Pentoxifylline

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Pentoxifylline
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Systematic (IUPAC) name
3,7-Dimethyl-1-(5-oxohexyl)-3,7-dihydro-1H-purine-2,6-dione
Clinical data
Trade names Many names worldwide[1]
AHFS/Drugs.com monograph
MedlinePlus a685027
Licence data US FDA:link
Pregnancy
category
  • AU: B1
  • US: C (Risk not ruled out)
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 YesY
ATC code C04AD03 (WHO)
PubChem CID: 4740
IUPHAR/BPS 7095
DrugBank DB00806 YesY
ChemSpider 4578 YesY
UNII SD6QCT3TSU YesY
KEGG D00501 YesY
ChEMBL CHEMBL628 YesY
Chemical data
Formula C13H18N4O3
Molecular mass 278.31 g/mol
  • O=C2N(c1ncn(c1C(=O)N2CCCCC(=O)C)C)C
  • InChI=1S/C13H18N4O3/c1-9(18)6-4-5-7-17-12(19)10-11(14-8-15(10)2)16(3)13(17)20/h8H,4-7H2,1-3H3 YesY
  • Key:BYPFEZZEUUWMEJ-UHFFFAOYSA-N YesY
  (verify)

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]

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

References

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External links

  1. ↑ 1.0 1.1 Drugs.com drugs.com international listings for Pentoxifylline. Page accessed Feb 1, 206
  2. ↑ 2.0 2.1 2.2 2.3 2.4 Lua error in package.lua at line 80: module 'strict' not found.
  3. ↑ 3.0 3.1 3.2 Lua error in package.lua at line 80: module 'strict' not found.
  4. ↑ 4.0 4.1 Lua error in package.lua at line 80: module 'strict' not found.
  5. ↑ 5.0 5.1 Lua error in package.lua at line 80: module 'strict' not found.
  6. ↑ 6.0 6.1 Lua error in package.lua at line 80: module 'strict' not found.
  7. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  8. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  9. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  10. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  11. ↑ 11.0 11.1 Lua error in package.lua at line 80: module 'strict' not found.
  12. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  13. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  14. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  15. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  16. ↑ 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
  17. ↑ Anele UA, Morrison BF & Burnett AL, "Molecular pathophysiology of priapism: Emerging targets", Current Drug Targets, 2015;16(5):474–83. PMID 25392014.
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