A Comprehensive Monograph on Pentoxifylline (DB00806): Pharmacology, Clinical Efficacy, and Therapeutic Context

Introduction and Drug Identification

Overview of Pentoxifylline: A Xanthine-Derivative Hemorheologic Agent

Pentoxifylline (PTX), known also by the alternative name oxpentifylline, is a synthetic, small-molecule drug belonging to the dimethylxanthine class.[1] It is a tri-substituted xanthine derivative, sharing a structural lineage with other well-known methylxanthines such as caffeine, theophylline, and theobromine.[3] This chemical relationship is clinically relevant, as hypersensitivity to other xanthines is a contraindication for pentoxifylline use.[3]

Primarily classified as a hemorheologic agent, pentoxifylline's main therapeutic goal is to improve the flow properties (rheology) of blood.[4] It is also characterized as a blood viscosity reducer and a competitive, non-selective phosphodiesterase (PDE) inhibitor, a mechanism that underpins many of its physiological effects.[2]

The drug was originally developed and subsequently approved for the symptomatic treatment of intermittent claudication (IC), a condition characterized by muscle pain on exertion that is a hallmark of peripheral artery disease (PAD).[1] However, the scientific and clinical understanding of pentoxifylline has evolved significantly over the decades. Its recognized pleiotropic effects—which encompass anti-inflammatory, antioxidant, and immunomodulatory properties—have spurred extensive investigation into a diverse range of conditions far beyond its initial indication.[1] These investigational uses include venous leg ulcers, osteoradionecrosis, alcoholic hepatitis, and various diabetic complications, reflecting a growing appreciation for its complex pharmacological profile.[1]

Chemical and Physical Properties