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pentoxifylline (Trental)

Tradename: Trental. Indications: 1) treatment of intermittent claudication associated with peripheral vascular disease (PVD) -> a structured exercise program is the treatment of choice & superior to pentoxifylline for PVD 2) treatment of severe alcoholic hepatitis* [6,7] 3) treatment of venous ulceration* * may be useful MediCal: intermittent claudication & over 65 years or diabetic Dosage: 1) 400 mg PO TID 2) 800 mg PO TID used for venous stasis ulcers -> increased incidence of adverse effects (nausea, dizziness) 3) re-evaluate in 2 months & discontinue if no improvement 4) try 400 mg BID if excessive side effects occur Tabs: (controlled-release): 400 mg. Pharmacokinetics: 1) peak levels 1 hour after oral administration 2) 1st pass metabolism in liver 3) two active metabolites a) 5-8 fold higher plasma levels than parent compound b) eliminated in urine (< 4% recovered in feces) 4) elimination 1/2life a) parent compound: 0.4-0.8 hours b) metabolites: 1-1.6 hours 5) elimination prolonged in patients with cirrhosis 6) renal insufficieny can prolong clearance of metabolites Adverse effects: 1) not common (1-10%) - dyspepsia, nausea/vomiting, dizziness, headache 2) uncommon (< 1%) - mild hypotension, angina, agitation, blurred vision, earache 3) other [4] - diarrhea - tremor Drug interactions: - anticoagulants in combination may increase risk of bleeding or increase prothrombin time, but no definitive proof Mechanism of action: 1) improves blood flow by decreasing viscosity 2) enhances tissue oxygenation 3) reduces plasma fibrinogen & increases fibrinolytic activity 4) inhibits platelet aggregation 5) increase erythrocyte flexibility 6) stimulates synthesis & release of prostacyclin 7) antagonizes adenosine receptor [3] 8) diminishes tumor necrosis factor-alpha [3]

General

hematologic agent

Properties

MISC-INFO: elimination route LIVER pregnancy-category C safety in lactation ? 1/2life 0.4-0.8 HOURS

Database Correlations

PUBCHEM cid=4740

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. PDR 1998, pg 1247-48
  3. Navarro et a Am J Kidney Disease 33: 458 1999
  4. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998 - not on National VA formulary
  5. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  6. Journal Watch 21(3):21, 2001 Akriviadis et al, Gastroenterology 119:1637, 2000
  7. Prescriber's Letter 8(3):17 2001
  8. Drug Facts and Comparisons, 1996 editions, Facts and Comparisons, St Louis