API: Pentoxifylline

What Is Pentoxifylline and How Does It Work?

Pentoxifylline is a methylated xanthine derivative, and, as such, is a competitive nonselective phosphodiesterase inhibitor with significant vasodilatation properties.1 Although the exact mechanism of action for this drug is not well understood, pentoxifylline belongs to a group of drugs that enhance oxygenation of and blood flow in peripheral tissues. The drug relaxes certain smooth muscles, such as those in peripheral blood vessels, resulting in vasodilatation. Pentoxifylline also improves the flexibility of red blood cells and promotes platelet deaggregation, thereby decreasing blood viscosity.2 The drug is used to treat vascular disorders and other conditions associated with reduced blood flow.

For more information, including a MSDS sheet, please see PNA’s Pentoxifylline page.

Approved Indications

  • Vascular disorders: Pentoxifylline is approved for treating reduced blood flow in patients with chronic occlusive peripheral vascular disorders in the extremities. Symptoms that may be eased include intermittent claudication and trophic ulcers.
  • Other Uses: Pentoxifylline is sometimes prescribed off-label, alone, or as an adjunct, for a number of conditions, such as peripheral neuropathy, hemorrhagic fever, and venous ulcer healing.

Side Effects and Drug Interactions

Common side effects in patients taking Pentoxifylline include3:

  • Bloating
  • Belching
  • Indigestion
  • Gas
  • Upset stomach
  • Dizziness or flushing
  • Nausea and vomiting

Patients who suffer from severity of these common side effects should contact their pharmacist or physician right away. Patients who experience severe allergic reactions (itchy rash or hives, difficulty breathing, tightness in the chest, swelling of the mouth, face, lips, or tongue), blurred vision or changes in vision, chest pain or irregular heartbeat, fainting or severe dizziness, lightheadedness, stomach pain, unusual bruising or bleeding, fatigue, or jaundice should inform their physician immediately.

Patients who are allergic to pentoxifylline should not take this drug. This drug should not be given to patients with recent cerebral and/or retinal hemorrhage or to patients who are intolerant to ketorolac or other methylxanthines, such as caffeine, theophylline, or theobromine.4 Patients who take this drug may experience bleeding and/or prolonged prothrombin time—the drug should be used cautiously in patients taking warfarin, or who have other risk factors complicated by hemorrhage.

Patients who are breastfeeding should not take pentoxifylline as the drug is excreted in breast milk.

Latest News and Research

There has long been a controversy over the use of pentoxifylline for the treatment of alcoholic hepatitis, a liver disease that often does not have a good outcome. A review of the literature in six studies covering 884 patients shows that while pentoxifylline is better than placebo for treatment of alcoholic hepatitis, corticosteroid remain the preferred treatment.5 However, for patients who cannot take corticosteroids, pentoxifylline offers a suitable alternative.

Pentoxifylline is also used experimentally to protect organs from ischemic injury and reperfusion.6 Animal studies of the bowel, liver, and even the brain show that pentoxifylline may protect the organ, or at least attenuate the effects of ischemia in animal models.7 The results are promising for getting approval for the use of the drug to treat and pre-treat patients for ischemia and resulting effects across different organs.

Pentoxifylline may also have activity against progressive renal loss due to elevated levels of albuminuria in patients suffering from diabetic or hypertensive nephropathy or another primary renal disease.8

Buying Guide

PNA is a recommended bulk supplier of Pentoxifylline and other APIs. You can learn more about Pentoxifylline here.

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Resources

Show 8 footnotes

  1. “Effects of the non-selective phosphodiesterase inhibitor Pentoxifylline on regional cerebral blood flow and large arteries in healthy subjects,” November 2000, http://www.ncbi.nlm.nih.gov/pubmed/11136348
  2. “Trental,” 2016, http://www.rxlist.com/trental-drug/clinical-pharmacology.htm
  3. “Pentoxifylline,” January 4, 2016, http://www.drugs.com/cdi/pentoxifylline.html
  4. “trental (pentoxifylline)  tablet, film coated,” October, 2007, https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=6084
  5. “Systematic review: pentoxifylline for the treatment of severe alcoholic hepatitis,” March 13, 2013, http://onlinelibrary.wiley.com/doi/10.1111/apt.12279/full
  6. “Pentoxifylline protects the small intestine after severe ischemia and reperfusion,” November 2013, http://europepmc.org/abstract/med/23767943
  7. “Pentoxifylline Attenuates Hypoxic-Ischemic Brain Injury in Immature Rats,” 2004, http://www.nature.com/pr/journal/v47/n1/abs/pr200014a.html
  8. “Albuminuria Is an Appropriate Therapeutic Target in Patients with CKD: The Pro View,” 2015, http://cjasn.asnjournals.org/content/early/2015/04/17/CJN.11511114.short