|Pronunciation||/ - /,|
|Trade names||Pentoxil, Trental, others|
|Other names||Oxpentifylline (former AAN)|
|Metabolism||Liver and via erythrocytes|
|Elimination half-life||0.4–0.8 hours (1–1.6 hours for active metabolite)|
|Excretion||Urine (95%), faeces (<4%)|
|Chemical and physical data|
|Molar mass||278.312 g·mol−1|
|3D model (JSmol)|
Pentoxifylline, also known as oxpentifylline, is a medication used to treat peripheral artery disease that results in pain with walking and venous leg ulcers. There is tentative evidence that it may improve peoples ability to walk. Use is not recommended in the United Kingdom. It is taken by mouth.
Common side effects include nausea, dizziness, and heart burn. Other side effects may include bleeding. It is a xanthine derivative and is believed to work by increasing red blood cell flexibility.
Pentoxifylline was approved for medical use in the United States in 1984. It is available as a generic medication. In the United Kingdom it costs the NHS about £19 a month as of 2021. This amount in the United States is about 36 USD.
Pentoxifylline has been tested for use in sarcoidosis as an alternative or compliment to prednisone and other steroids, as the drug can inhibit excess levels of TNF-a, which is associated with granuloma formation.
It is taken at a dose of 400 mg two to three times per day.
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.
Society and culture
There is some evidence that pentoxifylline 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".[needs update]
- 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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- 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.
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