Overview:
Etoricoxib is a medicine coming under the class of non-steroidal anti-inflammatory drugs which is commonly known as NSAIDs (non-steroidal anti-inflammatory drugs). It is mainly prescribed to treat pain and inflammation. The US Food and Drug Administration (FDA) approved Etoricoxib in 2002.
It is mainly indicated in adults for treating rheumatoid arthritis (RA), osteoarthritis (OA), and ankylosing spondylitis. It is also indicated for short-term treatment of pain associated with dental surgery.
How Does Etoricoxib Work?
Etoricoxib comes under the class of COX-2 inhibitors. It acts by preventing the release of chemical messengers such as prostaglandins which are responsible for pain and inflammation. They do so by inhibiting the cyclooxygenase-2 (COX-2) pathway. This action results in a decrease of the peripheral tissue prostaglandins that induce pain and mediate inflammation.
How Is Etoricoxib Supplied?
Etoricoxib is available in tablet format in a dose like 50 milligrams, 100 milligrams, 200 milligrams, and 400 milligrams oral capsule. It is also available as 25 milligrams/1 milliliter of oral solution.
What Are the Warnings and Precautions?
1. Gastrointestinal Effects: An increased incidence of upper gastrointestinal complications which include perforations or ulcers have been reported in patients taking Etoricoxib. Hence, patients who are at risk of developing gastrointestinal complications, or those with a prior history of gastrointestinal diseases should be cautiously prescribed this drug.
2. Cardiovascular Events: According to clinical studies, Etoricoxib increases the risk of thrombotic events, including myocardial infarction (MI) and stroke. Since Etoricoxib's cardiovascular hazards could rise with dose and exposure length, the shortest duration and lowest effective dose should be used. Patients with comorbidities like hypertension, hyperlipidemia, diabetes mellitus, and smoking should only be treated with Etoricoxib after careful consideration.
3. Renal Effects: Renal prostaglandins play a major role in maintaining renal perfusion. Therefore, treatment with Etoricoxib may result in a decrease in prostaglandin production and, subsequently, impairment in renal blood flow, impairing renal function in circumstances of reduced renal perfusion. Patients with cirrhosis, uncompensated heart failure, or markedly reduced renal function are at risk for this reaction. In such patients, renal function monitoring should be taken into consideration.
4. Hepatic Effects: Elevations of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) have been noted in about 1 percent of patients in clinical trials treated for up to one year with Etoricoxib 30, 60, and 90 mg daily. Patients who exhibit symptoms of liver impairment or who have had an abnormal liver function test should be closely monitored. Etoricoxib should be stopped, if symptoms of hepatic insufficiency appear or if persistently abnormal liver function tests (three times the upper limit of normal) are seen.
For Patients:
How Is Etoricoxib Gven?
Etoricoxib should be taken exactly as prescribed by the doctor. It should be swallowed whole with a glass of water. It can be taken with or without food. It is recommended to take the medicine without food as it can enhance the working of the medicine.
What Are the Things to Do After Starting Etoricoxib?
After starting Etoricoxib, the doctor may monitor for any adverse effects such as gastrointestinal side effects or cardiovascular complications. It is essential to appear for consultation regularly as scheduled by the physician to assess the patient's response to therapy and to monitor side effects.
What Are the Side Effects of Etoricoxib?
Some individuals may experience adverse effects after taking the medication. Notify the doctor if these side effects appear. The side effects of Etoricoxib include:
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Flu-like symptoms such as a high rise in temperature and weakness.
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Diarrhea.
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Flatulence.
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Headache.
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Dizziness, palpitations, vomiting, nausea.
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Edema (swelling) of the legs and hands.
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Abdominal pain.
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High blood pressure.
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Stomach inflammation.
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Constipation.
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Gastro-esophageal reflux disease.
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Dyspepsia.
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Oral ulcer.
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Altered enzymatic activity such as; increased levels of alanine aminotransferase and aspartate aminotransferase.
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Ecchymosis (discoloration of the skin resulting from bleeding underneath).
What Should Be Done if a Dose Is Missed?
Do not take a double dose if a dose is missed. Take it as soon as you recall. Take the next dose at the correct time.
What Should Be Done to Treat Overdose?
In case of an overdose, the doctor should be notified immediately. The usual supportive measures are employed which include removing unabsorbed material from the gastrointestinal tract, and clinical monitoring.
How to Store Etoricoxib?
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Keep the medication away from infants and children.
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Etoricoxib should be stored in the original package in order to protect from moisture.
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Do not use the medication if the expiry date shown in the label is over.
For Doctors:
What Are the Indications?
Etoricoxib is indicated for the treatment and reduction of pain and inflammation associated with osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and short-term pain relief after dental surgery.
What Is the Mechanism of Action?
Etoricoxib is an NSAID that has analgesic, antipyretic, and anti-inflammatory properties. It inhibits COX-2 enzyme thereby inhibiting prostaglandin synthesis. Prostaglandin is a chemical mediator for pain and inflammation and inhibiting its synthesis helps in the reduction of pain and inflammation.
Pharmacokinetics:
Absorption:
Etoricoxib, when orally administered, is well absorbed with an absolute bioavailability of approximately 100 percent. Normal peak plasma concentration occurs in one hour after the oral administration. The presence of food does not have an effect on the extent of absorption.
Distribution:
Etoricoxib is 92 percent protein-bound with albumin and acid-1 glycoprotein. The apparent volume of distribution at steady state is approximately 0.37 gallons in humans.
Metabolism:
Etoricoxib is extensively metabolized by the CYP enzymes. CYP3A4 contributes to the metabolism of Etoricoxib in vivo. Studies have also shown that CYP2D6, CYP2C9, CYP1A2, and CYP2C19 also can catalyze the main metabolic pathway. The principal metabolite is the 6-carboxylic acid derivative of Etoricoxib.
Elimination:
Etoricoxib is eliminated primarily by metabolism followed by renal excretion through urine.
Contraindications:
Etoricoxib is contraindicated in the following conditions:
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Hypersensitivity to Etoricoxib or any components of the drug.
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Patients who are predisposed to gastrointestinal bleeding or ulceration.
Drug interactions:
Etoricoxib interacts with the following drugs:
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Antiplatelet agents and NSAIDs when given together may increase the risk of bleeding.
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When potassium-sparing diuretics and NSAIDs are administered concurrently, it may result in reduced diuretic effectiveness, hyperkalemia, and nephrotoxicity.
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Concurrent use of NSAIDs and corticosteroids can further increase the risk of gastrointestinal bleeding or ulcers.
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NSAIDs and tricyclic antidepressants when administered concurrently may increase the risk of bleeding.
Clinical Teaching for Etoricoxib:
The following things should be remembered while using Etoricoxib;
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Report immediately if symptoms such as gastrointestinal bleeding or perforation occur.
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Report immediately if symptoms of hepatotoxicity occur.
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Avoid administration of Etoricoxib in pregnant women at 20 weeks of gestation and later, as the drug may cause oligohydramnios, anemia, or upper respiratory tract infection.
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Report immediately if symptoms of skin reactions like rashes, exfoliative dermatitis or toxic epidermal necrolysis occur.
Conclusion:
Etoricoxib is a non-steroidal antiinflammatory drug. It is used for curing pain and inflammation. It is indicated for the treatment of rheumatoid arthritis (RA), osteoarthritis (OA), and ankylosing spondylitis. Gastrointestinal and cardiac complications are common drawbacks of the drugs. It should be cautiously used in patients suffering from gastric problems, heart diseases, and liver problems.
