As a COX-2 inhibitor, etoricoxib belongs to the non-steroidal anti-inflammatory drugs (NSAIDs). The active ingredient, which is used particularly as an anti-inflammatory and pain reliever, is thought to have properties that are gentler on the stomach and intestines than traditional nonsteroidal anti-inflammatory drugs.
What is etoricoxib?
Etoricoxib is generally applied in tablet form. Etoricoxib (molecular formula: C18H15ClN2O2S) is a drug from the coxibe or COX-2 inhibitor group of active ingredients, which exert an analgesic and anti-inflammatory effect through their targeted inhibition of the enzyme cyclooxygenase 2 (COX-2). COX-2 inhibitors belong to the group of non-steroidal anti-inflammatory drugs (NSAIDs). The active ingredient is a dipyridyl derivative that has phenylsulfonamide interacting with the binding pocket of COX-2. The substance is used primarily in the symptomatic treatment of swelling and pain associated with degenerative (due to wear and tear) and/or inflammatory rheumatic joint diseases. Etoricoxib is generally applied in tablet form.
Pharmacologic action
The active ingredient etoricoxib is used in particular because of its anti-inflammatory and analgesic characteristics. This effect is achieved comparatively promptly (after 25 minutes on average) by selective inhibition of cyclooxygenase 2, i.e., affecting only one subform. Cyclooxygenase 2 is an important enzyme in the biosynthesis of prostaglandins, which trigger fever as well as inflammatory processes and pain symptoms in the organism. In addition, etoricoxib inhibits thromboxanes, which are involved in the synthesis of prostaglandins, and prostacyclins (pro-inflammatory subform of prostaglandins). Since etoricoxib does not inhibit COX-1 (cyclooxygenase 1) or prostaglandin synthesis in the stomach or affect platelet function, its inhibitory effect, as with all coxibs, is highly targeted and selective. Thus, due to the lack of inhibition of the sister enzyme COX-1, which participates in the biosynthesis of mucosal protective prostaglandins in the stomach, etoricoxib therapy is thought to result in less pronounced gastrointestinal tract (GI) impairment and fewer manifestations of ulcers and bleeding than conventional nonsteroidal anti-inflammatory drugs. However, by inhibiting COX-2, etoricoxib may mask fever as well as other signs of inflammatory or infectious disease.
Medicinal use and application
Etoricoxib is applied primarily for the therapy of pain and inflammatory symptoms that occur in the context of inflammatory rheumatic joint diseases such as osteoarthritis, in active gout attacks (acute joint inflammation), and rheumatoid arthritis. In addition, therapy with etoricoxib may be indicated for chronic movement pain, primary menstrual cramps, postoperative dental pain, or ankylosing spondylitis. Due to the long half-life (about 22 hours) of etoricoxib, a single application per day is usually sufficient, which is usually administered orally in the form of tablets (30, 60, 90 or 120 mg). Since the risk of cardiovascular events such as myocardial infarction increases with increasing treatment duration and/or dosage, the risk-benefit ratio should be thoroughly weighed in therapy with etoricoxib and, if necessary, the shortest possible therapy and lowest possible dosage should be selected. In addition, regular monitoring for therapeutic success and potential side effects is indicated, particularly in patients affected by osteoarthritis and with pathologically altered liver function values. If symptoms of liver dysfunction and/or persistently elevated liver values are present, etoricoxib therapy should be discontinued. Similarly, the agent should be discontinued if initial signs of mucosal impairment, skin rashes, and/or other hypersensitivity reactions are present.
Risks and Side Effects
Etoricoxib use is associated with a number of adverse side effects and drug interactions. For example, long-term, high-dose use of the drug may increase the risk of cardiovascular events, among other adverse effects. Most commonly, dizziness and headache, edema, hypertension, palpitations, digestive and gastrointestinal symptoms, fatigue, skin bleeding, nausea, elevation of liver enzymes, and flu-like illnesses are described as adverse side effects.Therapy with etoricoxib is also contraindicated, particularly in the presence of pregnancy, hypersensitivity to the active substance, active intestinal and/or gastric ulcers, inflammatory diseases of the intestine, gastrointestinal bleeding, marked liver dysfunction, renal or moderate to severe heart failure, and coronary artery disease. In addition, etoricoxib therapy in combination with warfarin may result in prolonged blood clotting time, while parallel treatment with acetylsalicylic acid may cause gastric ulcers and other complications. The concomitant use of etoricoxib with tacrolimus and ciclosporin may lead to an increase in the renal toxic effect of the two immunosuppressants mentioned. Likewise, therapy with concomitant use of ketoconazole (antifungal), rifampicin (antibiotic), and orally administered salbutamol and minoxidil (antihypertensive) should be carefully weighed with respect to the risk-benefit ratio. Other interactions of etoricoxib are observed in the context of concomitant treatment with ACE inhibitors, diuretics, lithium, sartans, estrogens, methotrexate, digoxin, and prednisone.
