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| Clinical data | |
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| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral,transdermal |
| ATC code | |
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| Pharmacokinetic data | |
| Protein binding | 97% |
| Metabolism | Liverglucuronidation |
| Eliminationhalf-life | 75 minutes |
| Excretion | Kidney |
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| ChEBI | |
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| Chemical and physical data | |
| Formula | C15H18O3 |
| Molar mass | 246.306 g·mol−1 |
| 3D model (JSmol) | |
| Chirality | Racemic mixture |
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Loxoprofen is anonsteroidal anti-inflammatory drug (NSAID) in thepropionic acid derivatives group, which also includesibuprofen andnaproxen among others. It is available in some countries for oral administration. Atransdermal 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]
Loxoprofen is aprodrug. It is quickly converted to its activetrans-alcoholmetabolite following oral administration, and reaches its peak plasma concentration within 30 to 50 minutes.
As mostNSAIDs, loxoprofen is a non-selectivecyclooxygenase inhibitor, and works by reducing the synthesis ofprostaglandins fromarachidonic acid.
Loxoprofen should not be administered at the same time as second-generationquinolone antibiotics such asciprofloxacin andnorfloxacin, as it increases their inhibition ofGABA and this may causeseizures.[3]It may also increase the plasma concentration ofwarfarin,methotrexate,sulfonylurea derivatives andlithium salts, so care should be taken when loxoprofen is administered to patients taking any of these drugs.[3]
It is marketed in Brazil, Mexico, China and Japan bySankyo 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 byAché as Oxotron. In Japan, twofixed dose combinations are available: Loxonin S Plus, withmagnesium oxide, and Loxonin S Premium, withapronal,caffeine, and aluminium magnesium silicate.
| pyrazolones / pyrazolidines | |
|---|---|
| salicylates | |
| acetic acid derivatives and related substances | |
| oxicams | |
| propionic acid derivatives (profens) |
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| n-arylanthranilic acids (fenamates) | |
| COX-2 inhibitors (coxibs) | |
| other | |
| NSAID combinations | |
Key:underline indicates initially developed first-in-class compound of specific group;#WHO-Essential Medicines;†withdrawn drugs;‡veterinary use. | |
