Dose-response effects of pentoxifylline on erythrocyte filterability: clinical and animal model studies

Clin Pharmacol Ther. 1990 Jul;48(1):50-6. doi: 10.1038/clpt.1990.117.


Ten patients with chronic occlusive arteriosclerosis received single oral doses of 100, 200, 400, 800, and 1200 mg pentoxifylline in a single-blind, placebo-controlled study. Blood samples were drawn at baseline and at 2 hour intervals for 6 hours. Drug and metabolite levels, as well as red cell filterability (deformability), were determined on all blood samples. Statistically significant dose-response increases of red cell filterability were found 4 and 6 hours after oral medication with the dosages of 200 to 1200 mg pentoxifylline. These changes were proportional to the plasma levels of pentoxifylline and metabolites 1 and 5 of this agent. Attempts were made to develop a suitable animal-screening method for agents with similar activity and to determine whether red blood cells in the absence of disease-related abnormalities may respond to this type of therapy. Five healthy Macaca arctoides monkeys were given 24 mg/kg pentoxifylline intravenously, and measurable but lesser increases in red cell deformability were recorded than in the patients.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Animals
  • Arteriosclerosis / blood
  • Arteriosclerosis / drug therapy*
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Erythrocyte Deformability / drug effects*
  • Female
  • Humans
  • Macaca
  • Male
  • Middle Aged
  • Pentoxifylline / administration & dosage
  • Pentoxifylline / pharmacology*
  • Randomized Controlled Trials as Topic
  • Single-Blind Method
  • Theobromine / analogs & derivatives*


  • Theobromine
  • Pentoxifylline