Pentoxifylline

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Indications :

  • Raynaud’s phenomenon: 400 mg three to four times daily.
  • Livedoid vasculopathy.
  • Necrobiosis lipoidica: 400 mg twice daily.
  • Psoriasis.
  • Pemphigus vulgaris: 400 mg pentoxifylline + 500 mg sulfasalazine three times daily as adjunctive therapy.
  • Behçet disease and recuurent aphthosis.
  • Venous insuffciency with ulcers: 400 mg 3 times daily.
  • Cutaneous polyarteritis nodosa.
  • Schamberg’s disease.
  • Cutaneous and mucocutaneous leishmaniasis : djuvant to pentavalent antimony.
  • Pain and pruritus associated with giant keloids.
  • Renal pruritus: 600 mg iv
  • Pruritus in HIV-infected patients.
  • Peyronie’s disease.
  • Radiation induced fibrosis and burns.
  • Lipodermatosclerosis.

Dosage

  • Usual dose : 400 mg 3–4 times daily for 2–4 months to obtain the maximal therapeutic effect.
  • It may take up to 2–4 months to obtain the maximal therapeutic beneft from pentoxifylline.

Mechanism of action

  • Immune modulation
    • Pentoxifylline increases erythrocyte and leukocyte deformability.
    • Decreases endothelial leukocyte adhesion.
    • Decreases leukocyte responsiveness to interleukin 1 (IL-1) and TNF.
    • Inhibits T and B lymphocyte activation.
    • Decreases natural killer cell activity.
    • Inhibits neutrophil adhesion and activation.
  • Anti-fibrinolytic
    • Pentoxifylline increases fibroblast collagenases and decreases the production of collagen, fibronectin and glycosaminoglycan.
  • Hemorheological effects
    • It reduces platelet aggregation and activation.
    • It increases red blood cell deformability and decreased blood viscosity.
  • Anti-TNF-α effects
    • Inhibitor of tumor necrosis factor-α.
  • Other
    • It is a non-selective inhibitor of cyclic-3’, 5’-phospho-diesterase (PDE), leading to a broad-spectrum effect against cell proliferation and inflammation.

Monitoring

Baseline

  • Check if allergic to caffeine containing products (coffee, tea, colas), pentoxifylline, theobromine, theophylline or any other drugs.
  • Ask about anticoagulants (“blood thinners”) such as warfarin (Coumadin) and vitamins.
  • Ask about Kidney disease.
  • Ask if pt is Pregnant, planning pregnancy or lactating.
  • Any surgery in the near future.

Follow Up

  • PERIODICALLY: blood pressure monitoring.

Side effects

  • Used with caution in patients with severe cardiac disease.
  • Nausea, gastrointestinal disturbances.
  • Dizziness, and headache.

Contraindications

  • Hypersensitivity to pentoxifylline or xanthine derivatives.
  • Recent retinal or cerebral hemorrhage.

Interactions

  • There may be an interaction between pentoxifylline and any of the following:
    • Antidiabetes medications (e.g., glyburide, insulin, metformin).
    • Blood pressure reducing medications (e.g., metoprolol, ramipril).
    • Cimetidine.
    • Ciprofloxacin.
    • Erythromycin.
    • Medications that affect blood clotting (e.g., clopidogrel, heparin, warfarin).
    • Sympathomimetic medications (e.g., pseudoephedrine).
    • Theophylline.

Pregnancy & Lactation

  • Pregnancy category: C.
  • Lactation: Drug excreted in breast milk; discontinue therapy, or do not nurse.

Precautions

  • Use caution with risk factors for hemorrhage.
  • Discontinue at first sign of anaphylaxis.
  • Use with caution in renal impairment; exposure to pentoxifylline and/or active metabolites may increase; significance unknown.
  • Use with caution in the elderly due to potential for renal impairment.
  • Use with caution in hepatic impairment; exposure to pentoxifylline and/or active metabolites may increase; significance unknown.
  • Advice to avoid driving a car or operating machinery.

Drug Info

  • The safety and effectiveness of using this medication have not been established for children below the age of 18 years.


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