II. Indications

III. Contraindications

  1. Recent major bleeding (Hemorrhagic CVA, Retinal Hemorrhage)

IV. 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

V. 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

VI. Efficacy

  1. Full effect may be delayed for 8 weeks after starting medication
  2. Claudication symptoms (myalgias, exertional pain) may persist despite increased perfusion

VII. 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

VIII. Safety

  1. Pregnancy Category C
  2. Unknown safety in Lactation

X. References

  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia

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Related Studies

Cost: Medications

pentoxifylline (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
PENTOXIFYLLINE ER 400 MG TAB Generic $0.22 each