Etodolac Tablets

Mechanism

Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic and antipyretic activities in animal models. The mechanism of action of Etodolac, like that of other NSAIDs, is not completely understood, but may be related to prostaglandin synthetase inhibition. Etodolac is a racemic mixture of [-]R- and [+]S-Etodolac. As with other NSAIDs, it has been demonstrated in animals that the [+]S-form is biologically active. Both enantiomers are stable and there is no [-]R to [+]S conversion in vivo.

Pharmacokinetics

• Absorption: Rapid oral absorption; peak plasma levels within 1–2 hours
• Distribution: Highly protein bound
• Metabolism: Hepatic metabolism via CYP enzymes
• Elimination: Excreted in urine and feces
• Half-life: ≈ 7 hours

Side Effects

• Nausea
• Dyspepsia
• Abdominal pain
• Dizziness
• Edema
• Rare: gastrointestinal bleeding, Stevens-Johnson syndrome

Contraindication

• Hypersensitivity to Etodolac or other NSAIDs
• History of asthma, urticaria, or allergic reactions to NSAIDs
• Active gastrointestinal bleeding or peptic ulcer
• Severe renal or hepatic impairment
• Pregnancy (especially third trimester)

Interaction

• Anticoagulants — increased risk of bleeding
• Other NSAIDs — additive gastrointestinal toxicity
• ACE inhibitors/Diuretics — reduced antihypertensive effect
• Lithium — increased plasma lithium levels
• Methotrexate — increased toxicity risk

Warning and Precautions

• Monitor renal and hepatic function during therapy
• Use cautiously in patients with cardiovascular disease
• Discontinue if gastrointestinal bleeding occurs
• Long-term use may increase risk of cardiovascular events
• Use lowest effective dose for shortest duration possible