(Etoricoxib) used as NSAID

Etoricoxib

Managing pain and inflammation

Etoricoxib is a non-steroidal anti-inflammatory drug (NSAID) used to relieve pain and reduce inflammation in conditions like osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and gout.

 What to learn?

·    Clinical uses

·    Mechanism of action

·    Pharmacokinetics

·    Drug interaction

·    Contraindications

·    Drug interactions

·    Toxicity

Clinical uses

·    Etoricoxib is used for long-term treatment (taken for 3-months and more) and short-term treatment (taken for 1 to 3 weeks). It is used to manage pain in the following ways:

·    In conditions like osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis, Etoricoxib is prescribed to reduce pain and swelling in the joints and muscles for long-term treatment. Its clinical trials have shown a comparatively better safety profile and tolerance than Ibuprofen.

·    Etoricoxib is also used for treating pain following dental surgery in the short term.

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.^[10] This reduces the generation of prostaglandins (PGs) from arachidonic acid. The clinical relevance of the drug stems from the role of PGs in the inflammation cascade.

·    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.

 

Pharmacokinetics

·    Oral bioavailability (%)

·    Time to maximal plasma concentration (h)

·    Maximal plasma concentration (ng/ml)

·    Half-life (h)

·    Volume dist. (l)

·    Bound in plasma (%) 

 Contraindication

·    Etoxib is contraindicated: in patients with severe heart failure; for the treatment of peri-operative pain in the setting of coronary artery bypass graft surgery.
Do not take Etoxib: if allergic to etoricoxib or any of the other ingredients of this medicine (listed in Description); if allergic to non-steroidal anti-inflammatory drugs (NSAIDs), including acetylsalicylic acid and COX-2 inhibitors (see Side Effects); if there is a current stomach ulcer or bleeding in the stomach or intestines; if there is serious liver disease; if there is serious kidney disease; if pregnant or could be pregnant or breast-feeding (see Use in Pregnancy & Lactation); if under 16 years of age; if there is inflammatory bowel disease, such as Crohn's Disease, Ulcerative Colitis, or Colitis; if there is high blood pressure that has not been controlled by treatment (check with the doctor or nurse if not sure whether the blood pressure is adequately controlled); if the doctor has diagnosed heart problems including heart failure (moderate or severe types), angina (chest pain); if there had been a heart attack, bypass surgery, peripheral arterial disease (poor circulation in legs or feet due to narrow or blocked arteries); if there had been any kind of stroke (including mini-stroke, transient ischaemic attack or TIA).

·    Etoricoxib may slightly increase the risk of heart attack and stroke and this is why it should not be used in those who have already had heart problems or stroke.
If any of these are relevant, do not take the tablets until the doctor has been consulted.

Drug interactions  

Interactions with other medications:

• Methotrexate, Ciclosporin, Tacrolimus
• Diuretics
• Antibiotics like Rifampicin
• Oral hormonal birth control pills
• Blood thinners like warfarin
• Lithium - a medicine used to treat mania
• Using Etoricoxib together with Aspirin increases your chance of developing stomach ulcers.

 Toxicity

This reduced activity is the cause of reduced gastrointestinal toxicity, as demonstrated in several large clinical trials performed with different COXIB (see below links on NEJM and The Lancet). Some clinical trials and meta-analysis showed that treatment with COXIB lead to increased incidence of cardiovascular adverse events compared to placebo.