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

Ontology: Pentoxifylline (C0030899)

Definition (NCI) A methylxanthine derivative with hemorrheologic and immunomodulating properties. Pentoxifylline inhibits phosphodiesterase, resulting in increased levels of cyclic adenosine monophosphate (cAMP) in erythrocytes, endothelium, and the surrounding tissues. This leads to vasodilation, improves erythrocyte flexibility, and enhances blood flow. In addition, the increased level of cAMP in platelets inhibits platelet aggregation, which may contribute to a reduction in blood viscosity. This agent also inhibits production of tumor necrosis factor-alpha and interferon-gamma, while it induces Th2-like (T-helper 2) cytokine production, thereby inhibiting Th1-mediated (T-helper 1) inflammatory and autoimmune responses.
Definition (NCI_NCI-GLOSS) A drug used to prevent blood clotting and as a treatment that may help decrease weight loss in people with cancer.
Definition (CSP) metabolite of pentifylline (a preparation of theobromine and hexyl halide); used as a vasodilator.
Definition (MSH) A METHYLXANTHINE derivative that inhibits phosphodiesterase and affects blood rheology. It improves blood flow by increasing erythrocyte and leukocyte flexibility. It also inhibits platelet aggregation. Pentoxifylline modulates immunologic activity by stimulating cytokine production.
Definition (PDQ) A methylxanthine derivative with hemorrheologic and immunomodulating properties. Pentoxifylline inhibits phosphodiesterase, resulting in increased levels of cyclic adenosine monophosphate (cAMP) in erythrocytes, endothelium, and the surrounding tissues. This leads to vasodilation, improves erythrocyte flexibility, and enhances blood flow. In addition, the increased level of cAMP in platelets inhibits platelet aggregation, which may contribute to a reduction in blood viscosity. This agent also inhibits production of tumor necrosis factor-alpha and interferon-gamma, while it induces Th2-like (T-helper 2) cytokine production, thereby inhibiting Th1-mediated (T-helper 1) inflammatory and autoimmune responses. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41432&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41432&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C733" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D010431
SnomedCT 91376007, 387522004
LNC LP14918-4, MTHU035938, MTHU002178
English Oxpentifylline, 1H-Purine-2,6-dione, 3,7-dihydro-3,7-dimethyl-1-(5-oxohexyl)-, 3,7-Dihydro-3,7-dimethyl-1-(5-oxohexyl)-1H-purine-2,6-dione, pentoxifylline, PTX, Dentoxifylline, pentoxifylline (medication), PENTOXIFYLLINE, Pentoxifylline ER, Pentoxifylline [Chemical/Ingredient], pentoxyphylline, Pentoxyfylline, Pentoxyphylline, Pentoxifylline (product), Pentoxifylline (substance), oxpentifylline, Pentoxifylline
Swedish Pentoxifyllin
Czech pentoxifylin
Finnish Pentoksifylliini
Russian TRENTAL, PENTOKSIFILLIN, ПЕНТОКСИФИЛЛИН, ТРЕНТАЛ
Italian Oxpentifillina, Pentossifillina
Croatian PENTOKSIFILIN
Polish Pentoksyfilina
Japanese ペントキシフィリン, オクスペンチフィリン
Spanish oxpentifilina, pentoxifilina (producto), pentoxifilina (sustancia), pentoxifilina, Pentoxifilina
French Pentoxifylline
German Pentoxifyllin
Portuguese Pentoxifilina

Ontology: Trental (C0699487)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D010431
English trental, TRENtal, Trental