Properties
What is it?
Composition 1 ml contains: Aceclofenac I. P. - 150 mg; anhydrous base - sufficient quantity. Pharmacodynamics: Aceclofenac is a new generation non-steroidal anti-inflammatory drug whose mechanism of action consists of many factors. Aceclofenac provides highly effective analgesic therapy with a minimal side effect profile, especially regarding the gastrointestinal tract, which is a common complication with the use of non-steroidal anti-inflammatory drugs. Pharmacokinetics: Aceclofenac blocks cyclooxygenase, an essential component of prostaglandin synthesis. Absorption: After oral administration, aceclofenac is rapidly absorbed from the gastrointestinal tract. Bioavailability is almost 100%. Peak plasma concentrations are reached approximately 1.25-3 hours after administration. Food intake increases the time to reach maximum concentration (Tmax) but does not affect the extent of absorption. Distribution: Aceclofenac is significantly bound to plasma proteins (> 99.7%). Aceclofenac passes into synovial fluid, where its concentration is approximately 60% of the plasma concentration. The volume of distribution is approximately 30 L. Elimination: The mean elimination half-life (T1/2) is 4-4.3 hours. Clearance is 5 L/h. Approximately 2/3 of the administered dose is excreted in the urine, mainly in the form of conjugated hydroxymetabolites. Only 1% of a single oral dose is excreted unchanged. Aceclofenac is likely metabolized with the participation of CYP2C9 enzymes, forming 4-hydroxy diclofenac. The main metabolites are diclofenac and 4-hydroxy diclofenac. Indications: Aceclofenac is used for acute and chronic pain and inflammatory processes, e.g., rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, cervicalgia, lumbago, tendinitis, ligament sprains, and periarthritis of the shoulder. Aceclofenac is also used for painful conditions, e.g., odontalgia, back pain, myalgia, pain after episiotomy, postpartum pain, primary dysmenorrhea, and extra-articular rheumatism. Dosage and Administration: Aceflex™ injection is administered intramuscularly. Adults: The recommended dose is 150 mg once or twice daily for 5 days or as recommended by a doctor. Elderly: Dose reduction is not necessary; however, use with caution. Children: Safety and efficacy in children and adolescents have not been established. Hepatic Impairment: The dose of aceclofenac should be reduced in patients with mild to moderate hepatic impairment. The recommended starting dose is 100 mg per day. Renal Impairment: Dose adjustment is not necessary in mild renal impairment; however, use with caution. Contraindications: Contraindicated in patients with peptic ulcer disease, gastrointestinal bleeding, and hypersensitivity to the drug. Patients in whom similar acting substances (e.g., aspirin or other non-steroidal anti-inflammatory drugs) cause asthma attacks, bronchospasm, acute rhinitis, or urticaria, or patients with hypersensitivity to the drugs. Severe heart failure, impaired liver or kidney function, last trimester of pregnancy. Pregnancy and Lactation: Pregnancy. Regular use of aceclofenac during pregnancy can cause premature closure of the arterial duct in the fetus and prolonged pulmonary hypertension in the newborn, inhibit the onset of labor and prolong the labor process and blood loss. Avoidance of aceclofenac use in the first and third trimesters of pregnancy is necessary. Lactation. Unknown. Whether aceclofenac passes into breast milk. The decision to stop breastfeeding or use aceclofenac will be made after assessing the expected benefit to the mother and the potential risk to the child. Side Effects: Major and minor side effects of 150 mg injectable aceclofenac: abdominal pain, constipation, diarrhea, vomiting, skin rash. Overdose and Toxic Effects: No data on aceclofenac overdose are available. Given the route of administration and pharmaceutical form, overdose with injectable aceclofenac is unlikely. Standard measures of supportive therapy are carried out if necessary. Interactions with Other Drugs and Other Types of Interactions: Lithium and Digoxin: Like other non-steroidal anti-inflammatory drugs, aceclofenac increases plasma concentrations of lithium and digoxin. Diuretics: Like other non-steroidal anti-inflammatory drugs, aceclofenac may inhibit the action of diuretics. Although no effect on blood pressure was observed with concomitant use of bendroflumethiazide, interaction with other diuretics cannot be ruled out. With concomitant use of potassium-sparing diuretics, monitoring of serum potassium levels is necessary. Antihypertensive Agents: Non-steroidal anti-inflammatory drugs may reduce the effect of antihypertensive agents. The risk of reversible acute renal failure may increase in patients with impaired renal function (e.g., dehydrated patients or the elderly) with concomitant use of ACE inhibitors or angiotensin II receptor antagonists and non-steroidal anti-inflammatory drugs. Therefore, this combination should be used with caution, especially in elderly patients. Adequate hydration and monitoring of renal function are necessary when initiating concomitant therapy and periodically during treatment. Anticoagulants: Like other non-steroidal anti-inflammatory drugs, aceclofenac may enhance the effects of anticoagulants. Close monitoring of patients is necessary during combined therapy with anticoagulants and aceclofenac. Antidiabetic Drugs: Dose adjustment of hypoglycemic agents may be necessary with concomitant use of aceclofenac. Methotrexate: Interaction should be considered with concomitant use of non-steroidal anti-inflammatory drugs and low-dose methotrexate, especially in patients with impaired renal function. If combined therapy is necessary, regular monitoring of renal function is recommended. Use with caution when non-steroidal anti-inflammatory drugs and methotrexate are used within 24 hours, which increases methotrexate levels and its toxicity. Other Non-Steroidal Anti-Inflammatory Drugs: Concomitant use of acetylsalicylic acid and other non-steroidal anti-inflammatory drugs may increase the frequency of side effects. Warnings and Special Safety Precautions: Undesirable effects can be minimized by using the lowest effective dose for the shortest duration necessary to control symptoms. Gastrointestinal bleeding, ulcers, or perforation, which can be fatal, are reported with the use of all non-steroidal anti-inflammatory drugs, with or without warning symptoms. The risk of bleeding, ulceration, or perforation is higher with high doses of non-steroidal anti-inflammatory drugs, in patients with a history of ulcers, especially complicated by hemorrhage or perforation, and in the elderly. These patients should start treatment with low doses. Combined therapy with protective agents (e.g., misoprostol or proton pump inhibitors) is recommended. If gastrointestinal bleeding develops during aceclofenac use, treatment should be discontinued. Like other non-steroidal anti-inflammatory drugs, allergic reactions, including anaphylactic/anaphylactoid reactions, are expected. Serious skin reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, are very rarely reported with the use of non-steroidal anti-inflammatory drugs. Aceclofenac use should be discontinued upon the development of rash or any other signs of hypersensitivity. Regular monitoring of patients with mild to moderate renal impairment is necessary, as renal function may deteriorate with the use of non-steroidal anti-inflammatory drugs. Renal impairment is usually reversible and recovers upon discontinuation of aceclofenac. Regular monitoring of patients with mild to moderate hepatic impairment is necessary. Aceclofenac use should be discontinued if signs or symptoms of liver disease development or other manifestations (eosinophilia, rash) are observed. Adequate monitoring is necessary in patients with hypertension and/or mild to moderate heart failure, as fluid retention and edema may occur with the use of non-steroidal anti-inflammatory drugs. Aceclofenac is also used with caution and under strict medical supervision in patients with a history of cerebrovascular bleeding. Clinical studies and epidemiological data confirm that the use of some non-steroidal anti-inflammatory drugs (especially at high doses and for prolonged use) is associated with a small risk of arterial thrombotic events (e.g., myocardial infarction or stroke). Aceclofenac may reduce platelet aggregation. The incidence of adverse reactions caused by non-steroidal anti-inflammatory drugs, especially gastrointestinal bleeding and perforation, which can be fatal, is increased in the elderly. All patients on long-term treatment with non-steroidal anti-inflammatory drugs should take preventive measures (e.g., monitoring of kidney and liver function and blood tests). Effect on Driving and Operating Machinery: In the presence of dizziness or other central nervous system disorders while using non-steroidal anti-inflammatory drugs, driving and operating hazardous machinery should be avoided. Storage Conditions: Store in a dark and dry place at a temperature not exceeding 25 °C. Protect from direct sunlight. Dispensing Category: Pharmaceutical Product Group III, available without a prescription.