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Contents

   



(Top)
 


1 Pharmacokinetics  





2 Mechanism of action  





3 Interactions  





4 Brand names  





5 References  














Loxoprofen






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Loxoprofen
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration
Oral, transdermal
ATC code
Legal status
Legal status
  • JP: Class 1 OTC
    BR: Red Stripe (Rx only)
Pharmacokinetic data
Protein binding97%
MetabolismLiver glucuronidation
Elimination half-life75 minutes
ExcretionKidney
Identifiers
  • (RS)-2-{4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid

CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H18O3
Molar mass246.306 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  • O=C2C(Cc1ccc(cc1)C(C(=O)O)C)CCC2

  • InChI=1S/C15H18O3/c1-10(15(17)18)12-7-5-11(6-8-12)9-13-3-2-4-14(13)16/h5-8,10,13H,2-4,9H2,1H3,(H,17,18) checkY

  • Key:YMBXTVYHTMGZDW-UHFFFAOYSA-N checkY

 ☒NcheckY (what is this?)  (verify)

Loxoprofen is a nonsteroidal anti-inflammatory drug (NSAID) in the propionic acid derivatives group, which also includes ibuprofen and naproxen among others. It is available in some countries for oral administration. A transdermal preparation was approved for sale in Japan in January 2006;[1] medicated tape and gel formulations followed in 2008 and 2010.

It was patented in 1977 and approved for medical use in 1986.[2]

Pharmacokinetics[edit]

Loxoprofen is a prodrug. It is quickly converted to its active trans-alcohol metabolite following oral administration, and reaches its peak plasma concentration within 30 to 50 minutes.

Mechanism of action[edit]

As most NSAIDs, loxoprofen is a non-selective cyclooxygenase inhibitor, and works by reducing the synthesis of prostaglandins from arachidonic acid.

Interactions[edit]

Loxoprofen should not be administered at the same time as second-generation quinolone antibiotics such as ciprofloxacin and norfloxacin, as it increases their inhibition of GABA and this may cause seizures.[3] It may also increase the plasma concentration of warfarin, methotrexate, sulfonylurea derivatives and lithium salts, so care should be taken when loxoprofen is administered to patients taking any of these drugs.[3]

Brand names[edit]

It is marketed in Brazil, Mexico, China and JapanbySankyo as its sodium salt, loxoprofen sodium, under the trade name Loxonin; in Argentina as Oxeno; in India as Loxomac; in Thailand as Japrolox; and in Saudi Arabia as Roxonin and Roxonin Tape.

Ageneric drug is marketed in Brazil by Aché as Oxotron. In Japan, two fixed dose combinations are available: Loxonin S Plus, with magnesium oxide, and Loxonin S Premium, with apronal, caffeine, and aluminium magnesium silicate.

References[edit]

  1. ^ Daiichi Sankyo Co. (January 24, 2006). "Percutaneous Absorption-Type Analgesic and Anti-inflammatory Drug Loxonin Poultice 100mg Receives Approval for Manufacture" (Press release). Doctor's Guide Global Edition. Retrieved 2007-04-19.
  • ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 521. ISBN 9783527607495.
  • ^ a b "LOXONIN - Bula do Medicamento [Label Information]" (in Portuguese). Centralx. 2007. Retrieved 2007-04-19.

  • Retrieved from "https://en.wikipedia.org/w/index.php?title=Loxoprofen&oldid=1234029745"

    Categories: 
    Nonsteroidal anti-inflammatory drugs
    Prodrugs
    Cycloalkanones
    Propionic acids
    Daiichi Sankyo
    Cyclopentanes
    Hidden categories: 
    CS1 Portuguese-language sources (pt)
    Articles with short description
    Short description is different from Wikidata
    Drugs with non-standard legal status
    Articles with changed CASNo identifier
    Articles with changed EBI identifier
    Drugboxes which contain changes to verified fields
    Drugboxes which contain changes to watched fields
    Commons category link from Wikidata
     



    This page was last edited on 12 July 2024, at 06:22 (UTC).

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