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Cardiovascular & Hematological Agents in Medicinal Chemistry

Maria Campos, C Batista, N R Jesus, C M Silva, T P Silva
Cardiovascular patients frequently use herbal medicinal products, in order to contribute to the improvement of their chronic condition without medical intervention. However, they are likely to suffer from adverse effects from natural products and herb-drug interactions. This work aimed to alert cardiovascular patients and healthcare providers of the potential of occurrence of herb-drug interactions with cardiovascular therapy. Information obtained from the campaign "Aprender Saúde Entre as Plantas e os Medicamentos", carried out by the Observatory of Herb-Drug Interactions (www...
October 7, 2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
Muharrem Akin, Thomas Skripuletz, L Christian Napp, Dominik Berliner, Ibrahim Akin, Arash Haghikia, Elvan Akin, Johann Bauersachs
Statins are the most widely prescribed drugs to reduce serum low density lipoprotein cholesterol (LDL-C) by inhibiting 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase. LDL-C reduction is associated with a decreased risk of atherosclerotic cardiovascular disease (ASCVD), including cardiovascular disease (CVD) and stroke. Statins reduce LDL-C by 30 to 40%, and the combination with other lipid-lowering agents such as ezetimibe leads to a further reduction by 20 to 25%. However, even the combination of these two agents might not be sufficient in high risk patients to require aggressive LDL-C reduction...
July 27, 2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
Pasquale Niscola, Andrea Tendas, Marco Giovannini, Adriana Costa, Daniela Venditti, Laura Volta, Luigi Malandruccolo, Stefania Sabbadini, Rosa Lasorella, Paolo de Fabritiis, Rita Cassetta, Alessiox Pio Perrotti
Pressure sores are a major complication in the bed-ridden older patient. In this report, we present the case of platelet rich plasma (PRP) application for the treatment of a pressure sore in an 88-year-old female affected by transfusion-dependent chronic inflammatory disease anemia associated with the congenital and inherited condition of thalassemic trait carrier. A weekly application schedule was planned at-home, given the patient's debilitation and her decreased performance status as well as personal and family difficulties to go as outpatients at our treatment center...
June 8, 2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
Saad Syed Hussain, Alan H Tyroch, Debabrata Mukherjee
Anticoagulation therapy is indicated for management of various clinical conditions to prevent adverse events and introduction of direct oral anticoagulants (DOACs) has ushered in a new era in anticoagulation therapy. Major advantages of DOACS include fewer drug interactions and that they do not need periodic monitoring. Several patients who were not on anticoagulation before due to older age, polypharmacy/drug interaction concerns, and logistics of periodic monitoring are now on anticoagulation with DOACs. Despite their many advantages, a challenge while prescribing DOACs is very limited availability of specific reversal agents and lack of understanding or guidance about the treatment strategy in case of major life threatening bleeding or need for urgent surgery...
May 24, 2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
M Praveen Kumar, T N Raju, R Ravindar Naik
Diabetic patients are susceptible to the development of chronic health complications responsible for a significant increase in their morbidity and mortality. Mechanisms related to glucose toxicity, namely oxidative stress, processes of non-enzymatic glycation and enhanced polyol pathway significantly contribute to the development of secondary complications of diabetes. There is an urgent need for inexpensive, non-surgical approaches to the treatment of diabetic complications. Recently, considerable attention has been devoted to the search for phytochemical therapeutics...
May 18, 2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
Yogita Dhas, Neetu Mishra, Joyita Banerjee
Vitamin D deficiency is common in metropolitan cities of India and worldwide due to faulty life style. The prevalence of vitamin D deficiency has tremendously increased in India despite the fact that it is located between 8.4° and 37.6° north latitude and majority of the Indian population exposed to ample sunlight throughout the year. From published data regarding vitamin D deficiency in India estimated prevalence of vitamin D deficiency is 70%-100% in the adult population. The main identified reason for vitamin D deficiency is the lack of appropriate sunlight exposure and no consumption (in case of vegetarian population) or less consumption of vitamin D containing diet (e...
April 26, 2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
V V Sathibabu Uddandrao, Parim Brahmanaidu, G Saravanan
Plants derived constituents with impending therapeutic values have been used long time to cure various diseases and disorders including Diabetes mellitus (DM). Many of the medicinal plants and herbs are also part of our diet as spices, vegetables and fruits. In recent years, there is growing evidence that plant-foods molecules, due to their biological properties, may be unique nutraceuticals and supplementary treatments for various aspects of Diabetes mellitus. In this review, we addressed the potential efficacies of S-Allylcysteine (SAC), a sulfur containing amino acid, derived from garlic, on Diabetes mellitus and other disorders...
April 18, 2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
M Hebi, M Ajebli, B El Bouhali, N A Zeggwagh, M Eddouks
This study aims to evaluate the underlying mechanism of action involved in the hypotensive effect of Chamaemulum nobile L. (Cn) aqueous extract and in anesthetized Wistar rats. Lyophilized aqueous extract was administered in the jugular vein, arterial blood pressure and heart rate were measured in the carotide artery over 120 min of injection throughout an invasive direct blood pressure measuring procedure. Intravenous bolus injection of aqueous Cn extract at the doses of 50, 100 and 200 mg/kg produced a dose dependent reduction in arterial blood pressure and heart rate (p<0...
April 7, 2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
Ana Rita Santos Estrela, Frederico Cerveira, Bárbara Regadas Correia, Ana Reis, Margarida Fardilha, Pedro Domingues, Rita Ferreira, M Rosário M Domingues
Hypovitaminosis D is a worldwide clinical problem, affecting populations in numerous ways. Several factors seem to affect vitamin D metabolism, including the suggestion that therapy with the lipid lowering HMG-CoA inhibitors might modulate vitamin D levels. However, the relationship between statins intake and serum levels of vitamin D is still controversial. The present work aimed to add new insights on the association between statins therapy, and more specifically the generation of statins, and the lipid profile in a population of 106 subjects treated with these HMG-CoA inhibitors...
February 11, 2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
Aitbay Bulashev, Orken Akibekov, Sadybek Tokpan, Shynar Serikova, Gulmira Abulgazimova
OBJECTIVES: To study the hematological findings of dogs infected with echinococcosis and the possibility of using in vitro reared Echinococcus granulosus excretory-secretory antigen (ES-Ag) as a reagent for serological diagnosis of canine echinococcosis. METHODS: Eight dogs were infected orally with protoscoleces, extracted from ovine fertile hydatid cysts. Two additional dogs were infected with Cysticercus tenuicollis, obtained from infested sheep. The hematological parameters of dogs were determined with the ADVIA 2120i automatic hematology analyzer with a blood smear staining module...
2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
Miha Tibaut, Daniel Petrovič
The worldwide increasing prevalence of obesity and sedentary lifestyle is the main cause of the rising incidence of T2DM. Due to chronic macrovascular and microvascular complications, T2DM represent a huge socioeconomic burden in the world. Oxidative stress is a key pathogenic mechanism implicated in diabetic coronary artery disease (CAD). Polymorphisms of oxidative stress genes are known to influence oxidative stress levels and are therefore thought to impact CAD pathogenesis. Identifying higher risk groups would be rational, since it would allow better sample selection and thus better results in antioxidant trials...
2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
Gregorio A Brunetti, Giovanna Palumbo, Giacomo S Morano, Erminia Baldacci, Ida Carmosino, Giorgia Annechini, Romina Talone, Sara Kiflom, Giada Mastrogiacomo, Sara Grammatico, Marta Chisini, Adriana Costa, Andrea Tendas, Laura Scaramucci, Marco Giovannini, Pasquale Niscola, Maria T Petrucci, Claudio Cartoni
BACKGROUND: More than 50% of oncohematological patients suffer from pain syndrome, mostly originating from the bone, which often include nociceptive and neuropathic complaints. Tapentadol, a recently available treatment option for cancer pain, exerts a dual analgesic mechanisms (opioid and noradrenergic), allowing for a high clinical efficacy as well as for a reduction in adverse events compared to traditional opioids. AIM: To explore the safety and efficacy of tapentadol as a suitable agent for the pain management in the setting of oncohematology...
2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
Yury Kaminsky, Elena Kosenko, Gjumrakch Aliev
This study investigated the effect of antihypertensive therapy with lisinopril on plasma cholesterol concentration and erythrocyte catalase activity in hypertensive patients. We observed, for the first time, significant inverse correlations between systolic blood pressure (BP) and erythrocyte catalase activity and between diastolic BP and erythrocyte catalase activity. Plasma total and low density lipoprotein (LDL) cholesterol as well as triglyceride levels were similar between baseline and 1-, 3-, and 6-month treatment values in the same patients; however, systolic and diastolic BP levels were expectedly reduced after the therapy...
2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
Joshua Brampton, Philip I Aaronson
There is increasing interest in the possible therapeutic benefits of the gasotransmitter hydrogen sulfide (H2S sulfide), and drugs which release sulfide are currently being evaluated in both preclinical and clinical studies as treatments for conditions ranging from cancer to cardiovascular disease to inflammation. Sulfide is generally considered to act as a vasodilator, and it is therefore not surprising that the effects of sulfide donors on both systemic and pulmonary hypertension are being examined. In this review, we provide a critical evaluation of both the evidence that H2S may be of benefit in treating systemic and pulmonary hypertension, and of current hypotheses regarding the cellular mechanisms underlying sulfide's effects on the systemic and pulmonary vascular systems...
2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
Prakash Chandwani, Puneet Verma, Sudheer Saxena, Padma K Ramachandran, Atul Abhyankar, Manjinder S Sandhu, Nikhil Parikh, Ashok Bhupali, Sharad Jain, Jayesh Prajapati
BACKGROUND: Drug-eluting stents (DES) have been shown to reduce the rate of acute complications and the need for subsequent revascularization in cases where single-vessels are treated. The performance of DES in patients with multivessel disease and complex lesions, however, remains controversial. This study assessed and compared clinical outcomes following single vs. multivessel percutaneous coronary intervention (PCI), using the Supraflex sirolimus-eluting stent (SES), in an all-comers patient population...
2016: Cardiovascular & Hematological Agents in Medicinal Chemistry
Xiu Jie Liu
A new class of 4-ethoxyisophthalamides is reported, based on the novel approach of linking the 4-ethoxy to Picotamide. Picotamide, as a combined inhibitor of Thromboxane A2 synthase and receptor, is synthesized in 1985 and attracted the attention of researchers. To improve our knowledge of the structure-activity relationship (SAR) and to obtain new anti-platelet drugs, total 24 unreported compounds of 4-ethoxyisophthalamides were designed and synthesized and were devised taking example by structural features of Picotamide and 4-methoxy-N1,N3-diphenylisophthalamide...
September 11, 2015: Cardiovascular & Hematological Agents in Medicinal Chemistry
Rose Mary Ferreira Lisboa Da Silva
The prevalence of atrial fibrillation (AF) increases with age and two-thirds of patients with AF aged over 75 years. In addition, co-morbidities are frequent in the elderly and worsen the prognosis. There are poorer quality of life, increased number of hospitalizations and cardiovascular events. The annual death rate was 8% in patients older than 75 years, and higher among women. There is a significant association between AF and cognitive disorders. Despite highest stroke risk, elderly have been paradoxically less likely to receive oral anticoagulation...
September 11, 2015: Cardiovascular & Hematological Agents in Medicinal Chemistry
Valeria Hirschler, Gustavo Maccallini, Milva Sanchez, Gonzalez Claudio, Claudia Molinari, Marcelo Figueroa, Claudio Arnada, Mariana Hidalgo
OBJECTIVE: To determine whether vitamin D supplementation improves non-traditional cardiovascular risk factors such as Apo B levels among indigenous children. METHODS: A prospective two-year study evaluated a treated cohort of 190 children (104 males) aged 9.4+ 2.2 years. Children were divided into group A (n=104; 54.7%) and group B (n=86; 45.3%). Both groups received vitamin D supplementation with 100,000 u/year; group B was treated in 2013 and group A in 2014...
2015: Cardiovascular & Hematological Agents in Medicinal Chemistry
Xiu J Liu, Tian En Shi, Xiao Wang, Ting T Wei, Xia Meng
In our search for new compounds among the structural analogues of the Picotamide acting on antiplatelet aggregation activities, a new series 2 of 4-ethoxyisophthal-amides were synthesized and their in vitro anti-platelet aggregation activities were evaluated by Born's test in comparison with their structural analogues of the series 1 of 4-methoxyisophthal-amides. The results revealed, among the series 2, six compounds 200, 2a, 2k, 2n, 2q and 2r displayed good antiplatelet aggregation activities in vitro induced by 5...
2015: Cardiovascular & Hematological Agents in Medicinal Chemistry
Maryna Popp Switzer, Priyanka Wani, Sucheta Gosavi, Debabrata Mukherjee
Edoxaban is a factor Xa inhibitor that is approved for prevention of stroke in individuals with atrial fibrillation and treatment of venous thromboembolic disease at once daily 60 mg dose for individuals with normal renal function. A decrease of dose to 30 mg is recommended for those with moderate renal insufficiency, weight ≤ 60 kg or simultaneous administration of strong P-glycoprotein inhibitors. At this time, it is not recommended for use in persons with either end stage renal disease or with GFR exceeding 95 mL/min...
2015: Cardiovascular & Hematological Agents in Medicinal Chemistry
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