Pentoxifylline

Abstract

Pentoxifylline (oxpentifylline) is an orally active haemorheological agent for the treatment of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation. Pentoxifylline acts primarily by increasing red blood cell deformability, by reducing blood viscosity and by decreasing the potential for platelet aggregation and thrombus formation. Extensive open and placebo-controlled studies have shown that pentoxifylline 600 to 1200 mg/day for at least 6 weeks is associated with subjective and objective improvements in 60 to 100% of patients with peripheral vascular disease. The most commonly assessed clinical parameter, walking distance, is usually improved by about 100%, although much greater improvements have also been documented. Other parameters which have been clearly improved include lower limb rest pain, paraesthesia, muscle blood flow, cramps and leg ulcers. Pentoxifylline has produced consistently better results than placebo, and in those studies using comparative drugs, better results than nylidrin, adenosine and naftidrofuryl. In patients with cerebrovascular disorders, open studies with pentoxifylline, usually at a dosage of 600 to 1200 mg/day (300 to 600 mg/day in Japan), have shown marked overall clinical improvements in about 85% of patients. Symptomatic improvements in rehabilitation psychometric tests, neuromotor and speech deficits and other subjective symptoms have accompanied increased cerebral blood flow, particularly to ischaemic areas. Pentoxifylline would appear to be useful in most types of cerebrovascular disease including transient ischaemic attacks, sequelae of cerebral thrombosis and haemorrhage, and chronic ischaemic disorders. In patients with chronic cerebrovascular disease pentoxifylline 600 to 1200 mg/day conferred significant clinical benefit compared with placebo and in isolated studies proved to be superior to drugs such as co-dergocrine mesylate, adenosine and pyrithioxine. Preliminary studies indicate that pentoxifylline may also prove useful in vaso-occlusive crises of sickle cell disease, some hearing disorders, disorders of eye circulation, high altitude sickness and asthenozoospermia. Pentoxifylline is usually well tolerated when administered as the conventional controlled release formulation, gastrointestinal symptoms (about 3%) being the most common complaint, although these and other adverse effects have not occurred to a significantly greater extent than with placebo. Thus, pentoxifylline offers a well-tolerated and effective alternative to the treatment options available for patients with peripheral vascular disease.(ABSTRACT TRUNCATED AT 400 WORDS)

The Beneficial Effects of Pentoxifylline on Caerulein-Induced Acute Pancreatitis in Rats

“…Pentoxifylline exhibits anti-inflammatory properties by inhibiting the aggregation of neutrophils and thrombocytes, the movement and chemotaxis of polymorphonuclear cells, and blood viscosity [12,59,60]. Pentoxifylline reduces the number of neutrophils that adhere to the vascular endothelium and their transendothelial transport [61,62].…”

Pentoxifylline in the Treatment of Actinic Prurigo

“…Unfortunately, thalidomide is not easily available, associated with dose-related neuropathy and usage in women is restricted [12]. Pentoxifylline (PTX) is a substituted methylxanthine approved for the treatment of intermittent claudication and other conditions involving defective regional microcirculation [13]. Besides its hemorheologic activity, PTX has been found to suppress the production of TNF-α by murine and human leukocytes [14, 15, 16].…”

Pentoxifylline Synergizes with All-Trans Retinoic Acid to Induce Differentiation of HL-60 Myelocytic Cells, but Suppresses tRA-Augmented Clonal Growth of Normal CFU-GM

“…Moreover, several lines of studies have also provided evidence showing potential advantages for the combination of tRA with PTX. The reasons include (1) PTX could block cytokine induction and inhibit inflammatory leukocyte infiltration [38, 39], and thus inhibit the retinoic acid syndrome; (2) PTX given by the oral route has a widely safe therapeutic range [40], and oral administration of tRA is more potent than the parental route [41]; (3) PTX which could inhibit the interaction of leukocytes with endothelial cells [21, 22] may decrease the pulmonary leakage syndrome; (4) PTX, which could inhibit activation of coagulation and fibrinolysis induced by endotoxin [42], may further decrease the possibility of coagulopathies in patients with APL; (5) PTX which could improve postirradiation wound healing [43], decreases bone marrow transplantation- and chemotherapy-induced untoward reactions [44], and fortifies patients with malignancy-associated anorexia and cachexia [45], may promote the well-being of patients with tRA treatment who commonly exhibit dryness of skin, mucositis and headache. Thus, it may be worthwhile to further evaluate the effects of the combination of PTX with tRA simply given via oral route as induction therapy in patients with APL.…”

“…The therapeutic effect of circulation on the PTX is believed to be due to the attenuation of the postischemic hyperemia and increment of erythrocyte deformability [20, 21]. Several studies have also shown that PTX could inhibit the interaction of leukocytes with endothelial cells in vascular leakage syndrome and leukocyte inflammatory responses [22].…”