Movatterモバイル変換

[0]ホーム
URL:

Jump to content
WikipediaThe Free Encyclopedia
Search

Naftidrofuryl

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
Naftidrofuryl
Clinical data
Trade namesPraxilene, others
Other namesNafronyl; Naftidrofurile; Naftifurine; EU-1806; EU1806; LS-121; LS121
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral[1]
Drug classSerotonin 5-HT2A receptor antagonist;Vasodilator
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability20–78% (in different studies)[1]
Protein binding80%[1]
MetabolismHepatic[1]
Onset of action0.8–1.0 hours (TmaxTooltip time to peak levels)[1]
Eliminationhalf-life1.2–2 hours[1]
Duration of action2–3 hours[1]
Identifiers
  • (RS)-2-(diethylamino)ethyl 3-(1-naphthyl)-2-(tetrahydrofuran-2-ylmethyl)propanoate
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.045.960Edit this at Wikidata
Chemical and physical data
FormulaC24H33NO3
Molar mass383.532 g·mol−1
3D model (JSmol)
  • O=C(OCCN(CC)CC)C(Cc2c1ccccc1ccc2)CC3OCCC3
  • InChI=1S/C24H33NO3/c1-3-25(4-2)14-16-28-24(26)21(18-22-12-8-15-27-22)17-20-11-7-10-19-9-5-6-13-23(19)20/h5-7,9-11,13,21-22H,3-4,8,12,14-18H2,1-2H3 checkY
  • Key:KBAFPSLPKGSANY-UHFFFAOYSA-N checkY
  (verify)

Naftidrofuryl, also known asnafronyl and sold under the brand namePraxilene among others, is aserotonin5-HT2 receptorantagonist which is used as avasodilator in the treatment ofperipheral and cerebral vascular disorders.[1][2][3][4][5] It is takenorally.[1]

Medical uses

[edit]

Naftidrofuryl is used as avasodilator in the treatment ofperipheral and cerebral vascular disorders.[1][2][5] It is also licensed for the treatment ofintermittent claudication due toperipheral arterial disease.[1] Historically, it has been used to treat suddenidiopathic hearing loss and acutetinnitus.[6] Naftidrofuryl may be effective for relieving the pain of musclecramps.[7]

Adverse effects

[edit]

Naftidrofuryl has been associated withnausea,abdominal pain andrash.[8][1] Rarely,hepatitis andliver failure have been reported.[1][8]

Pharmacology

[edit]

Pharmacodynamics

[edit]

Naftidrofuryl acts as aselectiveantagonist of5-HT2 receptors (with action as aninverse agonist of the5-HT2A receptor specifically characterized).[1][5][9][10]

Pharmacokinetics

[edit]

Theoralbioavailability of naftidrofuryl is 20 to 78% in different studies.[1] Itstime to peak levels is 0.8 to 1.0 hours.[1] There is some evidence that naftidrofuryl crosses theblood–brain barrier and penetrates into thecentral nervous system.[11][12] The drug'splasma protein binding is 80%.[1] It ismetabolized in theliver.[1] Theelimination half-life of naftidrofuryl is 1.2 to 2 hours.[1] Its half-life is longer in theelderly than in younger people.[1] The drug'sduration of effects is 2 to 3 hours and closely parallels circulating levels of naftidrofuryl.[1]

History

[edit]

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

Society and culture

[edit]

Names

[edit]

Naftidrofuryl is thegeneric name of the drug and its (INNTooltip International Nonproprietary Name,BANTooltip British Approved Name,DCFTooltip Dénomination Commune Française, andJANTooltip Japanese Accepted Name.[2][3][4][5] It is also known asnaftidrofurile (DCITTooltip Denominazione Comune Italiana) or asnafronyl (USANTooltip United States Adopted Name.[2][3][4][5] Naftidrofuryl is marketed under a variety oftrade 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

[edit]

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

See also

[edit]

References

[edit]
  1. ^abcdefghijklmnopqrstuBarradell LB, Brogden RN (April 1996). "Oral naftidrofuryl. A review of its pharmacology and therapeutic use in the management of peripheral occlusive arterial disease".Drugs & Aging.8 (4):299–322.doi:10.2165/00002512-199608040-00005.PMID 8920176.
  2. ^abcdefIndex Nominum 2000: International Drug Directory. Taylor & Francis. 2000.ISBN 978-3-88763-075-1. Retrieved17 January 2026.
  3. ^abcde"Naftidrofuryl (International database)".Drugs.com. 6 January 2026. Retrieved17 January 2026.
  4. ^abcdeElks J (14 November 2014).The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer.ISBN 978-1-4757-2085-3. Retrieved18 January 2026.
  5. ^abcdeMorton IK, Hall JM (6 December 2012).Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media.ISBN 978-94-011-4439-1. Retrieved18 January 2026.
  6. ^"DER ARZNEIMITTELBRIEF: Infusionstherapie beim idiopathischen Hörsturz? Dextran Dextran Hörsturz Hydroxyethylstärke Pentoxifyllin Pentoxifyllin Procain Taprosten".www.der-arzneimittelbrief.de. Archived fromthe original on 2018-09-20. Retrieved2018-12-13.
  7. ^Katzberg HD, Khan AH, So YT (February 2010)."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.doi:10.1212/WNL.0b013e3181d0ccca.PMID 20177124.
  8. ^abBrayfield A, ed. (14 January 2014)."Naftidrofuryl Oxalate".Martindale: The Complete Drug Reference. Pharmaceutical Press. Retrieved6 August 2014.
  9. ^Lanzer P, Topol EJ (20 December 2013).Pan Vascular Medicine: Integrated Clinical Management. Springer. pp. 1394–.ISBN 978-3-642-56225-9.
  10. ^Aly SA, Hossain M, Bhuiyan MA, Nakamura T, Nagatomo T (August 2009)."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.doi:10.1254/jphs.09124FP.PMID 19672037.
  11. ^Castleden CM (January 1984)."Therapeutic possibilities in patients with senile dementia".Journal of the Royal College of Physicians of London.18 (1):28–31.PMC 5370945.PMID 6323706.
  12. ^Rico AG, Godfrain JC, Benard P, Braun JP, Fontaine L, Belleville L (1974). "[Study of the metabolism of naftidrofuryl using radioactive carbon. Determination by liquid scintillation after administration to rats. Autoradiography of mice]" [Study of the metabolism of naftidrofuryl using radioactive carbon. Determination by liquid scintillation after administration to rats. Autoradiography of mice].Therapie (in French).29 (2): 281–93 passim.PMID 4849813.
Phenylethanolamine derivatives
Alpha blockers
Nicotinic acid and derivatives
Purine derivatives
Ergot alkaloids
Other peripheral vasodilators
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Retrieved from "https://en.wikipedia.org/w/index.php?title=Naftidrofuryl&oldid=1337741842"
Categories:
Hidden categories:
[8]ページ先頭
©2009-2026 Movatter.jp