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Pentoxifylline
Systematic (IUPAC) name
3,7-dimethyl-1-(5-oxohexyl)-3,7-dihydro-1 H-purine-2,6-dione
Identifiers
CAS number 6493-05-6
ATC code C04AD03
PubChem 4740
DrugBank APRD00121
Chemical data
Formula C 13H18N4O3  
Mol. mass 278.31
Pharmacokinetic data
Bioavailability Near 100% for oral dosing
Metabolism Hepatic and via erythrocytes
Half life 0.4 - 0.8 hours (1 - 1.6 hours for active metabolite)
Excretion Mainly urine (<4% feces)
Therapeutic considerations
Pregnancy cat. C(US)
Legal status
Routes Oral
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Pentoxifylline is the International Nonproprietary Name (INN) of a drug sold by Aventis under the brand name Trental. Its chemical name is 1-(5-oxohexyl)-3, 7-dimethylxanthine. Pentoxifylline is a xanthine derivative. Other brand names include Pentox, Pentoxil, and Flexital.

This drug is passed into the breast milk. Animal studies have shown no evidence of teratogenicity at high doses.

Contents

Uses

It is used to treat intermittent claudication resulting from obstructed arteries in the limbs, and vascular dementia.[1]

Pentoxifylline improves blood flow through blood vessels and therefore helps with blood circulation in the arms and legs (e.g. intermittent claudication).

The drug is gaining acceptance for conservative treatment of Peyronie's disease and neuropathic injuries. It also helps prevent strokes, can be used in managing sickle cell disease and improves blood flow to the brain.

Pentoxifylline has also been used to treat nausea and headaches in the mountains (altitude sickness), and has been shown to reduce mortality in acute alcoholic and non-alcoholic steatohepatitis, presumably through its ability to inhibit TNF-alpha.

Pentoxifylline's anti-TNF properties indicates it for treatment of ALD, alcoholic liver disease.

A study demonstrated the possible use of Pentoxifylline administered in conjunction with vitamin E for reducing the extent of fibrotic lesions induced by radiation therapy for breast cancer. [2]

IV or oral pretreatment with Pentoxifylline has been attempted for the treatment of Cytokine Release Syndrome but it does not prevent symptoms in most studies.

Mechanism

Like other methylated xanthine derivatives, pentoxifylline is both a

  1. competitive nonselective phosphodiesterase inhibitor [3] which raises intracellular cAMP, activates PKA, inhibits TNF-alpha [4] [5] and leukotriene [6] synthesis, and reduces inflammation and innate immunity [6] and
  2. nonselective adenosine receptor antagonist [7].

In addition, pentoxifylline increases red blood cell deformability, reduces blood viscosity and decreases the potential for platelet aggregation and thrombus formation.[8]

Drug interaction

Co-administration of pentoxifylline and sodium thiopental causes death by acute pulmonary oedema in rats.[9]

Alternative brand names

  • Pentoxil (Upsher Smith)
  • Pentoxin (Ratiopharm)
  • Artal (Leiras)
  • Vasonit (Lannacher)

References

  1. ^ (1996) European Pentoxifylline Multi-Infarct Dementia Study. Eur Neurol. 36(5):315-21. PMID 8864715
  2. ^ Delanian S, Porcher R, Rudant J, et al.: Kinetics of response to long-term treatment combining pentoxifylline and tocopherol in patients with superficial radiation-induced fibrosis. J Clin Oncol 23: 8570-8579, 2005
  3. ^ Essayan DM. (2001). "Cyclic nucleotide phosphodiesterases.". J Allergy Clin Immunol. 108 (5): 671-80. doi:10.1067/mai.2001.119555. PMID 11692087.  
  4. ^ Deree J, Martins JO, Melbostad H, Loomis WH, Coimbra R. (2008). "Insights into the regulation of TNF-alpha production in human mononuclear cells: the effects of non-specific phosphodiesterase inhibition.". Clinics (Sao Paulo). 63 (3): 321-8. doi:10.1590/S1807-59322008000300006. PMID 18568240.  
  5. ^ 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. PMID 9927365. http://ajrccm.atsjournals.org/cgi/pmidlookup?view=long&pmid=9927365.  
  6. ^ 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. PMID 15634873. http://www.jimmunol.org/cgi/content/full/174/2/589.  
  7. ^ Daly JW, Jacobson KA, Ukena D. (1987). "Adenosine receptors: development of selective agonists and antagonists.". Prog Clin Biol Res. 230 (1):  :41-63. PMID 3588607.  
  8. ^ Ward A and Clissold SP, 1987. "Pentoxifylline. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic efficacy." Drugs, 34(1):50-97. PMID:3308412.
  9. ^ Pereda J, Gómez-Cambronero L, Alberola A, Fabregat G, Cerdá M, Escobar J, Sabater L, García-de-la-Asunción J, Viña J, Sastre J. Department of Physiology, School of Medicine, University of Valencia, Valencia, Spain. Br J Pharmacol. 2006 Oct;149(4):450-5. Epub 2006 Sep 4.PMID: 16953192.

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