Etoricoxib, sold under the trade name Arcoxia, is a selective

COX-2 inhibitor COX-2 inhibitors are a type of nonsteroidal anti-inflammatory drug (NSAID) that directly targets cyclooxygenase-2, COX-2, an enzyme responsible for inflammation and pain. Targeting selectivity for COX-2 reduces the risk of peptic ulceration and i ...

from McOLSON Research Laboratories. Currently it is approved in more than 80 countries worldwide but not in the US, where the

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...

(FDA) has required additional safety and efficacy data for etoricoxib before it will issue approval. It was patented in 1996 and approved for medical use in 2002.

Medical uses

Etoricoxib is indicated for the treatment of

rheumatoid arthritis Rheumatoid arthritis (RA) is a long-term autoimmune disorder that primarily affects joints. It typically results in warm, swollen, and painful joints. Pain and stiffness often worsen following rest. Most commonly, the wrist and hands are involv ...

psoriatic arthritis Psoriatic arthritis is a long-term inflammatory arthritis that occurs in people affected by the autoimmune disease psoriasis. The classic feature of psoriatic arthritis is swelling of entire fingers and toes with a sausage-like appearance. Thi ...

osteoarthritis Osteoarthritis (OA) is a type of degenerative joint disease that results from breakdown of joint cartilage and underlying bone which affects 1 in 7 adults in the United States. It is believed to be the fourth leading cause of disability in the w ...

ankylosing spondylitis Ankylosing spondylitis (AS) is a type of arthritis characterized by long-term inflammation of the joints of the spine typically where the spine joins the pelvis. Occasionally areas affected may include other joints such as the shoulders or hip ...

, chronic

low back pain Low back pain (LBP) or lumbago is a common disorder involving the muscles, nerves, and bones of the back, in between the lower edge of the ribs and the lower fold of the buttocks. Pain can vary from a dull constant ache to a sudden sharp feeli ...

, acute pain, and

gout Gout ( ) is a form of inflammatory arthritis characterized by recurrent attacks of a red, tender, hot and swollen joint, caused by deposition of monosodium urate monohydrate crystals. Pain typically comes on rapidly, reaching maximal intensit ...

. Approved indications differ by country. In the U.K. and Germany, it is also "used for the short term treatment of moderate pain after dental surgery" of adults.

Efficacy

Cochrane review Cochrane (previously known as the Cochrane Collaboration) is a British international charitable organisation formed to organise medical research findings to facilitate evidence-based choices about health interventions involving health professi ...

assessed the benefits of single-dose etoricoxib in reduction of acute post-operative pain in adults. Single-dose oral etoricoxib provides four times more pain relief post-operatively than placebo, with equivalent levels of adverse events. Etoricoxib given at a dose of 120 mg is as effective or even better than other analgesics that are commonly used.

Adverse effects

Like all other NSAIDs the COX-2 inhibitors too have their share of adverse effects. Fixed drug eruption and generalised

erythema Erythema (from the Greek , meaning red) is redness of the skin or mucous membranes, caused by hyperemia (increased blood flow) in superficial capillaries. It occurs with any skin injury, infection, or inflammation. Examples of erythema not assoc ...

acute generalized exanthematous pustulosis Acute generalized exanthematous pustulosis (AGEP) (also known as pustular drug eruption and toxic pustuloderma) is a rare skin reaction that in 90% of cases is related to medication administration. AGEP is characterized by sudden skin eruptions th ...

(AGEP),

erythema multiforme Erythema multiforme (EM) is a skin condition that appears with red patches evolving into target lesions, typically on both hands. It is a type of erythema possibly mediated by deposition of immune complexes (mostly IgM-bound complexes) in the s ...

like eruption and drug induced pretibial erythema are some serious side effects reported, besides the usual innocuous ones.

Mechanism of action

Like any other selective COX-2 inhibitor ("coxib"), etoricoxib selectively inhibits isoform 2 of the enzyme cyclooxygenase (COX-2). It has approximately 106-fold selectivity for COX-2 inhibition over

COX-1 Cyclooxygenase 1 (COX-1), also known as prostaglandin G/H synthase 1, prostaglandin-endoperoxide synthase 1 or prostaglandin H2 synthase 1, is an enzyme that in humans is encoded by the ''PTGS1'' gene. In humans it is one of two cyclooxygenases. ...

. This reduces the generation of

prostaglandin The prostaglandins (PG) are a group of physiologically active lipid compounds called eicosanoids having diverse hormone-like effects in animals. Prostaglandins have been found in almost every tissue in humans and other animals. They are derive ...

s (PGs) from

arachidonic acid Arachidonic acid (AA, sometimes ARA) is a polyunsaturated omega-6 fatty acid 20:4(ω-6), or 20:4(5,8,11,14). It is structurally related to the saturated arachidic acid found in cupuaçu butter. Its name derives from the New Latin word ''arachi ...

. Among the different functions exerted by PGs, their role in the inflammation cascade should be highlighted. Selective COX-2 inhibitors show less activity on COX-1 compared to traditional

non-steroidal anti-inflammatory drug Non-steroidal anti-inflammatory drugs (NSAID) are members of a therapeutic drug class which reduces pain, decreases inflammation, decreases fever, and prevents blood clots. Side effects depend on the specific drug, its dose and duration of ...

s (NSAID). This reduced activity is the cause of reduced gastrointestinal side effects, as demonstrated in several large clinical trials performed with different coxibs.

History

Some clinical trials and meta-analysis showed that treatment with some coxibs (in particular

rofecoxib Rofecoxib is a COX-2 inhibitor, COX-2 selective nonsteroidal anti-inflammatory drug (NSAID). It was marketed by Merck & Co. to treat osteoarthritis, rheumatoid arthritis, juvenile rheumatoid arthritis, acute pain conditions, migraine, and dysmenor ...

) led to increased incidence of adverse cardiovascular events compared to placebo. Because of these results, some drugs were withdrawn from the market (rofecoxib, in September 2004 and

valdecoxib Valdecoxib is a nonsteroidal anti-inflammatory drug (NSAID) used in the treatment of osteoarthritis, rheumatoid arthritis, and painful menstruation and menstrual symptoms. It is a selective cyclooxygenase-2 inhibitor. It was patented in 1995. V ...

in April 2005). In addition, the United States Food and Drug Administration and the

European Medicines Agency The European Medicines Agency (EMA) is an agency of the European Union (EU) in charge of the evaluation and supervision of medicinal products. Prior to 2004, it was known as the European Agency for the Evaluation of Medicinal Products or Euro ...

started revision processes of the entire class of both NSAIDs and COX-2 inhibitors.

Brand names

Brand names for etoricoxib include: *''Algix'' and ''Tauxib'' in Italy *''Anexia'' in Colombia *''Arcox'', ''Berrica'', and ''Starcox'' Etoxib in Pakistan *''Arcoxia'' in Australia, Brazil, Bulgaria, Chile, China, Colombia, Costa Rica, Croatia, Ecuador, Egypt, Estonia, Finland, Georgia, Greece, Guatemala, Hong Kong, Hungary, Indonesia, Ireland, Israel, Italy, Jordan, Lebanon, Lithuania, Luxembourg, Malaysia, Mexico, Morocco, Netherlands, New Zealand, Norway, Panama, Philippines, Poland, Portugal, Romania, Russian Federation, Saudi Arabia, Serbia, Singapore, South Africa, Spain, Sweden, Taiwan, Thailand, The Bahamas, Trinidad & Tobago, United Arab Emirates, United Kingdom and Ukraine. *''Atocib'' in Vietnam *''Dolicox'' in Morocco *''Dolocox'' in Argentina *''Coxit'' in Jordan *''Dabie'' in Singapore *''Doloxib'' in Poland *''E-Cox'' and ''Vecoxib'' in Nepal * ''Eberil'' in Thailand * ''Erciba'' in Greece *''Etoll, Etoshine, Nucoxia'' in India *''Etoricoxib'' in Germany *''Etorix'', ''Eto'', ''Tory'', ''Etoxib'', and ''Vargus'' in Bangladesh and Costa Rica *''Etozox'', ''Etospeed'', '' Intacoxia'', ''Nucoxia'', ''ETOS MR'', and ''Etoshine'' in India *''Exinef'' in Singapore and South Africa *''Exxiv'' in Portugal *''Foldox'' in Argentina and Paraguay * ''Gerocoxan'' in Romania *''Hetori'' in Brazil *''Kostarox'' in Poland * ''Roticox'' in Poland * ''Berica'' in Pakistan * ''Xumer'' in Chile, Peru and Mexico

References

{{Prostanoidergics COX-2 inhibitors Nonsteroidal anti-inflammatory drugs Pyridines Merck & Co. brands Chloropyridines