Source: Medicines Authority (MT) Revision Year: 2012 Publisher: Chiesi España, S.A.U., Plaça dEuropa, 41-43, Planta 10, 08908 LHospitalet de Llobregat, Barcelona (Spain)
Pharmacotherapeutic group: Antiinflamatory preparations, non-steroids for topical use: Etofenamate
ATC Code: M02AA06
Etofenamate is a non-steroidal anti-inflammatory with analgesic properties, which easily penetrates the skin and is used for the topical treatment of both rheumatic and traumatic pain. Its anti-inflammatory effect has been tested in animal studies and confirmed in several in-human studies. Etofenamate acts on different phases of the inflammatory process: it inhibits prostaglandins synthesis and the release of histamine, it is a serotonin and bradykinin antagonist and it also inhibits complement activation and the release of proteolytic enzymes. Its stabilising properties of the membrane limit proteolytic enzymes release. As a result, exudative and proliferative inflammatory processes and their symptoms are inhibited, favouring mobility recuperation and functionality of the affected areas.
Due to its physicochemical properties, etofenamate has a high cutaneous penetration capacity irrespective of the pH or the acidity of the skin. Etofenamate is absorbed after topical administration, where it primarily reaches inflamed areas, with concentrations 5 to 20 times higher in these areas than in non-inflamed areas. Plasma protein binding is about 98-99%.
Etofenamate is eliminated in the form of several metabolites (hydroxyl, ether and ester groups); mainly biliary and faecal excretion with 35% renal excretion. Significant interindividual and intraindividual fluctuations in bioavailability have been observed depending on the application site, the humidity of the skin and other factors. After cutaneous administration, the relative bioavailability, that is, the amount of systemic dose available, is similar to other etofenamate products (higher than 20%).
Toxicological studies of etofenamate in topical application showed a wide safety margin, as confirmed by decades of therapeutic use of the product.
It has not been possible to determine the DL50 for a topical application.
In a preclinical study, the administration of 2g/kg/day of etofenamate for 8 weeks in the same area showed no macroscopic differences in different organs or in the weight and blood parameters of the animals compared with a placebo.
The only observation was a notable thickening of the epidermis on the site of application with no erythema or oedema.
Studies conducted in animals have not shown a teratogenic effect of etofenamate in topical application and no variation in the number of offspring or reproductive parameters.
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