Pentoxifylline
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| Systematic (IUPAC) name | |
|---|---|
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3,7-Dimethyl-1-(5-oxohexyl)-3,7-dihydro-1H-purine-2,6-dione
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| Clinical data | |
| Trade names | Many names worldwide[1] |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a685027 |
| Licence data | US FDA:link |
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| Legal status | |
| Routes of administration |
Oral |
| Pharmacokinetic data | |
| Bioavailability | 10-30%[2] |
| Metabolism | Hepatic and via erythrocytes |
| Biological half-life | 0.4-0.8 hours (1-1.6 hours for active metabolite)[2] |
| Excretion | Urine (95%), faeces (<4%)[2] |
| Identifiers | |
| CAS Number | 6493-05-6  |
| ATC code | C04AD03 (WHO) |
| PubChem | CID: 4740 |
| IUPHAR/BPS | 7095 |
| DrugBank | DB00806 |
| ChemSpider | 4578 |
| UNII | SD6QCT3TSU |
| KEGG | D00501 |
| ChEMBL | CHEMBL628 |
| Chemical data | |
| Formula | C13H18N4O3 |
| Molecular mass | 278.31 g/mol |
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Pentoxifylline (INN, BAN, USAN) or oxpentifylline (AAN)[3] is a drug used to treat muscle pain in people with peripheral artery disease.[4] It is generic and sold under many brand names worldwide.[1]
Contents
Medical uses
Its primary use in medicine is in treating the symptoms of muscle pain resulting from peripheral artery disease.[4] This is its only FDA, MHRA and TGA-labelled indication.[3][5][6]
Adverse effects
Dizziness, headache, nausea, vomiting, indigestion and flushing are common side effects. Uncommon and rare side effects include angina, palpitations, hypersensitivity, itchiness, rash, hives, bleeding, hallucinations, arrhythmias, and aseptic meningitis.[2][3][5][6]
Contraindications include intolerance to pentoxifylline or other xanthine derivatives, recent retinal or cerebral haemorrhage, and risk factors for haemorrhage.[2]
Co-administration of pentoxifylline and sodium thiopental may cause death by acute pulmonary edema in rats.[7]
Mechanism
Like other methylated xanthine derivatives, pentoxifylline is a competitive nonselective phosphodiesterase inhibitor[8] which raises intracellular cAMP, activates PKA, inhibits TNF[9][10] and leukotriene [11] synthesis, and reduces inflammation and innate immunity.[11] 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.[12] Pentoxifylline is also an antagonist at adenosine 2 receptors.[13]
Effect of Pentoxifylline 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.[14]
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.[15] Animal studies have been conducted exploring the use of pentoxifylline for erectile dysfunction and Peyronie's disease.[16][17]
See also
- Lisofylline, an active metabolite of pentoxifylline
- Propentofylline
References
- ↑ 1.0 1.1 Drugs.com drugs.com international listings for Pentoxifylline. Page accessed Feb 1, 206
- ↑ 2.0 2.1 2.2 2.3 2.4 Lua error in package.lua at line 80: module 'strict' not found.
- ↑ 3.0 3.1 3.2 Lua error in package.lua at line 80: module 'strict' not found.
- ↑ 4.0 4.1 Lua error in package.lua at line 80: module 'strict' not found.
- ↑ 5.0 5.1 Lua error in package.lua at line 80: module 'strict' not found.
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- ↑ El-Sakka AI, "Reversion of penile fibrosis: Current information and a new horizon", Arab Journal of Urology, 2011 Mar;9(1):49–55. PMID 26579268 PMC4149188
- ↑ Anele UA, Morrison BF & Burnett AL, "Molecular pathophysiology of priapism: Emerging targets", Current Drug Targets, 2015;16(5):474–83. PMID 25392014.
