Etoricoxib

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Generic Name of Etoricoxib - Learn More

Etoricoxib

Etoricoxib Precaution - What You Need to Know

Etoricoxib is a nonsteroidal anti-inflammatory drug (NSAID) that selectively inhibits cyclooxygenase-2 (COX-2). It is primarily used for the management of pain and inflammation but requires caution in certain populations and conditions:

- Pregnancy and breastfeeding: Etoricoxib is classified as a Category C drug during pregnancy. It should only be used if the potential benefit justifies the potential risk to the fetus, especially in the first and second trimesters. It is contraindicated during the third trimester due to the risk of premature closure of the ductus arteriosus and other potential harm. Etoricoxib is not recommended during breastfeeding, as it is not known if it passes into breast milk.

- Cardiovascular risk: Like other COX-2 inhibitors, Etoricoxib can increase the risk of cardiovascular events, such as heart attack, stroke, and thrombosis. It should be used with caution in patients with existing cardiovascular disease, hypertension, or those at high risk of developing these conditions. The lowest effective dose should be used for the shortest duration possible.

- Gastrointestinal risk: Although Etoricoxib is selective for COX-2, it can still cause gastrointestinal adverse effects, including ulceration, bleeding, and perforation, especially in high-risk patients. It should be used cautiously in individuals with a history of peptic ulcers, gastrointestinal bleeding, or those taking other anticoagulants or corticosteroids.

- Renal impairment: Etoricoxib should be used with caution in patients with renal impairment, as it can cause fluid retention, elevate blood pressure, and exacerbate kidney dysfunction. Renal function should be monitored regularly, and dose adjustments may be necessary, especially in patients with moderate to severe renal impairment.

- Liver impairment: Caution is required in patients with liver disease, as Etoricoxib is metabolized in the liver. It should be avoided in patients with significant liver dysfunction (Child-Pugh Class C) due to the potential for further liver damage.

Etoricoxib Indication - Uses and Benefits

Etoricoxib is primarily indicated for the management of various pain conditions and inflammatory disorders:

- Osteoarthritis: It is commonly prescribed for the relief of pain and inflammation associated with osteoarthritis, where it helps improve joint mobility and reduce discomfort.

- Rheumatoid arthritis: Etoricoxib is used to manage pain and inflammation in patients with rheumatoid arthritis, offering symptomatic relief and helping to reduce the risk of joint damage associated with the disease.

- Acute pain: Etoricoxib is effective in treating moderate to severe acute pain, such as postoperative pain or musculoskeletal pain. It provides a rapid onset of pain relief and is generally well tolerated.

- Gouty arthritis: Etoricoxib can be used to alleviate pain and inflammation during acute gout flares, providing relief from the intense pain and swelling associated with this condition.

- Off-label uses: Although not as commonly used, Etoricoxib may be prescribed off-label for conditions such as ankylosing spondylitis, lower back pain, or dysmenorrhea (painful menstruation) if other treatments are not effective or tolerated.

Etoricoxib Contraindications - Important Warnings

Certain conditions and factors exclude the use of Etoricoxib due to its potential to exacerbate adverse effects:

- Hypersensitivity: Etoricoxib is contraindicated in patients with known hypersensitivity to the drug or any component of its formulation. Severe allergic reactions, including anaphylaxis, can occur in these individuals.

- Active gastrointestinal bleeding or ulcers: Etoricoxib should not be used in patients with a history of or active gastrointestinal bleeding, peptic ulcers, or gastrointestinal perforation, as it may worsen these conditions.

- Severe cardiovascular disease: Etoricoxib is contraindicated in patients with severe coronary artery disease, peripheral arterial disease, or cerebrovascular disease, as it increases the risk of thrombotic events such as heart attack and stroke.

- Severe liver impairment: Etoricoxib is contraindicated in patients with moderate to severe liver impairment (Child-Pugh Class B or C), as it can further impair liver function and increase the risk of hepatotoxicity.

- Pregnancy (third trimester) and breastfeeding: As mentioned, Etoricoxib is contraindicated in the third trimester of pregnancy due to risks to fetal development, particularly the premature closure of the ductus arteriosus. It is also not recommended during breastfeeding.

Etoricoxib Side Effects - What to Expect

While Etoricoxib is generally well tolerated, it can cause a range of side effects:

- Common side effects:
- Gastrointestinal: Although Etoricoxib is selective for COX-2, it may still cause mild gastrointestinal discomfort, nausea, or dyspepsia. These effects are typically less frequent than with non-selective NSAIDs but should be monitored.
- Headache and dizziness: These are common, especially in the initial phase of treatment, and usually resolve with continued use or dose adjustment.
- Peripheral edema: Swelling in the lower extremities can occur, particularly with long-term use or in patients with pre-existing cardiovascular or renal conditions.

- Serious side effects:
- Cardiovascular: Etoricoxib is associated with an increased risk of serious cardiovascular events, such as heart attack, stroke, and thrombotic events, particularly with long-term use or in patients with pre-existing heart disease.
- Gastrointestinal bleeding and ulceration: While less common than with non-selective NSAIDs, Etoricoxib can still lead to serious gastrointestinal complications, including ulcers, bleeding, and perforation.
- Kidney dysfunction: Etoricoxib can exacerbate kidney problems, leading to acute renal failure, especially in patients with pre-existing renal impairment.
- Liver dysfunction: Liver enzyme abnormalities and, in rare cases, severe liver toxicity, have been reported. Liver function should be monitored during long-term treatment.

- Allergic reactions: Severe allergic reactions, including rash, angioedema, and anaphylaxis, may occur in rare cases. Discontinuation of the drug is necessary if any signs of an allergic reaction occur.

Etoricoxib Mode of Action - How It Works

Etoricoxib is a selective COX-2 inhibitor, which means it specifically targets the cyclooxygenase-2 enzyme, a key enzyme involved in the production of prostaglandins, which mediate inflammation, pain, and fever:

- Pharmacodynamics: Etoricoxib inhibits COX-2, the enzyme responsible for synthesizing pro-inflammatory prostaglandins, without significantly inhibiting COX-1, which is involved in protecting the stomach lining and maintaining platelet function. This selectivity reduces the gastrointestinal side effects commonly associated with non-selective NSAIDs like ibuprofen.

- Pharmacokinetics: Etoricoxib is well absorbed after oral administration and reaches peak plasma concentrations within 1-3 hours. It has a long half-life of approximately 22 hours, allowing for once-daily dosing. The drug is extensively metabolized in the liver by the cytochrome P450 enzymes (CYP3A4 and CYP2C9) and is eliminated via urine, with only a small fraction excreted unchanged.

Etoricoxib Drug Interactions - What to Avoid

Etoricoxib can interact with several drugs, affecting either the efficacy or safety of treatment:

- Anticoagulants: Etoricoxib may increase the risk of bleeding when used with anticoagulants such as warfarin or other antithrombotic drugs. Close monitoring of prothrombin time (PT) or international normalized ratio (INR) is recommended for patients on anticoagulant therapy.

- ACE inhibitors and diuretics: Etoricoxib can reduce the efficacy of angiotensin-converting enzyme (ACE) inhibitors and diuretics, particularly in patients with pre-existing kidney problems. It may lead to kidney dysfunction and fluid retention, so renal function should be monitored closely.

- Other NSAIDs and corticosteroids: Combining Etoricoxib with other NSAIDs or corticosteroids increases the risk of gastrointestinal bleeding, ulcers, and perforation. Co-administration of multiple anti-inflammatory drugs should be avoided unless absolutely necessary.

- Lithium: Etoricoxib can increase lithium levels by reducing renal clearance. Monitoring lithium levels and adjusting the dose as necessary is advised when these drugs are used together.

- Methotrexate: Co-administration of Etoricoxib with methotrexate can increase the plasma levels of methotrexate, potentially leading to methotrexate toxicity. Careful monitoring of methotrexate levels is needed.

- Cytochrome P450 enzyme interactions: Etoricoxib is metabolized by CYP3A4 and CYP2C9 enzymes. Inhibitors of these enzymes (e.g., ketoconazole, fluconazole) may increase Etoricoxib levels, while inducers (e.g., rifampin) may decrease its efficacy. Dose adjustments may be needed when used with these drugs.

Etoricoxib Adult Dose - Recommended Dosage

The recommended dosage for adults depends on the condition being treated:

- Osteoarthritis: The usual dose is 30 mg once daily. In some cases, the dose may be increased to 60 mg once daily if needed.

- Rheumatoid arthritis: The typical dose is 60 mg once daily. The dose may be increased to 90 mg once daily for optimal symptom control.

- Acute pain: For acute pain, including postoperative pain, a dose of 90 mg once daily is typically used for short-term treatment.

- Gout: The dose for gouty arthritis during an acute flare is 120 mg once daily for up to 8 days.

Etoricoxib Child Dose - Dosage for Children

Etoricoxib is not recommended for children under 16 years of age due to insufficient safety data in this population. In some countries, it may be approved for specific conditions in adolescents over the age of 16, with dosing adjusted based on body weight and condition being treated. However, specific dosing guidance should be obtained from local prescribing information.

Etoricoxib Renal Dose - Dosage for Kidney Conditions

Etoricoxib should be used with caution in patients with renal impairment

. For patients with creatinine clearance of less than 30 mL/min, the use of Etoricoxib is contraindicated. In patients with mild to moderate renal impairment, dose adjustment may not be necessary, but it is important to monitor renal function closely.