Trade names Many names worldwide MedlinePlus a685027 | AHFS/Drugs.com Monograph License data US FDA: Pentoxifylline | |
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Pronunciation /ˌpɛntɒkˈsɪfᵻliːn, -ɪn/ Pregnancycategory AU: B1US: C (Risk not ruled out) | ||
Pentoxifylline (INN, BAN, USAN) or oxpentifylline (AAN) is a xanthine derivative used as a drug to treat muscle pain in people with peripheral artery disease. It is generic and sold under many brand names worldwide.
Contents
Medical uses
Its primary use in medicine is to reduce pain, cramping, numbness, or weakness in the arms or legs which occurs due to intermittent claudication, a form of muscle pain resulting from peripheral artery diseases. This is its only FDA, MHRA and TGA-labelled indication.
Adverse effects
Common side effects are belching, bloating, stomach discomfort or upset, nausea, vomiting, indigestion, dizziness, and flushing. Uncommon and rare side effects include angina, palpitations, hypersensitivity, itchiness, rash, hives, bleeding, hallucinations, arrhythmias, and aseptic meningitis.
Contraindications include intolerance to pentoxifylline or other xanthine derivatives, recent retinal or cerebral haemorrhage, and risk factors for haemorrhage.
Co-administration of pentoxifylline and sodium thiopental may cause death by acute pulmonary edema in rats.
Mechanism
Like other methylated xanthine derivatives, pentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity. In addition, pentoxifylline improves red blood cell deformability (known as a haemorrheologic effect), reduces blood viscosity and decreases the potential for platelet aggregation and thrombus formation. Pentoxifylline is also an antagonist at adenosine 2 receptors.
Effect on seizure
In a study, the effect of pentoxifylline as a phosphodiestrase inhibitor was study on the pentylenetetrazol-induced seziure in the wild-type mice. Pentoxifylline in that study reduced the anti-convulsive effect of H-89 and reduced the seizure threshold.
Research
There is some evidence that pentoxifyllinenon can lower the levels of some biomarkers in non-alcoholic steatohepatitis but evidence is insufficient to determine if the drug is safe and effective for this use. Animal studies have been conducted exploring the use of pentoxifylline for erectile dysfunction and also human studies on Peyronie's disease.