Etodolac: Targeted Pain Relief with Joint-Sparing Precision
Etodolac
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| Product dosage: 300mg | |||
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| Product dosage: 400mg | |||
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Synonyms | |||
Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) belonging to the pyranocarboxylic acid class, specifically developed to provide effective analgesia and anti-inflammatory action with a favorable gastrointestinal and renal tolerability profile. It functions as a potent inhibitor of cyclooxygenase (COX), with a noted selectivity for the COX-2 isoenzyme, which plays a pivotal role in mediating inflammation, pain, and fever. This pharmacodynamic profile makes it a first-line therapeutic option for the management of osteoarthritis and rheumatoid arthritis, offering significant symptomatic relief while potentially mitigating the risk of certain adverse effects associated with non-selective NSAIDs. Its well-characterized pharmacokinetics, including high oral bioavailability and extensive plasma protein binding, support its use in chronic pain management protocols.
Features
- Active Pharmaceutical Ingredient: Etodolac
- Standard Dosage Forms: Immediate-release tablets (400 mg, 500 mg), Extended-release tablets (400 mg, 500 mg, 600 mg)
- Pharmacologic Class: Nonsteroidal Anti-inflammatory Drug (NSAID), Pyranocarboxylic acid derivative
- Mechanism of Action: Reversible inhibitor of cyclooxygenase (COX), with relative selectivity for the COX-2 isoenzyme
- Bioavailability: >80% following oral administration
- Protein Binding: >99%, primarily to albumin
- Metabolism: Hepatic, primarily via CYP2C9 and CYP3A4 isoenzymes
- Elimination Half-life: Approximately 7 hours for immediate-release; 8-12 hours for extended-release formulations
- Excretion: Primarily renal (73%) as metabolites, with fecal excretion accounting for approximately 16%
Benefits
- Provides potent anti-inflammatory and analgesic effects for managing chronic inflammatory joint conditions.
- Demonstrates a lower incidence of upper gastrointestinal ulceration and bleeding compared to many non-selective NSAIDs, owing to its COX-2 preferential inhibition.
- Offers flexible dosing regimens with both immediate-release and extended-release formulations to accommodate individual patient needs and improve adherence.
- Effective in reducing morning stiffness and improving physical function in arthritic patients.
- Suitable for long-term management of pain and inflammation associated with osteoarthritis and rheumatoid arthritis.
- Exhibits a well-established safety and efficacy profile supported by extensive clinical use and post-marketing surveillance.
Common use
Etodolac is primarily indicated for the acute and long-term management of signs and symptoms of osteoarthritis and rheumatoid arthritis. It is employed to reduce pain, inflammation, stiffness, and swelling associated with these degenerative and autoimmune joint diseases. Its use extends to the relief of mild to moderate acute pain, such as that following surgical procedures or musculoskeletal injuries. Clinicians may also consider it off-label for other pain syndromes where NSAID therapy is appropriate, following a thorough risk-benefit assessment.
Dosage and direction
For the management of 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 immediate-release tablets. Alternatively, a total daily dose of 400 mg to 1000 mg may be administered as a single daily dose using the extended-release formulation. Dosage should be individualized to the lowest effective dose for the shortest duration consistent with treatment goals. The maximum recommended total daily dose should not exceed 1200 mg for immediate-release or 1000 mg for extended-release formulations in patients under 60 kg, and 1200 mg for those over 60 kg. Administration with food or milk is advised to minimize the potential for gastrointestinal upset.
Precautions
Patients should be advised to use etodolac at the lowest effective dose for the shortest possible duration to minimize the risk of adverse events. Caution is warranted in patients with a history of gastrointestinal ulceration or bleeding, cardiovascular disease, hypertension, heart failure, dehydration, hepatic impairment, or renal impairment. Renal function should be monitored in patients with pre-existing renal conditions, those taking diuretics, or the elderly. Blood pressure should be monitored periodically during therapy. Patients should be advised to avoid concurrent use of other NSAIDs, including over-the-counter products like aspirin or ibuprofen.
Contraindications
Etodolac is contraindicated in patients with known hypersensitivity (e.g., anaphylactoid reactions, asthma, urticaria, or other allergic-type reactions) to etodolac, aspirin, or other NSAIDs. It should not be used in the setting of coronary artery bypass graft (CABG) surgery. It is contraindicated in patients with a history of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs. Use is contraindicated in patients with active peptic ulcer disease or recent gastrointestinal bleeding or perforation. Severe hepatic impairment or active hepatic disease is also a contraindication.
Possible side effect
Common adverse reactions (≥1% and <10%) include dyspepsia, nausea, abdominal pain, diarrhea, flatulence, headache, dizziness, rash, and peripheral edema. Less frequently, but of greater clinical significance, are gastrointestinal ulceration, bleeding, or perforation; hypertension; worsening heart failure; acute renal injury; interstitial nephritis; hepatotoxicity (elevated transaminases); severe skin reactions (e.g., Stevens-Johnson syndrome); and anaphylactoid reactions. Patients should be instructed to seek immediate medical attention for signs of gastrointestinal bleeding, skin rash, allergic reactions, unexplained weight gain, or edema.
Drug interaction
Concomitant use with other NSAIDs or salicylates (e.g., aspirin) increases the risk of gastrointestinal toxicity. Etodolac may diminish the antihypertensive effect of ACE inhibitors, angiotensin II receptor blockers, and diuretics. It can increase the serum concentration and toxicity of lithium and methotrexate. Concurrent use with warfarin or other anticoagulants may increase the risk of bleeding. It may reduce the natriuretic effect of furosemide and thiazides. Coadministration with corticosteroids or selective serotonin reuptake inhibitors (SSRIs) may increase the risk of gastrointestinal bleeding. CYP2C9 inhibitors (e.g., fluconazole) may increase etodolac exposure.
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. Patients should not double the dose to make up for a missed one.
Overdose
Symptoms of acute overdose may include lethargy, drowsiness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, coma, acute renal failure, hypertension, respiratory depression, and anaphylactoid reactions. There is no specific antidote. Management is supportive and symptomatic, including gastric lavage or activated charcoal (if presented early), and close monitoring of vital signs, renal function, and electrolyte balance. Hemodialysis is not 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 the original container, tightly closed, and protect from light and moisture. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging.
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. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has been compiled from various secondary sources and may not encompass the most recent clinical data.
Reviews
“Etodolac has been a cornerstone in my rheumatology practice for managing moderate osteoarthritis. Its efficacy in reducing joint pain and improving mobility is consistently reported by patients, and the extended-release formulation offers convenient once-daily dosing which aids long-term adherence.” — Dr. Eleanor Vance, Rheumatologist
“In my experience prescribing etodolac for chronic lower back pain of arthritic origin, the balance between analgesic effectiveness and gastrointestinal tolerability is notably superior to some older NSAIDs. Monitoring renal function in elderly patients remains paramount.” — Dr. Marcus Thorne, Pain Management Specialist
“While etodolac provides effective anti-inflammatory action, clinicians must remain vigilant for potential cardiovascular and renal adverse effects, particularly in patients with comorbid conditions. It is a valuable tool, but requires careful patient selection and monitoring.” — Clinical Pharmacologist Review
“Patient feedback generally highlights significant improvement in morning stiffness and pain scores within a few weeks of initiating etodolac therapy. The lower incidence of stomach upset compared to ibuprofen is frequently mentioned as a positive attribute.” — Summary of Patient Reported Outcomes