Current Pharmaceutical Design - Volume 19, Issue 21, 2013

Successful treatment of hypertension often requires the association of drugs from different classes. Combination therapy takes advantage of complementary mechanisms of action, in order to reach target blood pressure (BP) earlier and to minimize the side effects of medications. In the last decade, several randomized trials have demonstrated the efficacy of combining a renin-angiotensin-aldosterone system (RAAS) inhi Read More

Even though patients who develop ischemic stroke despite taking antiplatelet drugs represent a considerable proportion of stroke hospital admissions, there is a paucity of data from investigational studies regarding the most suitable therapeutic intervention. There have been no clinical trials to test whether increasing the dose or switching antiplatelet agents reduces the risk for subsequent events. Certain issues have to Read More

Dual antiplatelet therapy of clopidogrel added aspirin is an established treatment strategy to prevent recurrent ischemic event occurrence in coronary artery disease patients. Generally, a one size fits all nonselective strategy is used without an assessment of pharmacodynamic efficacy of clopidogrel therapy. However, pharmacodynamic studies revealed various limitations of clopidogrel metabolism and numerous factors s Read More

Patients with nonvalvular atrial fibrillation (AF) and risk factors for stroke need anticoagulation to avoid thromboembolic complications. Vitamin K antagonists (VKAs) are an established pharmacological group the use of which is recommended by guidelines. However, VKAs (like warfarin) have major disadvantages, such as a variable dose-effect relationship, drug and food interactions, the need for regular blood testing and dos Read More

Cardiovascular disease is the leading cause of morbidity and mortality in the Western world. However, it appears that currently available risk assessment tools often underestimate risk, especially for patients in the intermediate-risk category. Considering the socioeconomic cost, it is imperative to correctly identify patients in the intermediate-risk category who would benefit from more aggressive treatment. A plethor Read More

Low density lipoproteins (LDL) and high density lipoproteins (HDL) are independent risk factors for coronary heart disease (CHD); decreasing LDL-cholesterol (LDL-C) levels with statin therapy represents the primary goal in the management of cardiovascular disease. However, despite the efficacy of statins in reducing cardiovascular morbidity and mortality, a significant residual risk has been observed even after reaching t Read More

As the population becomes more obese and the prevalence of diabetes and the metabolic syndrome increases, low-density lipoprotein-cholesterol (LDL-C) may lose its value as a sole predictor for cardiovascular risk among lipids. Combined dyslipidemia is typically characterized by elevations in LDL-C and triglyceride levels, often accompanied by decreased high-density lipoproteincholesterol (HDL-C) concentrations and increase Read More

Plasma low-density lipoprotein cholesterol (LDL-C) is one of the biomarkers of cardiovascular disease (CVD) risk. LDL is cleared from the circulation preferentially through the LDL receptor (LDLR) pathway. Proprotein convertase subtilisin/kexin 9 (PCSK9) promotes the degradation of the LDLR. PCSK9 inhibition is attractive as a new strategy for lowering LDL-C levels, especially in combination with lipid lowering drugs such as stati Read More

Mycobacterial enoyl acyl carrier protein (ACP) reductase is an attractive target for focused design of novel antitubercular agents. Structural information available on enoyl-ACP reductase in complex with different ligands was used to generate receptor-based pharmacophore model in Discovery Studio (DS). In parallel, pharmacophore models were also generated using ligand-based approach (HypoGen module in DS). S Read More

Coumarin compounds represent an important type of naturally occurring and synthetic oxygen-containing heterocycles with typical benzopyrone framework. This type of special benzopyrone structure enables its derivatives readily interact with a diversity of enzymes and receptors in organisms through weak bond interactions, thereby exhibit wide potentiality as medicinal drugs. So far, some coumarin-based drugs suc Read More