Chemistry:Naftidrofuryl

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Naftidrofuryl, also known as nafronyl and sold under the brand name Praxilene among others, is a serotonin 5-HT2 receptor antagonist which is used as a vasodilator in the treatment of peripheral and cerebral vascular disorders.[1][2][3][4][5] It is taken orally.[1]

Medical uses

Naftidrofuryl is used as a vasodilator in the treatment of peripheral and cerebral vascular disorders.[1][2][5] It is also licensed for the treatment of intermittent claudication due to peripheral arterial disease.[1] Historically, it has been used to treat sudden idiopathic hearing loss and acute tinnitus.[6] Naftidrofuryl may be effective for relieving the pain of muscle cramps.[7]

Adverse effects

Naftidrofuryl has been associated with nausea, abdominal pain and rash.[8][1] Rarely, hepatitis and liver failure have been reported.[1][8]

Pharmacology

Pharmacodynamics

Naftidrofuryl acts as a selective antagonist of 5-HT2 receptors (with action as an inverse agonist of the 5-HT2A receptor specifically characterized).[1][5][9][5][10]

Pharmacokinetics

The oral bioavailability of naftidrofuryl is 20 to 78% in different studies.[1] Its time to peak levels is 0.8 to 1.0 hours.[1] There is some evidence that naftidrofuryl crosses the blood–brain barrier and penetrates into the central nervous system.[11][12] The drug's plasma protein binding is 80%.[1] It is metabolized in the liver.[1] The elimination half-life of naftidrofuryl is 1.2 to 2 hours.[1] Its half-life is longer in the elderly than in younger people.[1] The drug's duration of effects is 2 to 3 hours and closely parallels circulating levels of naftidrofuryl.[1]

History

Naftidrofuryl was first described in the scientific literature by at least 1966.[4]

Society and culture

Names

Naftidrofuryl is the generic name of the drug and its (INN, BAN, DCF, and JAN.[2][3][4][5] It is also known as naftidrofurile (DCIT) or as nafronyl (USAN.[2][3][4][5] Naftidrofuryl is marketed under a variety of trade names, including Artocoron, Azunaftil, Di-Actane, Dusodril, Enelbin, Frilix, Gevatran, Iridus, Iridux, Luctor, Nafti, Naftilong, Naftodril, Nafoxal, Praxilene, Sodipryl Retard, Stimlor, and Vascuprax, among others.[2][3][4]

Availability

Naftidrofuryl is marketed and used widely throughout the world.[2][3]

See also

References

  1. ↑ 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 1.11 1.12 1.13 "Oral naftidrofuryl. A review of its pharmacology and therapeutic use in the management of peripheral occlusive arterial disease". Drugs & Aging 8 (4): 299–322. April 1996. doi:10.2165/00002512-199608040-00005. PMID 8920176. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 Index Nominum 2000: International Drug Directory. Taylor & Francis. 2000. ISBN 978-3-88763-075-1. https://books.google.com/books?id=5GpcTQD_L2oC&pg=PA712. Retrieved 17 January 2026. 
  3. ↑ 3.0 3.1 3.2 3.3 3.4 "Naftidrofuryl (International database)". 6 January 2026. https://www.drugs.com/international/naftidrofuryl.html. 
  4. ↑ 4.0 4.1 4.2 4.3 4.4 The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. 14 November 2014. ISBN 978-1-4757-2085-3. https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA849. Retrieved 18 January 2026. 
  5. ↑ 5.0 5.1 5.2 5.3 5.4 5.5 Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. 6 December 2012. ISBN 978-94-011-4439-1. https://books.google.com/books?id=tsjrCAAAQBAJ&pg=PA189. Retrieved 18 January 2026. 
  6. ↑ "DER ARZNEIMITTELBRIEF: Infusionstherapie beim idiopathischen Hörsturz? Dextran Dextran Hörsturz Hydroxyethylstärke Pentoxifyllin Pentoxifyllin Procain Taprosten". https://www.der-arzneimittelbrief.de/Jahrgang2004/Ausgabe12Seite89.htm. 
  7. ↑ "Assessment: symptomatic treatment for muscle cramps (an evidence-based review): report of the therapeutics and technology assessment subcommittee of the American academy of neurology". Neurology 74 (8): 691–696. February 2010. doi:10.1212/WNL.0b013e3181d0ccca. PMID 20177124. 
  8. ↑ 8.0 8.1 "Naftidrofuryl Oxalate". Martindale: The Complete Drug Reference. Pharmaceutical Press. 14 January 2014. http://www.medicinescomplete.com/mc/martindale/current/9256-a.htm. 
  9. ↑ Pan Vascular Medicine: Integrated Clinical Management. Springer. 20 December 2013. pp. 1394–. ISBN 978-3-642-56225-9. https://books.google.com/books?id=B8LsCAAAQBAJ&pg=PA1394. 
  10. ↑ "Assessment of binding affinity to 5-hydroxytryptamine 2A (5-HT2A) receptor and inverse agonist activity of naftidrofuryl: comparison with those of sarpogrelate". Journal of Pharmacological Sciences 110 (4): 445–450. August 2009. doi:10.1254/jphs.09124FP. PMID 19672037. 
  11. ↑ "Therapeutic possibilities in patients with senile dementia". Journal of the Royal College of Physicians of London 18 (1): 28–31. January 1984. PMID 6323706. 
  12. ↑ "[Study of the metabolism of naftidrofuryl using radioactive carbon. Determination by liquid scintillation after administration to rats. Autoradiography of mice]" (in French). Therapie 29 (2): 281–93 passim. 1974. PMID 4849813. 



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