Properties
- Form
- tableti
- Dosage mg
- 600
- Pack
- 14
What is it?
Composition Each Etodin SR 600 mg tablet contains 600 mg micronized etodolac as the active substance and lactose monohydrate and sodium as excipients and titanium dioxide (E171), HPMC 2910 / hypromellose 3cP (E464), HPMC 2910 / hypromellose 6 cP (E464), macrogol / PEG 400 (E1521), polysorbate 80 (E433) as coloring agents. Pharmacological properties Pharmacodynamic properties Pharmacotherapeutic group: Acetic acid derivatives and related substances Inhibition of prostaglandin synthesis and COX-2 selectivity: All non-steroidal anti-inflammatory drugs inhibit the formation of prostaglandins. This action is responsible for both their therapeutic effects and some of their side effects. The inhibition of prostaglandin synthesis observed with etodolac differs from other non-steroidal anti-inflammatory drugs. At the anti-inflammatory dose established in animal models, the PGE cytoprotective concentration in the gastric mucosa is reduced to a lesser extent and for a shorter duration than with non-steroidal anti-inflammatory drugs. These data are consistent with subsequent in vitro studies, which found etodolac to be selective for induced cyclo-oxygenase 2 (COX-2, associated with inflammation) over COX-1 (cytoprotective). Furthermore, studies on human cell models confirm that etodolac is selective for COX-2 inhibition. The clinical benefit of preferential inhibition of COX-2 over COX-1 still needs to be proven. Anti-inflammatory effects: Experiments show that etodolac has pronounced anti-inflammatory activity, being more potent than several clinically established non-steroidal anti-inflammatory drugs. Pharmacokinetic properties: In men, etodolac is well absorbed after oral administration. Etodolac is highly bound to serum proteins. The half-life averages seven hours in men. The main route of excretion is in urine, primarily as metabolites. In subjects receiving 400 mg or 600 mg daily at steady-state doses for a three-day period, peak plasma concentrations were 7.5 ug/mL at 7.9 hours and 11.9 ug/mL at 7.8 hours. Indications For the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout, acute musculoskeletal pain, postoperative pain, dysmenorrhea - for the management of acute and chronic pain. Contraindications: Etodin SR is not to be used in patients who have previously shown hypersensitivity to etodolac or any of the excipients. Etodin SR is not to be used in patients with severe heart failure. Etodin SR is not to be used in patients who currently have or have had a recurrent peptic ulcer in the past, or in the past history of peptic ulcer disease (with two or more distinct episodes of confirmed ulceration or bleeding). Non-steroidal anti-inflammatory drugs are contraindicated in patients who have previously shown hypersensitivity reactions (e.g., asthma, rhinitis, angioedema or urticaria) during therapy with ibuprofen, aspirin or other non-steroidal anti-inflammatory drugs. Severe heart failure, liver failure and renal failure (see section "Warnings/Precautions"). In the last trimester of pregnancy (see section "Fertility, Pregnancy and Lactation"). History of gastrointestinal bleeding or perforation associated with previous non-steroidal anti-inflammatory drug therapy. Warnings/Precautions Undesirable effects may be minimized by controlling symptoms with the lowest effective dose for the shortest period of time (see section "Dosage and Administration" and gastrointestinal and cardiovascular risks below). The use of Etodin SR in combination with non-steroidal anti-inflammatory drugs, including cyclooxygenase-2 selective inhibitors, should be avoided (see "Interactions with Medicinal Products"). Elderly: Elderly patients are more likely to experience adverse reactions to non-steroidal anti-inflammatory drugs, particularly gastrointestinal bleeding and perforation, which can be fatal (see section "Dosage and Administration"). Cardiovascular and cerebrovascular effects: Appropriate monitoring and advice are required for patients with a history of hypertension and/or mild to moderate congestive heart failure, as fluid retention and edema have been associated with non-steroidal anti-inflammatory drug therapy. Clinical trials and epidemiological data show that the use of some non-steroidal anti-inflammatory drugs (especially at high doses and for prolonged use) may be associated with a slightly increased risk of arterial thrombotic events (e.g., myocardial infarction or stroke). For Etodin SR, there is insufficient data to rule out such a risk. In patients with uncontrolled hypertension, congestive heart failure, established ischemic heart disease, peripheral arterial disease and/or cardiovascular disease, treatment with Etodin SR should only be undertaken after careful consideration. Such caution is also required in patients before starting long-term treatment who have cardiovascular risk factors (e.g., hypertension, hyperlipidemia, diabetes mellitus, smoking). Respiratory disorders: Caution should be exercised if Etodin SR is used in patients who have, or have had in the past, bronchial asthma, as non-steroidal anti-inflammatory drugs can cause bronchospasm in such patients. Cardiovascular, renal and hepatic impairment In patients with cardiovascular, renal and hepatic impairment, especially when the patient is receiving diuretics or in the elderly, renal function monitoring is necessary (see also section "Contraindications"). Caution should be exercised, as the use of non-steroidal anti-inflammatory drugs can cause dose-dependent reduction in prostaglandin production and renal failure. The lowest possible dose should be used. Renal or hepatic failure due to other causes may alter the metabolism of the drug; patients on long-term therapy should be monitored for potential side effects, and their drug doses should be adjusted or discontinued. Gastrointestinal bleeding, ulceration and perforation: Serious gastrointestinal adverse effects such as bleeding, ulceration and perforation have been reported, which can be fatal and can occur at any time, with or without warning symptoms, in patients being treated with non-steroidal anti-inflammatory drugs or with a history of serious gastrointestinal events. Upon detection of any signs of gastrointestinal bleeding, Etodin SR intake should be immediately discontinued. Platelets Although non-steroidal anti-inflammatory drugs do not have the same direct effects on platelets as aspirin, all drugs that inhibit prostaglandin biosynthesis may, to some extent, impair platelet function. Careful observation of patients taking Etodin SR who may be adversely affected by such actions is necessary. For prevention, regular monitoring of patients on long-term therapy with Etodin SR for changes in renal function, hematological parameters or liver function is necessary. The risk of gastrointestinal bleeding, ulceration or perforation is higher with increased non-steroidal anti-inflammatory drug doses, in patients with a history of ulcer, especially if complicated by hemorrhage or perforation (see section "Contraindications") and in the elderly. Treatment in these patients should be initiated at the lowest dose. Combination therapy with protective agents (e.g., misoprostol or proton pump inhibitors) should be considered for such patients and for patients requiring concomitant low-dose aspirin or other drugs that increase the risk of gastrointestinal events (see below and section "Interactions with Medicinal Products"). Patients with a history of gastrointestinal toxicity (especially gastrointestinal bleeding), particularly the elderly, should report any abdominal symptoms, especially at the initial stage of treatment. Caution should be exercised in patients who are concomitantly taking drugs that may increase the risk of ulceration or bleeding, such as oral corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors or antiplatelet agents such as aspirin (see section "Interactions with Medicinal Products"). If gastrointestinal bleeding or ulceration develops during etodolac intake, treatment should be withdrawn. Non-steroidal anti-inflammatory drugs should be used with caution in patients with a history of gastrointestinal disease (ulcerative colitis, Crohn's disease), as exacerbation of such conditions may occur (see section "Side Effects/Adverse Events"). Systemic lupus erythematosus and mixed connective tissue disease In systemic lupus erythematosus and mixed connective tissue disorders, the risk of aseptic meningitis may be increased (see section "Side Effects/Adverse Events"). Dermatological: Serious skin reactions, some of them fatal, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis, have been very rarely reported with the use of non-steroidal anti-inflammatory drugs (see section "Side Effects/Adverse Events"). Patients are at highest risk of such reactions early in therapy: in most cases, the reaction begins within the first month of treatment. Etodin SR intake should be discontinued as soon as the first signs of skin rash, mucosal lesions or any signs of hypersensitivity appear. Impaired female fertility The use of Etodin SR may impair female fertility and is therefore not recommended in women who wish to become pregnant. In women who have conception problems or who are undergoing investigation for infertility, discontinuation of Etodin SR intake should be considered. Sodium This medicinal product contains 27 mg of sodium per dose. This should be taken into account by patients on a sodium-controlled diet. Lactose This preparation is not intended for use in patients with hereditary problems of galactose intolerance, lactase deficiency or glucose-galactose malabsorption. Fertility, Pregnancy and Lactation Pregnancy: Drugs that inhibit prostaglandin biosynthesis may cause dystocia and delay of labor, as shown in studies in pregnant animals. Congenital anomalies have been observed with the use of non-steroidal anti-inflammatory drugs in men; however, these events occur with low frequency. Given the known effects of non-steroidal anti-inflammatory drugs on the fetal cardiovascular system, some inhibitors of prostaglandin biosynthesis prevent the closure of the arterial duct (ductus arteriosus), and their use in the last trimester of pregnancy is contraindicated. Labor may be delayed and the duration of labor may be increased with an increased tendency to bleeding in both mother and child (see section "Contraindications"). The use of non-steroidal anti-inflammatory drugs should not be used in the first two trimesters of pregnancy or during labor unless the potential benefit to the mother outweighs the potential risk to the fetus. Lactation: Existing limited studies show that non-steroidal anti-inflammatory drugs are excreted in breast milk in very low concentrations. During lactation, the use of non-steroidal anti-inflammatory drugs should be avoided whenever possible. See section "Warnings/Precautions" regarding female fertility. Effects on ability to drive and use machines: Etodin may cause dizziness, drowsiness, fatigue or visual disturbances. Before driving or operating machinery, patients should be aware of how they react to this medication. Side effects/Adverse Events: Edema, hypertension and heart failure have been reported with the use of non-steroidal anti-inflammatory drugs. Clinical trials and epidemiological data show that the use of non-steroidal anti-inflammatory drugs (especially at high doses and for prolonged use) may be associated with an increased risk of arterial thrombotic events (e.g., myocardial infarction or stroke) (see section "Warnings/Precautions"). Gastrointestinal tract: Reported side effects include nausea, epigastric pain, diarrhea, indigestion, heartburn, flatulence, abdominal pain, constipation, vomiting, ulcerative stomatitis, dyspepsia, hematemesis, melena, rectal bleeding, exacerbation of colitis, colitis, vasculitis, headache, dizziness, visual disturbances, drowsiness, pyrexia, tinnitus, rash, pruritus, fatigue, depression, insomnia, confusion, paresthesia, tremor, weakness/malaise, dyspnea, palpitations, bilirubinuria, liver function abnormalities and jaundice, increased urinary frequency, dysuria, angioedema, anaphylactoid reaction, photosensitivity, urticaria and Stevens-Johnson syndrome and Crohn's disease (see section "Warnings/Precautions") have been reported after administration of the preparation. Less frequently, gastritis has been reported. Pancreatitis has been reported very rarely. Hypersensitivity: Hypersensitivity reactions have been reported after taking non-steroidal anti-inflammatory drugs. These reactions include (a) non-specific allergic reactions and anaphylaxis (b) respiratory tract reactivity, including asthma, asthma exacerbation, bronchospasm or dyspnea, or (c) associated skin disorders, including various types of rash, pruritus, urticaria, purpura, angioedema and, more rarely, exfoliative and bullous dermatoses (including epidermal necrolysis and erythema multiforme). Cardiovascular and cerebrovascular: Edema, hypertension and heart failure have been reported in association with non-steroidal anti-inflammatory drug treatment. Clinical trials and epidemiological data show that the use of some non-steroidal anti-inflammatory drugs (especially at high doses and for prolonged use) may be associated with an increased risk of arterial thrombotic events (e.g., myocardial infarction or stroke) (see section "Warnings/Precautions"). Kidney: Nephrotoxicity in various forms, including interstitial nephritis, nephrotic syndrome and renal failure. Liver: Liver function abnormalities, hepatitis and jaundice. Neurological and sensory organs: Visual disturbances, optic neuritis, headache, paresthesia, aseptic meningitis (especially in autoimmune disorders such as systemic lupus erythematosus, mixed connective tissue disease) with symptoms such as neck stiffness, headache, nausea, vomiting, fever or disorientation (see section "Warnings/Precautions"), depression, confusion, hallucinations, tinnitus, vertigo, dizziness, malaise, fatigue and drowsiness. Hematological: Thrombocytopenia, neutropenia, agranulocytosis, aplastic anemia and hemolytic anemia. Dermatological: Bullous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis (very rarely). Photosensitivity. Consult your doctor for any adverse effects. Interactions with other medicinal products Since Etodin SR is extensively bound to proteins, dose reduction of other drugs that are also highly protein-bound may be necessary. Other analgesics, including cyclooxygenase-2 selective inhibitors: Avoid the simultaneous use of two or more non-steroidal anti-inflammatory drugs (including aspirin), as this may increase the risk of adverse effects (see Warnings/Precautions). Antihypertensives: Reduced antihypertensive effect. Diuretics: Reduced diuretic effect. Diuretics may increase the nephrotoxicity of non-steroidal anti-inflammatory drugs. Cardiac glycosides: The use of non-steroidal anti-inflammatory drugs may exacerbate heart failure, reduce GFღ and increase plasma glycoside levels. Lithium: Reduced elimination of lithium. Methotrexate: Reduced elimination of methotrexate. Cyclosporine: Increased risk of nephrotoxicity. Anticoagulants: The use of non-steroidal anti-inflammatory drugs may enhance the effects of anticoagulants such as warfarin (see "Warnings/Precautions"). Antiplatelet agents and selective serotonin reuptake inhibitors: Increased risk of gastrointestinal bleeding (see section "Warnings/Precautions"). Tacrolimus: Increased risk of nephrotoxicity has been observed with the concomitant use of non-steroidal anti-inflammatory drugs with tacrolimus. Zidovudine: There is an increased risk of hematological toxicity with the concomitant use of non-steroidal anti-inflammatory drugs with zidovudine. There is an increased risk of hemarthrosis and hematoma in HIV (+) hemophiliacs receiving concomitant zidovudine and ibuprofen. Bilirubin tests may show false positive results in urine due to the presence of phenolic metabolites of Etodin. Mifepristone: Non-steroidal anti-inflammatory drugs should not be used within 8-12 days of mifepristone administration, as non-steroidal anti-inflammatory drugs may reduce the effect of mifepristone. Corticosteroids: Increased risk of gastrointestinal ulceration or bleeding (see section "Warnings/Precautions"). Quinolone antibiotics: Animal data show that the use of non-steroidal anti-inflammatory drugs may increase the risk of convulsions associated with quinolone antibiotics. Patients taking non-steroidal anti-inflammatory drugs and quinolones have an increased risk of developing convulsions. Dosage and Administration To be taken orally. It is advisable to take with food or after meals. Undesirable effects can be reduced by using the lowest effective dose for symptom control (see section "Warnings/Precautions"). Adults: Etodin SR 600 mg tablets, one tablet daily, should be swallowed with a glass of water. The safety of doses higher than 600 mg per day has not been established. No development of tolerance or tachyphylaxis has been observed. Elderly: In general, no initial dose adjustment is required in the elderly (see section "Precautions"). Elderly patients are at increased risk of serious consequences from adverse reactions. If non-steroidal anti-inflammatory drug therapy is necessary, the lowest effective dose and shortest duration should be used. Patients on non-steroidal anti-inflammatory drug therapy require regular monitoring for gastrointestinal bleeding. Children Not recommended. Overdose: (a) Symptoms Symptoms include headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding, rarely diarrhea, disorientation, agitation, coma, drowsiness, dizziness, tinnitus, syncope, sometimes convulsions. In severe poisoning, acute renal failure and liver damage may occur. (b) Therapeutic measures Patients should be treated symptomatically as required. Within one hour of ingestion of a potentially toxic amount, administration of activated charcoal should be considered. Alternatively, in adults, gastric lavage should be performed within one hour of ingestion of a potentially life-threatening overdose. Adequate diuresis should be ensured. Careful monitoring of renal and hepatic function is necessary. Patients should be observed for at least four hours after ingestion of a potentially toxic amount. Frequent or prolonged convulsions should be treated with intravenous diazepam. Other measures are taken according to the patient's clinical condition. Standard measures include gastric lavage, administration of activated charcoal, and general supportive therapy. Storage conditions Store at up to 25°C, in its original packaging. Keep out of reach of children. Packaging: Etodin SR 600 mg tablets; 10 and 14 prolonged-release tablets in blister packs. Shelf life: 2 years. Dispensing category: Pharmaceutical product group III, over-the-counter.
