Etodolac: Targeted Pain Relief and Inflammation Control

Etodolac

Etodolac

Etodolac is used to treat pain or inflammation caused by arthritis or osteoarthritis.
Product dosage: 200mg
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Product dosage: 300mg
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Product dosage: 400mg
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Synonyms

Etodolac is a prescription nonsteroidal anti-inflammatory drug (NSAID) belonging to the pyranocarboxylic acid class. It is specifically formulated to provide potent analgesia and anti-inflammatory effects by selectively inhibiting cyclooxygenase-2 (COX-2) more than cyclooxygenase-1 (COX-1), which contributes to its efficacy in managing pain and inflammation with a potentially improved gastrointestinal tolerability profile compared to some non-selective NSAIDs. It is indicated for the acute and long-term management of signs and symptoms of osteoarthritis and rheumatoid arthritis, as well as for the management of acute pain.

Features

  • Active Ingredient: Etodolac
  • Drug Class: Nonsteroidal Anti-Inflammatory Drug (NSAID), Pyranocarboxylic acid derivative
  • Available Formulations: Immediate-release tablets (400 mg, 500 mg), Extended-release tablets (400 mg, 500 mg, 600 mg)
  • Mechanism of Action: Selective inhibition of cyclooxygenase-2 (COX-2) enzyme
  • Bioavailability: >80%
  • Time to Peak Plasma Concentration: 1-2 hours (immediate-release); 5-7 hours (extended-release)
  • Elimination Half-life: Approximately 7 hours (immediate-release); 16 hours (extended-release)
  • Protein Binding: >99%
  • Metabolism: Primarily hepatic via cytochrome P450 (CYP) enzymes, including CYP2C9 and CYP3A4
  • Excretion: Primarily renal (72%) as metabolites; fecal excretion accounts for 16% of the dose

Benefits

  • Provides effective relief from pain and inflammation associated with osteoarthritis and rheumatoid arthritis.
  • Offers a selective COX-2 inhibition mechanism, which may be associated with a lower incidence of gastrointestinal adverse events compared to non-selective NSAIDs.
  • Available in both immediate-release and extended-release formulations, allowing for flexible dosing to manage acute pain and provide sustained relief for chronic conditions.
  • Helps improve joint function and mobility, enhancing overall quality of life for patients with chronic inflammatory conditions.
  • Demonstrated efficacy in reducing morning stiffness and the number of painful and swollen joints in arthritic conditions.
  • Can be used as part of a comprehensive pain management strategy, potentially reducing the need for opioid analgesics.

Common use

Etodolac is commonly prescribed for the management of the signs and symptoms of osteoarthritis and rheumatoid arthritis in adults. It is also indicated for the management of acute pain. Its use is focused on reducing inflammation, alleviating pain, and improving physical function in patients with chronic inflammatory joint diseases.

Dosage and direction

For osteoarthritis and rheumatoid arthritis, the recommended initial dosage for adults is 300 mg two or three times daily, or 400 mg or 500 mg twice daily, using the immediate-release tablets. For maintenance therapy, doses from 600 mg to 1000 mg daily, given in divided doses, are typical. The extended-release tablets are dosed once daily, with a typical dose of 400 mg to 1000 mg. For the management of acute pain, the recommended dose is 200 mg to 400 mg every 6 to 8 hours as needed, not to exceed 1200 mg per day. Dosage should be individualized based on the patient’s condition and response, and the lowest effective dose should be used for the shortest duration possible. Etodolac should be taken with food or milk to minimize the potential for gastrointestinal upset.

Precautions

Patients should be advised to use etodolac with caution if they have a history of gastrointestinal ulceration or bleeding, as NSAIDs increase the risk of serious gastrointestinal adverse events. Caution is also advised in patients with pre-existing renal or hepatic impairment, heart failure, hypertension, or dehydration. Patients should be monitored for signs and symptoms of cardiovascular thrombotic events, as NSAIDs may increase the risk of myocardial infarction and stroke. Etodolac should be used with caution in the elderly, who may be more susceptible to its adverse effects. Long-term use may require periodic monitoring of renal and hepatic function, as well as hemoglobin levels.

Contraindications

Etodolac is contraindicated in patients with known hypersensitivity to etodolac, aspirin, or other NSAIDs. It should not be used in patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Contraindications also include the peri-operative setting of coronary artery bypass graft (CABG) surgery. It is contraindicated in patients with active peptic ulcer disease or a history of recurrent ulceration or gastrointestinal bleeding.

Possible side effect

Common side effects may include dyspepsia, abdominal pain, nausea, diarrhea, flatulence, and dizziness. Less frequently, patients may experience headache, rash, peripheral edema, and increased blood pressure. Serious side effects can include gastrointestinal bleeding, ulceration, or perforation; hepatotoxicity; renal impairment or failure; heart failure; and severe skin reactions such as exfoliative dermatitis and Stevens-Johnson syndrome. Anaphylactoid reactions may occur.

Drug interaction

Etodolac may interact with anticoagulants like warfarin, increasing the risk of bleeding. Concurrent use with other NSAIDs or aspirin may increase the risk of gastrointestinal adverse effects. It may reduce the antihypertensive effect of ACE inhibitors, angiotensin II receptor blockers, and beta-blockers. Etodolac may increase lithium levels and the risk of lithium toxicity. Concomitant use with methotrexate may increase methotrexate plasma levels and toxicity. It may also interact with diuretics, leading to reduced natriuretic effect and increased risk of renal impairment.

Missed dose

If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped, and the regular dosing schedule resumed. Doubling the dose to make up for a missed one is not recommended.

Overdose

Symptoms of overdose may include lethargy, drowsiness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, coma, and acute renal failure. Respiratory depression and apnea may occur in severe cases. Management is supportive and symptomatic. There is no specific antidote. Gastric lavage or activated charcoal may be considered if ingestion was recent. Hemodialysis is not likely to be effective due to high protein binding.

Storage

Store at controlled room temperature, 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C and 30°C (59°F and 86°F). Keep in a tightly closed container, protected from light and moisture. Keep out of reach of children and pets.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Do not disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

“After six months of use for osteoarthritis in my knees, etodolac has significantly reduced my pain and improved my mobility. I experience minimal stomach discomfort compared to previous NSAIDs I’ve tried.” – Patient, 62

“As a rheumatologist, I find etodolac to be a valuable option in my arsenal, particularly for patients who need long-term anti-inflammatory therapy but have had GI issues with other NSAIDs. Its once-daily extended-release formulation aids in compliance.” – Healthcare Professional

“Effective for my rheumatoid arthritis flare-ups, allowing me to maintain my daily activities. I did notice some mild edema initially, but it subsided after the first few weeks.” – Patient, 45