Ezepain

Approved Indications:

• Osteoarthritis: Symptomatic management of pain and inflammation.
• Rheumatoid Arthritis: Treatment of signs and symptoms.
• Ankylosing Spondylitis: Relief of symptoms and inflammation.
• Acute Gouty Arthritis: Short-term treatment of acute flare-ups.
• Chronic Musculoskeletal Pain: Including chronic low back pain.
• Postoperative Pain: Management of moderate to severe pain after dental surgery or orthopedic procedures.

Off-label / Clinically Accepted Uses:

• Management of other inflammatory arthritides as determined by clinician.
• Pain relief in conditions requiring selective COX-2 inhibition.

Route: Oral

Adults:

• Osteoarthritis: 30 mg once daily; may increase to 60 mg once daily if needed.
• Rheumatoid Arthritis & Ankylosing Spondylitis: 60 mg once daily; may increase to 90 mg if inadequate response.
• Acute Gout: 120 mg once daily for up to 8 days.
• Chronic Musculoskeletal Pain: 60 mg once daily.
• Postoperative Pain: Single 90 mg dose; may repeat after 24 hours if necessary.

Special Populations:

• Elderly: Start at lowest effective dose; monitor for adverse effects.
• Renal Impairment: Not recommended in severe impairment (eGFR <30 mL/min).
• Hepatic Impairment: Use with caution in mild to moderate; avoid in severe.

Duration: Use shortest duration necessary to control symptoms.

Etoricoxib is a selective cyclooxygenase-2 (COX-2) inhibitor, which selectively inhibits the COX-2 enzyme responsible for prostaglandin synthesis at sites of inflammation. By sparing COX-1, which protects the gastric mucosa and supports platelet function, etoricoxib reduces inflammation and pain with a lower incidence of gastrointestinal toxicity compared to traditional NSAIDs. This selective inhibition decreases prostaglandin-mediated inflammation, swelling, and pain.

• Absorption: Rapid and complete; peak plasma concentrations in 1 hour.
• Bioavailability: Approximately 100%.
• Distribution: Plasma protein binding ~92%, mainly to albumin.
• Metabolism: Hepatic metabolism predominantly via CYP3A4.
• Active Metabolites: None clinically significant.
• Elimination Half-life: Approximately 22 hours, supporting once-daily dosing.
• Excretion: Primarily via urine (~70%) and feces (~20%).

• Pregnancy: Classified as FDA Category C; avoid use especially during third trimester due to risk of fetal cardiovascular effects (e.g., premature closure of ductus arteriosus).
• Lactation: Unknown if excreted in human milk; caution advised, and breastfeeding not recommended during treatment.

• Primary Class: Nonsteroidal Anti-inflammatory Drug (NSAID)
• Subclass: Selective COX-2 inhibitor (Coxib)

• Known hypersensitivity to etoricoxib or any excipients.
• History of asthma, urticaria, or allergic reactions related to NSAIDs.
• Active or history of recurrent peptic ulcer or gastrointestinal bleeding.
• Severe hepatic impairment.
• Severe renal impairment.
• Established ischemic heart disease, peripheral arterial disease, or cerebrovascular disease.
• Congestive heart failure (NYHA Class II-IV).
• Third trimester of pregnancy.

• Cardiovascular Risk: Increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke; caution in patients with risk factors.
• Gastrointestinal Risk: Risk of GI bleeding, ulceration, and perforation; use cautiously in patients with history of ulcers.
• Renal Effects: May cause renal impairment; monitor renal function especially in volume-depleted or elderly patients.
• Hepatic Effects: Monitor liver enzymes; discontinue if significant hepatic dysfunction occurs.
• Hypersensitivity Reactions: Potential for severe allergic reactions; monitor for rash or anaphylaxis.
• Hypertension: Can cause new or worsening hypertension; monitor blood pressure regularly.

Common Adverse Effects:

• Gastrointestinal: Dyspepsia, abdominal pain, nausea.
• Central Nervous System: Headache, dizziness.
• Respiratory: Upper respiratory tract infections.
• Edema and fluid retention.

Serious/Rare Side Effects:

• Cardiovascular events (MI, stroke).
• Gastrointestinal bleeding or ulcers.
• Severe hypersensitivity reactions.
• Hepatic injury.
• Renal impairment or failure.

• ACE Inhibitors / ARBs: May reduce antihypertensive effect; increased risk of renal impairment.
• Diuretics: Possible decreased efficacy; increased nephrotoxicity risk.
• Anticoagulants (Warfarin): Increased bleeding risk.
• Other NSAIDs or corticosteroids: Increased GI toxicity.
• Lithium: Increased lithium levels and toxicity.
• CYP3A4 inhibitors (e.g., ketoconazole): May increase etoricoxib plasma levels.
• CYP3A4 inducers (e.g., rifampin): May decrease etoricoxib levels.

• Recent updates reinforce cardiovascular warnings consistent with all NSAIDs.
• EMA and FDA recommend restricting use in patients with high cardiovascular risk.
• No new indications approved recently.
• Emphasis on using the lowest effective dose for the shortest duration.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep tablets in original container tightly closed.
• Keep out of reach of children.