Karolina Stachura, Elżbieta Pękala, Henryk Marona

Właściwości farmakologiczne pentoksyfiliny i jej metabolitów

Pharmacological properties of pentoxifylline and its metabolites. Pentoxifylline (PTX) is a methylxanthine derivative known as a non-selective phosphodiesterase inhibitor. The drug is a hemorheologic agent widely used in the treatment of various peripheral vascular and cerebrovascular disorders. PTX improves microvascular blood flow due to an increase of erythrocyte and leukocyte deformability and a reduction of platelet and erythrocyte aggregability. Furthermore, it possess some immunomodulatory and anti-inflammatory properties. In humans PTX is metabolized to at least seven metabolites (M1-M7). (R)-enantiomer of M1 (lisofylline/ LSF) is a therapeutic drug candidate and a novel inflammatory compound that inhibits stress-activated lipid metabolic pathways. LSF has been under investigation for acute lung injury, acute respiratory distress syndrome and septic shock. However, information on the bioactivity of the remaining metabolites of PTX is scanty.