Lefgen

Aceclofenac.

Round, white, biconvex film-coated tablet.
Each film-coated tablet contains Aceclofenac 100 mg.
Excipients/Inactive Ingredients: Colloidal anhydrous silica, glycerol distearate, copovidone, croscarmellose sodium, microcrystalline cellulose E460, Talcum E53b, Titanium Dioxide, microcrystalline cellulose, hypromellose, polyoxyl 40 stearate, Opadry.

Pharmacotherapeutic Group: Anti-inflammatory and antirheumatic, non-steroidal. ATC Code: M01AB16.
Pharmacology: Pharmacodynamics: Aceclofenac is a derivative of phenylacetic acid, with anti-inflammatory and analgesic effects. It works by inhibiting cyclooxygenase (COX), an enzyme that plays a crucial role in the formation of prostaglandins (chemical mediators involved in inflammation and pain reactions).
Pharmacokinetics: After oral administration, aceclofenac is rapidly absorbed. Peak plasma concentration is reached within 1.25 to 3 hours.
Aceclofenac is highly bound to plasma proteins (over 99%). It distributes into synovial fluid at a concentration of approximately 57% compared to plasma concentration. The volume of distribution is approximately 25 L.
The average half-life is about 4 hours. Aceclofenac in plasma is mainly in its unchanged form. The primary metabolite found in plasma is 4'-Hydroxyaceclofenac. About ²/₃ of the dose is excreted through the kidneys, primarily in its hydroxylated form.
The pharmacokinetic properties of aceclofenac remain unchanged in elderly individuals.

Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) indicated for pain relief and anti-inflammatory treatment in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.

To minimize the risk of adverse events, LEFGEN should be used at the lowest effective daily dose for the shortest duration possible (see Precautions).
It should be taken with food or immediately after a meal.
Adults: The recommended dose is 100 mg twice daily.
Children: There is no clinical data regarding the use of Aceclofenac in children, and therefore it should not be used in children under 18 years old.
Elderly: Elderly individuals are more likely to have impaired renal, cardiovascular, or hepatic function and may be using other medications concurrently, which increases the risk of serious adverse effects. If NSAID therapy is required, the lowest effective dose for the shortest duration should be used. Patients should be regularly monitored for gastrointestinal bleeding during NSAID treatment.
Aceclofenac's pharmacokinetics are not altered in elderly patients, so no dosage adjustments or changes in treatment duration are required.
Renal impairment: There is no evidence to suggest that dose adjustment is necessary for patients with mild renal impairment. However, like other NSAIDs, caution is advised.
Hepatic impairment: There is some evidence suggesting that the dose of Aceclofenac should be reduced in patients with liver impairment, with the starting dose reduced to 100 mg/day.

Symptoms: Headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding, rarely diarrhea, disorientation, agitation, coma, drowsiness, dizziness, tinnitus, fainting, and occasionally seizures. In severe cases of poisoning, acute renal failure and liver failure may occur.
Management: Symptomatic treatment and supportive care. Within one hour of ingestion of a potentially toxic amount, gastric lavage, and activated charcoal should be administered. Ensure good urinary output, closely monitor liver and kidney function and observe the patient for at least 4 hours. If seizures occur, intravenous diazepam may be administered. Diuresis, dialysis, or hemofiltration are not effective in removing the drug from the body.

Patients with congestive heart failure (from class II to class IV according to the New York Heart Association - NYHA classification), ischemic heart disease, peripheral arterial disease, cerebrovascular disease.
Patients with a history of cardiovascular disease due to atherosclerosis, localized myocardial ischemia, peripheral vascular disease, or cerebrovascular disease.
Patients with asthma, hypersensitivity, angioedema, or urticaria after using other NSAIDs.
Hypersensitivity to aceclofenac, aspirin, other NSAIDs, or any component of the medication.
Progressive gastric ulcers, history of peptic ulcers, or gastrointestinal bleeding.
Severe liver failure, severe heart failure.
Moderate to severe renal impairment.
Patients with active infections.
It should not be used during pregnancy, particularly during the third trimester.

Adverse effects can be minimized by using the lowest effective dose for the shortest time necessary to control symptoms and gastrointestinal and cardiovascular risks.
Aceclofenac should be avoided when used with other NSAIDs, including selective cyclooxygenase-2 inhibitors.
Respiratory Disorders: Caution should be exercised when administering to patients with respiratory diseases or a history of bronchial asthma, as NSAIDs have been reported to reduce bronchial constriction in these patients.
Cardiovascular, Renal, and Hepatic Impairment: The use of NSAIDs may cause dose-dependent reductions in prostaglandin formation and lead to renal failure. Patients at the highest risk for this reaction include those with impaired renal function, heart failure, liver dysfunction, individuals taking diuretics, those recovering from major surgery, and the elderly. The importance of prostaglandins in maintaining renal blood flow should be considered in these patients. Renal function should be monitored in these patients.
Renal Impairment: Patients with mild to moderate renal impairment should be monitored, as NSAID use can lead to further decline in kidney function. The lowest effective dose should be used, and renal function should be monitored regularly. Renal function impairment is usually reversible upon withdrawal of Aceclofenac.
Hepatic Impairment: If abnormal liver function test results persist or worsen, clinical signs or symptoms consistent with liver disease develop, or other manifestations occur (such as eosinophilia or rash), Aceclofenac should be discontinued. Close medical monitoring is necessary for patients with mild to moderate liver impairment. Hepatitis may occur without prodromal symptoms.
The use of Aceclofenac in patients with hepatic metabolic disorders may trigger certain attacks.
Cardiovascular Thrombotic Risk: Non-steroidal anti-inflammatory drugs (NSAIDs), other than aspirin, when taken systemically, can increase the risk of cardiovascular thrombotic events, including heart attack and stroke, which can be fatal. This risk may occur early, within the first few weeks of use, and may increase with prolonged use. The cardiovascular thrombotic risk is primarily associated with high doses.
Doctors should periodically assess for cardiovascular events, even if the patient has no prior cardiovascular symptoms. Patients should be warned about the symptoms of serious cardiovascular events and should seek medical attention immediately if these symptoms occur.
To minimize the risk of adverse events, LEFGEN should be used at the lowest effective daily dose for the shortest duration necessary.
Careful consideration should be given when using diclofenac in patients with significant risk factors for cardiovascular events (such as hypertension, hyperlipidemia, diabetes, or smoking).
Gastrointestinal Bleeding, Ulceration, and Perforation: Caution is needed when using the medication in patients with gastrointestinal diseases, such as ulcerative colitis, Crohn's disease, blood abnormalities, or liver porphyria.
Skin Reactions: Severe skin reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, have been reported very rarely with NSAID use. Patients appear to be at the highest risk for these reactions early in treatment, with the majority of these reactions occurring within the first month of treatment. Aceclofenac should be discontinued if a rash, mucosal lesions, or signs of hypersensitivity occur.
Caution should be exercised when using Aceclofenac in breastfeeding women, as it may be present in breast milk at very low concentrations.
Side effects such as dizziness, drowsiness, fatigue, or visual disturbances may occur.
Effect of the Drug on the Ability to Drive and Operate Machinery: Caution should be exercised when driving or operating machinery.
Use in the Elderly: Elderly individuals are at higher risk of increased adverse effects from NSAIDs, especially gastrointestinal bleeding and perforation, which can be fatal.

Pregnancy: NSAIDs can affect the cardiovascular system of the fetus (risk of premature closure of the ductus arteriosus), so they are contraindicated during the third trimester of pregnancy. During labor, NSAIDs may slow uterine contractions and prolong delivery, leading to an increased risk of bleeding for both the mother and the child. NSAIDs should not be used in the first and second trimesters or during labor unless the benefit to the mother outweighs the potential risk to the fetus.
Breastfeeding: In limited studies, NSAIDs may be present in breast milk at very low concentrations. Therefore, NSAIDs should be avoided in breastfeeding mothers if possible.

Cardiovascular Risk: Clinical trials and epidemiological studies show that the use of diclofenac is associated with an increased risk of cardiovascular events (such as myocardial infarction or stroke), especially when used at high doses (150 mg/day) and for prolonged periods.
Gastrointestinal: Gastric ulcers, perforation, or gastrointestinal bleeding, sometimes fatal, especially in the elderly, may occur. Nausea, vomiting, diarrhea, bloating, constipation, indigestion, abdominal pain, black stools, hemorrhage, and ulcerative stomatitis exacerbation of colitis ulcerative and Crohn's disease have been reported after taking the drug. Less frequently, gastritis has been observed. Pancreatitis has been reported very rarely.
Hypersensitivity Reactions: Hypersensitivity reactions have been reported following treatment with NSAIDs. These may include non-specific allergic reactions and respiratory anaphylaxis, including asthma, severe asthma, bronchospasm, or difficulty breathing, as well as various skin disorders, including rashes, itching, urticaria, angioedema, and, rarely, epidermal necrolysis and polycythemia.
Other less common adverse reactions reported include: Renal: Interstitial nephritis.
Neurological and Special Senses: Optic neuritis, reports of aseptic meningitis (especially in patients with pre-existing autoimmune disorders, such as systemic lupus erythematosus or mixed connective tissue disease), with symptoms such as neck stiffness, headache, nausea, vomiting, fever, disorientation, confusion, hallucinations, discomfort, and drowsiness.
Hematologic: Agranulocytosis, aplastic anemia.
Dermatology: Severe reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis (very rare). Hypersensitivity.
If adverse effects occur, aceclofenac should be discontinued.
Common: Loss of appetite, abdominal pain, nausea, diarrhea; dizziness; elevated liver enzymes.
Uncommon: Bloating, gastritis, constipation, vomiting, gastric ulcer; fatigue; itching, rash, eczema, dermatitis, urticaria; increased BUN, increased blood creatinine.
Rare: Anemia, hypersensitivity reactions, visual disturbances, shortness of breath, black stools, angioedema.
Report any side effects to a doctor.

Lithium, digoxin: Increases the plasma concentrations of lithium and digoxin.
Anticoagulants: Enhances the anticoagulant effect.
Methotrexate: Increases plasma concentrations of methotrexate, leading to increased toxicity when combined with NSAIDs within 24 hours after taking methotrexate.
Cyclosporine: Increases the nephrotoxicity of cyclosporine.
Antihypertensive drugs: Reduces the antihypertensive effect.
Diuretics: Reduces the diuretic effect and increases NSAID nephrotoxicity.
Monitor potassium levels when using potassium-sparing diuretics or ACE inhibitors.
Corticosteroids, other NSAIDs, antiplatelet drugs, and selective serotonin reuptake inhibitors (SSRIs): Increases the risk of gastrointestinal ulcers and bleeding.
Quinolones: Increase the risk of seizures.
Mifepristone: NSAIDs should not be used after mifepristone within 8-12 days as they may reduce the effectiveness of mifepristone.
Tacrolimus: Increases the risk of nephrotoxicity.
Zidovudine: Increases the risk of hematological toxicity.
Ritonavir: Increases the plasma concentration of aceclofenac.

Store below 30°C.
Shelf-life: 36 months from date of manufacture.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M01AB16 - aceclofenac ; Belongs to the class of acetic acid derivatives and related substances of non-steroidal antiinflammatory and antirheumatic products.