Pentoxifylline

Pentoxifylline is a medication that reduces the viscosity or "stickiness" of your blood, allowing it to flow more freely. It helps relieve the painful leg cramps caused by "intermittent claudication," a condition that results when hardening of the arteries reduces the leg muscles' blood supply. Benefits include improving the flow properties of blood by decreasing its viscosity, erythrocyte flexibility of blood cells, and increases blood flow to the affected microcirculation and enhances tissue oxygenation .

Pentoxifylline is used in humans for the treatment of peripheral vascular diseases and cerebrovascular disease caused by impairment of the microcirculation. It is chemically similar to theophylline and caffeine. Although its mechanism of action is not well understood, pentoxifylline is thought to both decrease the viscosity of blood and increase the flexibility of red blood cells.

Pentoxifylline and its metabolites improve the flow properties of blood by decreasing its viscosity. In patients with chronic peripheral arterial disease, this increases blood flow to the affected microcirculation and enhances tissue oxygenation. The precise mode of action of pentoxifylline and the sequence of events leading to clinical improvement are still to be defined. Pentoxifylline administration has been shown to produce dose-related hemorrheologic effects, lowering blood viscosity, and improving erythrocyte flexibility. Leukocyte properties of hemorrheologic importance have been modified in animal and in vitro human studies. Pentoxifylline has been shown to increase leukocyte deformability and to inhibit neutrophil adhesion and activation. Tissue oxygen levels have been shown to be significantly increased by therapeutic doses of pentoxifylline in patients with peripheral arterial disease.

Pentoxifylline is indicated for the treatment of patients with intermittent claudication on the basis of chronic occlusive arterial disease of the limbs. Pentoxifylline changes the shape of red blood cells in your blood. This makes it easier for these blood cells to fit into small arteries (blood vessels). Pentoxifylline is used to improve blood flow. Improved blood flow helps to reduce leg cramps and other symptoms of vascular disease (disease related to veins and arteries). Pentoxifylline may also be used for purposes other than those listed in this medication guide.

Pentoxifylline is a well characterized off-patent drug used for the treatment of intermittent claudication or pain associated with deep vein venoccllusive disease. Significant new research has demonstrated Pentoxifylline or its functional derivatives are useful in the diagnosis and treatment of a range of target diseases associated with fibrosis. These include conditions characterized by elevated levels of platelet derived growth factor (PDGF) in which the data clearly demonstrates that pentoxifylline effectively reduces PDGF induced c-jun gene expression, without altering c-fos gene expression. Pentoxifylline has been demonstrated to be useful in the diagnosis and treatment of a range of target diseases associated with fibrosis, for which there may be no useful treatment currently available. Pentoxifylline is well tolerated. It has very low toxicity and minimal side effects associated with chronic use. This makes this agent a very desirable drug for treatment of chronic conditions. As a well characterized off-patent drug, the original long-term studies can be referenced to assure a short pipeline to FDA approved IND status for these new indications.