe Manfroni ◽  
Francesco Ragonese ◽  
Lorenzo Monarca ◽  
Andrea Astolfi ◽  
Loretta Mancinelli ◽  
...  
Keyword(s):  
Potassium Channel ◽  
Critical Role ◽  
Calcium Signalling ◽  
Typical Feature ◽  
Open Probability ◽  
Pharmacological Agents ◽  
Channel Modulation ◽  
Calcium Dependent ◽  
Modelling Techniques ◽  
Calcium Activated Potassium Channel

The human intermediate conductance calcium-activated potassium channel, KCa3.1, is involved in several pathophysiological conditions playing a critical role in cell secretory machinery and calcium signalling. The recent cryo-EM analysis provides new insights for understanding the modulation by both endogenous and pharmacological agents. A typical feature of this channel is the low open probability in saturating calcium concentrations and its modulation by potassium channel openers (KCOs), such as benzo imidazolone 1-EBIO, without changing calcium-dependent activation. In this paper, we proposed a model of KCOs action in the modulation of channel activity. The KCa3.1 channel has a very rich pharmacological profile with several classes of molecules that selectively interact with different binding sites of the channel. Among them, benzo imidazolones can be openers (positive modulators such as 1-EBIO, DC-EBIO) or blockers (negative modulators such as NS1619). Through computation modelling techniques, we identified the 1,4-benzothiazin-3-one as a promising scaffold to develop new KCa3.1 channel modulators. Further studies are needed to explore the potential use of 1-4 benzothiazine- 3-one in KCa3.1 modulation and its pharmacological application.

Recent Advances in Rational Diagnosis and Treatment of Normal Pressure Hydrocephalus: A Critical Appraisal on Novel Diagnostic, Therapy Monitoring and Treatment Modalities

2019 ◽  
Vol 20 (10) ◽  
pp. 1041-1057 ◽  
Author(s):  
Lei Zhang ◽  
Zahid Hussain ◽  
Zhuanqin Ren
Keyword(s):  
Cerebrospinal Fluid ◽  
Normal Pressure Hydrocephalus ◽  
Critical Appraisal ◽  
Therapy Monitoring ◽  
Normal Pressure ◽  
Treatment Modalities ◽  
Pharmacological Agents ◽  
Recent Advances ◽  
Rational Diagnosis ◽  
Neuroimaging Techniques

Background:Normal pressure hydrocephalus (NPH) is a critical brain disorder in which excess Cerebrospinal Fluid (CSF) is accumulated in the brain’s ventricles causing damage or disruption of the brain tissues. Amongst various signs and symptoms, difficulty in walking, slurred speech, impaired decision making and critical thinking, and loss of bladder and bowl control are considered the hallmark features of NPH.Objective:The current review was aimed to present a comprehensive overview and critical appraisal of majorly employed neuroimaging techniques for rational diagnosis and effective monitoring of the effectiveness of the employed therapeutic intervention for NPH. Moreover, a critical overview of recent developments and utilization of pharmacological agents for the treatment of hydrocephalus has also been appraised.Results:Considering the complications associated with the shunt-based surgical operations, consistent monitoring of shunting via neuroimaging techniques hold greater clinical significance. Despite having extensive applicability of MRI and CT scan, these conventional neuroimaging techniques are associated with misdiagnosis or several health risks to patients. Recent advances in MRI (i.e., Sagittal-MRI, coronal-MRI, Time-SLIP (time-spatial-labeling-inversion-pulse), PC-MRI and diffusion-tensor-imaging (DTI)) have shown promising applicability in the diagnosis of NPH. Having associated with several adverse effects with surgical interventions, non-invasive approaches (pharmacological agents) have earned greater interest of scientists, medical professional, and healthcare providers. Amongst pharmacological agents, diuretics, isosorbide, osmotic agents, carbonic anhydrase inhibitors, glucocorticoids, NSAIDs, digoxin, and gold-198 have been employed for the management of NPH and prevention of secondary sensory/intellectual complications.Conclusion:Employment of rational diagnostic tool and therapeutic modalities avoids misleading diagnosis and sophisticated management of hydrocephalus by efficient reduction of Cerebrospinal Fluid (CSF) production, reduction of fibrotic and inflammatory cascades secondary to meningitis and hemorrhage, and protection of brain from further deterioration.

Prophylaxis of Venous Thromboembolism Following Orthopedic Surgery: Mechanical and Pharmacological Approaches and the Need for Extended Prophylaxis

1999 ◽  
Vol 82 (08) ◽  
pp. 918-924 ◽  
Author(s):  
R.D. Hull ◽  
G.F Pineo
Keyword(s):  
Clinical Trials ◽  
Venous Thromboembolism ◽  
Orthopedic Surgery ◽  
Total Joint Replacement ◽  
Case Series ◽  
Pharmacological Agents ◽  
Thrombotic Disease ◽  
Vein Thrombosis ◽  
Major Orthopedic Surgery ◽  
Mechanical Devices

IntroductionMajor orthopedic surgery, particularly total joint replacement or hip fracture, represents a high risk of future development of postoperative venous thromboembolism and warrants the routine use of prophylaxis with either mechanical devices or pharmacological agents. The aim of prophylaxis is to prevent fatal pulmonary embolism (PE) and the morbidity of deep vein thrombosis (DVT), particularly the development of post-thrombotic syndrome. Patterns of clinical practice, with respect to the prevention of venous thromboembolism and the appropriate use of anticoagulants for the treatment of thrombotic disease, have been strongly influenced by recent consensus conferences.1,2 Rules of evidence for assessing the literature have been applied to all recommendations regarding the prevention and treatment of thrombotic disease. These results were extrapolated using evidence gleaned from major clinical disorders and are based only on nonrandomized clinical trials or case series.1-3 Data from a large number of Level I clinical trials in patients undergoing orthopedic surgery have provided answers to many of the questions regarding prophylaxis of venous thromboembolism. In this review, we will discuss the prevention of venous thromboembolism following orthopedic surgery and discuss some of the controversial issues where further studies are required.

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