ETR-120

Indications

• Osteoarthritis
• Rheumatoid arthritis
• Acute pain
• Gouty arthritis
• Chronic pain conditions

Dosage

Children: Refer to the BNF for Children for appropriate dosing information in the paediatric population.

Adults: Refer to the BNF for specific dosing guidelines, as they vary based on condition and patient characteristics.

Mechanism of action

Etoricoxib selectively inhibits the cyclooxygenase-2 (COX-2) enzyme, an important mediator in the inflammatory process. By inhibiting COX-2, etoricoxib decreases the production of prostaglandins, which are responsible for pain, fever, and inflammation. This selective inhibition provides analgesic and anti-inflammatory effects while minimizing gastrointestinal side effects associated with non-selective NSAIDs.

Pharmacodynamics

Etoricoxib exhibits anti-inflammatory, analgesic, and antipyretic properties. Its selective action on COX-2 reduces inflammatory mediators in tissues, leading to decreased inflammation and pain relief. The drug's efficacy in managing conditions such as arthritis is attributed to its ability to target inflammatory pathways specifically.

Pharmacokinetics

Etoricoxib is well absorbed following oral administration, with peak plasma concentrations occurring within 1 to 2 hours. It has an extensive volume of distribution and is highly protein-bound (approximately 92%). The drug undergoes hepatic metabolism primarily via cytochrome P450 2C9, producing metabolites that are excreted in urine. The elimination half-life is approximately 22 hours, allowing for once-daily dosing in most cases.

Contra-indications

• Hypersensitivity to etericoxib or any of its components
• Active peptic ulcer disease
• Severe heart failure
• History of gastrointestinal bleeding or perforation related to NSAIDs
• Severe hepatic impairment
• Severe renal impairment

Adverse effects

• Cardiovascular events such as myocardial infarction or stroke
• Gastrointestinal effects including nausea, diarrhea, and abdominal pain
• Renal effects including decreased renal function
• Hepatic effects including elevated liver enzymes
• Skin reactions such as rash or pruritus
• Hypertension

Interactions

• Anticoagulants such as warfarin - increased risk of bleeding
• Other NSAIDs - increased risk of gastrointestinal side effects
• Diuretics - may diminish the antihypertensive effect
• ACE inhibitors - may reduce effects and increase renal impairment risk
• Lithium - may increase lithium levels

Precautions

• Monitor blood pressure regularly, especially in patients with hypertension
• Use with caution in patients with a history of cardiovascular disease
• Assess renal function prior to initiation and during therapy
• Use with caution in elderly patients due to increased risk of adverse effects

Pregnancy

Etericoxib is generally not recommended during pregnancy, especially in the third trimester, as it may cause harm to the fetus.

Breast-feeding

It is not known if etericoxib is excreted in human breast milk. Caution is advised when administering to nursing mothers.

Storage

Store at room temperature, protected from light and moisture. Keep out of reach of children.

Formulations

• Oral tablets of various strengths