Etoricoxib
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Oral |
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| Bioavailability | 100% |
| Protein binding | 92% |
| Metabolism | Hepatic, extensively involved (mainly CYP3A4) |
| Biological half-life | 22 hours |
| Excretion | Renal (70%) and fecal (20%) |
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| ECHA InfoCard | 100.207.709 |
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| Formula | C18H15ClN2O2S |
| Molar mass | 358.842 g/mol |
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Etoricoxib (Arcoxia) is a selective COX-2 inhibitor from Merck & Co. 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.
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.
A Cochrane systematic review assessed the benefits of single-dose etoricoxib in reduction of acute post-operative pain in adults. Single-dose oral etoricoxib provides good quality pain relief post-operatively in adults and adverse events are similar to placebo in the studies included. Etoricoxib given at a dose of 120 mg is as effective or even better than other analgesics that are commonly used.
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.
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.
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