Pentoxifylline, Trental

  • Contraindications
  1. Recent major bleeding (Hemorrhagic CVA, Retinal Hemorrhage)
  • Mechanism
  1. Methylxanthine derivative
  2. Inhibits phosphodiesterase, increasing cAMP levels within Red Blood Cells, Platelets, vascular endothelium
    1. Results in vasodilation and increased red cell flexibility, with secondary increased arterial perfusion
    2. Also inhibits Platelet aggregation
  3. Inhibits Tumor Necrosis Factor-alpha (TNFa) and Interferon-gamma and increases TH2 Cytokines
    1. Inhibits T-Helper 1 (Th1) inflammatory and autoimmune activity
  • Dosing
  1. Take 400 mg orally three times daily with meals
    1. May reduce to twice daily for significant adverse effects
  2. Renal Insufficiency (GFR <30 ml/min)
    1. Reduce dose to 400 mg orally daily
  • Efficacy
  1. Full effect may be delayed for 8 weeks after starting medication
  2. Claudication symptoms (myalgias, exertional pain) may persist despite increased perfusion
  • Drug Interactions
  1. Increased bleeding risk
    1. Concurrent Anticoagulants, antiplatelet medications or NSAIDs
  2. Pentoxifylline increases levels of other medications
    1. Theophylline
    2. Warfarin with increased INR levels
  3. Other medications that increase Pentoxifylline levels
    1. Strong CYP1A2 Inhibitors (Ciprofloxacin, Fluvoxamine)
    2. Cimetidine
  • Safety
  1. Pregnancy Category C
  2. Unknown safety in Lactation
  • References
  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia