Current Pharmaceutical Design - Volume 11, Issue 4, 2005

Fondaparinux is the first drug from the pentassaccharide factor X inhibitor class of anticoagulants to be approved for clinical use. It has been shown to be effective in the prevention of deep vein thrombosis in patients undergoing major orthopaedic surgery of the lower limbs. The drug is also being evaluated for use in the acute coronary syndromes and established thromoboembolic events. The pharmacology of fondaparinux Read More

In-stent restenosis remains the limitation of coronary stent implantation despite numerous efforts of its prevention by catheter-based techniques or by drug therapy. Today, only intravascular irradiation has proven to effectively reduce neointima formation, restenosis rate and major adverse cardiovascular events by approximately 50%. Its efficiency is demonstrated for high-risk subsets like long lesions, lesions in saphenous v Read More

Levosimendan is a new calcium sensitizer developed for the treatment of congestive heart failure. Experimental studies indicate that levosimendan increases myocardial contractility and dilates both the peripheral and coronary vessels. Its positive inotropic effect is based on calcium-dependent binding of the drug to cardiac troponin C. It also acts as an opener of ATP-dependent potassium channels in vascular smooth muscle, th Read More

The clinical role of magnetic resonance in diseases of the heart and great vessels is rapidly evolving. Cardiovascular magnetic resonance (CMR) has become an established non-invasive imaging modality for the assessment of various cardiac disorders, such as congenital heart disease, cardiac masses, cardiomyopathies, aortic and pericardial diseases. Moreover, due to its accuracy and reproducibility, CMR is currently considere Read More

The extracellular matrix (ECM) is a dynamic microenvironment and a major contributor to the adverse ventricular remodelling that follows myocardial infarction (MI), via activation of both direct pro-fibrotic pathways and matrix metalloproteinases (MMPs) that enhance collagenase activity. Reactive fibrosis, i.e. deposition of ECM materials remote from the region of the MI is clearly detrimental to ventricular function Read More

The heart is a pump, but also a furnace able to produce at each moment a large amount of energy and to adapt fast enough to face the changes in both fuel supply and energy demand. The pharmacological treatment of angina has been largely focused on the “pump” through hemodynamic agents aimed at decreasing cardiac effort to decrease energy demand. A new concept arose focusing the “furnace” through metabolic Read More

The discovery of B-type natriuretic peptide (BNP) and n-terminal pro BNP (nt-proBNP) as markers for the diagnosis, severity and prognosis of patients with congestive heart failure has been called a true breakthrough for patients and physicians faced with this disorder. Moreover, the literature on their prognostic value in other clinical conditions like acute coronary syndromes, right-sided heart failure and even in the g Read More

Ximelagatran is an oral direct thrombin inhibitor (DTI), the active form of which is melagatran. Approximately 20% of an oral ximelagatran dose becomes bioavailable as melagatran, which binds noncovalently and reversibly to both fibrin-bound and freely circulating thrombin. Oral ximelagatran dosing not only inhibits thrombin activity rapidly, competitively, and potently, but also delays and suppresses thrombin gen Read More

The pivotal role of leptin in regulating body weight and energy homeostasis is very well established. More recently, leptin also emerged as an important regulator of T-cell-dependent immunity. Reduced leptin levels, as observed during periods of starvation, correlate with an impaired cellular immune response, whereby especially the TH1 proinflammatory immune response appears to be affected. Physiologically, this c Read More

The identification of protein kinase C isozymes in distinct localities within the cell has led to the suggestion that each isozyme mediates a unique function. This has necessitated the development of methodologies that are capable of assigning specific function to an isozyme. For many years the location of individual isozymes in a particulate fraction was used to correlate specific isozymes with cellular function. More recently over- Read More