An experimental overview of a new vasoactive drug: buflomedil HCl.

Abstract

A brief review of the pharmacology, pharmacokinetics, and metabolism of buflomedil-HCl is presented providing a pharmacologic basis for buflomedil therapy of ischemia associated with peripheral vascular disease. Buflomedil is readily absorbed in the gastrointestinal tract and has a plasma half-life of approximately 2-3 hours. The para-desmethyl derivative of buflomedil has been identified as a urinary metabolite. Pharmacologically, buflomedil increases perfusion to impaired vascular beds of the microcirculation, increases arterial perfusion with minimal effects on central hemodynamics, exhibits apparent oxygen "sparing" effects in animal experiments, demonstrates inhibitory effects on platelet aggregation, and, in preliminary experiments, appears to improve deformability of erythrocytes with abnormal fluidity. A nonspecific alpha-receptor blocking activity appears to be involved, at least in part, in these pharmacologic effects. The relative importance of these mechanisms/effects in the treatment of symptoms of vascular disease is unknown.