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Loxoprofen
Systematic (IUPAC) name
2-{4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid
Identifiers
CAS number 68767-14-6
ATC code M01AE
PubChem 3965
Chemical data
Formula C 15H18O3  
Mol. mass 246.302 g/mol
304.314 g/mol (sodium salt)
Pharmacokinetic data
Bioavailability  ?
Protein binding 97%
Metabolism Hepatic glucuronidation
Half life 75 minutes
Excretion Renal
Therapeutic considerations
Pregnancy cat.  ?
Legal status Red Stripe (Brazil)
Routes Oral, transdermal

Loxoprofen (INN) is a non-steroidal anti-inflammatory drug in the propionic acid derivatives group, which also includes ibuprofen and naproxen among others. It is marketed in Brazil, Mexico and Japan by Sankyo as its sodium salt, loxoprofen sodium, under the trade name Loxonin,Argentina as Oxeno and in India as Loxomac . It is available in these countries for oral administration, and a transdermal preparation was approved for sale in Japan on January 2006.[1]

Contents

Pharmacokinetics

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

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

Interactions

Loxoprofen should not be administered concomitantly with second-generation quinolone antibiotics such as ciprofloxacin and norfloxacin, as it increases their inhibition of GABA and this may cause seizures.[2] 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.[2]

References








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