Pentoxifylline

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Pentoxifylline
Pentoxifylline2DCSD.svg
Pentoxifylline xtal 2005 ball-and-stick.png
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
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
Molar mass 278.31 g/mol
  (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[edit]

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[edit]

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[edit]

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]

Research[edit]

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.[14]

See also[edit]

References[edit]

  1. ^ a b Drugs.com drugs.com international listings for Pentoxifylline. Page accessed Feb 1, 206
  2. ^ a b c d e "Trental, Pentoxil (pentoxifylline) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 3 February 2014. 
  3. ^ a b c "PRODUCT INFORMATION TRENTAL® 400" (PDF). TGA eBusiness Services. sanofi-aventis australia pty limited. 25 March 2010. Retrieved 3 February 2014. 
  4. ^ a b Salhiyyah, Kareem; Senanayake, Eshan; Abdel-Hadi, Mohammed; Booth, Andrew; Michaels, Jonathan A (Jan 18, 2012). Salhiyyah, Kareem, ed. "Pentoxifylline for intermittent claudication". Cochrane Database Syst Rev 1 (1): CD005262. doi:10.1002/14651858.CD005262.pub2. PMID 22258961. 
  5. ^ a b "PENTOXIFYLLINE tablet, extended release [Apotex Corp.]". DailyMed. Apotex Corp. February 2013. Retrieved 3 February 2014. 
  6. ^ a b "Trental 400 - Summary of Product Characteristics (SPC)". electronic Medicines Compendium. Sanofi. 10 October 2013. Retrieved 3 February 2014. 
  7. ^ Pereda, J; Gómez-Cambronero, L; Alberola, A; Fabregat, G; Cerdá, M; Escobar, J; Sabater, L; García-De-La-Asunción, J; Viña, J; Sastre, J (2006). "Co-administration of pentoxifylline and thiopental causes death by acute pulmonary oedema in rats". British Journal of Pharmacology 149 (4): 450–5. doi:10.1038/sj.bjp.0706871. PMC 1978439. PMID 16953192. 
  8. ^ Essayan DM. (2001). "Cyclic nucleotide phosphodiesterases". J Allergy Clin Immunol. 108 (5): 671–80. doi:10.1067/mai.2001.119555. PMID 11692087. 
  9. ^ Deree J, Martins JO, Melbostad H, Loomis WH, Coimbra R. (2008). "Insights into the Regulation of TNF-α Production in Human Mononuclear Cells: The Effects of Non-Specific Phosphodiesterase Inhibition". Clinics (Sao Paulo). 63 (3): 321–8. doi:10.1590/S1807-59322008000300006. PMC 2664230. PMID 18568240. 
  10. ^ Marques LJ, Zheng L, Poulakis N, Guzman J, Costabel U (February 1999). "Pentoxifylline inhibits TNF-alpha production from human alveolar macrophages". Am. J. Respir. Crit. Care Med. 159 (2): 508–11. doi:10.1164/ajrccm.159.2.9804085. PMID 9927365. 
  11. ^ a b Peters-Golden M, Canetti C, Mancuso P, Coffey MJ. (2005). "Leukotrienes: underappreciated mediators of innate immune responses". J Immunol. 174 (2): 589–94. doi:10.4049/jimmunol.174.2.589. PMID 15634873. 
  12. ^ Ward, A; Clissold, SP (1987). "Pentoxifylline. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic efficacy". Drugs 34 (1): 50–97. doi:10.2165/00003495-198734010-00003. PMID 3308412. 
  13. ^ Rodríguez-Morán M, Guerrero-Romero F (February 2008). "Efficacy of pentoxifylline in the management of microalbuminuria in patients with diabetes". Curr Diabetes Rev 4 (1): 55–62. doi:10.2174/157339908783502343. PMID 18220696. 
  14. ^ Li, W; Zheng, L; Sheng, C; Cheng, X; Qing, L; Qu, S (April 2011). "Systematic review on the treatment of pentoxifylline in patients with non-alcoholic fatty liver disease." (PDF). Lipids in health and disease 10: 49. doi:10.1186/1476-511X-10-49. PMC 3088890. PMID 21477300. 

External links[edit]