Loxoprofen

drugbox
IUPAC_name = 2-{4- [(2-oxocyclopentyl)methyl] phenyl}propanoic acid

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CAS_number = 68767-14-6
ATC_prefix = M01
ATC_suffix = AE
PubChem = 3965
DrugBank =
C = 15 |H = 18 |O = 3
molecular_weight = 246.302 g/mol
304.314 g/mol (sodium salt)
bioavailability =
protein_bound = 97%
metabolism = Hepatic glucuronidation
elimination_half-life = 75 minutes
excretion = Renal
pregnancy_category =
legal_status = Red Stripe (Brazil)
routes_of_administration = 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, and in Argentina as Oxeno. It is available in these countries for oral administration, and a transdermal preparation was approved for sale in Japan on January 2006. [cite press release | url = http://www.pslgroup.com/dg/2570a2.htm | title = Percutaneous Absorption-Type Analgesic and Anti-inflammatory Drug Loxonin Poultice 100mg Receives Approval for Manufacture | author = Daiichi Sankyo Co. | date = January 24, 2006 | accessdate = 2007-04-19 | publisher = Doctor's Guide Global Edition]

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.pt icon cite web | url = http://bulas.cxpass.net/index.asp?C=A&V=66506F737449443D36323834266163743D73686F7752656164436F6D6D656E7473 | title = LOXONIN - Bula do Medicamento [Label Information] | year = 2007 | accessdate = 2007-04-19 | publisher = Centralx] 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.

References