|Trade names||Many names worldwide|
|Synonyms||oxpentifylline (former AAN)|
|Metabolism||Hepatic and via erythrocytes|
|Elimination half-life||0.4–0.8 hours (1–1.6 hours for active metabolite)|
|Excretion||Urine (95%), faeces (<4%)|
|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||278.31 g/mol g·mol−1|
|3D model (JSmol)|
Pentoxifylline, also known as oxpentifylline, 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.
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.[needs update] This is its only FDA, MHRA and TGA-labelled indication. However, pentoxifylline is also recommended for off-label use as an adjunct to compression bandaging for the treatment of chronic venous leg ulcers by the Scottish Intercollegiate Guidelines Network) (SIGN)  as this has been shown to improve healing rates.
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.
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 blood clot formation. Pentoxifylline is also an antagonist at adenosine 2 receptors.
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 hearing loss. Human studies have been conducted for Peyronie's disease.
In a Cochrane systematic review on the use of Pentoxifylline for intermittent claudication in 2015, the following was concluded "The quality of included studies was generally low, and very large variability between studies was noted in reported findings including duration of trials, doses of pentoxifylline and distances participants could walk at the start of trials. Most included studies did not report on randomisation techniques or how treatment allocation was concealed, did not provide adequate information to permit judgement of selective reporting and did not report blinding of outcome assessors. Given all these factors, the role of pentoxifylline in intermittent claudication remains uncertain, although this medication was generally well tolerated by participants".
- Lisofylline, an active metabolite of pentoxifylline
- Cilostazol, a PDE-3 inhibitor with better evidence for intermittent claudication on the Cochrane review cited above.
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- Latoni, J.; Shivapuja, B.; Seidman, M. D.; Quirk, W. S. (May 1996). "Pentoxifylline maintains cochlear microcirculation and attenuates temporary threshold shifts following acoustic overstimulation". Acta Oto-Laryngologica. 116 (3): 388–94. doi:10.3109/00016489609137862. PMID 8790737.
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- Delanian, S., Chatel, C., Porcher, R., Depondt, J. and Lefaix, J.L., 2011. Complete restoration of refractory mandibular osteoradionecrosis by prolonged treatment with a pentoxifylline-tocopherol-clodronate combination (PENTOCLO): a phase II trial. International Journal of Radiation Oncology* Biology* Physics, 80(3), pp.832-839.
- Patel, V., Gadiwalla, Y., Sassoon, I., Sproat, C., Kwok, J. and McGurk, M., 2016. Prophylactic use of pentoxifylline and tocopherol in patients who require dental extractions after radiotherapy for cancer of the head and neck. British Journal of Oral and Maxillofacial Surgery, 54(5), pp.547-550.
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