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Merck & Co.
Etoricoxib
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Etoricoxib

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Etoricoxib
Etoricoxib.svg
Clinical data
AHFS/Drugs.com International Drug Names
Pregnancy
category
  • AU: C
  • Not recommended
Routes of
administration		 By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
Pharmacokinetic data
Bioavailability 100%
Protein binding 92%
Metabolism Hepatic, CYP extensively involved (mainly CYP3A4)
Elimination half-life 22 hours
Excretion Renal (70%) and fecal (20%)
Identifiers
  • 5-Chloro-6'-methyl-3-[4-(methylsulfonyl)phenyl]-2,3'-bipyridine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.207.709
Chemical and physical data
Formula C18H15ClN2O2S
Molar mass 358.84 g·mol−1
3D model (JSmol)
  • O=S(=O)(c3ccc(c2cc(Cl)cnc2c1cnc(cc1)C)cc3)C
  • InChI=1S/C18H15ClN2O2S/c1-12-3-4-14(10-20-12)18-17(9-15(19)11-21-18)13-5-7-16(8-6-13)24(2,22)23/h3-11H,1-2H3 checkY
  • Key:MNJVRJDLRVPLFE-UHFFFAOYSA-N checkY
  (verify)

Etoricoxib, sold under the trade name Arcoxia, is a selective COX-2 inhibitor 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 (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, psoriatic arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain, and gout. 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

A Cochrane review 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,acute generalized exanthematous pustulosis (AGEP),erythema multiforme 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. This reduces the generation of prostaglandins (PGs) from arachidonic acid. 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 drugs (NSAID). This reduced activity is the cause of reduced gastrointestinal side effects, as demonstrated in several large clinical trials performed with different coxibs.

Adverse Cardiovascular Events

Some clinical trials and meta-analysis showed that treatment with some coxibs (in particular rofecoxib) 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 in April 2005). In addition, the United States Food and Drug Administration and the European Medicines Agency 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, Czechia, Ecuador, Egypt, Estonia, Finland, Georgia, Germany, 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
  • Berica in Pakistan
  • 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
  • Etori in Germany
  • Etoriax in Germany
  • Etorican in Germany
  • Etoriconio in Germany
  • Etoricox in Germany
  • 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
  • Xumer in Chile, Peru and Mexico

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