Brands of Etodolac in Kenya:
Proxym®, Emcure Pharmaceuticals Ltd
Etova®, Ipca Laboratories Limited
ETODOLAC MODE OF ACTION
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 the prostaglandin synthetase inhibition.
Etodolac is indicated:
- For acute and long-term use in the management of signs and symptoms of the following:
- Rheumatoid arthritis
- For the management of acute pain
DOSAGE AND ADMINISTRATION:
The recommended total daily dose of etodolac for acute pain is up to 1000 mg, given as 200-400 mg every 6 to 8 hours. Doses of etodolac greater than 1000 mg/day have not been adequately evaluated in well-controlled trials.
Osteoarthritis and Rheumatoid Arthritis
The recommended starting dose of etodolac for the management of the signs and symptoms of osteoarthritis or rheumatoid arthritis is 300 mg b.i.d., t.i.d., or 400 mg b.i.d., or 500 mg b.i.d. A lower dose of 600 mg/day may suffice for long-term administration. Physicians should be aware that doses above 1000 mg/day have not been adequately evaluated in well-controlled clinical trials.
In chronic conditions, a therapeutic response to therapy with etodolac is sometimes seen within one week of therapy, but most often is observed by two weeks. After a satisfactory response has been achieved, the patient’s dose should be reviewed and adjusted as required.
- Etodolac is contraindicated in patients who have a previous history of hypersensitivity to etodolac or any of the excipients.
- Active, or history of recurrent peptic ulcer/hemorrhage (two or more distinct episodes of proven ulceration or bleeding).
- NSAIDs are contraindicated in patients who have previously shown hypersensitivity reactions (e.g. asthma, rhinitis, angioedema or urticaria) in response to ibuprofen, aspirin, or other non-steroidal anti-inflammatory drugs.
- History of gastrointestinal bleeding or perforation, related to previous NSAIDs therapy.
- Etodolac should not be used in patients with severe heart failure, hepatic failure, and renal failure.
- During the last trimester of pregnancy
- Etodolac is Contraindicated In the setting of coronary artery bypass graft (CABG) surgery
ADVERSE DRUG REACTIONS:
The most commonly-observed adverse events are gastrointestinal in nature.
Blood and lymphatic system disorders
Thrombocytopenia, neutropenia, agranulocytosis, aplastic anemia and hemolytic anemia.
Immune system disorders
Hypersensitivity reactions have been reported following treatment with NSAIDs. These may consist of (a) non-specific allergic reactions and anaphylaxis, anaphylactoid reaction
(b) respiratory tract reactivity comprising asthma, aggravated asthma, bronchospasm or dyspnoea, or (c) assorted skin disorders, including rashes of various types, pruritus, urticaria, purpura, angioedema and, more rarely exfoliative and bullous dermatoses (including epidermal necrolysis and erythema multiforme)
Nervous System disorders
Depression, headaches, dizziness, insomnia, confusion, hallucinations, disorientation paraesthesia, tremor, weakness, nervousness and drowsiness, reports of aseptic meningitis (especially in patients with existing auto-immune disorders, such as systemic lupus erythematosus, mixed connective tissue disease), with symptoms such as the stiff neck, headache, nausea, vomiting.
Visual disturbances (abnormal vision), optic neuritis
Ear and labyrinth disorders
Oedema, hypertension, palpitation, and cardiac failure, have been reported in association with NSAID treatment.
Clinical trial and epidemiological data suggest that use of some NSAIDs (particularly at high doses and in long term treatment) may be associated with an increased risk of arterial thrombotic events (for example myocardial infarction or stroke).
Peptic ulcers, perforation or GI bleeding, sometimes fatal, particularly in the elderly, may occur
Nausea, vomiting, diarrhea, dyspepsia, epigastric pain, ulcerative stomatitis, abdominal pain, constipation, flatulence, haematemesis, melaena, gastrointestinal ulceration, indigestion, heartburn, rectal bleeding. Exacerbation of colitis and Crohn’s disease (See section 4.4) have been reported following administration. Less frequently, gastritis has been observed. Pancreatitis has been reported very rarely.
Abnormal liver function (bilirubinuria) hepatitis and jaundice.
Skin and subcutaneous tissue disorders:
Bullous reactions including Stevens-Johnson Syndrome and Toxic Epidermal Necrolysis (very rare). Photosensitivity.
Renal and urinary disorders
Dysuria, urinary frequency (<1%), nephrotoxicity in various forms, including interstitial nephritis, nephritic syndrome, and renal failure.
Malaise, fatigue, asthenia, chills, fever
Since etodolac is extensively protein-bound, it may be necessary to modify the dosage of other high protein-bound drugs.
Other analgesics including cyclooxygenase-2 selective inhibitors: Avoid concomitant use of two or more NSAIDs (including aspirin) as this may increase the risk of adverse effects.
Anti-hypertensives: Reduced anti-hypertensive effect.
Diuretics: Reduced diuretic effect. Diuretics can increase the risk of nephrotoxicity of NSAIDs.
Cardiac glycosides: NSAIDs may exacerbate cardiac failure, reduce GFR, and increase plasma glycoside levels.
Lithium: Decreased elimination of lithium
Methotrexate: Decreased elimination of methotrexate.
Ciclosporin: Nephrotoxicity associated with cyclosporine may be enhanced.
Mifepristone: NSAIDs should not be used for 8-12 days after mifepristone administration as NSAIDs can reduce the effect of mifepristone.
Corticosteroids: Increased risk of gastrointestinal ulceration or bleeding.
Anti-coagulants: NSAIDs may enhance the effects of anti-coagulants, such as warfarin. Prothrombin time may be prolonged when etodolac and other NSAIDs are given along with warfarin thus leading to increased risk of bleeding.
Quinolone antibiotics: Animal data indicate that NSAIDs can increase the risk of convulsions associated with quinolone antibiotics. Patients taking NSAIDs and quinolones may have an increased risk of developing convulsions.
Anti-platelet agents and selective serotonin reuptake inhibitors (SSRIs): Increased risk of gastrointestinal bleeding.
Tacrolimus: Possible increased risk of nephrotoxicity when NSAIDs are given with tacrolimus.
Zidovudine: Increased risk of hematological toxicity when NSAIDs are given with zidovudine. There is evidence of an increased risk of haemarthroses and hematoma in HIV (+) hemophiliacs receiving concurrent treatment with zidovudine and ibuprofen.
Laboratory test: Bilirubin tests can give a false-positive result due to the presence of phenolic metabolites of etodolac in the urine.
Clinical | Pharmacokinetic data
Pregnancy Category: C
Routes of Administration: Oral
Bioavailability: Not Available
Protein Binding: 100%
Onset of Action: Not Available
Elimination Half life: 7.3 ± 4.0 hours
Legal Status | Dosage forms & Strengths
Prescription only Medicine (POM) , ℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This drug is not a controlled substance under Narcotic Drugs and Psychotropic Substances (Control ) Act
Dosage Forms | Strengths:
|CompTox Dashboard (EPA)|
- PPB Drugs Retention Register
- Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 517. ISBN 9783527607495.
- Glaser, Keith, et al. “Etodolac selectively inhibits human prostaglandin G/H synthase 2 (PGHS-2) versus human PGHS-1.” European journal of pharmacology 281.1 (1995): 107-111.